Synthesis and anti-HIV-1 activity of the conjugates of gossypol with oligopeptides and D-glucosamine |
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Authors: | Jian Yang, Ju-Rong Li, Jing-Xiang Yang, Long-Long Li, Wen-Jie Ouyang, Shu-Wen Wu, Fang Zhang |
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Affiliation: | a Department of Pharmacy, Renmin Hospital of Wuhan University, Wuhan 430060, China;b The College of Life Sciences, State Key Laboratory of Virology, Modern Virology Research Center, Wuhan University, Wuhan 430072, China;c Wuhan University School of Pharmaceutical Sciences, Wuhan 430071, China |
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Abstract: | A series of novel gossypol derivatives were synthesized and screened for their in vitro anti-HIV-1 activity.The results showed that replacing the aldehyde groups of gossypol with certain oligopeptides and Dglucosamine not only reduced the cytotoxicity of gossypol derivatives but also enhanced their antiviral activity against HIV-1. Interestingly, D-glucosamine derivative of gossypol that lacked the COONa group also exhibited the same potent anti-HIV-1 activity as oligopeptide derivatives with the COONa group.These compounds blocked the entry of HIV-1IIIBinto target cell, which was similar to T20. Furthermore,the molecular docking analysis rationalized their anti-HIV-1 activity. The results also implied that certain oligopeptides and D-glucosamine were important moities to prepare gossypol derivatives as HIV-1 entry inhibitors besides certain amino acids. |
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Keywords: | Gossypol D-Glucosamine derivative Oligopeptide derivative Anti-HIV-1 |
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