Abstract：Objective:To investigate the effect of modified Si Junzitang on angiogenesis in transplanted tumor of H22 tumor-bearing mice.Method:The effect of modified Si Junzitang on tumor inhibition and growth of peripheral blood vessels in tumor-bearing mice was observed by tumorigenesis experiment in mice. Hematoxylin-eosin (HE) staining and immunohistochemistry (IHC) were used to detect the distribution of blood vessels and the expression of vascular endothelial markers (CD31) in tumor-bearing mice. Reverse transcription-polymerase chain reaction (RT-PCR) was used to detect the mRNA expression levels of vascular endothelial growth factor (VEGF), vascular endothelial growth factor receptor 2 (VEGFR2) and tumor necrosis factor-α (TNF-α) in tumor tissue.Result:The inhibition rates of modified Sijunzi Tang in low-dose group (ig, 11.83 mg·kg-1·d-1), middle-dose group (ig, 23.66 mg·kg-1·d-1) and high-dose group (ig, 47.32 mg·kg-1·d-1) were 29.97%, 59.80%and 82.34%, respectively. Compared with the model group, the average tumor weight was lower in middle and high-dose groups, with statistically significant differences (P<0.05). Through the observation of the number and morphology of pericardial vessels, the number of pericytes in middle and high-dose modified Sijunzitang groups was reduced compared with the model group(P<0.05), and the vascular lumen was narrow. HE staining showed that the distribution of blood vessels in middle and high-dose modified Si Junzitang groups was less than that of the model group. IHC showed that the positive expression of CD31 in each dose modified Si Junzitang group was lower than that in the model group (P<0.01). RT-PCR showed that the mRNA expressions of VEGF, VEGFR2 and TNF-α in middle and high-dose modified Si Junzitang groups were lower than those in the model group (P<0.01).Conclusion:Modified Si Junzitang can inhibit the tumor growth of H22 tumor-bearing mice and the angiogenesis of transplanted tumors, which may be related to the reduction of TNF-α, VEGF and VEGFR2 expression levels.
Abstract：Objective:To explore the effect of Zhizhuwan on intestinal conduction and expressions of Phospholipase C-γ1 (PLC-γ1)/Phospholipase C-γ2 (PLC-γ2) signaling pathway of slow transit constipation (STC) with spleen deficiency syndrome.Method:Special pathogen free (SPF) healthy mice were randomly divided into normal group and model making group. Folium Sennae gavage was used to induce the spleen deficiency status, and then diet and drinking water were controlled to establish the mice model of spleen deficiency constipation. After the modeling, the mice in modelling group were randomly divided into model group, Zhizhuwan group and mosapride group. Zhizhuwan group was given drug at the dose of 9.0 g·kg-1·d-1, mosapride group was given 2.5 mg·kg-1·d-1, model group and normal group were given the equal dose of distilled water for 7 consecutive days. At the end of the treatment, the length of Indian ink in the colon was used to calculate the intestinal propulsion rate of the mice. The D-xylose kit was used to determine the content of D-xylose in serum of mice. The hematoxylin eosin (HE) staining was used to observe the pathological changes of colon tissues in mice. The immunohistochemistry and Western blot were used to detect the expression levels of PLC-γ1 and PLC-γ2 proteins in colon tissues of mice. Real-time PCR was used to detect the mRNA expression levels of PLC-γ1 and PLC-γ2.Result:Compared with normal group, the intestinal propulsive rate and the serum D-xylose value in model group were significantly decreased (P<0.01). Obvious hyperemia and edema of colonic mucosa were observed by HE staining. The protein and mRNA expression levels of PLC-γ1 and PLC-γ2 in colon tissues were significantly decreased (P<0.01). Compared with model group, the intestinal propulsion rate and the content of D-xylose in Zhizhuwan group and mosapride group were significantly increased (P<0.01). Colonic mucosal hyperemia, edema and inflammatory cell infiltration were improved according to HE staining. The protein and mRNA expression levels of PLC-γ1 and PLC-γ2 were significantly increased (P<0.01).Conclusion:Zhizhuwan can promote the intestinal movement in slow transit constipation model mouse with spleen deficiency syndrome, and alleviate the symptoms of constipation in mice. The related mechanism may be related to the increase of the expressions of PLC-γ1 and PLC-γ2 in colon tissues of mice with spleen deficiency and constipation.
Abstract：Objective:To observe the clinical efficacy of modified Shenling Baizhu San combined with thyroxine tablets in the treatment of Hashimoto's thyroiditis (HT).Method:The 68 patients with HT were randomly divided into treatment group and control group, with 34 patients in each group. Control group was treated with thyroxine tablets alone, while treatment group was treated with modified Shenling Baizhu San in addition to the therapy of control group. Free triiodothyronine (FT3), free Thyroxine (FT4), thyroid stimulating hormone (TSH), serum thyroid peroxidase antibody (TPOAb) and thyroglobulin were observed before and after treatment in the two groups of HT patients. The changes of thyroglobulin antibody (TgAb) and traditional Chinese medicine (TCM) syndrome score, and the safety of TCM prescription were observed.Result:After 3 months of treatment, the effective rate of treatment group was 91.2%, which was significantly higher than 70.6% of control group, with statistically significant difference (P<0.05); after 3 months of treatment, the scores of TCM syndromes in two groups were significantly lower than those before treatment (P<0.05), and the scores of TCM syndromes in treatment group were significantly lower than those in control group (P<0.05). FT3 and FT4 in treatment group and control group increased significantly after 3 months of treatment (P<0.01), but treatment group increased more significantly than control group (P<0.01); TSH, TgAb and TPOAb in treatment group and control group decreased significantly after 3 months of treatment (P<0.05), and treatment group decreased more significantly than before treatment (P<0.05), with no adverse reaction during the treatment.Conclusion:Modified Shenling Baizhu San combined with thyroxine tablets in the treatment of HT is more effective than simple thyroxine tablets, which is worthy of further clinical and experimental study.
Keywords：Shenling Baizhu San;Hashimoto's thyroiditis (HT);integrated traditional Chinese and western medicine;clinical observation;adverse reactions
Abstract：Objective:To explore the molecular mechanism of cantharidin(CTD) in inducing morphological changes and dissociation in human colon cancer HCT116 cells, in order to study the correlation with tumor metastasis and provide a new basis for clinical use of cantharidin.Method:Different concentrations of CTD (0, 2.5, 5, 10, 15, 20 μmol·L-1) were added to each hole to culture for 7 to 10 days, so as to determine the inhibitory effect of CTD on HCT116 cells; and changes of F-actin cytoskeleton and integrin in HCT116 cells were detected by immunofluorescence staining. Western blot analysis of protein expressions of RhoA, RhoB, RhoC, Cdc42 and Rac1/2/3 of Rho family were performed before and after cantharidin treatment. overexpression of RhoA was constructed by plasmid transient transfection, and effect of 10 μmol·L-1 cantharidin on the morphology and adhesion of overexpressing cells was also observed.Result:Cantharidin induced cytoskeletal remodeling and decreased integrin content in HCT116 colon cancer cells. RhoA protein was a member of Rho enzyme family with the greatest variation after cantharidin action. The proportion of transfected RhoA cells with green fluorescence was about 60%, the expression of RhoA protein in constructed RhoA overexpression cells was significantly increased, compared with wild-type HCT116 cells (P<0.01). However, cantharidin can act on RhoA overexpressed HCT116 cells, reverse its overexpression(P<0.01), and affect its morphology.Conclusion:Cantharidin can inhibit the expression of RhoA protein, induce the morphological changes of HCT116 cells and weaken the adhesion to the basement, thereby inhibiting cell migration.
