最新刊期
卷 25 ， 期 14 ， 2019
- 摘要：The experienced prescriptions of famous prestigious Chinese physicians are effective prescriptions developed by prestigious Chinese doctors during their long-time clinical practice, which reflect the traditional Chinese medicine (TCM) understanding of the disease development regularity and core pathogenesis. These experienced prescriptions provide valuable experience for medication and prescription regularities, and represent the highest level of TCM treatment and the major sources of new drug research, development and technology innovation. It is of great significance to inherit academic thoughts and clinical experiences of prestigious Chinese physicians, explore and summarize experienced prescriptions, and develop new Chinese drugs. The researches of new drugs based on experienced prescriptions are the major direction encouraged by the government, with the maximum amount of new TCM drug applications but a low approval rate in recent years. The main reason for the low number of approved new TCM drug applications is that researchers know less about evaluation concepts and relevant techniques, leading to problems in research and development strategy. To facilitate a smooth advance of the new drug research and development and take full advantage of the experienced prescriptions, in this paper, we focus on the problems about new drug development of experienced prescriptions, lay emphasis on the new TCM drug research and development concepts of clinical value, history of human application and whole-process quality control, and deeply and systematically analyze concerns in such links as pharmacy, pharmacodynamics, toxicology and clinic application. The purpose of this article is to provide the reference in solving actual problems, the reliable basis of further researches on experienced prescriptions, and the important guarantee for developing more safe, effective and high-quality controllable drugs to meets clinical requirements, so as to achieve the strategy of a healthy China.关键词：prestigious Chinese physicians;experienced prescription;new traditional Chinese medicine;new drug research and development;research and development strategy
- 26
- |
- 9
- |
- 5
发布时间：2021-02-09
Monograph
- 摘要：Objective:To observe effect of Zeqi Tang in intervening mice with orthotopic lung cancer model, in order to observe its anti-tumor mechanism.Method:An in situ mouse model of non-small cell lung cancer was established through intrapulmonary injection with 1×105 LLC-luc cells. The model mice were intragastrically administered with Zeqi Tang(0.171 g·mL-1) or normal saline for 35 days. Appearance (spirit, hair, appetite, sleep), survival period and Zeqi Tang anti-tumor effect were observed, weekly vital imaging was performed to detect the fluorescence signal in the lungs of mice. Flow cytometry was used to detect the NK cell content in the spleen of the model mice. CD107α was used to detect the degranulation of NK cells in the spleen of mice after administration of Zeqi Tang. Kromasil 100 5 C18 column was used and eluted with acetonitrile-0.025%phosphoric acid in a gradient mode, with flow rate at 1.0 mL·min-1, column temperature at 35 ℃ and detection wavelength of 265 nm, as to establish the fingerprint of Zeqi Tang. The fingerprints of 10 batches of samples was evaluated by using the Chinese Medicine Chromatographic Fingerprint Similarity Evaluation System Software (2012 Edition) recommended by the Chinese Pharmacopoeia Commission, in order to complete the quality control of Zeqi Tang.Result:Zeqi Tang could significantly inhibit the lung fluorescence signal of lung cancer in situ model mice and prolong the survival of mice(P<0.05, P<0.01). After the intervention with Zeqi Tang, the NK cells in the tumors increased significantly(P<0.01), and the degranulation of CD107α also increased significantly(P<0.01). Moreover, the HPLC-DAD fingerprint of Zeqi Tang showed a significant increase in the fingerprint similarity of 10 batches of lacquer soup aqueous extract. Moreover, the HPLC-DAD fingerprint of Zeqi Tang showed that the fingerprint similarity of 10 batches of lacquer soup aqueous extract was ≥0.9, indicating that small differences between the batches.Conclusion:Zeqi Tang may enhance the tumor growth and prolong the survival period of mice by up-regulating the number of NK cells in mice and enhancing their degranulation function. The evaluation of similarity of HPLC fingerprint of Zeqi Tang reflects the quality of lacquer soup to a certain extent, and can provide reference for further study.关键词：Zeqi Tang;pulmonary mouse model;NK cells;quality evaluation
- 22
- |
- 10
- |
- 1
发布时间：2021-02-09 - 摘要：Objective:To study the mechanism of aloesin in inducing apoptosis in human non-small cell lung cancer (NSCLC) A549 cells, so as to inhibit its proliferation.Method:A549 cells in logarithmic growth phase were collected, and cell counting kit-8 (CCK-8) was used to detect the effect of different concentrations of aloesin (2, 4, 8, 16, 32, 64, 128 μmol·L-1) on the proliferation of A549. Effect of aloesin (0, 16 μmol·L-1) on the number of clones formed in A549 cells and the size of clone formation was determined by crystal violet staining. effect of aloesin on apoptosis of A549 cells was detected by annexin V/propidium iodide(PI)apoptosis kit staining. Hoechst staining was used to detect the phenomenon of apoptotic nuclear pyknosis. Western blot was used to detect aloesin's effect on death-related protein expressions of Bcl-xl/Bcl-2 associated death promoter (Bad), cleaved-Caspase-3, cl-Caspase-3(Asp175), Caspase-3, cleaved poly ADP-ribose polymerase (cl-PARP), poly ADP-ribose polymerase (PARP) in A549 cells. In vivo, 5-week-old nude mice were subcutaneously inoculated with 2×106 A549 cells, and randomly divided into the medication group and the blank group. aloesin or normal saline was intraperitoneally injected for 4 weeks, and the tumor volume of nude mice was measured weekly. The body weight of the mice was observed, and the appearance of the nude mice was observed.Result:Aloesin inhibited the proliferation and cloning of A549 cells in a concentration-dependent manner (P<0.05). After treatment with aloesin, the number of apoptosis and the phenomenon of nuclear pyknosis in A549 cells increased significantly (P<0.01). At the same time, aloesin significantly down-regulated the expression of apoptosis-related protein Bcl-xl (P<0.05), and increased the expression of Bad protein (P<0.01). The expression levels of cl-PARP (P<0.01) and cl-Caspase-3 (P<0.05) were also significantly increased. In addition, in vivo, aloesin significantly shrank the volume of subcutaneous tumors in mice, reduced tumor weight, with a better appearance than that of the control group.Conclusion:Aloesin may inhibit the expression of NSCLC by inducing apoptosis of A549 cells, and is safe to use, with no inhibitory effect on the body weight of mice.关键词：aloesin;non-small cell lung cancer;inhibition of cell proliferation;apoptosis
- 24
- |
- 8
- |
- 1
发布时间：2021-02-09 - 摘要：Objective:To investigate the effect of astragaloside on the macrophage polarization and the possible anti-tumor immunity mechanism of astragaloside.Method:The cytotoxic effect of different concentrations of astragaloside at different time points on macrophage was measured by methylthiazolyldiphenyl-tetrazolium bromide (MTT), in order to choose the suitable concentration of astragaloside, macrophages were co-cultured with tumor cells at the ratio 1∶1, and the effect of astragaloside on macrophage-mediated lysis of tumor cells was performed by biophotonic cytotoxicity assay after the mixed cells were effected with 0.1 mg·L-1 astragaloside for 24 h. Macrophages were dealt with 0.1 mg·L-1 astragaloside for 24h, the expressions of CD16/32 and CD206 in macrophages were performed by flow cytometry, the mRNA expressions of macrophage inducible nitric oxide synthase (iNOS), Arginine-1 (Arg-1), interleukin-1β (IL-1β), tumor necrosis factor-α (TNF-α), interleukin-12 (IL-12), interleukin-10 (IL-10) and transforming growth factor-β (TGF-β) were measured by Real-time PCR, the protein expressions of macrophage signal transducers and activators of transcription 1 (STAT1) and phosphorylation signal transducers and activators of transcription 1 (p-STAT1) were determined by Western blot.Result:Astragaloside had no effect on the viability of macrophages with 0.1 mg·L-1. Compared with control group, astragaloside obviously enhanced the macrophage-mediated lysis of tumor cells according to the biophotonic cytotoxicity assay, induced the M1 macrophage marker CD16/32 expression according to flow cytometry, increased the mRNA expressions of iNOS, IL-1β, TNF-α and IL-12 according to the Real-time PCR, and promoted the phosphorylation of STAT1 in macrophages on the basis of Western blot.Conclusion:Astragaloside could induce M1 macrophage polarization by increasing the phosphorylation of STAT1, and initiate macrophage-related anti-tumor immunity response.关键词：astragaloside;macrophage;lung cancer;immunity regulation
- 26
- |
- 10
- |
- 15
