New Anti‐HIV Agents Isolated From Two <i>Euphorbia</i> Species

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<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 6 showed no activity against either strain, while compound 4 was only slightly active against HIV-2 (EC<sub>50</sub> = 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 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 2 is also more favorable compared with MT-4 cells with CC<sub>50</sub> = 50 μM.

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Publication Details

Journal
Archiv der Pharmazie
Published
2025-09-01
DOI
https://doi.org/10.1002/ardp.70080
Primary Topic
Bioactive Natural Diterpenoids Research
Type
article
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article

New Anti‐HIV Agents Isolated From Two Euphorbia Species

Vele Tešević, Milka Jadranin, Dominique Schols, Karlo Wittine et al.
Archiv der Pharmazie
Bioactive Natural Diterpenoids Research
article

New Anti‐HIV Agents Isolated From Two Euphorbia Species

Vele Tešević, Milka Jadranin, Dominique Schols, Karlo Wittine, Gordana Krstić, Boris Mandić, Sandra Claes
article en

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<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 6 showed no activity against either strain, while compound 4 was only slightly active against HIV-2 (EC<sub>50</sub> = 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 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 2 is also more favorable compared with MT-4 cells with CC<sub>50</sub> = 50 μM.

Archiv der PharmazieVol. 358(9)
Rega Institute for Medical Research (BE), University of Belgrade (RS), Croatian Science Foundation (HR)
Openalex Percentile: Top 79%
Bioactive Natural Diterpenoids Research
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New Anti‐HIV Agents Isolated From Two <i>Euphorbia</i> Species — Vele Tešević, Milka Jadranin, et al. · Archiv der Pharmazie (2025) | TGRS Research Map | TGRS