丹酚酸组分中各代表性成分药效贡献率的评价及其油水分配系数的整合表征(1)
[摘要]该实验利用人脐静脉内皮细胞氧化损伤实验、家兔体外凝血4项实验和大鼠心肌缺血实验相结合的方法比较了丹酚酸组分中3个代表性成分的药效活性的差异，并利用CRITIC权重法评价代表性成分的药效贡献率;结果得到丹酚酸组分中代表性成分丹酚酸B、迷迭香酸、丹参素的贡献率分别为28.85%，30.11%，41.04%。采用摇瓶法测定了丹酚酸组分在水以及不同pH缓冲液中的油水分配系数，进一步以质量权重系数和药效贡献率相结合的方法整合表征了该组分整体的油水分配系数，结果表明丹酚酸组分在正辛醇-水/pH 1.2的盐酸溶液/pH 2.0，2.5，5.0，5.8，6.8，7.4，7.8的磷酸盐缓冲液中表观油水分配系数0.32，1.06，0.89，0.98，0.90，0.13，0.02，0.20，0.56。该实验为组分整体性质的表征提供了一定的参考。
[关键词]代表性成分;油水分配系数;药效贡献率;CRITIC权重
[收稿日期]2014-09-30
, 百拇医药
[基金项目]江苏省社会发展科技支撑计划项目(BE2010756);江苏省中医药科技项目(LZ11065)
[通信作者]*贾晓斌，Tel/Fax： (025) 85637809，E-mail：jiaxiaobinpharmacy@163.com;*张振海，Tel/Fax： (025) 83271102，E-mail：davidpharm@yeah.net
[作者简介] 严红梅，博士研究生，Tel：(025)85608672，E-mail：yanhongmei0716@163.comEvaluation on contribution rate of each component total salvianolic acids and
characterization of apparent oil/water partition coefficient
, 百拇医药
YAN Hong-mei1，2， CHEN Xiao-yun1， XIA Hai-jian1， LIU Dan1， JIA Xiao-bin1，2*， ZHANG Zhen-hai1*
(1. Key Laboratory of New Drug Delivery System of Chinese Materia Medica， Jiangsu Provincial Academy of
Chinese Medicine， Nanjing 210028， China;
2. Nanjing University of Chinese Medicine， Nanjing 210046， China)
[Abstract]The difference between three representative components of total salvianolic acids in pharmacodynamic activity were compared by three different pharmacological experiments： HUVECs oxidative damage experiment， 4 items of blood coagulation in vitro experiment in rabbits and experimental myocardial ischemia in rats. And the effects of contribution rate of each component were calculated by multi index comprehensive evaluation method based on CRITIC weights. The contribution rates of salvianolic acid B， rosmarinic acid and Danshensu were 28.85%， 30.11%， 41.04%. Apparent oil/water partition coefficient of each representative components of total salvianolic acids in n-octyl alcohol-buffer was tested and the total salvianolic acid components were characterized based on a combination of the approach of self-defined weighting coefficient with effects of contribution rate. Apparent oil/water partition coefficient of total salvianolic acids was 0.32，1.06，0.89，0.98，0.90，0.13，0.02，0.20，0.56 when in octanol-water/ pH 1.2 dilute hydrochloric acid solution/ pH 2.0，2.5，5.0，5.8，6.8，7.4，7.8 phosphate buffer solution. It provides a certain reference for the characterization of components.
[Key words]representative components;apparent oil/water partition coefficient;contribution rate;CRITIC weights, 百拇医药(严红梅 陈小云 夏海建 刘丹 贾晓斌 张振海)
[关键词]代表性成分;油水分配系数;药效贡献率;CRITIC权重
[收稿日期]2014-09-30
, 百拇医药
[基金项目]江苏省社会发展科技支撑计划项目(BE2010756);江苏省中医药科技项目(LZ11065)
[通信作者]*贾晓斌，Tel/Fax： (025) 85637809，E-mail：jiaxiaobinpharmacy@163.com;*张振海，Tel/Fax： (025) 83271102，E-mail：davidpharm@yeah.net
[作者简介] 严红梅，博士研究生，Tel：(025)85608672，E-mail：yanhongmei0716@163.comEvaluation on contribution rate of each component total salvianolic acids and
characterization of apparent oil/water partition coefficient
, 百拇医药
YAN Hong-mei1，2， CHEN Xiao-yun1， XIA Hai-jian1， LIU Dan1， JIA Xiao-bin1，2*， ZHANG Zhen-hai1*
(1. Key Laboratory of New Drug Delivery System of Chinese Materia Medica， Jiangsu Provincial Academy of
Chinese Medicine， Nanjing 210028， China;
2. Nanjing University of Chinese Medicine， Nanjing 210046， China)
[Abstract]The difference between three representative components of total salvianolic acids in pharmacodynamic activity were compared by three different pharmacological experiments： HUVECs oxidative damage experiment， 4 items of blood coagulation in vitro experiment in rabbits and experimental myocardial ischemia in rats. And the effects of contribution rate of each component were calculated by multi index comprehensive evaluation method based on CRITIC weights. The contribution rates of salvianolic acid B， rosmarinic acid and Danshensu were 28.85%， 30.11%， 41.04%. Apparent oil/water partition coefficient of each representative components of total salvianolic acids in n-octyl alcohol-buffer was tested and the total salvianolic acid components were characterized based on a combination of the approach of self-defined weighting coefficient with effects of contribution rate. Apparent oil/water partition coefficient of total salvianolic acids was 0.32，1.06，0.89，0.98，0.90，0.13，0.02，0.20，0.56 when in octanol-water/ pH 1.2 dilute hydrochloric acid solution/ pH 2.0，2.5，5.0，5.8，6.8，7.4，7.8 phosphate buffer solution. It provides a certain reference for the characterization of components.
[Key words]representative components;apparent oil/water partition coefficient;contribution rate;CRITIC weights, 百拇医药(严红梅 陈小云 夏海建 刘丹 贾晓斌 张振海)