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Cytotoxic Triterpenes from Salacia crassifolia and Metabolite Profiling of Celastraceae Species.

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.

SUBMITTER: Espindola LS 

PROVIDER: S-EPMC6099938 | biostudies-literature | 2018 Jun

REPOSITORIES: biostudies-literature

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Cytotoxic Triterpenes from <i>Salacia crassifolia</i> and Metabolite Profiling of Celastraceae Species.

Espindola Laila S LS   Dusi Renata G RG   Demarque Daniel P DP   Braz-Filho Raimundo R   Yan Pengcheng P   Bokesch Heidi R HR   Gustafson Kirk R KR   Beutler John A JA  

Molecules (Basel, Switzerland) 20180620 6

The new pentacyclic triterpene 11<i>β</i>-hydroxypristimerin (<b>1</b>), along with the known metabolites pristimerin (<b>2</b>), 6-oxopristimerol (<b>3</b>) and vitideasin (<b>4</b>), were isolated from a <i>Salacia crassifolia</i> 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 <b>2</b> was the most acti  ...[more]

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