Integrative Biology Journals

Natural Products and Bioprospecting ›› 2020, Vol. 10 ›› Issue (1): 37-44.DOI: 10.1007/s13659-020-00231-7

• ORIGINAL ARTICLES • Previous Articles     Next Articles

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. 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
  • Received:2019-12-03 Revised:2020-01-14 Online:2020-02-29 Published:2020-02-24
  • Contact: Yong-Tang Zheng, Xiao-Jiang Hao
  • Supported by:
    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).

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. 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
  • 通讯作者: Yong-Tang Zheng, Xiao-Jiang Hao
  • 基金资助:
    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).

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.

Key words: Trigonostemon lii, Daphnane diterpenoid, Trigonolactone, Anti-HIV

摘要: 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.

关键词: Trigonostemon lii, Daphnane diterpenoid, Trigonolactone, Anti-HIV