发布时间：2021-02-09 - 摘要：Early diagnoses and treatment methods are being constantly improved, but cancer metastasis remains a main cause of mortality in malignant tumor patients. Lung is thought to be the organ most prone to distal metastasis among malignant tumors due to its unique physiological and pathological character. Tumor lung metastasis is unpredictable and may result in irreversible damages. Presently, no exact mechanism or specific targeting therapies are found. Depending on the unique theory system-treatment based on symptom differentiation, traditional Chinese medicine has made significant progress on controlling tumor lung metastasis, but its application methods and mechanism still need further study and exploration. More appropriate and idealized animal models are required as a studying medium. Therefore, the establishment of animal models to simulate lung metastasis of cancer patients has become the key to the study of tumor lung metastasis. In order to produce a better platform for investigating the pathogenesis, underlying mechanism, early diagnosis and therapeutics for tumor lung metastasis, and to provide reference for the selection and establishment of mouse lung metastasis model, this article would introduce the implementation, application and estimation of several common methods (tail vein injection, mammary fat pad orthotopic injection, tibia injection, tissue orthotopic implantation, transgenic mice and so on). Meanwhile, the development of mouse lung metastasis model still needs expanding of thoughts, rational and flexible utilization of existing models, and interdisciplinary cooperation to establish preferable animal models and make results more reliable.关键词：tumor lung metastasis;mouse tumor lung metastasis models;application
- 20
- |
- 8
- |
- 0
发布时间：2021-02-09 - 摘要：Lung cancer is a common malignancy with a high morbidity and high mortality. Although chemoradiotherapy is still the main therapy, the side effects caused by radiotherapy and chemotherapy cannot be ignored. There is an urgent need to find a targeted anti-cancer compound with a low toxicity and strong effect. Therefore, a large number of natural product-derived compounds have received increasing attention for their anti-cancer effect. They are diverse in structure, rich in variety but simpler in composition than natural plants, with a clear efficacy. This facilitates research, and the enriched ingredients have stronger pharmacological effect and clinical efficacy than natural plants. Quinonoids are natural bioactive molecules that widely exist in more than 100 species of higher and lower plants, including naphthoquinones, phenanthrenequinones, benzoquinones and pyrenes. Most of them have anti-tumor effect. They are applied and studied in many cancers, especially lung cancer; and the mechanism of action involves multiple pathways, which play a role in promoting apoptosis, inhibiting proliferation, inducing autophagy, inhibiting angiogenesis and cell invasion and migration. When they are used in combination with other drugs, there is also an anti-tumor effect. With the development of researches, many synthetic quinonoid derivatives with similar structures also increase the diversity of anti-cancer steroids, and quinonoids have broad application prospects in lung cancer. On the basis of a large amount of literature, this article reviews current studies on the molecular mechanisms of antitumor activity of quinonoids, summarizes the common research targets with different effect, and analyzes the relationship between the pharmacological effects and anti-lung cancer effects of quinonoids, and proposes the direction of further research, so as to provide the reference for the follow-up research and development of other quinonoids.关键词：natural quinonoids;lung cancer;mechanism
- 20
- |
- 7
- |
- 1
发布时间：2021-02-09 - 摘要：The diagnosis and treatment methods for cancer are being improved continually, but the mortality of cancer still remains high. At present, the academic circle has realized deficiency of existing treatment ideas, and the concept of cancer cells has been gradually changed from " extremely extinct" to " peaceful coexistence" . The concept of " survival with tumors" is universally accepted in the cancer academia. The tumor microenvironment is the place where tumor cells survive and develop. Therefore, regulation of the tumor microenvironment has become an important new strategy for tumor treatment. Myeloid-derived suppressor cells (MDSCs) are a group of heterogeneous cells that have immunosuppressive properties on T cells in the tumor microenvironment and play an important role in tumor immune escape. Now, therapy with MDSCs in the tumor microenvironment as the treatment targets also provides new ideas for the tumor treatment. As MDSCs subpopulations are similar with neutrophils and monocytes, they can be divided into two major subtypes: granulocyte-like myeloid-derived suppressor cells (G-MDSCs) and monocyte-myeloid-derived suppressor cells(M-MDSCs). But how to differ these two subtypes from neutrophils and monocytes. What are the differences in the functional characteristics of different subtypes of MDSCs. How do they accumulate, differentiate, and exert immunosuppressive effects through different pathways. Traditional Chinese medicine(TCM) has always been good at modulating the body's microenvironment. More and more researches have shown that, the recruitment, amplification and activation of MDSCs can be effectively inhibited by TCM compound and its active ingredients, providing scientific basis for Chinese medicine targeting MDSCs in the tumor microenvironment. However, which specific pathways could regulate G-MDSCs or M-MDSCs is still in need of further studies. Most previous literature focus on the overall level of MDSCs, while the this paper would be based on the specific subpopulations of MDSCs to clarify the biological characteristics of these two subtypes of MDSCs, so as to achieve more precise targeted therapy in the tumor microenvironment.关键词：myeloid-derived suppressor cells (MDSCs);two subtypes;tumor microenvironment;traditional Chinese medicine
- 26
- |
- 7
- |
- 6
发布时间：2021-02-09
Research on Anti-lung Cancer Effect of TCM Compound and Its Effective Components
- 摘要：Objective:To explore the neuroprotective effect and mechanism of Buyang Huanwu Tang (BYHWT) on experimental autoimmune encephalomyelitis (EAE) at different stages.Method:The 36 female C57BL/6 mice were immunized subcutaneously with myelin oligodendrocyte glycoprotein peptides (MOG35-55), then randomly divided into 9, 17, 28 d EAE control group. Each BYHWT group was orally given drugs on the 3rd day after immunization (50 g·kg-1·d-1), and EAE control group was given the same volume of normal saline in the same way once a day for 9, 17 and 28 d after immunization. The effect of BYHWT on EAE mice was observed with internationally accepted clinical score. Brain and spinal cord specimens were collected at 9, 17 and 28 d after immunization. The neuroprotective effect of BYHWT was observed by hematoxylin-eosin(HE)staining and solid blue staining (LFB). The expressions of BDNF and GAP-43 in spinal cord and brain were detected by Western blot.Result:After treatment, BYHWT can significantly inhibit myelitis cell infiltration and alleviate myelin loss. Compared with EAE group, the expression of Nogo-A in the spinal cord of each BYHWT group was significantly down-regulated (P<0.01), and the expression of BDNF in the spinal cord was significantly up-regulated (P<0.05, P<0.01) in the BYHWT group 17 and 28 d group compared with EAE group 17 and 28 d group. Compared with EAE 9, 17 d group, GAP-43 expression was significantly up-regulated in the spinal cord of BYHWT 9, 17 d group (P<0.01).Conclusion:BYHWT can improve the local nerve growth microenvironment and promote the expression of NTFs, reduce the expressions of neuroinhibitory factors, and play a role in neuroprotection.关键词：Buyang Huanwu Tang;experimental autoimmune encephalomyelitis;brain-derived neurotrophic factor;growth-related protein-43;Nogo-A protein;nerve growth microenvironment
- 22
- |
- 7
- |
- 4
发布时间：2021-02-09 - 摘要：Objective:To establish the HPLC fingerprint test method for the medicinal materials, decoction pieces and substance benchmarks of Shaoyao Gancaotang for investigating the quality transmitting of substance group in preparation process of the medicinal materials-decoction pieces-substance benchmarks, then to evaluate the scientificity and rationality of preparation process of substance benchmarks of Shaoyao Gancaotang by combining with yields of dry extract, transfer rates of effective components and other indexes.Method:Substance benchmarks of Shaoyao Gancaotang was prepared according to the method recorded in ancient medical books, fingerprints of 15 batches of medicinal materials, decoction pieces and substance benchmarks were detected by HPLC, and the contents of effective ingredients were determined. At the same time, the correlation analysis of quality transmitting of substance group during the preparation of substance benchmarks was carried out by combining the yields of dry extract and transfer rates of effective components.Result:The established HPLC fingerprint method has good precision, repeatability and stability, it can be used for the simultaneous determination of fingerprint of medicinal materials, decoction pieces and substance benchmarks. In the fingerprint of substance benchmarks, 16 common peaks were determined by taking liquiritin as the reference peak, of which 6 chromatographic peaks belong to Paeoniae Radix Alba and 11 chromatographic peaks belong to Glycyrrhizae Radix et Rhizoma, 7 major chromatographic peaks were identified. The similarities of fingerprints of 15 batches of medicinal materials, decoction pieces and substance benchmarks of Shaoyao Gancaotang were good by comparing with their respective reference fingerprints(≥0.90), the average dry extract rate of 15 batches of substance benchmarks was 24.81%, and no discrete data were found; the average transfer rates of paeoniflorin, liquiritin and glycyrrhizic acid from decoction pieces to substance benchmarks were 79.68%, 63.70% and 51.20%, respectively, and no discrete data were found.Conclusion:In this paper, a scientific and reasonable method for evaluating the process of substance benchmarks of Shaoyao Gancaotang is established by means of the fingerprint method controlled by the whole substance group, the research idea of quality transmitting of substance group in the preparation process, and the evaluation of technical and economic indicators. It can be used as a reference for the evaluation and research of material benchmarks in other famous classical formulas.关键词：famous classical formulas;Shaoyao Gancaotang;substance benchmarks;fingerprint;quality transmitting;paeoniflorin;liquiritin
