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来自长柱三宝木的瑞香烷二萜类化合物及其对HIV-1的抑制活性。

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

作者信息

Tan Cheng-Jian, Li Shi-Fei, Huang Ning, Zhang Yu, Di Ying-Tong, Zheng Yong-Tang, Hao Xiao-Jiang

机构信息

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.

School of Ethnic Medicine, Guizhou Minzu University, Guiyang, 550025, Guizhou, People's Republic of China.

出版信息

Nat Prod Bioprospect. 2020 Feb;10(1):37-44. doi: 10.1007/s13659-020-00231-7. Epub 2020 Feb 11.

DOI:10.1007/s13659-020-00231-7
PMID:32048186
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC7046902/
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 EC 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.

摘要

天然产物是发现更有效的抗HIV药物的重要来源。在本研究中，从海南三宝木中分离出6种瑞香烷二萜类化合物，其中包括3种未报道的结构，这些化合物在纳摩尔/皮摩尔范围内对HIV-1毒株的复制表现出显著活性。同时，这些二萜类化合物显著抑制H9/HIV-1 IIIB细胞与未感染的C8166细胞的融合，其半数有效浓度（EC）为1.06至8.73 ng/mL，并且对HIV-1逆转录酶未表现出任何抑制活性。此外，所有二萜类化合物对T20耐药HIV-1毒株PNL4-3gp41(36G)V38E、N42S和pNL4-3gp41(36G)V38A、N42T均表现出显著抑制作用。结果表明，这6种二萜类化合物可能是一种新型的潜在先导化合物，可作为HIV进入抑制剂，特别是对于那些感染T20耐药变体的患者。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/78ae/7046902/da6b558e17b1/13659_2020_231_Fig5_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/78ae/7046902/f49d718f570d/13659_2020_231_Fig1_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/78ae/7046902/f2e4fd69769c/13659_2020_231_Fig2_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/78ae/7046902/7fd4d63f4d69/13659_2020_231_Fig3_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/78ae/7046902/a3f570c59196/13659_2020_231_Fig4_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/78ae/7046902/da6b558e17b1/13659_2020_231_Fig5_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/78ae/7046902/f49d718f570d/13659_2020_231_Fig1_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/78ae/7046902/f2e4fd69769c/13659_2020_231_Fig2_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/78ae/7046902/7fd4d63f4d69/13659_2020_231_Fig3_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/78ae/7046902/a3f570c59196/13659_2020_231_Fig4_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/78ae/7046902/da6b558e17b1/13659_2020_231_Fig5_HTML.jpg

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