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纸质出版日期:2018
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苏青, 吴婷婷, 黄雅兰, 等. 黄芩提取物制备过程中化学成分及药效的变化规律分析[J]. 中国实验方剂学杂志, 2018,24(14):1-6.
SU Qing, WU Ting-ting, HUANG Ya-lan, et al. Research on Changes of Composition and Efficacy of Scutellariae Radix Extract in Process of Preparation[J]. Chinese journal of experimental traditional medical formulae, 2018, 24(14): 1-6.
苏青, 吴婷婷, 黄雅兰, 等. 黄芩提取物制备过程中化学成分及药效的变化规律分析[J]. 中国实验方剂学杂志, 2018,24(14):1-6. DOI: 10.13422/j.cnki.syfjx.20181401.
SU Qing, WU Ting-ting, HUANG Ya-lan, et al. Research on Changes of Composition and Efficacy of Scutellariae Radix Extract in Process of Preparation[J]. Chinese journal of experimental traditional medical formulae, 2018, 24(14): 1-6. DOI: 10.13422/j.cnki.syfjx.20181401.
目的:分析黄芩提取物制备过程中化学成分及药效的动态变化规律,探寻确定合理提取工艺的研究思路。方法:根据2015年版《中国药典》收载的黄芩提取物制备工艺制备4个中间产物,分别记为水提物(样1),第1次酸沉产物(样2),醇沉精制后产物(样3)和第2次酸沉产物(样4),分别测定以上4个样品中各成分的含量及其解热、抗炎作用,采用灰色关联度分析和双变量相关分析考察成分与药效的相关性。结果:酸沉精制能明显提高黄芩提取物中5种黄酮类成分的含量,但醇沉精制对提高这5种黄酮类成分含量的作用不明显。样1对干酵母致大鼠发热试验的解热效应最强,样2对二甲苯致小鼠耳肿胀和角叉菜胶致大鼠足肿胀的抑制作用最明显,样3和样4的解热抗炎作用有所减弱,即进一步的纯化精制存在功效损失。黄芩苷与体温升高值、耳肿胀率和足肿胀率的灰色关联系数分别为0.78,0.81和0.70,双变量相关系数分别为0.957,0.848和0.819,均为5种成分中的最大值,说明黄芩苷对药效的影响最大;此外,除黄芩苷外,其他4种成分与体温升高值、耳及足肿胀率的双变量相关系数为负值(解热效应中的黄芩素除外),提示提高其他4种成分的含量有利于增强提取物的解热抗炎效果。结论:虽然黄芩苷对黄芩提取物药效的影响最大,但也不是该成分含量越高越好,且增加除黄芩苷外的其他成分的含量有利于提高该提取物的整体解热抗炎效果。黄芩提取物解热抗炎作用是多种成分的综合效应,在确定制备工艺时应综合考虑多种成分对药效的影响,避免过度纯化造成功效损失。
Objective: The dynamic changes of composition and efficacy were analyzed during the process of preparation of Scutellariae Radix extract(SRE)
and the research ideas to determine the reasonable extraction process were explored. Method: Four products were prepared according to the preparation procedure of SRE collected in the 2015 edition of Chinese Pharmacopoeia
which were water extract(sample 1)
first acid precipitation product(sample 2)
alcohol precipitation product(sample 3) and second acid precipitation product(sample 4).The content of each component in the above four samples and their antipyretic and anti-inflammatory effects were determined
respectively.The correlation between composition and efficacy were analyzed by grey correlation analysis and bivariate correlation analysis. Result: Acid precipitation could significantly increase the content of five flavonoids in SRE
but alcohol precipitation was not obvious to improve the content of five flavonoids.Sample 1 had the strongest antipyretic effect on the fever induced by dry yeast in rats
the inhibitory effect of sample 2 on dimethylbenzene-induced mouse ear swelling and carrageenan-induced foot swelling was the most obvious.The antipyretic and anti-inflammatory effects of sample 3 and 4 obtained by further purification were weakened
which meant further purification caused loss of efficacy.The gray correlation coefficients between baicalin and temperature increase
ear swelling rate and foot swelling rate were 0.78
0.81 and 0.70
the bivariate correlation coefficients were 0.957
0.848 and 0.819
respectively;which were all maximum among the five components
indicated that baicalin had the greatest impact on efficacy.In addition to baicalin
the bivariate correlation coefficients between other four components and temperature increase
ear swelling rate and foot swelling rate were negative(except for baicalein in antipyretic effect)
which indicated that the overall antipyretic and anti-inflammatory activity for SRE can be enhanced by increasing the content of these four components. Conclusion: In summary
although baicalin has the greatest impact on the efficacy of SRE
but not the higher the better;on the contrary
the overall antipyretic anti-inflammatory effect of SRE can be enhanced due to the addition of other four components.The antipyretic and anti-inflammatory effect of SRE is a contribution of a variety of ingredients.During the preparation of SRE
we should take into account the impact of a variety of ingredients on the efficacy
in order to void loss of efficacy due to over-purification.
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