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从北美檫木中分离出的化合物的抗利什曼原虫活性

Antileishmanial Activity of Compounds Isolated from Sassafras albidum.

作者信息

Pulivarthi Divya, Steinberg Kelly Marie, Monzote Lianet, Piñón Abel, Setzer William N

出版信息

Nat Prod Commun. 2015 Jul;10(7):1229-30.

Abstract

Leishmaniasis is a neglected tropical disease caused by Leishmania parasitic protozoa, which currently lacks efficient treatment. Natural products have shown promise as a potential source for antiprotozoal drugs. This work focuses on the antileishmanial potential of Sassafras albidum (Lauraceae) bark extract. The crude bark extract of S. albidum showed excellent antileishmanial activity with an IC50 value less than 12.5 μg/mL against promastigotes of L. amazonensis. The chloroform stem bark extract of S. albidum was subjected to preparative column chromatography. Five compounds were isolated, purified by recrystallization, and identified as sesamin, spinescin, β-sitosterol, hexatriacontanal, and 1-triacontanol. Antileishmanial and cytotoxic screening were performed on these compounds. Sesamin exhibited the best activity against L. amazonensis with an IC50 of 15.8 μg/mL and was not cytotoxic to mouse macrophage cells (CC50 > 100 μg/mL).

摘要

利什曼病是一种由利什曼原虫寄生原生动物引起的被忽视的热带疾病,目前缺乏有效的治疗方法。天然产物已显示出作为抗原生动物药物潜在来源的前景。这项工作聚焦于北美檫木(樟科)树皮提取物的抗利什曼原虫潜力。北美檫木的粗树皮提取物对亚马逊利什曼原虫前鞭毛体表现出优异的抗利什曼原虫活性,IC50值小于12.5μg/mL。对北美檫木的氯仿茎皮提取物进行了制备柱色谱法分离。分离出五种化合物,通过重结晶进行纯化,并鉴定为芝麻素、刺芒柄花素、β-谷甾醇、二十六醛和正三十烷醇。对这些化合物进行了抗利什曼原虫和细胞毒性筛选。芝麻素对亚马逊利什曼原虫表现出最佳活性,IC50为15.8μg/mL,对小鼠巨噬细胞无细胞毒性(CC50>100μg/mL)。

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