Cytotoxic Triterpenes from Salacia crassifolia and Metabolite Profiling of Celastraceae Species

厚叶五层塔的细胞毒性三萜和卫矛科植物的代谢物分析

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作者:Laila S Espindola, Renata G Dusi, Daniel P Demarque, Raimundo Braz-Filho, Pengcheng Yan, Heidi R Bokesch, Kirk R Gustafson, John A Beutler2

Abstract

The new pentacyclic triterpene 11β-hydroxypristimerin (1), along with the known metabolites pristimerin (2), 6-oxopristimerol (3) and vitideasin (4), were isolated from a Salacia crassifolia root wood extract, following a bioassay-guided fractionation approach. Both the extract and the purified triterpenes displayed pronounced cytotoxic activity against human cancer cell lines. The NCI-60 cell line screen revealed that compound 2 was the most active, with a mean GI50 of 0.17 μM, while compound 1 had a mean GI50 of 8.7 μM. A COMPARE analysis of the screening results showed that pristimerin is likely to be the main compound responsible for the cytotoxic activity of the extract (mean GI50 of 0.3 μg·mL−1). A targeted search for pristimerin and related derivatives using LC-MS/MS revealed the presence of pristimerin (2) and 6-oxopristimerol (3) in all Celastraceae species examined and in all plant parts tested, while vitideasin (4) was only detected in the genus Salacia.

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