Antiparasitic Activity of Compounds Isolated from Ganoderma tuberculosum (Agaricomycetes) from Mexico.

Victoria Espinosa-García, Jose J Fernandez, Desirée San Nicolás-Hernández, Iñigo Arberas-Jiménez, Rubén L Rodríguez-Expósito, María L Souto, José E Piñero, Guillermo Mendoza, Jacob Lorenzo-Morales, Ángel Trigos
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Abstract

The genus Ganoderma has a long history of use in traditional Asiatic medicine due to its different nutritional and medicinal properties. In Mexico, the species G. tuberculosum is used in indigenous communities, for example, the Wixaritari and mestizos of Villa Guerrero Jalisco for the treatment of diseases that may be related to parasitic infections; however, few chemical studies corroborate its traditional medicinal potential. Thereby, the objective of this study was to isolate and identify anti-parasitic activity compounds from a strain of G. tuberculosum native to Mexico. From the fruiting bodies of G. tuberculosum (GVL-21) a hexane extract was obtained which was subjected to guided fractioning to isolate pure compounds. The in vitro anti-parasitic activity of the pure compound (IC50) was assayed against Leishmania amazonensis, Trypanosoma cruzi, Acanthamoeba castellanii Neff, and Naegleria fowleri. Furthermore, the cytotoxicity (CC50) of the isolated compounds was determined against murine macrophages. The guided fractioning produced 5 compounds: ergosterol (1), ergosta-4,6,8(14),22-tetraen-3-one (2), ergosta-7,22-dien-3β-ol (3), 3,5-dihydroxy-ergosta-7,22-dien-6-one (4), and ganoderic acid DM (5). Compounds 2 and 5 showed the best anti-parasitic activity in an IC50 range of 54.34 ± 8.02 to 12.38 ± 2.72 µM against all the parasites assayed and low cytotoxicity against murine macrophages. The present study showed for the first time the in vitro anti-parasitic activity of compounds 1-5 against L. amazonensis, T. cruzi, A. castellanii Neff, and N. fowleri, corroborating the medicinal potential of Ganoderma and its traditional applications.

从墨西哥结核灵芝中分离的化合物的抗寄生虫活性。
灵芝属由于其不同的营养和药用特性,在传统的亚洲医学中有着悠久的使用历史。在墨西哥,G.tuberculosum物种被用于土著社区,例如Villa Guerrero Jalisco的Wixaritari和mestizos,用于治疗可能与寄生虫感染有关的疾病;然而,很少有化学研究证实其传统药用潜力。因此,本研究的目的是从墨西哥原产的结核分枝杆菌菌株中分离和鉴定抗寄生虫活性化合物。从结核分枝杆菌(GVL-21)的子实体获得己烷提取物,其经过引导分级以分离纯化合物。测定了纯化合物(IC50)对亚马逊利什曼原虫、克鲁兹锥虫、卡斯特拉尼棘阿米巴和福氏奈格里线虫的体外抗寄生虫活性。此外,测定了分离的化合物对小鼠巨噬细胞的细胞毒性(CC50)。引导分馏产生了5种化合物:麦角甾醇(1)、麦角甾-4,6,8(14)、22-四烯-3-酮(2)、麦角甾醇-7,22-二烯-3β-醇(3)、3,5-二羟基麦角甾醇-7,7,22-二烯-6-酮(4)和甘草酸DM(5)。化合物2和5对所有测定的寄生虫显示出最佳的抗寄生虫活性,IC50范围为54.34±8.02至12.38±2.72µM,对小鼠巨噬细胞显示出低细胞毒性。本研究首次显示了化合物1-5对亚马逊乳杆菌、克鲁兹乳杆菌、卡斯特利亚尼乳杆菌和福氏乳杆菌的体外抗寄生虫活性,证实了灵芝的药用潜力及其传统应用。
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