دورية أكاديمية
أعرض في EDS

Mangiferin, an anti-HIV-1 agent targeting protease and effective against resistant strains.

التفاصيل البيبلوغرافية
العنوان: Mangiferin, an anti-HIV-1 agent targeting protease and effective against resistant strains.
المؤلفون: Wang RR; 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., Gao YD, Ma CH, Zhang XJ, Huang CG, Huang JF, Zheng YT
المصدر: Molecules (Basel, Switzerland) [Molecules] 2011 May 24; Vol. 16 (5), pp. 4264-77. Date of Electronic Publication: 2011 May 24.
نوع المنشور: Journal Article; Research Support, Non-U.S. Gov't
اللغة: English
بيانات الدورية: Publisher: MDPI Country of Publication: Switzerland NLM ID: 100964009 Publication Model: Electronic Cited Medium: Internet ISSN: 1420-3049 (Electronic) Linking ISSN: 14203049 NLM ISO Abbreviation: Molecules Subsets: MEDLINE
أسماء مطبوعة: Original Publication: Basel, Switzerland : MDPI, c1995-
مواضيع طبية MeSH: Anti-HIV Agents/*pharmacology , Drug Resistance, Viral/*drug effects , HIV Protease/*metabolism , HIV-1/*drug effects , HIV-1/*enzymology , Xanthones/*pharmacology, Anti-HIV Agents/chemistry ; Catalytic Domain/drug effects ; Cell Line ; Drug Resistance, Viral/genetics ; HIV Protease/genetics ; Humans ; Leukocytes, Mononuclear/drug effects ; Leukocytes, Mononuclear/virology ; Models, Molecular ; Mutation/genetics ; Protein Binding/drug effects ; Xanthones/chemistry
مستخلص: The anti-HIV-1 activity of mangiferin was evaluated. Mangiferin can inhibit HIV-1(Ⅲ)(B) induced syncytium formation at non-cytotoxic concentrations, with a 50% effective concentration (EC₅₀) at 16.90 μM 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.
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المشرفين على المادة: 0 (Anti-HIV Agents)
0 (Xanthones)
1M84LD0UMD (mangiferin)
EC 3.4.23.- (HIV Protease)
EC 3.4.23.- (p16 protease, Human immunodeficiency virus 1)
تواريخ الأحداث: Date Created: 20110526 Date Completed: 20110921 Latest Revision: 20211020
رمز التحديث: 20240628
مُعرف محوري في PubMed: PMC6263262
DOI: 10.3390/molecules16054264
PMID: 21610656
قاعدة البيانات: MEDLINE
الوصف
تدمد:1420-3049
DOI:10.3390/molecules16054264