中国中药杂志

2020, v.45(16) 3852-3856

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抗心肌缺血赤芍萜苷组分的各代表性成分药效贡献率评价及其油水分配系数的整体表征
Characterization of oil/water partition coefficient of chishao terpene glucoside components based on contribution rate of representative components for myocardial ischemia

柯仲成;程小玲;林传燕;封亮;贾晓斌;
KE Zhong-cheng;CHENG Xiao-ling;LIN Chuan-yan;FENG Liang;JIA Xiao-bin;College of Chemistry and Chemical Engineering, Huangshan University;College of Pharmacy, Nanjing University of Chinese Medicine;Health Supervision Institute,Tunxi District Health Bureau;College of Traditional Chinese Medicine, China Pharmaceutical University;

摘要(Abstract):

中药组分是中药制剂原料的基本单元,其理化性质直接影响剂型选择和处方优化。然而,中药组分大都是个多成分复杂体系,其整体性质的表征仍然处于探索阶段。以生物活性为导向辨识中药组分的代表性成分,再以药效贡献率为权重系数,将各代表性成分的个体性质进行拟合,或许可表征中药组分的整体性质提供借鉴。该文以异丙肾上腺素(ISO)诱导心肌缺血大鼠的体内药理效应为指标,利用多指标数据归一化加权法对赤芍萜苷组分中3个代表性成分的药效贡献率进行了综合评价,得到芍药苷、芍药内酯苷、苯甲酰芍药苷的药效贡献率分别为54.87%,32.46%和12.67%。采用摇瓶法对赤芍萜苷组分在水以及不同pH缓冲液中的油水分配系数进行测定,再利用药效贡献率为权重对赤芍萜苷组分整体的油水分配系数进行表征,结果表明赤芍萜苷组分在正辛醇-水,pH 2.0,2.5,5.0,5.8,6.8等磷酸盐缓冲体系中的表观油水分配系数log P为0.18~0.22,表明赤芍萜苷组分在体内吸收一般,为低渗透性中药组分,可为以赤芍萜苷组分为原料的中药制剂研究提供依据。
The components of traditional Chinese medicine(TCMCs) are the basic unit of raw materials for Chinese medicines, and their physical and chemical properties directly affect the choice of dosage forms and the optimization of prescriptions. However, most of TCMCs are multi-component complex systems, and the characterization of their overall properties is still in the exploration stage. On the basis of biological activity, the representative components are determined, and then the individual characteristics are fitted with the weight coefficient of efficacy contribution rate, which may provide reference for characterizing the overall properties of TCMCs. In this study, with the pharmacological effects of isoproterenol(ISO)-induced myocardial ischemia in rats as the indicators, the pharmacodynamic contribution rates of three representative components of chishao terpene glucoside components(CSTGCs) were evaluated by the normalization weighting method. The contribution rates of paeoniflorin, paeoniflorin and benzoylpaeoniflorin were 54.87%, 32.46% and 12.67%, respectively. The oil-water partition coefficients of paeoniflorin, albiflorin, benzoylpaeoniflorin in water and buffer solutions with different pH values were measured, and the oil-water partition coefficients of CSTGCs were characterized by the weight of their pharmacodynamics contribution rate. The results showed that the apparent oil-water partition coefficient(log P) of CSTGCs in the phosphate buffer system such as n-octanol-water(pH 2.0, 2.5, 5.0, 5.8, 6.8) were 0.18-0.22, indicating that CSTGCs have common absorption and low permeability, providing basis for the preparation of CSTGCs.

关键词(KeyWords): 赤芍萜苷;心肌缺血;代表性成分;油水分配系数;药效贡献率
chishao terpene glucoside components;myocardial ischemia;representative components;oil-water partition coefficient;contribution rate

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基金项目(Foundation): 国家自然科学基金项目(81573620);; 安徽省自然科学基金面上项目(2008085MH269);; 安徽省高校省级自然科学研究重点项目(KJ2017A394);; 黄山学院人才启动项目(2018xkjq017);黄山学院教学研究项目(2020JXYJ007)

作者(Author): 柯仲成;程小玲;林传燕;封亮;贾晓斌;
KE Zhong-cheng;CHENG Xiao-ling;LIN Chuan-yan;FENG Liang;JIA Xiao-bin;College of Chemistry and Chemical Engineering, Huangshan University;College of Pharmacy, Nanjing University of Chinese Medicine;Health Supervision Institute,Tunxi District Health Bureau;College of Traditional Chinese Medicine, China Pharmaceutical University;

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