CNRS - UMR Ecofog, Université des Antilles et de la Guyane, BP792, 97337 Cayenne cedex, France.
J Ethnopharmacol. 2011 Sep 1;137(1):875-9. doi: 10.1016/j.jep.2011.07.008. Epub 2011 Jul 8.
The study of traditional remedies used by the Chayahuita, an ethnic group from the Peruvian Amazonia, has prompted us to investigate in detail the ethanolic extract of Pseudelephantopus spicatus (Juss. ex Aubl.) C.F. Baker, which has demonstrated strong biological activity towards Leishmania amazonensis. Our goal was to discover the active compound of this plant-based remedy.
A bioguided fractionation of the crude extract was undertaken based on the biological activity recorded against Leishmania amazonensis axenic amastigotes in in vitro bioassays.
Three strongly to moderately active compounds were isolated: two hirsutinolides (the 8,13-diacetyl-piptocarphol and the 8-acetyl-13-O-ethyl-piptocarphol) and ursolic acid. IC(50) against Leishmania amazonensis axenic amastigotes are respectively 0.2, 0.37 and 0.99 μM (while IC(50) of amphotericin B is 0.41 μM). These compounds have never been isolated from this plant species, and germacranolides have never been identified as potential antileishmanial agents.
The compounds isolated from Pseudelephantopus spicatus account for the antileishmanial activity of the plant, thus giving support to its use by the Chayahuita in Peru.
对来自秘鲁亚马逊地区的 Chayahuita 民族使用的传统疗法的研究促使我们详细研究了 Pseudelephantopus spicatus（Juss. ex Aubl.）C.F. Baker 的乙醇提取物，该提取物对 Leishmania amazonensis 具有很强的生物活性。我们的目标是发现这种植物疗法的活性化合物。
根据体外生物测定中对 Leishmania amazonensis 无鞭毛体的生物活性，对粗提取物进行了生物导向的分级分离。
分离出三种活性较强或中等的化合物：两种毛蕊花糖苷（8,13-二乙酰-刺桐醇和 8-乙酰-13-O-乙基-刺桐醇）和熊果酸。对 Leishmania amazonensis 无鞭毛体的 IC50 分别为 0.2、0.37 和 0.99 μM（而两性霉素 B 的 IC50 为 0.41 μM）。这些化合物从未从该植物种中分离出来，并且从未将倍半萜烯内酯鉴定为潜在的抗利什曼原虫药物。
从 Pseudelephantopus spicatus 中分离出的化合物解释了该植物的抗利什曼活性，从而支持了 Chayahuita 在秘鲁使用该植物。