- 25
- |
- 9
- |
- 12
发布时间：2021-02-09 - 摘要：Objective:To observe the Toll-like receptor 4(TLR4)and its negative regulating factorInterleukin-1 receptor-associated kinase-M(IRAK-M)in colonic mucosa of rats with experimental ulcerative colitis(UC), and to discuss the mechanism of the Chinese medicine Sishenwan.Method:The 90 Wistar rats were randomly divide into six groups, blank group, model group, sulfasalazine group(0.36 g·kg-1), Sishenwan low, medium and high-dose group(2.5, 5, 10 g·kg-1), 15 cases in each group. A rat model of UC was prepared by using a solution of trinitrobenzenesulfonic acid / ethano.The histopathological changes of colon were observed by hematoxylin-eosin (HE) staining. The contents of serum free triiodothyroid acid (FT3), serum free thyroxine (FT4), immunoglobulin (Ig) E and interleukin (IL)-2 were determined by radioimmunoassay. The activity of superoxide dismutase (SOD) in rat serum was determined by xanthine oxidation method. The activity of malondialdehyde (MDA) in serum of rats was determined by thiobarbituric acid (TBA) colorimetry.Result:Compared with blank group, intestinal mucosal injury score of rats in model group was significantly increased (P<0.01), serum IgE and MDA contents were significantly increased (P<0.01). The expression levels of FT3, FT4, IL-2 and SOD were significantly decreased (P<0.01). The TLR4 mRNA and protein expression in model group increased significantly(P<0.01). The expression of IRAK-M mRNA and protein decreased significantly(P<0.01). Compared with model group, scores of each treatment group were significantly decreased (P<0.01), IgE and MDA contents were significantly decreased (P<0.05, P<0.01), FT3, FT4, IL-2, and SOD contents were significantly increased (P<0.05, P<0.01). The expression of TLR4 mRNA and proteinin each treatment group was significantly reduced(P<0.05, P<0.01), IRAK-M mRNA and protein expression level increased(P<0.01).Conclusion:The unbalanced expressions of TLR4 and its negative regulating factor IRAK-M are connected with the pathogenesis of UC.Sishenwan can cure UC and control the expression of TLR4 and promote the expression of IRAK-M.关键词：Toll-like receptor 4(TLR4);interleukin-1 receptor-associated kinase-M(IRAK-M);ulcerative colitis;Sishenwan;mechanism
- 17
- |
- 7
- |
- 13
发布时间：2021-02-09
Classic Prescriptions
- 摘要：Objective:To observe the expression levels of niemann-pick C1-like 1 (NPC1L1) and adenosine triphosphate-binding cassette transporters G8 (ABCG8) in intestine of hyperlipidemic model rats, in order to investigate the therapeutic mechanism of Shuangyu Tiaozhi decoction on hyperlipidemia.Method:A total of 40 SD rats were selected, including 8 for normal control group. The remaining 32 rats were used to establish hyperlipemic model. After modeling, the rats were randomly divided into the model group (equivalent normal saline), the high and low-dose Shuangyu Tiaozhi groups (15.6, 7.8 g·kg-1), and the Simvastatin group (4 mg·kg-1), with 8 in each group. They were given drugs by gavage for 8 weeks. The levels of total cholesterol (TC), triglyceride (TG) in serum and total cholesterol (TTC), free cholesterol (FTC) in liver of rats in each group were determined by biochemical and enzymatic methods. The morphological changes of liver were observed by hematoxylin-eosin (HE) staining, and the levels of expressions of NPC1L1, ABCG8 and liver X receptor-α (LXR-α) in intestine were detected by Real-time fluorescence quantitative polymerase chain reaction (Real-time PCR) and Western blot. The expression of ABCG8 protein was determined by immunohistochemistry.Result:After successful replication of the hyperlipidemia model, the blood lipid level was abnormally increased, and the liver steatosis became obvious in the model group compared with the normal control group. The expression levels of NPC1L1, LXR-α and ABCG8 increased significantly (P<0.05, P<0.01). Compared with the model group, the blood lipid levels were significantly reduced in the Shuangyu Tiaozhi decoction group. The expressions of NPC1L1 and LXR-α were significantly down-regulated, but ABCG8 was obviously up-regulated in a dose-dependent manner (P<0.05, P<0.01). The results of immunohistochemistry indicated that the protein expression of ABCG8 in intestine of the model group increased significantly (P<0.01). Compared with the model group, the expression of ABCG8 in each drug-administered groups increased obviously (P<0.05, P<0.01), especially in high-dose Shuangyu Tiaozhi group (P<0.05).Conclusion:Shuangyu Tiaozhi decoction can reduce the blood lipid level of hyperlipemic rat model by reducing the absorption of cholesterol. Its mechanism may be correlated with the down-regulation of NPC1L1 expression and the up-regulation of ABCG8 expression.关键词：Shuangyu Tiaozhi decoction;spleen tonifying turbid method;hyperlipidemia;niemann-pick C1-like 1 (NPC1L1);liver X receptor-α (LXR-α);adenosine triphosphate-binding cassette transporters G8 (ABCG8)
- 18
- |
- 7
- |
- 5
发布时间：2021-02-09 -
Comparation of Effect on Tripterygium Glycosides Tablet from Two Different Manufacturers in CIA Rats
摘要：Objective:To compare the effects and multi-organ intervention of tripterygium glycosides(TG) tablet from Hunan Qianjin Xieli (QJ) and Zhejiang Deende (DED) on type Ⅱ collagen-induced arthritis (CIA) in rats.Method:The 72 SD rats were randomly divided into normal group, model group, QJ TG clinical group 2 times, 6 times equivalent dose group (QJ-TG 0.018, 0.054 g·kg-1), derende TG clinical group 2 times, 6 times equivalent dose group (DED-TG 0.018, 0.054 g·kg-1). The intragastric administration was started on the day after the first immunization, once a day. After the second immunization, the symptoms such as redness and swelling of joints were observed, and the clinical score of arthritis were evaluated. The materials were taken for pathological examination of the inflammatory joints on the 21th and 42th day. The concentration of alkaline phosphatase(ALP), alanine aminotransferase(ALT), aspartate aminotransferase(AST), gamma-glutamyltransferase(GGT), total bilirubin(TBIL), creatinine(CRE) and urea(UREA) in serum were detected by enzymatic assay. The rate of sperm deformity, testicular and ovarian tissue damage in the rat epididymis was assessed.Result:TG from two manufacturers attenuated the inflammation, redness, swelling and deformity of joints in CIA rats, reduced the clinical score and incidence of arthritis in CIA rats. Meanwhile, it also exhibited obvious reduction in all pathological features such as joint synovitis, pannus, cartilage erosion and bone destruction. There were significant differences between the QJ-TG high and low dose groups and the DED-TG high dose group compared with the model group (P<0.05, P<0.01). There was no significant change in the low dose group of DED-TG compared with the model group.Compared with the same dose of TG in the two manufacturers, the DED-TG 0.054 g·kg-1 group had a significant inhibitory effect on the clinical scores on the 15th and 18th days than the QJ-TG same dose group (P<0.05). In addition to 0.054 g·kg-1 dose of DED-TG, the white blood cell count and spleen index were significantly increased.At the same time, two different manufacturers of TG had no effect on body weight, organ index, digestive system, liver and kidney function, liver and kidney pathology of CIA model rats. QJ-TG and DED-TG all significantly increased the rate of male rats sperm malformation and significant damage to testicular seminiferous tubules and the toxicity increased with the increase of dose and time. while the mole reproductive toxicity of DED-TG was higher than that of QJ-TG at the same dose. In the DED-TG 0.054 g·kg-1 and QJ-TG 0.054 g·kg-1 group, there were only the reduction of vascular distribution in the ovarian tissue and the reduction of the corpus luteum, and no other toxic effects were observed.Conclusion:Two manufacturers TG2 times (0.018 g·kg-1) and 6 times (0.054 g·kg-1) clinical equivalent dose can delay the onset of CIA in rats, reduce the clinical score of arthritis, improve the pathological changes of joints, but have a certain degree of male reproductive toxicity. The high-dose DED-TG is more toxic than the QJ-TG.关键词：Hunan Qianjin Xieli tripterygium glycosides tablet;Zhejiang Deende tripterygium glycosides tablet;rheumatoid arthritis;collagen-induced arthritis rat model;anti-arthritis effect;toxicity- 24
- |
- 8
- |
- 9
