Daphnane Diterpenoids from Trigonostemon lii and Inhibition Activities Against HIV-1
Daphnane Diterpenoids from Trigonostemon lii and Inhibition Activities Against HIV-1
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DOI：
10.1007/s13659-020-00231-7
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发表时间：
2020-01
影响因子：
4.7
通讯作者：
Cheng-Jian Tan;Shi-fei Li;Ning Huang;Yu Zhang;Y. Di;Yong-tang Zheng;X. Hao
中科院分区：
文献类型：
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作者：
Cheng-Jian Tan;Shi-fei Li;Ning Huang;Yu Zhang;Y. Di;Yong-tang Zheng;X. Hao
摘要天然产物是发现更有效的抗 HIV 药物的重要来源。在这项研究中，从三叶草中分离出六种瑞香二萜类化合物，包括三种未报道的结构，它们在纳摩尔/皮摩尔范围内表现出显着的抗 HIV-1 病毒株复制活性。同时，这些二萜类化合物显着抑制H9/HIV-1 IIIB细胞与未感染的C8166细胞的融合，EC50为1.06至8.73 ng/mL，并且对HIV-1逆转录酶没有表现出任何抑制活性。此外，所有二萜类化合物均对 T20 抗性 HIV-1 菌株 PNL4-3gp41(36G)V38E、N42S 和 pNL4-3gp41(36G)V38A、N42T 表现出显着的抑制作用。结果表明，这六种二萜类化合物可能是一种新型潜在的主要候选药物，可作为 HIV 进入抑制剂，特别是对于那些感染 T20 耐药变种的人。 图文摘要
AbstractNatural products are the important source for the discovery of more potent anti-HIV agents. In this study, six daphnane diterpenoids including three unreported structures were isolated fromTrigonostemon lii, which showed significant activities against HIV-1 strains replication in the nanomolar/picomolar range. Meanwhile, these diterpenoids significantly inhibited the fusion of H9/HIV-1 IIIB cells with uninfected C8166 cells, with the EC50sfrom 1.06 to 8.73 ng/mL, and did not show any inhibition activities against HIV-1 reverse transcriptase. Moreover, all of the diterpenoids shows significant inhibitions against T20-resistan HIV-1 strains, PNL4-3gp41(36G)V38E, N42S and pNL4-3gp41(36G)V38A, N42T. The results revealed that the six diterpenoids could be a new type of potential lead candidate as an HIV entry inhibitor, particularly for those infected by T20-resistant variants.Graphic Abstract