Leaves of Vitellaria paradoxa, 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 V. paradoxa leaves possessing antiparasitic activities was investigated. Five pentacyclic triterpenic acids together with 6 ester derivatives were isolated and identified by standards comparison, MS and 1H-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 in vitro on Plasmodium falciparum, Trypanosoma brucei brucei, and Leishmania mexicana mexicana 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-O-p-E/Z-coumaroyltormentic acids, showed an attractive promising antitrypanosomal activity (IC50 = 0.7 µM) with low cytotoxicity (IC50= 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. In vivo efficacy evaluation of this compound, at 50 mg/kg by intraperitoneal route on a T. b. brucei-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.

中文翻译：

---

从 Vitellaria paradoxa 叶中分离的三萜酸和酯衍生物的抗原生动物活性

Vitellaria paradoxa 的叶子，也称为“乳木果树”，在传统医学中用于治疗各种症状，包括疟疾热、痢疾或皮肤感染。研究了具有抗寄生虫活性的 V. paradoxa 叶二氯甲烷提取物的组成。通过标准比较、MS 和 1H-NMR 分析分离和鉴定了五种五环三萜酸和 6 种酯衍生物。首次从该植物中分离出科罗索酸、山楂酸和苦味香豆酸酯及其相应的三萜酸。11 种分离的化合物在体外对恶性疟原虫、布氏锥虫和墨西哥利什曼原虫的抗寄生虫活性进行了评估，并通过对 WI38 细胞的细胞毒性评估确定了它们的选择性。没有一个分离的化合物显示出良好的抗疟原虫活性。单个化合物的抗锥虫活性一般高于它们的抗利什曼原虫。平衡中的一种分离的三萜酯混合物 3-OpE/Z-香豆酰tormentic 酸显示出有吸引力的有前途的抗锥虫活性 (IC50 = 0.7 µM)，与相应的酸相比具有低细胞毒性 (IC50 = 44.5 µM)。对该酯的急性毒性试验未显示对小鼠腹膜内最大累积剂量 100 mg/kg 有任何毒性。该化合物的体内功效评估，以 50 mg/kg 通过腹膜内途径对 T. b. 布鲁氏菌感染小鼠模型显示，感染后第 4 天寄生虫血症显着减少，存活率提高 33.3%。