Abstract：Objective:To study the effect of Shenlian extract (SL extract) on macrophage function and inflammatory resolution in lipid peroxidation inflammatory injury models.Method:The effects of different concentrations of SL extract (2.5, 5.0, 10.0, 20.0 mg·L-1) on the polarization type, foam formation and chemotactic function of macrophages were detected with RAW264.7 cells induced by oxidized low-density lipoprotein(ox-LDL). Western blot was used to detect pro-inflammatory resolution factor arachidonate 5-lipoxygenase(ALOX5) and inducible inducible nitric oxide synthase(iNOS), and phosphorylated p65 (p-p65) and phosphorylated IκK (p-IκK) in nuclear factor(NF)-κB related signaling pathways.Result:Compared with the control group, ox-LDL enhanced the expressions of M1 macrophage markers TNF-α, IL-1β, iNOS (P<0.01), inhibited the expressions of IL-10 of M2 markers, promoted foam cell formation (P<0.01), induced THP-1 chemotaxis ability, increased the content of MCP-1 (P<0.01), and inhibited the expression of ALOX5.Compared with the model group, SL extract reduced the expressions of TNF-α, IL-1β, and iNOS (P<0.01), increased the expression of IL-10 (P<0.05), and down-regulated the formation of foam of macrophages (P<0.01). In transwell assay, SL extract obviously decreased the MCP-1 secretion and the number of chemotaxis cells (P<0.01), and promoted the increase of the inflammatory resolution factor ALOX5.The phosphorylation of p65 and IκK was inhibited significantly (P<0.01).Conclusion:In the inflammatory damage model of lipid peroxidation, SL extract can regulate the polarization of macrophage, inhibit the chemotaxis and foaming of ox-LDL, increase the inflammatory resolution molecular expression, and improve the state of lipid peroxidation, which may be related to the inhibition of NF-κB signaling pathway.
Abstract：Objective:To explore the effective dose range of Kaihoujian throat spray (for children) in treating acute pharyngitis and acute tonsillitis, in order to provide the reference for the usage and dosage in clinic.Method:A total of 160 juvenile SD rats were divided into 16 groups according to the body mass grade, namely normal group, model group, amoxicillin or ribavirin group, compound Yizhi Huanghua group and different doses of Kaihoujian (for children) groups. The different doses of Kaihoujian (for children) groups were divided into 12 treatment groups based on 2 sprays/time, 4 times/day, 4 sprays/time, 4 times/day, 6 sprays/time, 4 times/day, 8 sprays/time, 4 times/day, 2 sprays/time, 6 times/day, 4 sprays/time, 6 times/day, 6 sprays/time, 6 times/day, 8 sprays/time, 6 times/day, 2 sprays/time, 8 times/day, 4 sprays/time, 8 times/day, 6 sprays/time, 8 times/day, and 8 sprays/time, 8 times/day. Except for normal group, all of the remaining groups were included in three animal models, namely 5%ammonia-induced acute pharyngitis in rat, B type streptococcus haemolyticus-induced acute pharyngitis and tonsillitis in rabbit, and adenovirus-induced acute pharyngitis in mice. Then the optimal usage and dosage of Kaihoujian throat spray (for children) were evaluated based on pharyngeal lesion score and htoxylin eosin(HE) staining.Result:There were significant differences in pharyngeal and tonsil lesions between the model group and the normal group (P<0.01). All of the 12 treatment groups could alleviate pharyngeal and tonsil lesions in three animal models, and the best dose range with significant potency were 4~8 sprays/times, 6 times/day and 2~6 sprays/times, 8 times/day(P<0.05, P<0.01).Conclusion:The clinical usage and dosage of Kaihoujian throat spray (for children) in treating acute pharyngitis and tonsillitis were suggested to be 2 sprays/times, 6~8 times/day for 1~3 year-old children; 3~6 sprays/times, 6~8 times/day for 4~6 year-old children and 5~8 sprays/times, 6~8 times/day for 7~12 year-old children.
Abstract：Objective:To explore the protective effect of Tianlong Tongxin tablet on myocardial ischemia reperfusion injury in rats, and observe its effect on thrombosis, blood viscosity and platelet aggregation in rabbits.Method:Totally 56 Wistar rats were collected. Except for the sham operation group, all of the remaining rats were involved in the establishment of the rat myocardial ischemia reperfusion injury model. The successfully established model was divided model group, Hexinshuang group, compound Danshen tablet group and Tianlong Tongxin tablet groups (4, 2, 1 g·kg-1 ). Nitrotetrazolium blue (N-BT) method was used to observe the alleviation of myocardial infarction. Colorimetry was used to detect the effect of the test drug on serum superoxide dismutase (SOD) and malondialdehyde (MDA). The Chandler in vitro method was used to detect thrombosis and blood viscosity in vitro of control group, Tianlong Tongxin tablets groups (4, 2, 1 g·kg-1), compound Danshen tablets group and aspirin group. The Born turbidimetric method was used to observe the platelet aggregation levels of control group, Tianlong Tongxin tablets groups (2, 1, 0.5 g·kg-1), compound Danshen tablets group and aspirin group.Result:Compared with the sham operation group, the myocardial infarction area, serum SOD and MDA in the model group were significantly increased (P<0.05). Compared with the model group, Tianlong Tongxin tablets groups, Hexinshuang group and compound Danshen tablets group could reduce the degree of myocardial infarction, and the percentage of infarction area in the ventricle and heart decreased significantly (P<0.05, P<0.01). Compared with the control group, Tianlong Tongxin tablets groups (4, 2 g·kg-1), compound Danshen tablets group and Aspirin tablets group could significantly shorten the length of thrombosis (P<0.05, P<0.01), and significantly reduce the wet weight and dry weight of thrombosis (P<0.05, P<0.01). In addition, the whole blood viscosities under 150, 60 and 5 s-1 shear rates were significantly reduced (P<0.05, P<0.01). Compared with the control group, the platelet aggregation rates induced by collagen, adenosine bisphosphate (ADP) and arachidonic acid (AA) in rabbits were significantly reduced in Tianlong Tongxin tablet group (2, 1 g·kg-1), compound Danshen tablet group and Aspirin tablet group (P<0.05, P<0.01).Conclusion:Tianlong Tongxin tablet can protect rat myocardial ischemia reperfusion injury, inhibit platelet aggregation and thrombosis, and reduce blood viscosity.
