New Anti-HIV Agents Isolated From Two Euphorbia Species

IF 3.6 3区 医学 Q2 CHEMISTRY, MEDICINAL
Gordana B. Krstić, Dominique Schols, Sandra Claes, Milka B. Jadranin, Boris M. Mandić, Karlo Wittine, Vele V. Tešević
{"title":"New Anti-HIV Agents Isolated From Two Euphorbia Species","authors":"Gordana B. Krstić,&nbsp;Dominique Schols,&nbsp;Sandra Claes,&nbsp;Milka B. Jadranin,&nbsp;Boris M. Mandić,&nbsp;Karlo Wittine,&nbsp;Vele V. Tešević","doi":"10.1002/ardp.70080","DOIUrl":null,"url":null,"abstract":"<div>\n \n <p>Four previously unreported tigliane diterpenes (<b>1</b>, <b>2</b>, <b>4</b>, and <b>6</b>), along with two known tiglianes (<b>3</b> and <b>5</b>), were isolated from the latex of <i>Euphorbia palustris</i> and <i>Euphorbia lucida</i>. The structures of the isolated compounds were elucidated by spectroscopic techniques. Antiviral activity assays for compounds <b>1</b>‒<b>4</b> and <b>6</b> against HIV-1 and HIV-2 replication were performed on a CD4<sup>+</sup> T cell line, MT-4 cells. The compounds were tested for their ability to inhibit infection by the HIV-1 strain NL4.3 and the HIV-2 strain ROD. Compound <b>6</b> showed no activity against either strain, while compound <b>4</b> was only slightly active against HIV-2 (EC<sub>50</sub> = 12.778 µM). Compounds <b>1</b>, <b>2</b>, and <b>3</b> were able to inhibit both HIV-1 and HIV-2 infections. Among them, compound <b>2</b> was the most potent, with EC<sub>50</sub> values of 0.069 µM for HIV-1 NL4.3 and 0.023 µM for HIV-2 ROD. The PBMC toxicity profile for compound <b>2</b> is also more favorable compared with MT-4 cells with CC<sub>50</sub> = 50 μM.</p></div>","PeriodicalId":128,"journal":{"name":"Archiv der Pharmazie","volume":"358 9","pages":""},"PeriodicalIF":3.6000,"publicationDate":"2025-09-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"Archiv der Pharmazie","FirstCategoryId":"3","ListUrlMain":"https://onlinelibrary.wiley.com/doi/10.1002/ardp.70080","RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q2","JCRName":"CHEMISTRY, MEDICINAL","Score":null,"Total":0}
引用次数: 0

Abstract

Four previously unreported tigliane diterpenes (1, 2, 4, and 6), along with two known tiglianes (3 and 5), were isolated from the latex of Euphorbia palustris and Euphorbia lucida. The structures of the isolated compounds were elucidated by spectroscopic techniques. Antiviral activity assays for compounds 14 and 6 against HIV-1 and HIV-2 replication were performed on a CD4+ T cell line, MT-4 cells. The compounds were tested for their ability to inhibit infection by the HIV-1 strain NL4.3 and the HIV-2 strain ROD. Compound 6 showed no activity against either strain, while compound 4 was only slightly active against HIV-2 (EC50 = 12.778 µM). Compounds 1, 2, and 3 were able to inhibit both HIV-1 and HIV-2 infections. Among them, compound 2 was the most potent, with EC50 values of 0.069 µM for HIV-1 NL4.3 and 0.023 µM for HIV-2 ROD. The PBMC toxicity profile for compound 2 is also more favorable compared with MT-4 cells with CC50 = 50 μM.

Abstract Image

从两种大戟中分离出新的抗hiv药物
从palustris和Euphorbia lucida的乳胶中分离出四种以前未报道的tigliane二萜(1,2,4和6),以及两种已知的tigliane(3和5)。分离得到的化合物的结构用光谱技术进行了鉴定。化合物1-4和6对HIV-1和HIV-2复制的抗病毒活性测定在CD4+ T细胞系MT-4细胞上进行。检测了化合物对HIV-1株NL4.3和HIV-2株ROD的抑制能力。化合物6对两种病毒均无活性,而化合物4对HIV-2只有轻微活性(EC50 = 12.778µM)。化合物1、2和3能够抑制HIV-1和HIV-2感染。其中化合物2对HIV-1 NL4.3的EC50值为0.069µM,对HIV-2 ROD的EC50值为0.023µM。与CC50 = 50 μM的MT-4细胞相比,化合物2的PBMC毒性谱也更有利。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
求助全文
约1分钟内获得全文 求助全文
来源期刊
Archiv der Pharmazie
Archiv der Pharmazie 医学-化学综合
CiteScore
7.90
自引率
5.90%
发文量
176
审稿时长
3.0 months
期刊介绍: Archiv der Pharmazie - Chemistry in Life Sciences is an international journal devoted to research and development in all fields of pharmaceutical and medicinal chemistry. Emphasis is put on papers combining synthetic organic chemistry, structural biology, molecular modelling, bioorganic chemistry, natural products chemistry, biochemistry or analytical methods with pharmaceutical or medicinal aspects such as biological activity. The focus of this journal is put on original research papers, but other scientifically valuable contributions (e.g. reviews, minireviews, highlights, symposia contributions, discussions, and essays) are also welcome.
×
引用
GB/T 7714-2015
复制
MLA
复制
APA
复制
导出至
BibTeX EndNote RefMan NoteFirst NoteExpress
×
提示
您的信息不完整,为了账户安全,请先补充。
现在去补充
×
提示
您因"违规操作"
具体请查看互助需知
我知道了
×
提示
确定
请完成安全验证×
copy
已复制链接
快去分享给好友吧!
我知道了
右上角分享
点击右上角分享
0
联系我们:info@booksci.cn Book学术提供免费学术资源搜索服务,方便国内外学者检索中英文文献。致力于提供最便捷和优质的服务体验。 Copyright © 2023 布克学术 All rights reserved.
京ICP备2023020795号-1
ghs 京公网安备 11010802042870号
Book学术文献互助
Book学术文献互助群
群 号:604180095
Book学术官方微信