发布时间：2021-02-09 - 摘要：Objective:To observe the effect of isopimpinellin on primary hippocampal neuron cells γ-aminobutyric acid (GABA), 5-hydroxytryptamine (5-HT) and receptor genes expressions, in order to explore its hypnotic mechanism.Method:The primary hippocampal neurons of neonatal Sprague-Dawley rats were cultured in vitro. And subsequent experiments were conducted in the optimal state of cell growth, and the purity was identified by immunohistochemistry of neuron-specific enolase. Hippocampal neurons were randomly divided into five groups, namely blank control group, diazepam group (25 mg·L-1), and low-dose (5 mg·L-1), moderate-dose (10 mg·L-1) and high-dose (20 mg·L-1) isopimpinellin groups. Early apoptosis of hippocampus neuron cells were detected using flow cytometry technique after 24 h administration, and the changes in the levels of GABA and 5-HT were detected using enzyme-linked immunosorbent. The changes in mRNA expressions of receptor genes relating to gamma-aminobutyric acid type A receptor(GABAA) genes GABRA1, GABRA5, GABBR1, gamma-aminobutyric acid type B receptor genes (GABAB) GABRB2, 5-hydroxytryptamine 1A receptor (5-HT1A)5-HT1A(A), 5-HT1A(B), 5-HT1A(C) were detected by real-time quantitative PCR(Real-time PCR).Result:On the 7th day, the hippocampal neurons grew in a good condition, and the purity was above 90%. Apoptosis rates of hippocampal neurons in the low-dose and moderate-dose groups were significantly lower than that in the blank control group (P<0.01). The level of GABA secreted by hippocampal neurons in the high-dose isopimpinellin group were significantly higher than that in the blank control group (P<0.01). The mRNA expression levels of GABRA1, GABRA5, 5-HT1A(A), 5-HT1A(C) in the moderate-dose and high-dose isopimpinellin groups were significantly higher than those in the blank control group (P<0.05, P<0.01). The mRNA expression levels of GABBR1, 5-HT1A(B) in the low-dose, moderate-dose and high-dose isopimpinellin groups were significantly higher than those in the blank control group (P<0.05, P<0.01).Conclusion:The hypnotic mechanism of isopimpinellin may be related to the inhibition of hippocampal neuron apoptosis, the increase of the content of inhibitory neurotransmitter GABA, and the up-regulation of GABA and 5-HT-related receptor genes.关键词：isopimpinellin;hippocampal neuron;inhibitory neurotransmitter;cell apoptosis;in vitro culture
- 18
- |
- 7
- |
- 0
发布时间：2021-02-09 - 摘要：Objective:To explore the effect of celastrol in inhibiting the lipid metabolism disorder in hepatic L02 cells and its possible mechanism on endoplasmic reticulum stress (ERS) of non-alcoholic fatty liver cells by intervening non-alcoholic fatty liver disease(NAFLD) cell model with celastrol.Method:Hepatic L02 cells were divided into control group, model group, low-dose celastrol treatment group (Cel 0.5 mg·L-1), high-dose celastrol treatment group (Cel 1 mg·L-1) and simvastatin group (SIM 6 mg·L-1) for cultivation. The contents of total cholesterol (TC) and total triglyceride (TG) in hepatic L02 cells were detected, and the oil red staining was used to detected the lipid accumulation in hepatic L02 cells. Reverse transcription polymerase chain reaction (RT-PCR) and Western blot were used to detect the mRNA and protein expression levels of endoplasmic reticulum stress (ERS)-related signal molecules activating transcription factor 6 (ATF6), glucose regulated protein 78 (GRP78), inositol-requiring enzyme 1 (IRE1), sterol regulatory element-binding protein cleavage-activating protein (SCAP), sterol regulatory element-binding protein-1c (SREBP-1c) and sterol regulatory element-binding protein-2 (SREBP-2) in hepatic L02 cell model respectively.Result:The contents of TC and TG in hepatic L02 cells of NAFLD group were significantly higher than those in control group (P<0.05). The TC and TG contents in hepatic L02 cells of Cel 0.5 mg·L-1 group, Cel 1 mg·L-1 group and SIM 6 mg·L-1 group were significantly lower than those in NAFLD group (P<0.05). Oil red O staining showed that a large amount of red-stained lipid particles were deposited in the hepatic L02 cells of the NAFLD group, while the red-stained lipid particles in the Cel 0.5 mg·L-1 group, the Cel 1 mg·L-1 group, and the SIM 6 mg·L-1 group were lower than the NAFLD group to different degrees. According to the results of RT-PCR and Western blot, the mRNA transcription and protein expression levels of ERS-related signaling molecules ATF6, GRP78, IRE1, SCAP, SREBP-1c and SREBP-2 in hepatic L02 cells of NAFLD group were higher than those of control group (P<0.05). The mRNA transcription and protein expression levels of ERS-related signaling molecules ATF6, GRP78, IRE1, SCAP, SREBP-1c and SREBP-2 in hepatic L02 cells of Cel 0.5 mg·L-1 group, Cel 1 mg·L-1 group and SIM 6 mg·L-1 group were lower than those of NAFLD group (P<0.05). There was no significant difference in the mRNA transcription and protein expression levels of ATF6, GRP78, IRE1, SCAP, SREBP-1c and SREBP-2 between the Cel 1 mg·L-1 group and the SIM 6 mg·L-1 group.Conclusion:Celastrol can reduce the lipid metabolism disorder in hepatic L02 cells by down-regulating the expressions of ERS-related signaling molecules ATF6, GRP78, IRE1, SCAP, SREBP-1c and SREBP-2 in hepatic L02 cells, so as to improve NAFLD.关键词：celastrol;non-alcoholic fatty liver disease;endoplasmic reticulum stress;hepatic L02 cells
- 22
- |
- 8
- |
- 0
发布时间：2021-02-09 - 摘要：Objective:To discuss the effect of volatile oil from Xanthii Fructus on airway remodeling of rats with bronchial asthma, in order to discuss the mechanism of action through matrix metalloteinases-9 (MMP-9), tissue inhibitor of metalloproteinase-1 (TIMP-1), platelet derived growth factor (PDGF), transforming growth factor-β1 (TGF-β1), Smad2, Smad3 and Smad7 mRNA expressions.Method:Forty-eight rats (half males and half females) were randomly divided into six groups (n=8), namely normal saline group, model group, volatile oil from Xanthii Fructus (7.5, 15, 30 mg·kg-1) groups and dexamethasone group (0.5 mg·kg-1). Except for normal saline group, airway remodeling of rats were established through ovalbumin sensitization and atomization inhalation method. At volatile oil group, rats got volatile oil spray since the first time (the 4th week after modeling) of inspiration of asthma to the last day before the end of test. Histopathological changes of bronchus and lung were analyzed by htoxylin eosin (HE) stain. And airway remodeling was observed, and perimeter of bronchial lumen (Pi), smooth muscle area of bronchi (S), tube wall area (W) and nuclei of smooth muscle cells (N) were recorded. And levels of endothelin-1 (ET-1) and insulin-like growth factor-1(IGF-1) in irrigation solution of Alveoli (BALF) were detected. And mRNA expressions of MMP-9, TIMP-1, PDGF, TGF-β1, Smad2, Smad3 and Smad7 were detected by real-time quantitative-polymerase chain reaction (Real-time PCR).Result:In the model group, infiltration of a large number of inflammatory cells were found at the peribronchial wall, airway smooth muscle thickness and basement membrane increased, and bureaucratic cavity was narrower and flatter. Volatile oil from Xanthii Fructus can ameliorate pathological damage of bronchopulmonary tissue. Levels of S/Pi, W/Pi and N/Pi, BALF, ET-1, IGF-1 and MMP-9/TIMP-1 and mRNA expressions of MMP-9 and PDGF in volatile oil group and dexamethasone group were lower than those in model group (P<0.01). Compared with model group, mRNA expressions of TGF-β1, Smad2 and Smad3 were less than those in model group (P<0.01), while mRNA expression of Smad7 was more than that in model group (P<0.01).Conclusion:Volatile oil from Xanthii Fructus can regulate levels of MMP-9, TIMP-1, MMP-9/TIMP-1, TGF-β1/Smad, inhibit expressions of PDGF, ET-1 and IGF-1, and suppress subepithelial fibrosis, extracellular matrix synthesis, proliferation and migration of airway smooth muscle cells to relieve or inhibit airway remodeling, so as to prevent and treat asthma.关键词：Xanthii Fructus;volatile oil;bronchial asthma;airway remodeling
- 26
- |
- 8
- |
- 3
发布时间：2021-02-09 - 摘要：Objective:To explore the effect of salvianolic acid B (Sal-B) on the myocardial apoptosis in rats with sepsis.Method:The 50 male SD rats were randomly divided into sham operation group, model group (cecal ligation and perforation were performed to replicate the animal model of sepsis)and Sal-B low, medium and high-dose group(6, 12, 24 mg·kg-1). The myocardial necrosis markers troponin T(TnT), cardiac troponin I (cTnI), creatine kinase-MB (CK-MB) and the tumor necrosis factor-α (TNF-α), interleukin-1β (IL-1β) and interleukin-6 (IL-6) were assayed by enzyme-linked immunosorbent assay(ELISA). The antioxidant enzyme superoxide dismutase (SOD) activities and malonaldialdehyde (MDA) levels in myocardial homogenates were determined by spectrophotometrically. Haematoxylin-eosin (HE) staining was used to evaluate the pathological change in rats. Terminal deoxynucleotidyl transferase-mediated dUTP-biotin nick end labeling assay (TUNEL) was used to detect apoptosis of myocardial cells in hearts, respectively. Western blot was used to detect the expression levels of apoptosis-related protein cysteine protease-3 (Caspase-3), b-lymphocytoma-2 (Bcl-2), Bcl-2-related X protein (Bax), autophagy microtubule-related light chain 3 (LC3) and Beclin-1 in myocardial tissue.Result:Compared with sham group, the levels of TnT, CK-MB and cTnI in model group were significantly increased (P<0.01). The levels of TNF-α, IL-1β and IL-6 in myocardial tissue were significantly increased (P<0.01). MDA content in myocardial tissue was significantly