Louvain Drug Research Institute-Pharmacognosy (LDRI-GNOS), Université catholique de Louvain Brussels, Belgium.
Laboratory of Pharmacognosy, CIRM, Université de Liège, Liège, Belgium.
Planta Med. 2021 Aug;87(10-11):860-867. doi: 10.1055/a-1286-1879. Epub 2020 Dec 7.
Leaves of , also called "Shea butter tree", are used in traditional medicine to treat various symptoms including malaria fever, dysentery, or skin infections. Composition of the dichloromethane extract of leaves possessing antiparasitic activities was investigated. Five pentacyclic triterpenic acids together with 6 ester derivatives were isolated and identified by standards comparison, MS and H-NMR analysis. Corosolic, maslinic, and tormentic coumaroyl esters and their corresponding triterpenic acids were isolated from this plant for the first time. The antiparasitic activities of the 11 isolated compounds were evaluated on , and and their selectivity determined by cytotoxicity evaluation on WI38 cells. None of the isolated compounds showed good antiplasmodial activity. The antitrypanosomal activity of individual compounds was in general higher than their antileishmanial one. One isolated triterpenic ester mixture in equilibrium, 3---coumaroyltormentic acids, showed an attractive promising antitrypanosomal activity (IC = 0.7 µM) with low cytotoxicity (IC= 44.5 µM) compared to the corresponding acid. Acute toxicity test on this ester did not show any toxicity at the maximal cumulative dose of 100 mg/kg intraperitoneally on mice. efficacy evaluation of this compound, at 50 mg/kg by intraperitoneal route on a -infected mice model, showed a significant parasitemia reduction on day 4 post-infection together with 33.3% survival improvement. Further bioavailability and PK studies are needed along with mode of action investigations to further assess the potential of this molecule.
, 又称“乳木果油树”，其叶子在传统医学中被用于治疗各种症状，包括疟疾发热、痢疾或皮肤感染。研究了具有抗寄生虫活性的 叶子的二氯甲烷提取物的成分。通过标准比较、MS 和 H-NMR 分析，分离并鉴定了 5 种五环三萜酸和 6 种酯衍生物。从这种植物中首次分离到了乳香酸、齐墩果酸和没食子酸的酯及其相应的三萜酸。评价了 11 个分离化合物对 、 和 的抗寄生虫活性，并通过 WI38 细胞的细胞毒性评价确定了它们的选择性。分离得到的化合物均无良好的抗疟原虫活性。个别化合物的抗锥虫活性普遍高于抗利什曼原虫活性。一个处于平衡状态的分离三萜酯混合物，即 3---没食子酰基苦木酸，具有良好的抗锥虫活性（IC=0.7 μM），同时具有低细胞毒性（IC=44.5 μM），与相应的酸相比具有吸引力。该酯在最大累积剂量为 100 mg/kg 时，对小鼠经腹腔给药的急性毒性试验未显示出任何毒性。在感染 - 的小鼠模型中，以 50 mg/kg 经腹腔途径进行该化合物的疗效评价，感染后第 4 天，寄生虫血症显著减少，存活率提高了 33.3%。需要进一步进行生物利用度和 PK 研究，并进行作用机制研究，以进一步评估该分子的潜力。
