Mangiferin, an Anti-HIV-1 Agent Targeting Protease and Effective against Resistant Strains
文献类型：期刊论文
| 作者 | Wang, Rui-Rui3; Gao, Yue-Dong1,2; Ma, Chun-Hui4; Zhang, Xing-Jie1,3; Huang, Cheng-Gang4 ; Huang, Jing-Fei2; Zheng, Yong-Tang3
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| 刊名 | MOLECULES
 |
| 出版日期 | 2011-05 |
| 卷号 | 16期号:5页码:4264-4277 |
| 关键词 | mangiferin HIV-1 protease anti-HIV agents drug resistance |
| ISSN号 | 1420-3049 |
| DOI | 10.3390/molecules16054264 |
| 文献子类 | Article |
| 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 (EC(50)) 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. |
| WOS关键词 | HERPES-SIMPLEX VIRUS ; NATURALLY-OCCURRING GLUCOSYLXANTHONE ; DRUG-RESISTANCE ; INDICA L. ; ANTIVIRAL ACTIVITY ; HIV ; INHIBITORS ; EXTRACT ; MICE ; MUTATIONS |
| 资助项目 | 973 Program[2009CB522306] ; Eleventh Five-Year Key Scientific and Technological Program of China[2009ZX09501-029] ; Eleventh Five-Year Key Scientific and Technological Program of China[2008ZX10001-002] ; Eleventh Five-Year Key Scientific and Technological Program of China[2009ZX09103-414] ; CAS[KSCX1-YW-10] ; CAS[KSCX2-YW-R-185] |
| WOS研究方向 | Biochemistry & Molecular Biology ; Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:000290955800057 |
| 出版者 | MDPI AG |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/278539]  |
| 专题 | 上海中药现代化研究中心 |
| 通讯作者 | Huang, Jing-Fei |
| 作者单位 | 1.Chinese Acad Sci, Grad Sch, Beijing 100039, Peoples R China; 2.Chinese Acad Sci, Kunming Inst Zool, State Key Lab Genet Resources & Evolut, Kunming 650223, Peoples R China; 3.Chinese Acad Sci, Kunming Inst Zool, Chinese Acad Sci & Yunnan Prov, Key Lab Anim Models & Human Dis Mech, Kunming 650223, Peoples R China; 4.Chinese Acad Sci, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Wang, Rui-Rui,Gao, Yue-Dong,Ma, Chun-Hui,et al. Mangiferin, an Anti-HIV-1 Agent Targeting Protease and Effective against Resistant Strains[J]. MOLECULES,2011,16(5):4264-4277. |
| APA | Wang, Rui-Rui.,Gao, Yue-Dong.,Ma, Chun-Hui.,Zhang, Xing-Jie.,Huang, Cheng-Gang.,...&Zheng, Yong-Tang.(2011).Mangiferin, an Anti-HIV-1 Agent Targeting Protease and Effective against Resistant Strains.MOLECULES,16(5),4264-4277. |
| MLA | Wang, Rui-Rui,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：上海药物研究所
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