increased (P<0.01), SOD activity in myocardial tissue was significantly decreased (P<0.01), the ratio of TUNEL positive myocardial cells was significantly increased (P<0.01), Bax and Caspase-3 protein expression levels were significantly increased, while Bcl-2 expression was significantly decreased (P<0.01), autophagy related protein LC3 and Beclin-1 expression levels were significantly increased (P<0.01). Compared with model group, the levels of TnT, CK-MB and cTnI in Sal-B medium and high-dose groups were significantly decreased (P<0.01), the levels of TNF-α, IL-1 and IL-6 in the myocardial tissue were significantly decreased (P<0.01), MDA content in myocardial tissue was significantly decreased (P<0.05, P<0.01), and the SOD activity in myocardial tissue was significantly increased (P<0.05, P<0.01). The ratio of TUNEL positive cardiomyocytes was significantly decreased (P<0.05), Bax and Caspase-3 protein expressions were decreased, and Bcl-2 expression was significantly increased (P<0.05, P<0.01). The autophagy response was enhanced, the LC3Ⅱ/LC3Ⅰ ratio was increased, and Beclin-1 expression was significantly up-regulated (P<0.05, P<0.01).Conclusion:Sal-B showed a protective effect on the myocardial apoptosis in septic rats maybe by depressing inflammatory infiltration, anti-oxidative effects and improving the exceptional expression of the proteins such as Bax, Bcl-2, Caspases-3 by enhancing the level of autophagy.关键词：salvianolic acid B;sepsis;myocardium injury;protect effect;autophagy
- 33
- |
- 11
- |
- 5
发布时间：2021-02-09
Pharmacology
- 摘要：Objective:To explore the clinical efficacy of modified Jinshui Liujunjian combined with salmeterol/fluticasone on senile asthma on persistent stage and its effect on vascular endothelial growth factor (VEGF) and transforming growth factor-β1 (TGF-β1) in serum.Method:The 100 cases of senile asthma who met inclusion criteria were selected and divided into two equal groups by random number table: the control group and the treatment group. Patients of the two groups were given oxygen therapy, phlegm reduction, infection control and salmeterol/fluticasone 50 μg·(500 μg)-1. Patients in control group were given sustained release capsule of theophylline in addition to the above therapy, while patients in treatment group were given modified Jinshui Liujunjian. The course of treatment was 8 weeks. The therapeutic effectiveness of traditional Chinese medicine (TCM) syndrome between two groups was observed. Asthma control test (ACT) scores at four different time points(before and after treatment, 3, 6 months after treatment), pulmonary function, the levels of VEGF and TGF-β1 in serum before and after treatment between two groups were also observed. The pharmic safety during treatment was evaluated.Result:The total effective rate of treatment group was significantly higher than that of control group(P<0.05). Compared with that in control group, ACT scores in treatment group were significantly higher at three different time points(after treatment, 3 and 6 months after treatment)(P<0.05). Compared with that in control group, peak expiratory flow (PEF) variability and the levels of VEGF and TGF-β1 in serum in treatment group were significantly lowered after treatment(P<0.05), while the percentage of forced expiratory volume in the first second and its predicted value (FEV1%), and the percentage of forced expiratory volume in the first second and its forced vital capacity (FEV1/FVC) were significantly higher(P<0.05). Compared with that in control group, the incidence of the untoward effect in treatment group were significantly lowered during treatment(P<0.05).Conclusion:Modified Jinshui Liujunjian combined with Salmeterol/Fluticasone was more effective than Sustained release capsule of theophylline combined with Salmeterol/Fluticasone in improving the clinical efficacy and pulmonary function of senile asthma on the persistent stage. Its mechanism of action is probable correlated with the reduction of levels of VEGF and TGF-β1 in serum.关键词：modified Jinshui Liujunjian;senile asthma;vascular endothelial growth factor(VEGF);transforming growth factor-β1(TGF-β1);clinical observation;Chinese traditional treatment
- 16
- |
- 7
- |
- 1
发布时间：2021-02-09 - 摘要：Objective:To observe clinical efficacy of Shengma Biejia Tang combined with Shenfutang on sepsis-induced myocardial dysfunction (SIMD) and study the controlling effect on inflammatory reaction.Method:Eighty-eight patients with SIMD were randomly divided into control group (44 cases) and observation group (44 cases) by random number table. Patients in control group received the early bundle therapy of sepsis, including fluid resuscitation, anti-infection treatment and vasoactive drugs. In addition to the therapy of control group, patients in observation were also given Shengma Biejia Tang combined with Shenfutang, 1 dose/day. And a course of treatment was 7 days. Before and after treatment, levels of troponin (cTnI), creatine kinase isoenzyme (CK-MB), N terminal brain natriuretic precursor (NT-proBNP), calcitonin (PCT), hypersensitivity C reactive protein (hs-CRP), tumor necrosis factor-α (TNF-α), interleukins-6 (IL-6) and blood lactic acid (LAC) were detected. And color Doppler ultrasound examination of the heart was performed to record left ventricular ejection fraction (LVEF), blood flow velocity of early mitral valve diastole and ratio of blood flow velocity at atrial systolic peak (E/A) and stroke volume (SV). And lactate clearance rate (LCR) was calculated. And sequential (sepsis-related) organ failure assessment (SOFA), acute physiology and chronic health (APACHEⅡ) and traditional Chinese medicine(TCM)syndromes were scored.Result:After treatment, levels of cTnI, NT-ProBNP, CK-MB, Hs-CRP, IL-6, PCT, TNF-α and LAC in observation group were lower than those in control group (P<0.01), and levels of LVEF, E/A, SV and LCR were higher than those in observation group (P<0.01). And scores of SOFA, APACHEⅡ and traditional Chinese inedicine(TCM) syndromes were lower than those in control group (P<0.01).Conclusion:In addition to the integrated western medicine, Shengma Biejia Tang combined with Shenfutang can control inflammatory reaction, relieve myocardial inhibition and myocardial damage, and protect and improve heart function, and alleviate the symptoms.关键词：sepsis-induced myocardial dysfunction;Shengma Biejia Tang;Shenfutang;yang warming, stasis dissipating and detoxifying;inflammatory reaction
- 24
- |
- 7
- |
- 4
发布时间：2021-02-09 - 摘要：Objective:To observe the effect of syndrome differentiation and treatment with Wandaitang on symptoms, quality of life and function of immunologic after operation of endometrial carcinoma (EC), in order to discuss the mechanism of action according to regulation of microenvironment of EC.Method:The 109 patients were divided into control group (54 cases) and observation group (55 cases) by random number table. Patients in control group got radiotherapy and/or chemotherapy according to different stages after operation. Patients in observation group were additionally given syndrome differentiation and treatment with Wandaitang, 1 dose/day. And a course of treatment was 3 months. Before and after treatment, symptoms, sign, functional assessment of cancer therapy-general (FACT-G) were scored. And levels of T lymphocyte subsets (CD3+ , CD4+ , CD8+ , CD4+ /CD8+ ), natural killer cell (NK), vascular endothelial growth factor (VEGF), transforming growth factor-β (TGF-β), insulin-like growth factor-1(IGF-1), interleukin-17 (IL-17) and IL-10 were detected.Result:After treatment, the scores of symptoms, signs and total scores of the patients in the observation group were lower than the control group (P<0.01). The scores of each dimension and total score of FACT-G scale in the observation group were higher than those in the control group(P<0.01). After treatment, NK, CD3 + , CD4 + and CD4 + /CD8 + in the observation group were higher than those in the control group(P<0.01), lower than the control group(P<0.01). After treatment, the serum levels of VEGF, TGF-β, IGF-1, IL-17 and IL-10 in the observation group were lower than those in the control group.Conclusion:Wandaitang can ameliorate clinical symptoms, improve quality of life of patients and immune function of organism, regulate multiple cytokines, change the tumor microenvironment of endometrial carcinoma.关键词：endometrial carcinoma;Wandaitang;quality of life;immune function;tumor microenvironment
- 17
- |
- 7
- |
- 1
发布时间：2021-02-09
Clinic
- 摘要：Objective:To explore the mechanism of Sailuotong capsules in treating acute cerebral ischemia from the perspective of metabonomics.Method:A total of 24 SD rats were randomly divided into 3 groups, including sham-operated group, model group and Sailuotong group (33 mg·kg-1). The rat model of acute multiple cerebral infarction was established by injecting fluorescent microspheres into internal carotid artery. After the successful operation, rats in Sailuotong group were administered by duodenal injection immediately, and the dosage volume was 2 mL·kg-1. Endogenous metabolites in rat brain tissues of each group were determined by UPLC-Q-TOF-MS. The relevant data and biomarkers were analyzed by principal component analysis (PCA) and partial least squares-discriminant analysis (PLS-DA).Result:The analysis of pattern recognition indicated that the metabolite profiles in model group and sham-operated group were separated obviously, and ten biomarkers related to acute cerebral ischemia were also identified. Compared with the sham-operated group, contents of N-acetylaspartate (NAA), fumaric acid, glutathione, dehydroascorbic acid, aspartic acid and S-adenosylhomocysteine were decreased, while the contents of arginine, citrulline, saccharopine and hydantoin-5-propionic acid were increased in the model group. Meanwhile, the ten abnormal biomarkers mentioned above got restoration in Sailuotong group.Conclusion:The main regulated metabolic pathways of Sailuotong capsules are NAA metabolism, arginine metabolism, energy metabolism, oxidative stress, etc.关键词：Sailuotong capsules;acute cerebral ischemia;metabonomics;biomarkers;metabolic pathways;N-acetylaspartate metabolism;arginine metabolism