Abstract：Objective:To study the protective effect of dihydroartemisinin (DHA) on adjuvant-induced arthritis (AIA) and collagen-induced arthritis (CIA) in rats, in order to explore its possible mechanism.Method:Wistar rats were randomly divided into eight groups, namely AIA control group, AIA model group, AIA DHA group and AIA methotrexate group, CIA control group, CIA model group, CIA DHA group and CIA methotrexate group. To establish adjuvant-induced arthritis (AIA) model, rheumatoid arthritis rats were induced through intradermal injection with 0.1 mL Freund's complete adjuvant (FCA) into right postpedes except for the control group. To establish the model of collagen-induced arthritis (CIA), except for control group, the caudal root of rats was immunized subcutaneously with 0.2 mL of emulsion containing 1 g·L-1 of Collagen type Ⅱ (CⅡ). One week later, CⅡ emulsion was injected for the second time. After the rheumatoid arthritis model was successfully established and the administration with DHA (30 mg·kg-1·d-1), the anti-inflammatory effect of DHA on AIA/CIA rats was observed, including the arthritis index (AI), paw swelling degree and effect of DHA on immune organ index of AIA/CIA rats. Interleukin (IL)-6 levels in serum was detected by enzyme-linked immunosorbent assay (ELISA) and pathological sections of ankle joints of AIA/CIA rats. RAW264.7 macrophage cells were cultured in vitro and treated with DHA at various doses (0.5, 1, 2, 4, 8, 16 μmol·L-1) for 24 h, and the cell viability was detected by methyl thiazolyl tetrazolium(MTT) assay. Lipopolysaccharides (LPS) group, LPS+ DHA groups (0.5, 1, 2 μmol·L-1) and control group were established. The level of IL-6 was detected by enzyme-linked immunosorbent assay(ELISA). The protein expression levels of nuclear transcription factor-κB p65 (NF-κB p65) was tested by Western blot.Result:Compared with control group, the paw swelling, AI, spleen index and IL-6 levels of model group were significantly increased (P<0.01, P<0.05). DHA could significantly reduce paw swelling (P<0.05), arthritis score index (P<0.05), and spleen index (P<0.01), thymus index (P<0.05) and serum IL-6 level of AIA rats (P<0.05). But the spleen index of CIA rats was not decreased, while the thymus index and IL-6 level were decreased but not statistically significant. In addition, DHA can significantly improve the pathological changes of ankle, and decrease the pathological score on AIA/CIA rats (P<0.01). Compared with control group, DHA (4, 8, 16 μmol·L-1) groups had a remarkable effect on the cell viability (P<0.05, P<0.01). The safe medication range of DHA was less than 2 μmol·L- 1. The level of IL-6 and the protein expression of NF-κB p65 in LPS group were higher than those of control group. Compared with LPS group, DHA (0.5 μmol·L-1) groups could significantly reduce the secretion of IL-6 (P<0.05), and inhibit the expression of NF-κB p65.Conclusion:DHA can alleviate the ankle joint lesion on rheumatoid arthritis rats. Its mechanism may be related to NF-κB signal pathway.
Abstract：Objective:To observe the regulatory effect of Guben Fangxiao decoction on Toll-like receptor (TLR)4, TLR7, nuclear factor-kappa B p65 (NF-κB p65) and NF-κB inhibitor protein alpha (IκBα) in mice with asthma remission, in order to explore the mechanism of Guben Fangxiao decoction in treating asthma remission.Method:Respiratory syncytial virus (RSV) combined with chicken ovalbumin (OVA) was used to build asthma remission model in 3-week-old BALB/c mice. Sixty mice were divided into blank group, model group, dexamethasone group (0.001 g·kg-1), low, medium and high-dose Guben Fangxiao decoction group (6.5, 13, 26 g·kg-1), respectively. Intervention was given once a day for 28 days. After administration, the mice were put to death. Hematoxylin-eosin (HE) staining was used to observe the pathological changes of lung tissue and score the pulmonary inflammation. Western blot was used to detect the expressions of TLR4, TLR7, IκBα and nuclear NF-κB p65 in lung tissue of mice. Immunofluorescence was used to observe the expression of NF-κB p65 in cellnucleuses.Result:Compared with blank group, the lung tissue of model group showed obvious inflammatory cell infiltration (P<0.01) and bronchial stenosis, the nuclear distribution of NF-κB p65 increased significantly (P<0.01), and the expressions of TLR4, TLR7 and IκBα proteins increased significantly (P<0.05). Compared with the model group, Guben Fangxiao decoction could significantly alleviate the inflammatory infiltration of lung tissue in mice (P<0.01), reduce the expression of nuclear protein NF-κB p65 (P<0.01), relieve the nuclear entry of nuclear protein NF-κB p65 (P<0.01), and increase the expressions of TLR4, TLR7 and IκBα proteins (P<0.01).Conclusion:Guben Fangxiao decoction can alleviate airway inflammation, and its therapeutic effect may be achieved by regulating TLR4, TLR7, NF-κB p65 and IκBα.
Abstract：Objective:To observe the effect of astragalus polysaccharide (APS) on taste receptor 1 member 2 (T1R2)/taste receptor 1 member 3 (T1R3) sweet taste receptor pathway in intestine of rat model induced by high-sugar and high-fat diet.Method:SD rats were randomly divided into normal group, high-sugar and high-fat group and astragalus polysaccharide group. Rats in high-sugar and high-fat group and astragalus polysaccharide groups were fed with high-sugar and high-fat diet for 16 weeks, while rats in astragalus polysaccharide group were fed with APS (0.7 g·kg-1, per day) for 8 weeks during this period. Serum samples were collected to determine the levels of fasting blood glucose, total cholesterol (TC), triglyceride (TG), high-density lipoprotein cholesterol (HDL-C) and low-density lipoprotein cholesterol (LDL-C). Intestinum tenue was collected to determine mRNA expressions of T1R2/T1R3, α-gustducin (Gα gust), transient receptor potential cation channel subfamily member 5 (TRPM5) and proglucagon (PG) gene by Real-time PCR, and protein expressions of T1R2, Gα gust and glucagon-like peptide-1 (GLP-1) protein by Western blot.Result:Rats in high-sugar and high-fat group had significantly higher levels of TC, TG and LDL-C, and lower HDL-C level in serum than those in normal group (P<0.05). Moreover, the expression levels of sweet receptor pathway molecules, including T1R2, Gα gust and PG genes in intestine, were significantly down-regulated in high-sugar and high-fat group (P<0.05). Rats in astragalus polysaccharide group had significantly lower levels of TC, TG and LDL-C, and higher HDL-C level in serum than those in high-sugar and high-fat group (P<0.05). The expression levels of T1R2, T1R3, Gα gust, TRPM5 and PG genes in intestine were significantly up-regulated in astragalus polysaccharide group (P<0.05). The trend of T1R2, Gα gust and GLP-1 protein expressions was consistent with that of T1R2, Gα gust and GLP-1 mRNA expressions. Protein expressions of T1R2, Gα gust and GLP-1 and mRNA expression of T1R3 were significantly lower in astragalus polysaccharide group than those of control group (P<0.05).Conclusion:APS could improve disturbance of lipid metabolism and impairment of intestinal sweet taste receptor pathway for rat model induced by high-sugar and high-fat diet.
Keywords：high-sucrose and high-fat diet;sweet taste receptor pathway;astragalus polysaccharides;proglucagon gene;taste receptor 1 member 2/taste receptor 1 member 3
Abstract：Objective:To observe the clinical efficacy of Jianpi Qingchang decoction in the treatment of spleen deficiency and damp-heat hormone-dependent ulcerative colitis and explore its possible target.Method:A total of 60 patients with spleen deficiency and damp-heat hormone-dependent ulcerative colitis were selected and collected from the outpatient department and the inpatient department of Longhua Hospital affiliated to Shanghai University of Chinese Medicine on April 31, 2012.Two groups were given the basic therapy of prednisone, and control group received orally bolus for spleen and spleen and intestines, 6 g/time, 3 times/d. The treatment continued for three months. The experimental group was given orally Jianpi Qingchang decoction, 1 dose per day, and 300 mL water decoction, 150 mL each time, 2 times /d, and took at different temperatures in the morning and evening. The treatment continued for three months. After treatment, changes in intestinal symptom score, traditional Chinese medicine (TCM) syndrome score and endoscopic score of two groups were observed.Result:Compared with before treatment, the symptom scores of diarrhea, mucous purulent in control group were significantly reduced after treatment (P<0.01). The scores of mucous purulent and bloody stool, diarrhea, abdominal pain, and tenesmus were significantly reduced in experimental group (P<0.01), and the scores of mucous purulent and bloody stool, and symptom of diarrhea were significantly decreased in experimental group after treatment than that of control group (P<0.01). Before treatment, the scores of TCM syndromes in two groups were compared, with no statistically significant difference. After treatment, the scores of TCM syndromes of two groups were significantly reduced (P<0.01), and the reduction of the experimental group was more significant than that of control group (P<0.05). Compared with before treatment, the endoscopy scores of two groups were significantly reduced after treatment (P<0.01), and the decrease of the experimental group was more significant than that of control group (P<0.01). Mayo scores were significantly reduced in both groups after treatment compared with that before treatment (P<0.01), and significantly reduced in the experimental group compared with control group (P<0.05).Conclusion:Jianpi Qingchang decoction can effectively improve mucous purulent stool and diarrhea symptoms in patients with spleen deficiency and damp-heat hormone-dependent ulcerative colitis, and reduce TCM syndrome score and endoscopic score, and thus is worthy of clinical reference and promotion.
