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来自卫矛科美登木的抗原生动物倍半萜吡啶生物碱。

Antiprotozoal sesquiterpene pyridine alkaloids from Maytenus ilicifolia.

机构信息

Departamento de Química Orgânica, Instituto de Química, Universidade Estadual Paulista (UNESP), Araraquara, SP 14800-900, Brazil.

出版信息

J Nat Prod. 2012 May 25;75(5):991-5. doi: 10.1021/np300077r. Epub 2012 May 4.

Abstract

As part of a bioprospecting program aimed at the discovery of antiprotozoal agents from the Brazilian flora, two new sesquiterpene pyridine alkaloids, ilicifoliunines A (1) and B (2), along with the known alkaloids aquifoliunine E-I (3) and mayteine (4), were isolated from the root bark of Maytenus ilicifolia. The structures of 1 and 2 were established on the basis of spectroscopic data interpretation. Alkaloid 3 displayed potent in vitro antiprotozoal activity against Leishmania chagasi and Trypanosoma cruzi, with IC(50) values of 1.4 and 41.9 μM, respectively, as well as low cytotoxicity against murine peritoneal macrophages (IC(50) of 1.8 mM).

摘要

作为从巴西植物群中发现抗原生动物剂的生物勘探计划的一部分,从 Maytenus ilicifolia 的根皮中分离得到了两种新的倍半萜吡啶生物碱ilicifoliunines A(1)和 B(2),以及已知的生物碱aquifoliunine E-I(3)和 mayteine(4)。根据光谱数据解释,确定了 1 和 2 的结构。生物碱 3 对 Leishmania chagasi 和 Trypanosoma cruzi 表现出很强的体外抗原生动物活性,IC 50 值分别为 1.4 和 41.9 μM,对鼠腹腔巨噬细胞的细胞毒性也很低(IC 50 为 1.8 mM)。

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