[1]彭游,熊小伟,胡华南,等.新型大豆素苯磺酸酯的细胞吸收利用与构性关系研究[J].大豆科学,2019,38(01):97-103.[doi:10.11861/j.issn.1000-9841.2019.01.0097]
　PENG You,XIONG Xiao-wei,HU Hua-nan,et al.Study on Apsorption of Daidzein Sulfonic Acid Ester on HAVSMCs and the Relationship Between Pharmaceutical Properties and Structure[J].Soybean Science,2019,38(01):97-103.[doi:10.11861/j.issn.1000-9841.2019.01.0097]
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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》[ISSN:1000-9841/CN:23-1227/S] 卷: 第38卷 期数: 2019年01期 页码: 97-103 栏目: 出版日期: 2019-01-20
Title:
Study on Apsorption of Daidzein Sulfonic Acid Ester on HAVSMCs and the Relationship Between Pharmaceutical Properties and Structure
作者:
彭游1; 熊小伟2; 胡华南1; 黄华南1
(1.九江学院 江西省生态化工工程技术研究中心, 江西 九江 332005; 2.南昌大学 药学院, 江西 南昌 33000)
Author(s):
PENG You1;  XIONG Xiao-wei2;  HU Hua-nan1;  HUANG Hua-nan1
(1.Jiangxi Province Engineering Research Center of Ecological Chemical Industry, Jiujiang University, Jiujiang 332005, China; 2. School of Pharmacy, Nanchang University, Nanchang 330000, China)
关键词:
大豆素; 苯磺酸酯; 细胞吸收; 脂溶性; 水溶性; 构性关系
Keywords:
Daidzein;  Benzene sulfonate;  Cell absorption;  Liposolubility;  Water solubility;  Structure properties relationship
DOI:
10.11861/j.issn.1000-9841.2019.01.0097
文献标志码:
A
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ChemAxon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。
Abstract:
To improve the effect of daidzein inhibiting the atherosclerosis, its structure was modified using the principle of pharmacokinetic group and its sulfonate derivatives(D1,D2) were synthesized. The pharmacological properties of the target derivatives were investigated by HPLC and ChemAxon. The absorptivity of daidzein and its derivatives were investigated by HAVSMCs and HPLC. The results showed that absorptivity on HAVSMCs of DD, its derivatives D1, D2 were maxmum with 20.3%、29.4% and 71.7% respectively and the maximum absorptivity were D2>D1>DD. The study on relationship of structure and properties showed that the absorption and utilization of drugs were closely related to the physicochemical properties of the drugs, and the absorption and utilization of the drugs on cells were optimal only with moderate liposolubility and water solubility.

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　WEN Rui-zhi,LI Shui-fang,and ZENG Dong.Structure Analysis of Genistein and Daidzein[J].Soybean Science,2008,27(01):128.[doi:10.11861/j.issn.1000-9841.2008.01.0128]

备注/Memo

收稿日期：2018-07-26

基金项目：国家自然科学基金（81660541）。
第一作者简介：彭游（1971-），男，博士，教授，主要从事食品化学研究。E-mail: trihydracid@126.com。

更新日期/Last Update: 2019-01-22