| ORIGINAL ARTICLES |
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Daphnane Diterpenoids from Trigonostemon lii and Inhibition Activities Against HIV-1 |
| Cheng-Jian Tan1,3, Shi-Fei Li1,4, Ning Huang2,5, Yu Zhang1, Ying-Tong Di1, Yong-Tang Zheng2, Xiao-Jiang Hao1 |
1 State Key Laboratory of Phytochemistry and Plant Resources in West China, Kunming Institute of Botany, Chinese Academy of Sciences, Kunming 650204, Yunnan, People's Republic of China;
2 Key Laboratory of Bioactive Peptides of Yunnan Province/Key Laboratory of Animal Models and Human Disease Mechanisms of the Chinese Academy of Sciences, Center for Biosafety Mega-Science, Kunming Institute of Zoology, Chinese Academy of Sciences, Kunming 650223, Yunnan, People's Republic of China;
3 School of Ethnic Medicine, Guizhou Minzu University, Guiyang 550025, Guizhou, People's Republic of China;
4 Institute of Molecular Science, Shanxi University, Taiyuan 030006, Shanxi, People's Republic of China;
5 School of Basic Medical, Kunming Medical University, Kunming 650500, Yunnan, People's Republic of China |
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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.
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| Keywords
Trigonostemon lii
Daphnane diterpenoid
Trigonolactone
Anti-HIV
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| Fund:This work was supported financially by grants from the National Science Foundation of China (21432010 and 81660612) and Technological leading talent project of Yunnan (2015HA020). Yunnan Applied Basic Research Project-Kunming Medical University Union Foundation (2017FE467 (-127), Scientific Research Fund Projects from the Department of Education of Yunnan (2016ZDX042) and the HundredTalent Program of Kunming Medical University (60117190441). |
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Corresponding Authors:
Yong-Tang Zheng, Xiao-Jiang Hao
E-mail: zhengyt@mail.kiz.ac.cn;haoxj@mail.kib.ac.cn
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Issue Date: 29 February 2020
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