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Molecules 2018, 23(6), 1494; https://doi.org/10.3390/molecules23061494

Cytotoxic Triterpenes from Salacia crassifolia and Metabolite Profiling of Celastraceae Species

1
Laboratório de Farmacognosia, Universidade de Brasília, Campus Universitário Darcy Ribeiro, Brasília 70910-900, Brazil
2
Molecular Targets Program, National Cancer Institute, Frederick, MD 21702, USA
3
FAPERJ/Departamento de Química, Universidade Federal Rural do Rio de Janeiro, Seropédica, RJ and Laboratório de Ciências Químicas, Universidade Estadual do Norte Fluminense, Campos dos Goytacazes, Rio de Janeiro 28013-602, Brazil
4
School of Pharmaceutical Sciences, Wenzhou Medical University, Wenzhou 325035, China
5
Basic Science Program, Leidos Biomedical Research, Inc., Frederick National Laboratory for Cancer Research Sponsored by the National Cancer Institute, Frederick, MD 21702, USA
*
Author to whom correspondence should be addressed.
Academic Editor: Roberto Fabiani
Received: 2 June 2018 / Revised: 15 June 2018 / Accepted: 18 June 2018 / Published: 20 June 2018
(This article belongs to the Special Issue Antitumoral Properties of Natural Products)
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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. View Full-Text
Keywords: cytotoxic activity; NCI-60 cancer cell line; pristimerin; Salacia crassifolia; Celastraceae; Brazilian Cerrado biome; Salacia elliptica; Cheiloclinium cognatum; Plenckia populnea cytotoxic activity; NCI-60 cancer cell line; pristimerin; Salacia crassifolia; Celastraceae; Brazilian Cerrado biome; Salacia elliptica; Cheiloclinium cognatum; Plenckia populnea
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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Espindola, L.S.; Dusi, R.G.; Demarque, D.P.; Braz-Filho, R.; Yan, P.; Bokesch, H.R.; Gustafson, K.R.; Beutler, J.A. Cytotoxic Triterpenes from Salacia crassifolia and Metabolite Profiling of Celastraceae Species. Molecules 2018, 23, 1494.

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