Abstract：Objective:To explore the clinical efficacy of Modified Qingqi Huatan Wan in treatment of acute exacerbation of chronic obstructive pulmonary disease and its effect on inflammatory reaction, airway remodeling and thrombokinesis.Method:A total of 80 patients of acute exacerbation of chronic obstructive pulmonary disease (AECOPD) were randomly divided into control group (40 cases) and therapy group (40 cases) by random number table. The control group was treated with conventional therapy. In addition to the therapy for the control group, the patients in therapy group also received modified Qingqi Huatan Wan. The treatment course was 14 days for both groups. Scores of traditional Chinese medicine(TCM) syndrome, chronic obstructive pulmonary disease and asthma physiology Score (CAPS), and chronic obstructive pulmonary disease patients self-assessment test questionnaire (CAT) were compared. The secondary indicators were pulmonary function, arterial blood gas analysis, and blood rheology indexes. In addition, the levels of serum nuclear factor kappa B (NF-κB), interleukin-6 (IL-6), interleukin-8 (IL-8), matrix metalloproteinase-2 (MMP-2), tissue inhibitor of metalloproteinase-2 (TIMP-2), transforming growth factor-beta1 (TGF-β1) and plasma tissue-plasminogen activator (t-PA), plasminogen activator inhibitor-1 (PAI-1), von-willebrand factor (v-WF), clinical efficacy and safety were evaluated.Result:The total clinical effective rate was 94.74% in therapy group, which was higher than 78.38% in control group (χ 2=4.341, P<0.05). After treatment, scores of TCM syndrome, CAPS, CAT and levels of PaCO2, serum NF-κB, IL-6, IL-8, MMP-2, TIMP-2, TGF-β1 and plasma PAI-1, v-WF in therapy group were lower than those in control group(P<0.05). However, levels of plasma t-PA, SaO2, PaO2, FEV1, FEV1%, FEV1/FVC in therapy group were higher than those in control group(P<0.05), therapy group was alleviated more than control group (P<0.05).Conclusion:Modified Qingqi Huatan Wan can control the symptoms safely, alleviate CAPS and lung function, effectively reduce the inflammatory response and inhibit the formation of airway remodeling and thrombosis, and its mechanism may be protect the lung tissue by reducing the level of inflammatory cytokines, regulating the balance of MMP-2/TIMP-2 and t-PA/PAI-1 and improving extracellular matrix and vascular endothelial function.
Keywords：acute exacerbation of chronic obstructive pulmonary disease;airway remodeling;thrombokinesis;matrix metalloproteinase-2/tissue inhibitor of metalloproteinase-2 (MMP-2/TIMP-2);plasma tissue-plasminogen activator/plasminogen activator inhibitor-1 (t-PA/PAI-1);modified Qingqi Huatan Wan
Abstract：Objective:To observe the effect of Erbao grains on levels of immunoglobulin, T cells, secretory immunoglobulin A from feces, and intestinal microecology index of children with diarrhea due to spleen deficiency.Method:One hundred and eighty patients with diarrhea due to spleen deficiency were randomly divided into control group (90 cases) and observation group (90 cases) by random number table. Patients in control group got Montmorillonite powder. In addition to the therapy in control group, patients in observation were additionally given Erbao grains. And the course of treatment was 10 days. Before and after treatment, levels of serum immunoglobulin G (IgG), IgM, IgA, CD3+ , CD4+ , CD8+ , ratio CD4+ and CD8+ , secretory immunoglobulin A from feces (SIgA), activity of salivary amylase and urine D-xylose were detected, the main symptoms and signs were scored, and the safety was discussed.Result:After treatment, the clinical total effective rate in observation group was 95.56%, which was higher than 80%in control group (χ2=10.149, P<0.01). Compared with the data before the treatment, levels of IgG, IgM, IgA and SIgA in observation group increased (P<0.05), which were higher than those in control group (P<0.05). After treatment, levels of CD3+ , CD4+ , CD4+ /CD8+ , activity of salivary amylase and urine D-xylose were higher than those in control group (P<0.05). Score of the main symptoms and signs were lower than those in control group (P<0.05).Conclusion:In addition to the therapy of Montmorillonite powder, Erbao grains can relieve the symptoms of children with diarrhea due to spleen deficiency, improve the efficacy, and ameliorate immunity of children.
Abstract：Objective:To observe the effect of addition and subtraction therapy of Guyinjian on oocyte quality, pregnancy outcome and ovarian reserve function in patients with poor ovarian response (POR) with kidney Yin deficiency syndrome.Method:Ninety patients were randomly divided into control group (45 cases) and observation group (45 cases) by random number table. The patients in both groups got antagonist. Based on such treatment, the patients in observation received additional addition and subtraction therapy of Guyinjian. The using time and amount of gonadotropin (Gn), ovum taking cycle, cycle canceling rate, fertilization rate, available embryo rate, quality embryo rate, ovulation cycle clinical pregnancy rate were recorded. Levels of follicle stimulating hormone (FSH), luteinizing hormone (LH), serum estradiol (E2) and endometrial thickness, anti mullerian hormone (AMH), resistance index (RI), pulsation index (PI), end diastolic velocity (EDV) and peak systolic velocity (PSV) were detected. Ratio of PSV/EDV (S/D) was calculated, and scores of kidney yin deficiency syndrome were graded before and after treatment.Result:Total amount of Gn in observation group was less than that in control group (P<0.01), but there was no statistically significant difference in Gn using days and ovum taking cycle between two groups. On the trigger day, level of FSH in observation group was lower than that in control group (P<0.01), while levels of LH and E2 were higher than those in control group (P<0.01). Endometrial thickness was superior to that in control group (P<0.01), and number of acquired eggs was larger than that in control group (P<0.01). Cycle canceling rate in observation group was 13.33%, lower than 17.91%in control group, and the quality embryo rate was 41.86%in observation group, higher than 31.43%in control group; ovulation cycle clinical pregnancy rate was 25%in observation group, higher than 11.94%in control group, but with no statistically significant differences. The fertilization rate was 82.12%in observation group, higher than 72.96%in control group (χ2=5.124, P<0.05). Available embryo rate was 73.71%in observation group, higher than 60.34%in control group (χ2=5.767, P<0.05). After treatment, level of AMH in observation group was higher than that in control group (P<0.01). Score of kidney Yin deficiency syndrome in observation group was lower than that in control group (P<0.01). And levels of RI, PI and S/D were lower than those in control group (P<0.01), while levels of PSV and EDV were lower than those in control group (P<0.01).Conclusion:Addition and subtraction therapy of Guyinjian can increase ovarian blood supply, improve high ovarian reserve function, reduce Gn consumption, increase number of acquired eggs, alleviate symptoms of kidney yin deficiency, and can ameliorate ovarian responsiveness and pregnancy outcome.
