Mangiferin, an Anti-HIV-1 Agent Targeting Protease and Effective against Resistant Strains

	Mangiferin, an Anti-HIV-1 Agent Targeting Protease and Effective against Resistant Strains
	Wang RR 1; Gao YD 2,3; Ma CH 4; Zhang XJ 1,3; Huang CG4; Huang JF2; Zheng YT*1; cghuang@mail.shcnc.ac.cn ; huangjf@mail.kiz.ac.cn ; zhengyt@mail.kiz.ac.cn
	2011
发表期刊	MOLECULES
卷号	16 期号:5 页码:4264-4277
合作性质	其它
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
关键词	Mangiferin Hiv-1 Protease Anti-hiv Agents Drug Resistance
资助者	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). ; 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). ; 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). ; 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).
收录类别	SCI
语种	英语
资助者	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). ; 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). ; 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). ; 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).
文献类型	期刊论文
条目标识符	http://ir.kiz.ac.cn/handle/353002/6626
专题	科研部门_分子免疫药理学（郑永唐）科研部门_动物模型与人类重大疾病机理重点实验室遗传资源与进化国家重点实验室结构生物信息学管理、支撑部门_大型仪器中心
通讯作者	cghuang@mail.shcnc.ac.cn; huangjf@mail.kiz.ac.cn; zhengyt@mail.kiz.ac.cn
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*.,...&zhengyt@mail.kiz.ac.cn.(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.

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