- 22
- |
- 8
- |
- 4
发布时间：2021-02-09 - 摘要：Objective:To observe the metabolic characteristics of effective components from Polygonum orientale inflorescences in intestinal flora of rats.Method:The incubating samples of effective components from P. orientale inflorescences in rat intestinal flora in vitro were detected by UPLC-ESI-Q-TOF-MS/MS, the mobile phase was consisted of 0.1%formic acid solution-0.1%formic acid acetonitrile solution and eluted in gradient mode at a flow rate of 0.3 mL·min-1.The mass spectral analysis was detected with electrospray ionization under positive ion mode and negative ion mode.The metabolites and possible biotransformation pathways of effective components form P. orientale inflorescences in rat intestinal flora in vitro was analyzed by Metabolite Tools™, mass defect filtration(MDF) and other metabolite analysis techniques and combined with the accurate relative molecular weight of the compounds, the fragment ion information and the literature data.Result:Eighteen metabolites were detected after incubation of effective components from P. orientale inflorescences in rat intestinal flora.The main biotransformation pathways were reduction, oxidation, hydrolysis in Ⅰ phase reaction and methylation in Ⅱ phase reaction.Conclusion:The effective components of P. orientale inflorescences can be transformed into a variety of metabolites under the action of intestinal flora in rats.It is suggested that whether the metabolites are bioactive components should be considered when P. orientale inflorescences is used as medicine.关键词：Polygonum orientale inflorescences;effective components;mass defect filtration;intestinal flora;metabolic pathways;methylation;in vitro incubation
- 17
- |
- 7
- |
- 2
发布时间：2021-02-09
Drug Metabolism
- 摘要：Objective:The homogeneity regularity of " imprinting templates" of compound preparation of traditional Chinese medicine(TCM) was revealed, which provided the basis for effectively controlling the quality of compound preparation of TCM, by clarifying the dynamic changeability in number and content of volatile ingredients in different batches of Houttuyniae Herba.Method:The volatile oil of Houttuyniae Herba was extracted by steam distillation.The volatile components in 11 batches of Houttuyniae Herba were determined by GC-MS(electron ionization, ion source temperature of 230 ℃, detection range of m/z 40-500) combined with literature and ChemicalBook database.The relative content of each component was calculated by peak area normalization method and analyzed by the total quantum statistical moments of fingerprint.Result:There were only 15 common ingredients in the volatile oil from 11 batches of Houttuyniae Herba, accounting for 3.35%of total number and 73.94%of total content, while the number of non-common ingredients was 433, accounting for 96.65%of total number.However, the RSD of total quantum first moment of GC-MS fingerprint was 6.8%, the RSD of total quantum second moment was 14.8%(RSD of standard deviation was 7.4%), and the RSD of similarity of total quantum statistical moment was 3.8%.The type and content of volatile ingredients in Houttuyniae Herba were heterogeneous, but their chromatographic behavior of GC-MS fingerprint was uniform, the whole " imprinting templates" was similar.Conclusion:The total quantum statistical moment(similarity) of TCM fingerprint is applicable to quality control of dynamic Chinese medicines, which will play a breakthrough role in the study of homogeneity and stability of material reference and compound preparation for ancient classical formulas.关键词：famous classical formulas;material references;compound preparations;homogenization;total quantum statistical moment;Houttuyniae Herba;supramolecular;"imprinting templates"
- 21
- |
- 9
- |
- 14
发布时间：2021-02-09 - 摘要：Objective:To investigate the skin irritation of essential oils(EOs) extracted from interior-warming medicines.Method:Three EOs from interior-warming medicines(Cinnamomi Cortex, Caryophylli Flos and Alpiniae Officinarum Rhizoma) were selected as research objects.The in vitro skin cytotoxicity and in vivo skin irritation of these EOs were determined and compared.Moreover, the skin irritation was also predicted by the novel skin test panels.Result:Toxicity of these three EOs to human skin fibroblasts(HSF) was significantly different, half-inhibitory concentration(IC50) values of EOs from Cinnamomi Cortex, Alpiniae Officinarum Rhizoma and Caryophylli Flos were (11.16±0.28), (53.33±1.71), (226.70±17.61) mg·L-1, respectively.However, in vivo skin irritation evaluation showed that the local toxicity of these three EOs was in the order of EO of Cinnamomi Cortex>EO of Caryophylli Flos>EO of Alpiniae Officinarum Rhizoma. The evaluation results of skin test panels for these three EOs were in accordance with the results of in vivo skin irritation evaluation.Conclusion:Toxicity of these three EOs against skin cells in vitro is inconsistent with their in vivo skin irritation. Skin test panels are expected to be able to accurately predict in vivo skin irritation of EOs instead of cytotoxicity evaluation.关键词：interior-warming medicines;essential oils;skin cytotoxicity;in vivo skin irritation;skin test panels;half-inhibitory concentration;rhodamine B
- 23
- |
- 7
- |
- 0
发布时间：2021-02-09 - 摘要：Objective:To optimize the processing technology of Moslae Herba processed with ginger juice, and to explore the changes of its volatile components in processing process.Method:The volatile components in Moslae Herba, ginger juice and Moslae Herba processed with ginger juice were extracted by steam distillation. Volatile components in these products were analyzed by HS-GC-MS and identified by NIST 11 standard mass spectra library. Gas chromatographic conditions were as following: HP-5MS elastic quartz capillary column(0.25 mm×30 m, 0.25 μm), helium as the carrier gas, flow rate of 1.0 mL·min-1, injector temperature at 250 ℃, sample quantity of 0.2 μL, split ratio of 50∶1, temperature program for initial temperature at 40 ℃, up to 60 ℃ with the heating rate at 5 ℃·min-1, keep 2 min, up to 160 ℃ with the heating rate at 5 ℃·min-1, keep 3 min, finally rise to 250 ℃ with the heating rate at 25 ℃·min-1, keep it for 2 min and finish, mass spectrometry conditions were as following: electron impact ionization(EI), electron collision energy of 70 eV, ion source temperature at 230 ℃, the interface temperature at 280 ℃, quadrupole temperature at 150 ℃, no delay of solvent, electronic multiplier voltage at 2.188 kV, taking full scan mode, scanning range of m/z 35-550.Taking frying time, solid-liquid ratio and moistening time as factors, orthogonal test was adopted to optimize the processing technology with the comprehensive score of relative contents of thymol and carvacrol, number of volatile components and extracting amount of volatile oil as index.Result:A total of 27 volatile components were detected in Moslae Herba. There were 81 volatile components in Zingiberis Rhizoma Recens. The processed products of orthogonal test(No. 1-9) had 31, 38, 29, 35, 38, 33, 34, 22 and 26 volatile components, respectively. Extracting amount of volatile oil was in the order of Moslae Herba processed with ginger juice>Zingiberis Rhizoma Recens>Moslae Herba. The best processing technology was as following: moistening Moslae Herba with equal volume of ginger juice for 6 h, stir-frying for 8 min.Conclusion:Processing has certain impact on the extracting amount of volatile oil in Moslae Herba and the types of volatile components. This optimized technology is stable and feasible, which can provide experimental data for the quality evaluation of processed products of Moslae Herba, and lay a foundation for clarifying its processing mechanism.关键词：Moslae Herba;ginger juice;processing technology;headspace injection;gas chromatography;volatile components;orthogonal test
- 21
- |
- 8
- |
- 1
发布时间：2021-02-09
Pharmacy and Processing
- 摘要：Objective:To study the chemical constituents in 95%ethanol extract of the whole plant of Camptosorus sibiricus and determine its antioxidant activity.Method:Compounds were isolated by a combination of various chromato-graphic techniques, including column chromatography over silica gel and Sephadex LH-20 and reversed-phase HPLC. Their structures were identified on the basis of physicochemical properties and spectral data reported in the literature.Result:Eleven compounds were identified as trans-p-coumaric acid (1), trans-p-coumaric acid 4-O-β-D-glucoside (2), cis-p-coumaric acid 4-O-β-D-glucoside (3), (E)-ferulic acid-4-O-β-D-glucoside (4), caffeic acid methyl ester (5), ferulic acid methyl ester (6), syringic acid (7), syringic acid-4-O-β-D-glucopyranoside (8), protocatechualdehyde (9), vanillain (10) and syringaldehyde (11), respectively.Conclusion:Compounds 3-11 are isolated from the genus Camptosorus for the first time. In the in vitro SOD-like activity assays, compounds 7, 9-11 show an antioxidant activity with half maximal inhibitory concentration(IC50)values of 16.70, 11.70, 12.23 and 13.52 μmol·L-1, respectively.关键词：Camptosorus sibiricus;95%ethanol extract;chemical constituents;structure identification;antioxidant activity
