Identification, structural modification, and dichotomous effects on human immunodeficiency virus type 1 (HIV-1) replication of ingenane esters from Euphorbia kansui

被引：39

作者：

Liu, Qingbo ^{[1
,2
]}

Li, Wei ^{[1
]}

Huang, Li ^{[3
]}

Asada, Yoshihisa ^{[1
]}

Morris-Natschke, Susan L. ^{[4
]}

Chen, Chin-Ho ^{[3
]}

Lee, Kuo-Hsiung ^{[4
,5
]}

Koike, Kazuo ^{[1
]}

机构：

[1] Toho Univ, Fac Pharmaceut Sci, Miyama 2-2-1, Funabashi, Chiba 2748510, Japan

[2] Shenyang Pharmaceut Univ, Minist Educ, Key Lab Struct Based Drug Design & Discovery, Shenyang 110016, Liaoning, Peoples R China

[3] Duke Univ, Med Ctr, Dept Surg, Surg Sci, Durham, NC 27710 USA

[4] Univ N Carolina, Eshelman Sch Pharm, Nat Prod Res Labs, Chapel Hill, NC 27599 USA

[5] China Med Univ & Hosp, Chinese Med Res & Dev Ctr, Taichung 40402, Taiwan

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2018年 / 156卷

关键词：

Euphorbia kansui; Anti-HIV; Latency-reversing agent; Ingenane; 3-(2-Naphthoyl)ingenol; ANTIRETROVIRAL THERAPY; DITERPENES; ACTIVATION; EXPRESSION; LATENCY; ROOTS;

D O I：

10.1016/j.ejmech.2018.07.020

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Euphorbia kansui showed potent anti-HIV-1 activity during screening of a library composed of plant extracts from Euphorbiaceae and Thymelaeaceae families. Bioassay-guided isolation led to identification of ingenane esters as the active compounds. Further chemical modification resulted in 3-(2-naphthoyl) ingenol (23), which exhibited the most potent anti-HIV-1 activity. Compound 23 also acted as an HIV-1-latency-reversing agent on activation of HIV-1 replication in a latently infected U1 cell model and a T cell latent HIV-1 model JLat-A2. (C) 2018 Elsevier Masson SAS. All rights reserved.

引用

页码：618 / 627

页数：10

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