Antiproliferative activity of semisynthetic xylopic acid derivatives.
Nat Prod Res
; 36(5): 1288-1295, 2022 Mar.
Article
em En
| MEDLINE
| ID: mdl-33487063
ABSTRACT
Two ent-kaurene diterpenoids, ent-15-ß-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].
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Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Diterpenos do Tipo Caurano
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Diterpenos
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Xylopia
Idioma:
En
Ano de publicação:
2022
Tipo de documento:
Article