- 23
- |
- 7
- |
- 2
发布时间：2021-02-09 - 摘要：Objective:The research group found in the early stage that the 75%alcohol extract of the Cinnamomi Ramulus had a significant physiological activity in inhibiting necroptosis by screening out the self-built sample library of 100 kinds of traditional Chinese medicines in Jiangxi. To identify the active components and find the target compounds, the 75%alcohol extracts of Cinnamomi Ramulus were isolated and studied systemically in chemistry.Method:The 20 kg dry Cinnamomi Ramulus was crushed into coarse powder, and extracted with 75%alcohol for four times, one time every 7 d. Then total extracts were obtained after solvent was recycled under decompression. The extract was separated by D101 macroporous resin column chromatography and eluted by water, 30%ethanol, 50%ethanol, 70%ethanol, 90%ethanol, so as to get the corresponding fraction finally. The compounds in the 30%ethanol and 50%ethanol fraction were isolated and purified by chromatography on silica gel, Sephadex LH-20 column and high pressure preparative chromatography, and their structures were determined according to physicochemical properties and spectral analysis.Result and Conclusion:Thirteen compounds were isolated and identified as (+ )-syringaresinol (1), (+ )-lyoniresinol (2), spicatolignan B (3), (-)-secoisolariciresinol (4), ovafolinin B (5), protocatechualdehyde (6), protocatechuic acid (7), syringaldehyde (8), vanillic acid (9), ethyl protocatechuate (10), syringic acid (11), ethyl gallate (12), 2-(3′, 4′-dihydroxyphenyl)-1, 3-pepper ring-5-aldehyde (13). Compounds 1-5, 10-13 were isolated from this plant for the first time.关键词：Cinnamomi Ramulus;75%alcohol extract;chemical constituents;structural identification
- 21
- |
- 8
- |
- 7
发布时间：2021-02-09 - 摘要：Objective:To establish a supercritical fluid chromatography(SFC) method for separating and purifying costunolide and dehydrocostus lactone in Aucklandiae Radix.Method:With supercritical carbon dioxide as the mobile phase, the effect of six factors, such as type of chromatographic columns, modifiers and modifiers ratio, flow rate of mobile phase, pressure and temperature, on the separation process of supercritical fluid chromatography were explored. The target components were separated and prepared by semi-preparative supercritical fluid chromatography. High performance liquid chromatography and nuclear magnetic resonance were used to analyze the components and study the thermodynamic regularity of the chromatographic process.Result:C18 column (10 mm×250 mm, 5 μm) was adopted, with supercritical fluid dioxide as the mobile phase, the ratio of methanol was 0.13%, the flow rate was 12 mL·min-1, column pressure was 13 MPa, column temperature was 318 ℃, and detection wavelength was 225 nm. The sample was injected for 20 times, crude extract was 4 mg, and each target component was collected according to the chromatogram. Its purity was determined to be more than 99%by HPLC, and its structure was determined as costunolide and dehydrocostus lactone by NMR. Under this condition, the SFC separation process was normal-phase chromatography.Conclusion:The method can be used to prepare effective components of Aucklandiae Radix with a high purity and low solvent residue.关键词：supercritical fluid chromatography;Aucklandiae Radix;purification;costunolide;dehydrocostus lactone
- 17
- |
- 7
- |
- 0
发布时间：2021-02-09 - 摘要：Objective:To study the secondary metabolites of the endophytic fungus Trichoderma harzianum, which was isolated from Physalis angulata.Method:The strains were cultured in a big-scale by oscillating incubator. Then the obtained culture liquid and mycelia were extracted by EtOAC and actone, respectively. The extracts were integrated after recovery of solvents, and then the active secondary metabolites were isolated and purified by comprehensive use of open ODS flash column, sephadex LH-20, HPLC, and LC-MS analysis techniques. Their structures were identified according to their physico-chemical properties and nuclear magnetic resonance (NMR) data. The cytotoxicities of the compounds were determined by methyl thiazolyl tetrazolium(MTT) assay.Result:Ten compounds isolated from T. harzianum were identified as destruxin A2(1), destruxin B2(2), 3-isobutyl-pyrrolopiperazine-2, 5-dione [cyclo (leu-pro dipeptide)] (3), cyclo (Phen-pro) dipeptide(4), cyclonerodiol(5), brevianamide F(6), N-acetyltryptamine(7), 9-hydroxyl-(2-methylpropyl) isobutyl phthalate(8), 5-hydroxy-3-hydroxymethyl-2-methyl-7-methoxychromone(9), and phenylpropionic acid(10). Compounds 1-10 didn't exhibit significant cytotoxicity to lung cancer cell line A549 in the MTT assay (IC50≥20 mg·L-1).Conclusion:All compounds were isolated from T. harzianum for the first time.关键词：Physalis angulata;endophytic fungus;Trichoderma harzianum;secondary metabolites;cytotoxicity
- 23
- |
- 7
- |
- 3
发布时间：2021-02-09 - 摘要：Objective:To prepare standard decoction of Saposhnikoviae Radix pieces, and conduct a study on the quality standards, in order to provide the scientific reference for the study of clinical application and other decoction standard decoctions.Method:By the traditional water decocting method, 11 batches of standard decoction of Saposhnikoviae Radix pieces were prepared to determine pH, prim-O-glucosylcimifugin and 4′-O-β-D-glucosyl-5-O-methylvisamminol content, calculate the paste rate and transfer rate, and investigate the feasibility of the measurement method. An analytical method for HPLC fingerprint was established. Hypersil ODS2 column (4.6 mm×250 mm, 5 μm) was adopted and eluted with methanol-water as the mobile phase in a gradient mode. The detection wavelength was 254 nm, the flow rate was 1 mL·min-1, and the column temperature was 25 ℃. The fingerprint analysis method was used to evaluate the similarity of the 11 batches of standard decoction of Saposhnikoviae Radix pieces.Result:Through the determination of 11 batches of standard decoctions of Saposhnikoviae Radix pieces, the average pH value was 5.5, the paste-out rates were between 34.3% and 46.3%, and the average paste-out rate was 41.4%, the standard deviation was 3.7%, the transfer rate of prim-O-glucosylcimifugin was 66.8%-93.5%, the average metastasis rate was 79.4%, the standard deviation was 12.1%, the transfer rate of 4′-O-β-D-glucosyl-5-O-methylvisamminol was 70.4%-98.2%, the average transfer rate was 83.40%, the standard deviation of 10.8%. The results of various methodological studies were consistent with the requirements of RSD. The fingerprinting analysis was performed using similarity evaluation software for traditional Chinese medicine fingerprints, and 9 principal common peaks were identified. The similarity was higher than 0.9.Conclusion:The quality evaluation method established in this study has a good stability, precision and repeatability. The fingerprints have a high similarity, which is suitable for the quality evaluation of standard decoctions of Saposhnikoviae Radix pieces, and can provide the scientific basis for the quality evaluation of other related preparations.关键词：Saposhnikoviae Radix;standard decoction;quality standard;fingerprint
- 18
- |
- 7
- |
- 2
发布时间：2021-02-09
Resource and Quality Evaluation
- 摘要：Objective:To explore the molecular mechanism of Lycii Fructus and Salviae Miltiorrhizae Radix et Rhizoma (FLRSM) in the treatment of retinitis pigmentosa (RP) based on network pharmacology and bioinformatics.Method:Possible intake active components and targets of FLRSM were screened out and predicted by traditional Chinese medicine systems pharmacology database and analysis platform(TCMSP). Gene targets related to RP were mined through disease gene databases. Protein-protein interaction (PPI) network of component-targets and disease-targets were mapped by functional protein association networks (STRING), and the intersection of the two networks was obtained. The gene ontology and kyoto encyclopedia of genes and genomes(KEGG) pathway of the intersection network were analyzed by the database for annotation, visualization and integrated discovery(DAVID). CytoHubba analysis was used to screen out the key targets.Result:A total of 390 active ingredients related to FLRSM were retrieved from TCMSP. According to pharmacokinetic parameters, 110 active ingredients were screened out, 19 active ingredients were further screened out, and 208 targets related to these constituents were retrieved. Totally 206 genes directly related to RP were obtained from the disease gene databases. And 79 genes were obtained from the intersection of PPI networks of component targets and disease targets. These genes mainly involved in biological processes, such as protein autophosphorylation, transcriptional regulation and cell proliferation, and the molecular functions mainly involved adenosine triphosphate binding, transcription factor activity, core promoter binding, and were enriched in nuclear, transcription factor complex, nucleus, cytoplasm and other regions. It was mainly related to neurotrophin signaling pathway, cell cycle related pathway and Wnt signaling pathway. And 8 key gene targets for FLRSM treatment of RP were identified by further screening.Conclusion:The material basis of pharmacodynamic action of FLRSM involves 19 active ingredients, such as porous sterol and tanshinone ⅡA. The key targets of FLRSM in the treatment of RP include 8 genes, such as E2F transcription factor 1(E2F1) and retinoblastoma gene1(RB1). The main mechanism is related to the regulation of neurotrophin signaling pathways, cell cycle related pathways and other signaling networks.关键词：retinal pigmentation;Lycii Fructus;Salviae Miltiorrhizae Radix et Rhizoma;network pharmacology;bioinformatics;molecular mechanism