Abstract：Objective:To investigate the tissue distribution of major bioactive components from Gegen qinlian Tang(GQT) in rats, and to reveal the mechanism for the efficacy of GQT by the tissue targeting of its bioactive ingredients in vivo.Method:After oral administration of GQT in rats, tissues were collected at different time points, including small and large intestine, liver, heart, spleen, lung, and kidney.Samples were prepared for determination of 14 bioactive components of GQT in tissue homogenate by HPLC-MS/MS.The chromatography separation was performed on an Agilent ZORBAX SB-C18 column(2.1 mm×100 mm, 3.5 μm) with acetonitrile-0.1% formic acid in water for gradient elution.Electrospray ionization(ESI) was applied and operated in the positive ion mode.Meanwhile, naringin was used as the internal standard for determining.Result:HPLC-MS/MS for simultaneous determination of 14 components from GQT in tissue homogenate was developed and validated by specificity, calibration curves, recovery test, matrix effect, precision, accuracy, and stability.In the small intestine, the the area under the curve(AUC0-10 h) of major isoflavonoids(puerarin, 3′-hydroxypuerarin, and daidzein) were 22 174.9, 15 893.1, 3 882.5 h·mg·L-1, major flavonoids(baicalein, wogonin, wogonoside, and baicalin) were 15 423.6, 15 408.4, 7 017.3, 3 697.7 h·mg·L-1, and major alkaloid(berberine) was 2 544.0 h·mg·L-1, respectively.The distribution of these ingredients in the small intestine was significantly higher than that in other tissues.Conclusion:The effective ingredients of GQT are mainly distributed in the intestinal tissues, which speculates that the anti-inflammatory and antidiarrheal activities of GQT may be related to its targeting in the intestine.
Abstract：Objective:To study on the pharmacokinetics and tissue distribution of baicalin magnesium salt in rats after tail vein injection, and compare pharmacokinetic differences between baicalin magnesium salt and baicalin.Method:After tail vein injection of baicalin magnesium salt and baicalin, orbital blood was collected at different time points.The drug concentration was measured by HPLC, the drug concentration-time curve was plotted, the pharmacokinetic parameters were calculated with DAS 3.0 software, SPSS 19.0 software was used for statistical analysis.At the same time, the drug distribution in heart, liver, spleen, lung and kidney was measured at different time points after tail vein injection of baicalin magnesium salt.Result:When the dose of baicalin magnesium salt was 25-100 mg·kg-1, area under the curve(AUC0-t and AUC0-∞) showed a good linear relationship with the dose(r>0.95), but most of the other pharmacokinetic parameters had no significant difference between different dose groups.The mean residence time(MRT0-t) of medium dose group of baicalin magnesium salt was significantly higher than that of equal molar dose group of baicalin.After intravenous injection of baicalin magnesium salt, the drug concentration was the highest in each tissue at 0.25 h, and the concentration of target component decreased rapidly at 0.75 h. The distribution of target component in kidney was the most, followed by lung.Conclusion:After injection, the baicalin magnesium salt can be rapidly distributed and quickly eliminated in vivo, which is mainly excreted from the kidney.
Abstract：Objective:To prepare magnetic solid lipid nanoparticles co-loaded quercetin and resveratrol(QR-MSLN), develop the reasonable characterization method, and investigate its inhibitory effect on transplanted hepatocarcinoma H22 tumor in mice.Method:Magnetic Fe3O4 particles coated with oleic acid(OA-Fe3O4) were synthesized and its structure was confirmed by Fourier transform infrared spectrometer(FT-IR). QR-MSLN was prepared by emulsion ultrasonic dispersion method, its morphology was examined by transmission electron microscopy, its particle size was determined by laser particle sizer.Concentration of Fe in the preparation was determined by phenanthroline spectrophotometry.The entrapment efficiency, saturation magnetization, in vitro release behavior were investigated by ultrafiltration centrifugation, vibrating sample magnetometer(VSM) and dialysis method, respectively.Mouse tumor model transplanted with hepatoma H22 ascites tumor was established and antitumor effect of QR-MSLN on H22 bearing mice were observed in the presence of an applied magnetic field.Result:Morphology of QR-MSLN was round, and black magnetic particles could be observed inside it, its particle size was (171.9±2.2) nm, the concentration of Fe was (1.40±0.46) g·L-1.The preparation exhibited apparent superparamagnetism and the saturation magnetization was 7.75 A·m2·kg-1.The entrapment efficiencies of quercetin and resveratrol in QR-MSLN were 99.10% and 80.83%, respectively.QR-MSLN had a significantly higher effect of tumor inhibition than SLN(containing quercetin and resveratrol) and free drug(P<0.01).Conclusion:QR-MSLN has uniform particle size and good magnetic response, and shows remarkable antitumor effect on H22 bearing mice.
Abstract：Objective:HPLC for the determination of five components in Descurainiae Semen was established to investigate the change rule of contents of five components in the herb before and after being processed.Method:The contents of quercetin-3-O-β-D-glucose-7-O-β-D-gentiobioside(QGG), sinapic acid, quercetin-3-O-β-D-glucopyranoside(QG), isorhamnetin-3-O-β-D-glucopyranoside(IG) and 1, 2-di-O-sinapoyl-β-D-glucopyranose(SG) was determined simultaneously by HPLC, the change rule of contents of these components before and after processing and its reasons were analyzed.Waters Symmetry® C18 column(4.6 mm×250 mm, 5 μm) was employed, and the mobile phase was acetonitrile(A)-1% acetic acid aqueous solution(B) for gradient elution(0-5 min, 5%-10%A; 5-15 min, 10%-13%A; 15-23 min, 13%-20%A; 23-43 min, 20%-25%A; 43-46 min, 25%A; 46-55 min, 25%-40%A; 55-60 min, 40%A). The flow rate was 1 mL·min-1.The detection wavelength was set at 265 nm, the injection volume was 10 μL, and the column temperature was 30 ℃.Result:Contents of the above five components before processing were 0.114 3%, 0.041 6%, 0.036 2%, 0.022 6% and 0.097 6%; after processing, the contents of these five components turn into 0.107 4%, 0.011 3%, 0.034 2%, 0.021 9% and 0.058 9%; among them, the contents of these five components decreased by 6.04%, 72.84%, 5.52%, 3.10% and 39.65%, respectively.Conclusion:The contents of these five components in Descurainiae Semen is reduced to varying degrees after processing.The contents of phenylpropanoids decrease significantly, while the contents of flavonoid glycosides do not change significantly.
Abstract：Objective:To study on the differences of profile spectra among chemical components in Magnoliae Officinalis Cortex from different varieties and habitats, and to screen and identify the characteristic components affecting the quality difference of this herb.Method:The chromatogram data sets of Magnoliae Officinalis Cortex from different varieties and habitats were obtained by liquid chromatography-time-of-flight-mass spectrometry(LC-TOF-MS). Principal component analysis, partial least squares-discriminant analysis and cluster analysis were used to compare the differences in chemical profiles among Magnoliae Officinalis Cortex from different varieties and habitats, and adopted to screen out the characteristic chemical constituents that resulted in these differences and to perform mass spectrometry analysis and comparison.Result:Eleven characteristic peaks were identified by LC-TOF-MS chromatographic data and reported in the literature.The use of chemical profile could distinguish different habitats of Magnoliae Officinalis Cortex, but could not completely distinguish different varieties of this herb.Conclusion:LC-TOF-MS can easily and quickly study on the profile differences of chemical substances in Magnoliae Officinalis Cortex from different varieties and different habitats, the results of this study can provide a theoretical basis for the quality evaluation and pharmacodynamic material basis of this herb.
