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- Title
Daphnane Diterpenoids from Trigonostemon lii and Inhibition Activities Against HIV-1.
- Authors
Tan, Cheng-Jian; Li, Shi-Fei; Huang, Ning; Zhang, Yu; Di, Ying-Tong; Zheng, Yong-Tang; Hao, Xiao-Jiang
- 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.
- Subjects
DITERPENES; ANTI-HIV agents; HIV fusion inhibitors; NATURAL products
- Publication
Natural Products & Bioprospecting, 2020, Vol 10, Issue 1, p37
- ISSN
2192-2209
- Publication type
Article
- DOI
10.1007/s13659-020-00231-7