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当前位置: 首页 > 文章 > 新型大豆素苯磺酸酯的细胞吸收利用与构性关系研究 大豆科学 2019 (1) 97-103
Position: Home > Articles > Study on Apsorption of Daidzein Sulfonic Acid Ester on HAVSMCs and the Relationship Between Pharmaceutical Properties and Structure Soybean Science 2019 (1) 97-103

新型大豆素苯磺酸酯的细胞吸收利用与构性关系研究

作  者：
彭游;熊小伟;胡华南;黄华南
单  位：
九江学院江西省生态化工工程技术研究中心;南昌大学药学院
关键词：
大豆素;苯磺酸酯;细胞吸收;脂溶性;水溶性;构性关系
摘  要：
为了提高大豆素衍生物的抗动脉粥样硬化等功效,利用药动团变换原理对大豆素进行结构修饰,合成了大豆素磺酸酯衍生物(D1、D2)。采用HPLC和软件Chem Axon对目标衍生物的药学性质进行考察和计算,利用人主动脉血管平滑肌细胞HAVSMCs和HPLC考察大豆素及其衍生物的吸收利用率。结果表明:大豆素(DD)、衍生物D1、D2在主动脉血管平滑肌细胞吸收率最大,分别为20. 3%、29. 4%和71. 7%,最大吸收率表现为D2> D1> DD。构性关系研究表明,药物的吸收利用与药物的理化性质密切相关,只有脂溶性和水溶性适宜,药物的细胞吸收利用才会得以提高。
译  名：
Study on Apsorption of Daidzein Sulfonic Acid Ester on HAVSMCs and the Relationship Between Pharmaceutical Properties and Structure
作  者：
PENG You;XIONG Xiao-wei;HU Hua-nan;HUANG Hua-nan;Jiangxi Province Engineering Research Center of Ecological Chemical Industry,Jiujiang University;School of Pharmacy,Nanchang University;
单  位：
PENG You%XIONG Xiao-wei%HU Hua-nan%HUANG Hua-nan%Jiangxi Province Engineering Research Center of Ecological Chemical Industry,Jiujiang University%School of Pharmacy,Nanchang University
关键词：
Daidzein;;Benzene sulfonate;;Cell absorption;;Liposolubility;;Water solubility;;Structure properties relationship
摘  要：
To improve the effect of daidzein inhibiting the atherosclerosis,its structure was modified using the principle ofpharmacokinetic group and its sulfonate derivatives(D1,D2) were synthesized. The pharmacological properties of the targetderivatives were investigated by HPLC and Chem Axon. The absorptivity of daidzein and its derivatives were investigated byHAVSMCs and HPLC. The results showed that absorptivity on HAVSMCs of DD,its derivatives D1,D2 were maxmum with20. 3% 、29. 4% and 71. 7% respectively and the maximum absorptivity were D2 > D1 > DD. The study on relationship ofstructure and properties showed that the absorption and utilization of drugs were closely related to the physicochemical proper-ties of the drugs,and the absorption and utilization of the drugs on cells were optimal only with moderate liposolubility and wa-ter solubility.

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