Keywords：liquid chromatography-mass spectrometry;Magnoliae Officinalis Cortex;characteristic components;chemical profile;alkaloids;lignans;origin of medicinal materials
Abstract：Objective:To study nitrogenous chemical constituents from the seeds of Brassica campestris.Method:The aerial parts of nonfat seeds were extracted with 75% ethanol heat refluxing method, then suspended in H2O and separated with ligarine and ethyl acetate to obtain respective fractions.Chemical constituents were isolated and purified by various chromatographic methods and identified by physicochemical characters and spectroscopic analysis or comparison with standard compounds.Result:Thirteen nitrogenous chemical compounds were isolated and identified as coixspirolactam C (1), indole-3-acetonitrile (2), 2-β-D-glucopyranosylsulfanyl-1H-indole-3-acetonitrile (3), nicotinic acid (4), adenosine (5), 1H-indole-3-carbaldehyde (6), 4-hydroxy-1H-indole-3-carbaldehyde (7), 6-hydroxy-1H-indole-3-carboxylic acid (8), ethyl 2-oxo-1, 2, 3, 4-tetrahydroquinoline-4-carboxylate (9), 5-hydroxy-4(1H)-quinazolinone (10), 4-hydroxy-2-quinazolinone (11), 5-hydroxy-quinazoline-2(1H), 4(3H)-dione (12), 5-allyloxazolidin-2-one (13).Conclusion:All of the compounds were isolated from this plant for the first time, and compounds 1, 3 and 13 were isolated from Brassica for the first time.
Keywords：Brassica campestris seed;nitrogenous chemical constituents;isolation;coixspirolactam C;2-β-D-glucopyranosylsulfanyl-1H-indole-3-acetonitrile;5-allyloxazolidin-2-one
Abstract：Objective:To systematically identify the chemical constituents in extract of Baihu Jia Guizhi Tang (BHGZT) by ultra-fast liquid chromatography/triple time-of-flight tandem mass spectrometry (UFLC-Triple-TOF-MS/MS).Method:Phenomenex C18 (3.0 mm×100 mm, 2.6 μm) was eluted with acetonitrile (containing 0.1%formic acid) and 0.1%formic acid solution as the mobile phase in a gradient mode. The column temperature was set at 40 ℃, the flow rate was 0.3 mL·min-1, and the injection volume was 5 μL. High-resolution triple quadrupole flight mass spectrometry was adopted to test in both positive and negative modes. Formula finder function in peakview software was used to calculate the element composition of the compounds, and IDA explore function in the software was invoked to obtain secondary fragmentation ions of this mass number. And the compounds were identified based on literature data and the reference substances.Result:On the basis of the mass fragmentation regularity of accurate molecular weight, 35 compounds were identified in BHGZT, including 16 steroid saponins, 6 triterpenoid saponins, 7 flavonoids, and 4 organic acids and 2 others. Among them, 10 components (timosaponin AⅢ, timosaponin I, timosaponin BⅢ, timosaponin BⅡ, new mangiferin, mangiferin, liquiritin apioside, liquiritin, glycyrrhizic acid and cinnamic acid) were confirmed by comparing with reference substances, and the sources of the compound were identified.Conclusion:UFLC-Triple-TOF-MS/MS can be used to characterize the chemical composition of BHGZT simply and quickly. Relevant researches provide references for the research of pharmacodynamic material basis, the quality control and the explanation of mechanism of action.
Keywords：Baihu Jia Guizhi Tang;UFLC-Triple-TOF-MS/MS;chemical material basis
Abstract：Objective:Fresh tubers of Gastrodiae Rhizoma were harvested at the right time. A saline water salting and drying technology was developed for obtaining the medicinal materials of Gastrodiae Rhizoma in the place of origin and avoiding rot and mildew.Method:Fresh tubers of Gastrodiae Rhizoma were dug in Yiliang, Yunnan, Dejiang, Guizhou, and Chenggu, Shaanxi, the experiments of natural drying, and saline water salting and drying were carried out in the place of origin and Beijing. After the dirt was removed, the samples were tiled in a container immediately, added with varied proportions of saline water (0.03-0.10 g·mL-1 NaCl in water), hermetically pickled for 6-15 d. after being soaked and rinsed with water, the samples were put in a cool ventilated place or under sunshine to prepare dried medicinal materials of Gastrodiae Rhizoma. We described the appearance characteristics, measured the moisture content, gastrodin and nitrite. And the appearance was observed after storage in a simple warehouse for one year later.Result:Fresh tubers of Gastrodiae Rhizoma from three origins were naturally dried, the surface of gastrodia tubers became black, decayed and moldy, then we could not get dried medicinal materials. The appearance and the content of gastrodins in the medicinal materials of Gastrodiae Rhizoma processed by saline water salting and drying technology met the requirements for Gastrodiae Rhizoma in the Pharmacopoeia of the People's Republic of China 2015 and relevant standards of nitrite in salted food in National Food Safety Standard Determination of Nitrite and Nitrate in Foods, Hygienic Standard for Preserved Vegetables, Green Food-Soybean Paste and Salted Vegetable.Conclusion:The saline water salting and drying technology is developed to make medicinal materials of Gastrodiae Rhizoma quickly from fresh tubers of Gastrodia elata in the place of origin and Beijing. The metamorphism had not been observed after being stored in simple warehouses for one year. This technology can guarantee the quality of Gastrodiae Rhizoma, and provide a new method for the filed processing of Gastrodiae Rhizoma.
Keywords：Gastrodiae Rhizoma;saline water salting method;processing in production place;drying technology;store;gastrodins
Abstract：Objective:To explore the correlation between the characters and chemical constituents of Glycyrrhizae Radix et Rhizoma through the analysis of characters and main chemical constituents of Glycyrrhizae Radix et Rhizoma, and establish the grade evaluation criteria of Glycyrrhizae Radix et Rhizoma, so as to provide reference for the quality evaluation and quality control of Glycyrrhizae Radix et Rhizoma.Method:Correlation analysis, principal component analysis and cluster analysis were carried out for appearance and intrinsic indexes of Glycyrrhizae Radix et Rhizoma.Result:Class Ⅰ of Glycyrrhizae Radix et Rhizoma: the diameter of big end was more than 1.60 cm, middle circumference was more than 3.76 cm, inner core chromaticity b* was more than13.88, outer skin chromaticity a* was more than 37.61, glycyrrhizin content was more than 1.13%, with no worm, rot and impurity. Class Ⅱ of Glycyrrhizae Radix et Rhizoma: the diameter of big end was 1.39-1.60 cm, the middle circumference was 3.09-3.76 cm, the inner core chromaticity b* was 10.22-13.88, the skin chromaticity a* was 35.57-37.61, glycyrrhizin content was 0.69%-1.13%, with no worm, rot and impurity. Class Ⅲ of Glycyrrhizae Radix et Rhizoma: the diameter of the big end was 1.08-1.39 cm, the middle circumference was 2.41-3.09 cm, the inner core chromaticity b* was 5.16-10.22, the skin chromaticity a* was 29.19-35.57, glycyrrhizin content was 0.55%-0.69%, with no worm and rot. Substandard Glycyrrhizae Radix et Rhizoma: the diameter of the big end was lower than 1.08 cm, the central circumference was lower than 2.41 cm, the inner core color b* was lower than 5.16, the outer skin color a* was lower than 29.19, and glycyrrhizin content was lower than 0.55%.Conclusion:The grade evaluation standards established in this paper include appearance and intrinsic indexes, with scientific, comprehensive and practical characteristics. It can be used for the grade evaluation of Glycyrrhizae Radix et Rhizoma medicinal materials.
