传统医学
细胞毒性
萜烯
牡丹
恶性疟原虫
化学
MTT法
甲醇
二萜
生物
立体化学
体外
医学
生物化学
疟疾
有机化学
免疫学
作者
Samyra Imad da Silva Boeno,Ivo José Curcino Vieira,Raimundo Braz-Filho,Michel de Souza Passos,Milena Gonçalves Curcino Vieira,Maria Fernanda Alves do Nascimento,Douglas Costa Gontijo,Alaíde Braga de Oliveira
标识
DOI:10.1016/j.jep.2021.114890
摘要
Different species of the Simaroubaceae family are used in traditional medicine to treat malaria. Among these is Homalolepis suffruticosa (syn. Simaba suffruticosa and Quassia suffruticosa), which is native to Central Brazil and popularly known as calunga. However, there is a lack of investigation concerning its antimalarial effects.To investigate the antiplasmodial and cytotoxic effects of the isolated metabolites and methanol extract from H. suffruticosa roots as well as to conduct the dereplication of this extract aiming to characterize its metabolic profile by UPLC-DAD-ESI-MS/MS.Methanol extract of the H. suffruticosa roots and six isolated compounds were evaluated against chloroquine-resistant Plasmodium falciparum W2 strain by the PfLDH method and cytotoxicity in HepG2 cells by the MTT assay. Dereplication of the extract was performed by UPLC-DAD-ESI-MS/MS.The six isolated compounds disclosed high to moderate antiplasmodial activity (IC50 0.0548 ± 0.0083 μg/mL to 26.65 ± 2.40 μg/mL) and cytotoxicity was in the range of CC50 0.62 ± 0.33 μg/mL to 56.43 ± 2.54 μg/mL, while 5-metoxycantin-6-one proved to be the most potent constituent of the six assayed ones. The methanol extract of the roots showed high in vitro antiplasmodial activity (IC50 1.88 ± 0.56 μg/mL), moderate cytotoxicity (CC50 41.93 ± 2.30 μg/mL), and good selectivity index (SI = 22.30). Finally, C20 quassinoids and canthin-6-one alkaloids were putatively identified in the H. suffruticosa methanol extract by LC-MS.Taken together, the isolated compounds, mainly the 5-metoxycantin-6-one and the methanol extract from H. suffruticosa roots, disclose good antiplasmodial activity, supporting the ethnopharmacological history of the Simaroubaceae species as traditional antimalarial drugs.
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