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Daphnane Diterpenoids from Trigonostemon lii and Inhibition Activities Against HIV-1.

ABSTRACT: Natural 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 from Trigonostemon 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 EC50s from 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.

SUBMITTER: Tan CJ

PROVIDER: S-EPMC7046902 | biostudies-literature | 2020 Feb

REPOSITORIES: biostudies-literature

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Daphnane Diterpenoids from Trigonostemon lii and Inhibition Activities Against HIV-1.

Tan Cheng-Jian CJ Li Shi-Fei SF Huang Ning N Zhang Yu Y Di Ying-Tong YT Zheng Yong-Tang YT Hao Xiao-Jiang XJ

Natural products and bioprospecting 20200211 1

Natural 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 from Trigonostemon 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 EC<sub>50s</sub> from 1.06 to 8.73 ng/mL, and did not show an ...[more]

PMID: 32048186

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