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, Dominique Schols, Sandra Claes, Milka B. Jadranin, Boris M. Mandić, Karlo Wittine, 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 1‒4 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.
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.