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.

Graphic Abstract

Details

Title
Daphnane Diterpenoids from Trigonostemon lii and Inhibition Activities Against HIV-1
Author
Cheng-Jian, Tan 1 ; Shi-Fei, Li 2 ; Huang, Ning 3 ; Zhang, Yu 4 ; Ying-Tong, Di 4 ; Yong-Tang, Zheng 5 ; Xiao-Jiang, Hao 4 

 Kunming Institute of Botany, Chinese Academy of Sciences, State Key Laboratory of Phytochemistry and Plant Resources in West China, Kunming, People’s Republic of China (GRID:grid.458460.b) (ISNI:0000 0004 1764 155X); Guizhou Minzu University, School of Ethnic Medicine, Guiyang, People’s Republic of China (GRID:grid.443389.1) 
 Kunming Institute of Botany, Chinese Academy of Sciences, State Key Laboratory of Phytochemistry and Plant Resources in West China, Kunming, People’s Republic of China (GRID:grid.458460.b) (ISNI:0000 0004 1764 155X); Shanxi University, Institute of Molecular Science, Taiyuan, People’s Republic of China (GRID:grid.163032.5) (ISNI:0000 0004 1760 2008) 
 Kunming Institute of Zoology, Chinese Academy of Sciences, 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, People’s Republic of China (GRID:grid.419010.d) (ISNI:0000 0004 1792 7072); Kunming Medical University, School of Basic Medical, Kunming, People’s Republic of China (GRID:grid.285847.4) (ISNI:0000 0000 9588 0960) 
 Kunming Institute of Botany, Chinese Academy of Sciences, State Key Laboratory of Phytochemistry and Plant Resources in West China, Kunming, People’s Republic of China (GRID:grid.458460.b) (ISNI:0000 0004 1764 155X) 
 Kunming Institute of Zoology, Chinese Academy of Sciences, 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, People’s Republic of China (GRID:grid.419010.d) (ISNI:0000 0004 1792 7072) 
Pages
37-44
Publication year
2020
Publication date
Feb 2020
Publisher
Springer Nature B.V.
ISSN
21922195
e-ISSN
21922209
Source type
Scholarly Journal
Language of publication
English
ProQuest document ID
2366514162
Copyright
Natural Products and Bioprospecting is a copyright of Springer, (2020). All Rights Reserved. This work is published under http://creativecommons.org/licenses/by/4.0/ (the “License”). Notwithstanding the ProQuest Terms and Conditions, you may use this content in accordance with the terms of the License.