Keywords：Glycyrrhizae Radix et Rhizoma;intrinsic index components;appearance characteristics;grade evaluation
Abstract：Objective:To explore the mechanism of treatment of jaundice with Canhuang tablets by molecular docking.Method:The compounds of Canhuang tablets were screened in traditional Chinese medicine systems pharmacology database and analysis platform(TCMSP), and targets for treatment of jaundice were collected from the comparative toxicogenomics database(CTD) and DrugBank database.Molecular docking was carry out on the LibDock module of Discovery Studio 2016 software to evaluate the compound-target interaction, and network characteristics were analyzed.Result:A total of 37 compounds in Canhuang tablets had strong interaction on 14 targets, such as pregnane receptor(PXR), constitutive androstane receptor(CAR), farnesoid X receptor(FXR), et al.These targets played an important role in the treatment of jaundice by regulating bilirubin metabolism, regulating bile acid synthesis and transport, inhibiting immune and inflammatory response, and affecting the formation of collagen in the liver.The compound-target network analysis found that moupinamide, canadine, quercetin, demethoxycurcumin, obacunone, curcumin, corchoroside A, berlambine, alnustone, naringenin were the possible main active compounds of Canhuang tablets, which could interact with more than 7 targets.Conclusion:Molecular docking reveals the possible active compounds and the mechanism of treatment of jaundice with Canhuang tablets, and which is conducive to improvement of quality control standard of this preparation and study of its mechanism for jaundice.
Abstract：Objective:In this paper, the network pharmacology method was used to explore the material basis and the mechanism of Magnoliae Officinalis Cortex(Houpo) on depressive disorder.Method:Firstly, the main chemical components of Houpo were gathered from CNKI, SciFinder, traditional Chinese medicine systems pharmacology database and analysis platform(TCMSP) and other databases.Next, the potential targets of the chemical ingredients in Houpo were searched and selected by BATMAN-TCM database.The targets of depressive disorder were collected from HPO database.Then all the targets were entered into the search tool(String database) for the retrieval of protein-protein interactions so as to confirm antidepressant chemistries and their related targets.Furthermore, the functional enrichment analysis was carried out through the David database.Based on these above results, the networks of " drug targets-disease targets" and " compounds-targets-pathways" of Houpo on depressive disorder were built by Cytoscape v3.5.1 software, respectively.Network topology analysis was used to screen the key targets and the corresponding components.Then molecular docking verification of " component-target proteins" was further conducted.Result:A total of 16 active compounds involving in 74 key targets for depressive disorder were selected and confirmed from 138 chemical components of Houpo.Molecular docking analysis showed that compared with other components, ten volatile components in the 16 active compounds had good binding activities with the top 5 key targets[the top 5 of degree value, including insulin receptor(INS), mitogen-activated protein kinase 1(MAPK1), guanine nucleotide binding protein alpha inhibition 3(GNAI3), phosphatidylinositol 3-kinase receptor 1(PIK3R1) and selective receptor B1(GNB1)] and the 3 direct acting targets of popular drugs for depression [muscarinic acetylcholine receptor M2(CHRM2), 5-hydroxytryptamine receptor(HTR)2B and HTR2C]. The functional enrichment analysis showed the antidepressant mechanism of Houpo mainly involved neurotrophin signaling pathway, MAPK signaling pathway, calcium signaling pathway and neuroactive ligand-receptor interaction, etc.Conclusion:This study reveals the active ingredients and the mechanism of anti-depression of Houpo based on network pharmacology, a total of 16 key active ingredients related to anti-depression are selected.This paper can provide references for development of antidepressants and the discovery of quality markers of Houpo for anti-depression.
Abstract：Objective:Screen out the antitumor constituents of Aconiti Lateralis Radix Praeparata-Pinelliae Rhizoma base on system pharmacology with chemical constituents of Aconiti Lateralis Radix Praeparata-Pinelliae Rhizoma as study objects, in order to provide the theoretical basis for the development of antitumor and nontoxic activities of Aconiti Lateralis Radix Praeparata-Pinelliae Rhizoma.Method:The small molecule ligand library of Aconiti Lateralis Radix Praeparata-Pinelliae Rhizoma was built based on Traditional Chinese Medicine Systems Pharmacology(TCMSP), energy of Aconiti Lateralis Radix Praeparata-Pinelliae Rhizoma was matched with the key protein targets of phosphatidylinositol 3-kinase/protein kinase B (PI3K/Akt) signal pathway by molecular docking (SYBYL2.1, Tripos), the Aconiti Lateralis Radix Praeparata-Pinelliae Rhizoma-targets network model was established based on Cytoscape 3.5.1, and the physicochemical properties of the antitumor activity in Aconiti Lateralis Radix Praeparata-Pinelliae Rhizoma were predicted by using SwissADME and admetSAR.Result:There were 25 small molecule constituents of Aconiti Lateralis Radix Praeparata-Pinelliae Rhizoma. Through the energy match, key antitumor constituents of Pinelliae Rhizoma were gondoic acid, 10, 13-eicosadienoic, baicalin, 12, 13-epoxy-9-hydroxynonadeca-7, 10-dienoic acid. Key antitumor constituents of Aconiti Lateralis Radix Praeparata were deltoin, sitosterol, neokadsuranic acid B, 11, 14-eicosadienoic acid. Phosphatidylinositol 3-kinase (PI3Kα), phosphatase and tensin homolog deleted on chromosome ten (PTEN), phosphoinositide dependent protein kinase 1 (PDK1) were key antitumor targets of Aconiti Lateralis Radix Praeparata-Pinelliae Rhizoma. There were 8 key antitumor constituents of Aconiti Lateralis Radix Praeparata-Pinelliae Rhizoma, which had a low CYP450 inhibition and basically followed the Lipinski rule.Conclusion:Antitumor nontoxic constituents of Aconiti Lateralis Radix Praeparata-Pinelliae Rhizoma and key targets are screened out from the molecular level, which provides the new ideas for the effective use of nontoxic traditional Chinese medicine(TCM) and breaks the restrictions in using nontoxic TCM.
Abstract：Objective:To analyze the known mechanism of toxicology and predict the unknown toxicity in Asari Radix et Rhizoma sinensis by establishing the network relationship of compound, protein, gene and toxicant reaction.Method:After comparing the Asari Radix et Rhizoma candidate compounds obtained from the traditional Chinese Medicine Systems Pharmacology Database and Analysis Platform(TCMSP) database and the toxicological information obtained from the Comparative Toxicogenomics Database(CTD) database, we screened out 13 toxic components from Asari Radix et Rhizoma. And use the Pharm Mapper Server website to find the detailed information of target proteins of the 13 components. The network structure of these 13 chemical components and their corresponding target proteins were drawn by using Cytospace software, and several target proteins with the highest degree of association were found. ClueGO+ CluePedia plug-in of Cytospace software was applied in gene ontology(GO) enrichment analysis of genes and kyoto encyclopedia of genes and genomes(KEGG) pathway enrichment analysis, so as to determine the pathways through which toxic substances in Asari Radix et Rhizoma might be harmful to human body.Result:The toxic substances in Asari Radix et Rhizoma may induce tumor and cancer formation through p53 signaling pathway, interleukin(IL)-17 signaling pathway, nuclear factor(NF)-kappa B signaling pathway, tumor necrosis factor(TNF)-signaling pathway. Asari Radix et Rhizoma could inhibit the central nervous system by regulating apoptosis pathways and neurons, and may also cause other autoimmune diseases by IL-17, TNF-α pathway and apoptosis regulation.Conclusion:This study preliminarily explores related mechanisms of toxicity of Asari Radix et Rhizoma, this method can be used to predict toxicity and explain toxicity mechanism of traditional Chinese medicine.
