Mangiferin, an Anti-HIV-1 Agent Targeting Protease and Effective against Resistant Strains
文献类型：期刊论文
| 作者 | Wang RR1; Gao YD2,3; Ma CH4; Zhang XJ1,3; Huang CG[*]4; Huang JF[*]2; Zheng YT[*]1 |
| 刊名 | MOLECULES
 |
| 出版日期 | 2011 |
| 卷号 | 16期号:5页码:4264-4277 |
| 关键词 | mangiferin HIV-1 protease anti-HIV agents drug resistance |
| 通讯作者 | cghuang@mail.shcnc.ac.cn ; huangjf@mail.kiz.ac.cn ; zhengyt@mail.kiz.ac.cn |
| 合作状况 | 其它 |
| 英文摘要 | The anti-HIV-1 activity of mangiferin was evaluated. Mangiferin can inhibit HIV-1(IIIB) induced syncytium formation at non-cytotoxic concentrations, with a 50% effective concentration (EC50) at 16.90 mu M and a therapeutic index (TI) above 140. Mangiferin also showed good activities in other laboratory-derived strains, clinically isolated strains and resistant HIV-1 strains. Mechanism studies revealed that mangiferin might inhibit the HIV-1 protease, but is still effective against HIV peptidic protease inhibitor resistant strains. A combination of docking and pharmacophore methods clarified possible binding modes of mangiferin in the HIV-1 protease. The pharmacophore model of mangiferin consists of two hydrogen bond donors and two hydrogen bond acceptors. Compared to pharmacophore features found in commercially available drugs, three pharmacophoric elements matched well and one novel pharmacophore element was observed. Moreover, molecular docking analysis demonstrated that the pharmacophoric elements play important roles in binding HIV-1 protease. Mangiferin is a novel nonpeptidic protease inhibitor with an original structure that represents an effective drug development strategy for combating drug resistance |
| 收录类别 | SCI |
| 资助信息 | This work was supported in part by grants from 973 Program (2009CB522306), the Eleventh Five-Year Key Scientific and Technological Program of China (2009ZX09501-029, 2008ZX10001- 002, 2009ZX09103-414), and the CAS Knowledge Innovation Project (KSCX1-YW-10, KSCX2-YW- R-185). |
| 语种 | 英语 |
| 公开日期 | 2011-06-13 |
| 源URL | [http://159.226.149.42:8088/handle/353002/6626]  |
| 专题 | 昆明动物研究所_分子免疫药理学 昆明动物研究所_动物模型与人类重大疾病机理重点实验室 昆明动物研究所_遗传资源与进化国家重点实验室 昆明动物研究所_结构生物信息学 管理、支撑部门_大型仪器中心 |
| 作者单位 | 1.Key Laboratory of Animal Models and Human Disease Mechanisms of the Chinese Academy of Sciences & Yunnan Province, Kunming Institute of Zoology, Chinese Academy of Sciences, Kunming 650223, China 2.State Key Laboratory of Genetic Resources and Evolution, Kunming Institute of Zoology, Chinese Academy of Sciences, Kunming 650223, China 3.Graduate School of Chinese Academy of Sciences, Beijing 100039, China 4.Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China |
| 推荐引用方式 GB/T 7714 | Wang RR,Gao YD,Ma CH,et al. Mangiferin, an Anti-HIV-1 Agent Targeting Protease and Effective against Resistant Strains[J]. MOLECULES,2011,16(5):4264-4277. |
| APA | Wang RR.,Gao YD.,Ma CH.,Zhang XJ.,Huang CG[*].,...&Zheng YT[*].(2011).Mangiferin, an Anti-HIV-1 Agent Targeting Protease and Effective against Resistant Strains.MOLECULES,16(5),4264-4277. |
| MLA | Wang RR,et al."Mangiferin, an Anti-HIV-1 Agent Targeting Protease and Effective against Resistant Strains".MOLECULES 16.5(2011):4264-4277. |
入库方式： OAI收割
来源：昆明动物研究所
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