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. 2022 Mar;36(5):1288-1295.
doi: 10.1080/14786419.2021.1876045. Epub 2021 Jan 25.

Antiproliferative activity of semisynthetic xylopic acid derivatives

Désiré Soh  1   2   3 , Nkwengoua Ernestine  3 , Emmanuella Marthe Tchana Satchet  3 , Ulrich Dzo Defokou  3 , Bernd Schneider  4 , Vidari Giovanni  5   6 , Barthélemy Nyassé  3
Affiliations

Antiproliferative activity of semisynthetic xylopic acid derivatives

Désiré Soh et al. Nat Prod Res. 2022 Mar.

Abstract

Two ent-kaurene diterpenoids, ent-15-β-acetyloxy-kaur-16-en-19-oic acid (xylopic acid) 1 and ent-7-oxo-kaur-16-en-19-oic acid 2 were isolated from the fruits of Xylopia aethiopica. Chemical manipulation of xylopic acid yielded ent-kaurane derivatives 3, 4, 5, and 6. Their structures were elucidated by spectroscopic analysis, including 1 D- and 2 D-NMR spectroscopies. The antiproliferative activities of compounds 1, 2, 3, 4, and 6 were tested on breast MCF7 and SkBr3, endometrial Ishikawa, ovarian BG-1, mesothelioma IST-MES1 and hepatocellular HepG2 human tumor cells, and on mammalian MRC-10 fibroblast cells. Ketone 2 showed significant antiproliferative activity against MFC7 human breast cancer cells (IC50 = 3 ± 1 µM) and A549 pulmonary adenocarcinoma (8 ± 1 µM), that was higher than the well-known anti-cancer agent cisplatin (IC50 = 19 ± 3 and 15 ± 4 µM, respectively).[Formula: see text].

Keywords: Xylopia aethiopica; annonaceae; antiproliferative activity; ent-kaurane diterpenoids; semisynthesis; xylopic acid.

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