- 21
- |
- 8
- |
- 4
发布时间：2021-02-09 - 摘要：Objective:To construct a " drug-target-pathway" network of Polygalae Radix and Gastrodiae Rhizoma in treating epilepsy, in order to explore the " multi-component, multi-target, multi-pathway" mechanism of the two kinds of traditional Chinese medicines.Method:According to the reverse pharmacophore matching method, potential targets of Polygalae Radix and Gastrodiae Rhizoma were predicted. Biological information annotation databases were used to analyze the molecular function and biological process of the action targets. Cytoscape 3.2.1 software was used to construct the " ingredient-core, target-pathway" network of Polygalae Radix and Gastrodiae Rhizoma for the treatment of epilepsy.Result:The 14 major constituents from Polygalae Radix exhibited interactions with 105 potential targets, and the 12 compounds from Gastrodiae Rhizoma showed interactions with 109 potential targets, involving several cancer signaling pathways, neuroactive ligand-receptor interaction and mitogen-activated protein kinase(MAPK) biological process played roles in the treatment of epilepsy.Conclusion:According to the screening for the potential targets relating to epilepsy and the evidences obtaining from docking study, we demonstrated that constituents from Polygalae Radix and Gastrodiae Rhizoma could play an anticonvulsant role by mediating the levels of monoamine substances. The conclusion is close to literatures published online to a certain degree, suggesting the accuracy of the study on the effect of Polygalae Radix and Gastrodiae Rhizoma in treating epilepsy according to the network pharmacology.关键词：Polygalae Radix;Gastrodiae Rhizoma;antiepilepsy;network pharmacology
- 22
- |
- 7
- |
- 3
发布时间：2021-02-09
Data Mining
- 摘要：Decoction pieces are the main body of traditional Chinese medicine (TCM) clinical medication. With the modernization of TCM medication, TCM formula granules have gradually developed and begun to take shape. Although there are processing forms of TCM injection and oral liquid, they only account for a small part of TCM market and are mainly taken orally. However, when oral administration of lipid soluble ingredients is conducted, the dissolution is limited and the absorption is relatively small. In addition, it has side effects of stimulating gastrointestinal tract, resulting in low tolerance of patients. Although there are topical preparations made by water extraction and alcohol extraction, most of them are crude preparations with random dosage, which results in the waste of lipid soluble components to a certain extent. Most of the lipid soluble components of TCM have good biological activities, such as schisandrin b, tanshinone, methyl chlorogenic acid, etc., but there is no suitable medicinal form. To make the best use of " medicine" , it is necessary to systematically study the lipid soluble components of TCM. On the basis of fairly mature extraction, separation and collection processes, a medicinal form with definite pharmacological effect and beneficial to its absorption is developed based on lipid soluble components. TCM essential oil has anti-aging, anti-dementia, anti-oxidation and other activities, which has been widely used in clinical, cosmeceuticals, health products and other fields. However, the effect of single essential oil is limited. Compatibility can not only enhance the efficacy and reduce toxicity, but also expand the application range of essential oil. Therefore, formula essential oil can be used as a new form of TCM, and mainly for external use, supplemented by internal use, to make up for the disadvantages of crude preparations and random dosing for external use of TCM, as well as the disadvantages of orally absorbed less and stimulated gastrointestinal tract, to meet the needs of clinical medication, faster, more accurate, better and stronger play the effect of lipid soluble components.关键词：formula essential oils;application form;lipid soluble components;modernization of traditional Chinese medicine
- 22
- |
- 10
- |
- 3
发布时间：2021-02-09
Academic Discussion
- 摘要：Linggui Zhugan Tang(LGZG), a representative of warming spleen to resolve fluid retention, is widely used in various diseases caused by spleen deficiency and fluid retention (SDFR). Ancient doctors mostly focused on the theme of SDFR to analysis the composition of LGZG. Modern research has now found that most of the components of LGZG contain anti-inflammatory, anti-tumor and immune-modulating effects. At present, the pharmacological research of LGZG mainly involves clearance of β-amyloid (Aβ) and anti-neuroinflammation, regulation of lipid metabolism and insulin resistance, protection of myocardial cells and regulation of liquid metabolism as follow. LGZG can promote the clearance of Aβ by regulating the expression of Aβ transporters, including low-density lipoprotein receptor-associated protein-1 and terminal glycosylation product receptors, as well as reduce the inflammation of nerve cells by inhibiting the secretion of pro-inflammatory factors such as interleukin(IL)-1β, IL-6 and tumor necrosis factor-α(TNF-α) by microglia. The prescription can also affect the lipid metabolism and insulin resistance by regulating the levels of adiponectin, insulin and leptin, thus producing therapeutic effects on metabolic syndrome and non-alcoholic fatty liver disease. The protective mechanism of LGZG on myocardial cells mainly contains inhibition of the over-activation of nuclear transcription factor-κB(NF-κB) signaling pathway, up-regulation of Smad7 expression and down-regulation of Smad3 expression, regulation of inhibitor of nuclear factor kappa-B kinase (IKK) /NF-κB inhibitor (IκB) /NF-κB signaling pathway, inhibition of inflammatory factor production, and down-regulation of Caspase-3 and Caspase-8 expression. In addition, LGZG can also regulate aquaporins to affect water metabolism. And it also has significant antioxidant effects. As is known to all, the functional mechanism of traditional Chinese medicine (TCM) compound is closely related to the network regulation of TCM disease syndromes. Considered from this angle, it is helpful to carry out the " disease-syndrome-formula" research by means of network pharmacology characterized by " disease-target-drug" , thus organically exploring the relationship between LGZG and SDFR from the microscopic perspective, and helping to explain the scientific connotation of SDFR and the biological mechanism of warming spleen to resolve fluid retention.关键词：Linggui Zhugan Tang;pharmacological mechanism;warm spleen to resolve fluid retention;spleen deficiency and fluid retention;network pharmacology
- 22
- |
- 9
- |
- 7
发布时间：2021-02-09 - 摘要：Synthetic biology is an emerging discipline that analyzes the biosynthesis pathways of active constituents in traditional Chinese medicine and explores genes involved in biosynthesis. Bupleuri Radix is one of the most commonly used Chinese medicinal materials with remarkable medicinal value, its index component is saikosaponins, which has significant anti-inflammatory, anti-viral and anti-tumor activities. However, the current wild resources of Bupleuri Radix have been destroyed, and there were some problems in the process of artificial cultivation. The application of biological culture technology and synthetic biology can expand the sources of saikosaponins and protect resources of Bupleuri Radix. The culture conditions of different plants can be followed without a fixed pattern, and the biosynthetic pathways of different medicinal active ingredients are also inconsistent. At present, there is no review report on the culture technology of Bupleuri Radix and the research on the biosynthesis pathway of saikosaponins. This paper introduces the research progress of biological culture techniques, such as callus culture, adventitious root culture, hairy root culture and suspension cell culture used in synthetic biology, and the biosynthesis pathway of saikosaponins and its key enzyme functional genes. It is suggested to optimize the biological culture technology of Bupleuri Radix by referring to the tissue culture technology of other traditional root medicinal materials, so as to provide a reference for the in-depth study on the biosynthesis pathway and metabolic regulation of saikosaponins.关键词：Bupleuri Radix;biological culture technique;saikosaponins;synthetic biology;adventitious roots;culture conditions;omics
- 21
- |
- 9
- |
- 2
发布时间：2021-02-09
Review
- Postal code：100700
- Tel：010-84076882 Email：syfjx_2010@188.com
- Technical support is provided by Beijing Founder electronics co., LTD 京ICP备11006657号-10
京公网安备11010802024621 - It is recommended to read the content of this site in Chrome&IE9+. Please switch to extreme mode in browser 360.
- Cookies We use cookies to help provide and enhance our service and tailor content. By continuing, you agree to the use of cookies.
0