Laboratório de Ciências Químicas, CCT, Universidade Estadual do Norte Fluminense Darcy Ribeiro, Av. Alberto Lamengo, 2000, Parque Califórnia, 28013-602, Campos dos Goytacazes, RJ, Brazil.
Instituto Federal de Educação, Ciência e Tecnologia, Rua Dr. Siqueira, 273, Parque Dom Bosco, 28030-130, Campos dos Goytacazes, RJ, Brazil.
J Ethnopharmacol. 2022 Mar 1;285:114890. doi: 10.1016/j.jep.2021.114890. Epub 2021 Dec 2.
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 (IC 0.0548 ± 0.0083 μg/mL to 26.65 ± 2.40 μg/mL) and cytotoxicity was in the range of CC 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 (IC 1.88 ± 0.56 μg/mL), moderate cytotoxicity (CC 41.93 ± 2.30 μg/mL), and good selectivity index (SI = 22.30). Finally, C 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.
Simaroubaceae 科的不同物种被用于传统医学治疗疟疾。其中包括原产于中美洲的 Homalolepis suffruticosa（同义词为 Simaba suffruticosa 和 Quassia suffruticosa），俗称 calunga。然而，关于其抗疟效果的研究还很缺乏。
研究从 H. suffruticosa 根部分离出的代谢产物和甲醇提取物的抗疟原虫和细胞毒性作用，并通过 UPLC-DAD-ESI-MS/MS 对该提取物进行去重，以表征其代谢谱。
用 PfLDH 法评价 H. suffruticosa 根的甲醇提取物和 6 种分离化合物对氯喹耐药的 Plasmodium falciparum W2 株的抗疟原虫活性，用 MTT 法评价 HepG2 细胞的细胞毒性。通过 UPLC-DAD-ESI-MS/MS 对提取物进行去重。
6 种分离化合物表现出高至中等的抗疟原虫活性（IC 0.0548 ± 0.0083 μg/mL 至 26.65 ± 2.40 μg/mL），细胞毒性范围为 CC 0.62 ± 0.33 μg/mL 至 56.43 ± 2.54 μg/mL，其中 5-甲氧基坎替宁-6-酮是 6 种被测试化合物中最有效的成分。根的甲醇提取物表现出高体外抗疟原虫活性（IC 1.88 ± 0.56 μg/mL）、中等细胞毒性（CC 41.93 ± 2.30 μg/mL）和良好的选择性指数（SI=22.30）。最后，通过 LC-MS 对 H. suffruticosa 甲醇提取物中的 C 苦木素和坎替宁-6-酮生物碱进行了推测性鉴定。
综上所述，分离出的化合物，主要是 5-甲氧基坎替宁-6-酮和 H. suffruticosa 根的甲醇提取物，表现出良好的抗疟原虫活性，支持 Simaroubaceae 物种作为传统抗疟药物的民族药理学历史。
