Rapid screening of anti--HIV ingredients in Artemisia rupestris L. extracts interacting with V3 loop region of HIV--1 gp120 and reverse transcriptase by affinity capillary electrophoresis and capillary zone electrophoresis  

利用亲和毛细管电泳和毛细管区带电泳快速筛选新疆一支蒿提取物中与HIV--1包膜蛋白gp120上V3环以及逆转录酶相互作用的活性成分（英文）

作　　者：赵怡然[1] 李中杰[1] 姜勇[2] 张晓丹[1] 凌笑梅[1] 

机构地区：[1]北京大学医学部药学院化学生物学系,北京100191 [2]北京大学医学部药学院天然药物学系,北京100191

出　　处：《Journal of Chinese Pharmaceutical Sciences》2015年第9期625-629,共5页中国药学（英文版）

基　　金：National Natural Science Foundation(Grant No.81373372);Specialized Research Fund for the Doctoral Program of Higher Education of China(Grant No.20110001110021 and 20130001110059)

摘　　要：HIV-1 gains entry into target cells by sequentially interacting with cellular receptors and co-receptors. Both the receptor and co-receptor are recognized by HIV-1 envelope protein gpl20, which plays a key role in the entry process of HIV-1 into cells. The development of new inhibitors is essential since the viral enzyme reverse transcriptase （RT） is one of the first targets of antiretroviral therapy. It has been reported that a variety of natural plants, such as Artemisia rupestris L., have anti-viral pharmacological activity, and they might be the potential inhibitors of RT or V3 loop of gpl20 against HIV-1. RIQRGPGRAFVT1GK （R15K）, the relatively conserved region of V3 loop, can be used for binding research. In this work, we analyzed the interactions between different extracts from Artemisia rupestris L. and R15K by affinity capillary electrophoresis （ACE）. Moreover, we analyzed the interactions between different extracts from Artemisia rupestris L. and RT by capillary zone electrophoresis （CZE）. Our data showed that the chloroform extract ofArtemisia rupestris L. was active among the different plant extracts, which was consistent with previous studies. Taken together, our study provided a rapid screening method to seek anti-HIV ingredients in natural plants＇ extracts.HIV--1侵入宿主细胞的过程中与一系列受体和协同受体结合。这些受体和协同受体都由HIV--1的包膜蛋白gp120识别,在病毒入侵过程中是重要环节之一。逆转录酶拮抗剂是最早针对抗病毒治疗的几个靶点之一,对其的改进对于寻找新型拮抗剂十分关键。许多天然植物如新疆一支蒿被报道具有抗病毒的生物活性。这些天然植物也许就是潜在的靶向针对包膜蛋白gp120上V3环或者逆转录酶的艾滋病毒抑制剂。V3环结构中的相对保守的肽段R15K可以被用来研究蛋白的相互作用。本研究利用毛细管亲和色谱方法研究了R15K与新疆一支蒿各种粗提物之间的相互作用。利用毛细管区带电泳法研究了逆转录酶与新疆一支蒿各种粗提物之间的相互作用。实验结果表明,新疆一支蒿的氯仿层提取物与R15k和逆转录酶之间均存在较明显的相互作用。本研究提供了一种可以快速高通量筛选天然植物中抗艾滋病毒的活性成分的方法。

关 键 词：HIV V3 loop RIQRGPGRAFVTIGK Reverse transcriptase Affinity capillary electropiaoresis Capillary zone electrophoresis 

分 类 号：R284.1[医药卫生—中药学]