Keywords：Asari Radix et Rhizoma;network toxicology;gene ontology(GO) enrichment analysis;kyoto encyclopedia of genes and genomes(KEGG) enrichment analysis
Abstract：Wendantang (WDT) is a classical traditional Chinese medicine prescription composed of Pinelliae Rhizoma, Bambuseae Caulis in Taenias, Aurantii Fructus Immaturus, Citri Reticulatae Pericarpium, Zingiberis Rhizoma Recens, Glycyrrhizae Radix et Rhizoma, with the effect in regulating Qi-movement and phlegm and relieving stomach and gallbladder. The clinical studies have proved that WDT has significant therapeutic effects on depression, insomnia, schizophrenia, Alzheimer's disease and other nervous system diseases, but wihtout systematic understanding of material basis and compatibility principle because of the complex chemical composition and the scattered research results. Focusing on the neurological diseases and based on the origin of ancient recipes and modern research examples, the author sorted out and summarized the active ingredients constituting the recipe, paid attention to the effect of the compatibility on the composition and efficacy transmission, and judged the rationality of composition intention and selection. On this basis, it comprehensively identifies the potential components and effective paths that can well treat the nervous system diseases, and had the overall understanding about mutual relationship between composition and efficiency. In this article, we expect to find its scientific basis of effective materials and the key technology of quality standards, and define the direction of future research, so as to provide valuable reference for secondary development and new preparations designed of classic prescriptions.
Keywords：Wendantang;nervous system diseases;pharmacodynamic material basis;action mechanism;research progress
Abstract：Araliaceae plant Notoginseng Radix et Rhizoma, Ginseng Radix et Rhizoma and Panacix Quinquefolii Radix are famous Chinese herbal medicines, with anti-inflammatory and anti-aging effect, as well as obvious effect on cardiovascular and cerebrovascular systems. Studies have found that the metabolism and transport of cholesterol may affect the function of the cardiovascular system. Cholesterol can be divided into high-density cholesterol and low-density cholesterol. Cholesterol has many physiological regulating effect. High-density cholesterol has a protective effect on cardiovascular disease. When the cholesterol metabolism in the body is disordered, low-density cholesterol is increased, and will cause the increase in the risk of cardiovascular and cerebrovascular diseases. By consulting relevant Chinese and foreign documents and materials, we found that traditional Chinese medicine Araliaceae has a significant regulatory effect on cholesterol. It can directly regulate the cholesterol level of experimental hyperlipidemia rats, reduce total cholesterol(TC) and low density lipoprotein cholesterol(LDL-C) in rats, and partially increase high-density lipoprotein cholesterol(HDL-C) level in rats. It can inhibit cholesterol synthesis by inhibiting cholesterol synthesis-regulating genes liver X receptor-α(LXR-α), peroxisome proliferator-activated receptor γ(PPARγ), cytochrome P450 7A1(CYP7A1); and up-regulate cholesterol metabolism genes peroxisome proliferator-activated receptor-α(PPARα), PPARγ, CYP8B1, CYP7A1, LXR) and body ATP-binding cassette transporter, ABC transporter(ABCA1, ABCG5/8)to promote cholesterol metabolism in the body. Araliaceae plants may play a neuroprotective role by regulating cholesterol metabolism and transport in the brain, and improve neurodegenerative diseases. Studies on the effect of Araliaceae plants on the metabolism and transport of cholesterol in brain will become a hot research topic in the future. The above review is expected to provide a reference for further research on the lipid-lowering effect and mechanism of Araliaceae plants.
Abstract：Gas chromatography (GC) is mainly used to detect the levels of short-chain fatty acids (SCFAs), but with the deepening of research, the drawbacks of GC have become more and more obvious in the fields of food, chemical engineering and clinical application. The analysis on existing research results showed that ultra performance convergence chromatography (UPC2) was appropriate for the analysis of lipid metabolism. The UPC2 is a new kind of chromatographic separation technology developed in recent five years and the level of SCFAs is associated with the research on multiple diseases. Therefore, application of UPC2 in the detection of SCFAs would be helpful for the scholars at home and abroad to carry out deeper researches, and also helpful to guide the treatment for various metabolic disorders. In this paper, the researches on SCFAs in recent ten years were reviewed; the shortcomings of GC and liquid chromatography (LC) in the detection of SCFAs were reviewed; the development process, basic characteristics and research status of UPC2,at home and abroad were introduced; feasibility and innovation of UPC2 in the detection of SCFAs were summarized. Pretreatment methods for UPC2 application to the detection of SCFAs in feces or serum were collected; the problems that should be noticed during the process of sample pretreatment were pointed out; meanwhile, an research outlook on methodology of UPC2 application in the detection of SCFAs was conducted. The effects of extracting solvent, mobile phase, and auxiliaryt solvent on chromatographic behavior as well as the physicochemical property, type and choice of UPC2 chromatographic column were mainly discussed in this paper. In addition, the choices of basic modifier, acid modifier, and salinity modifier were briefly outlined, in order to provide efficient, simple, environmental, and economic detection technologies for the research on SCFAs, and provide better reference solutions for the rapid detection of massive clinical samples.
Keywords：ultra performance convergence chromatography;short-chain fatty acids;sample pretreatment;research outlook
Abstract：Gramineous crops occupy a remarkable proportion of grain crops in the word, and wheat, rice and corn account for more than 80%of the world's food crops. Agricultural residues bring tremendous pressure on the environment, and inefficient development of resources has caused huge waste of resources. At present, the research on agricultural residues mainly focuses on energy, fertilizer, feed and materialization. However, there are still a lot of resources that have not been rationally utilized. The author has found that in recent years, the medicinal research on gramineous crop waste has focused on four varieties-rice, corn, wheat and sugar cane, and their waste rice bran, rice husk, rice straw, corn stigma, corn bract, wheat bran, sugar cane leaf, sugar cane skin. The compounds isolated and identified from agricultural residues include phenylpropanoids, flavonoids, steroids and their glycosides, organic acids and their esters, volatile oil and saccharides. Studies have shown that agricultural residues from gramineous crops have pharmacological activities, such as anti-oxidation, hypolipidemia, hypoglycemia, anti-inflammation, anti-tumor, anti-cardiovascular disease, anti-liver and kidney damage. This paper is a systematic review of the chemical composition and pharmacological effects of agricultural residues from the major gramineous crops, so as to provide useful information for further research and development of agricultural residues.
Abstract：Abri Herba, a kind of plant of Leguminosae family, is widely distributed in Guangdong and Guangxi, with rich resources.With a long medication history in China, its whole-plant, apart from plant seeds have been used as medicine, with the effects in removing dampness and removing jaundice, clearing heat and detoxifying, and clearing the liver and relieving pain. By accessing CNKI, Wanfang date, VIP Web, ScienceDirect, FMRS, Pubmed and multiple domestic and foreign databases, recent literatures on chemical constituents and pharmacological action and clinical trials of Abri Herba were collected and summarized in a review.According to a great quantity of relevant domestic and foreign literatures.Abri herba contains abundant chemical constituents, such as betulinic acid and other triterpenoids, catechin and other flavonoids, abrine and other alkaloids, chrysophanol and other anthraquinones, as well as inorganic elements.Abri Herba has a wide range of pharmacological effects due to rich material basis. Abri Herba, as a folk traditional herb, is used to treat jaundice with damp-heat pathogen, distending pain in the stomach, acute mastitisand gall, steatosis hepatis, hepatitis and internal traumatic injury. It also has many other effects in resisting tumor, oxidation, bacteria, virus and inflammation, relieving pain, promoting wound healing and regulating immunity.At present, there is single herb or traditional Chinese medicine compounds of Abri Herba in clinic, and the latter is the majority. Abri Herba can play a better pesticide effect by combining with traditional Chinese medicine. With a wide range of pharmacological effects, cheap price and easy cultivation. Abri Herba has high economic and social benefits, great potential for development and broad market prospects.Based on domestic and foreign studies on Abri Herba in past 30 years, the recent progress in the studies on chemical constituents, biological activities and clinical applications of this plant was reviewed in this paper, in the expectation of providing reference for further development and comprehensive utilization of Abri Herba medicinal resources.
Keywords：Abri Herba;chemical components;pharmacological action;clinical application;flavonoids;polysaccharide;anti-tumor;blood lipid regulating and liver protecting