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从具有高活性的(Roxb.)Benth. 果实中生物导向分离 - 丙二酰基-(+)色氨酸。

Bioguided isolation of -malonyl-(+)tryptophan from the fruit of (Roxb.) Benth. that showed high activity against .

机构信息

School of Chemical and Biological Sciences, Autonomous University of Sinaloa, Culiacan, Sinaloa, Mexico.

Research Unit in Environment and Health, Autonomous University of Occident, Culiacan, Sinaloa, Mexico.

出版信息

Nat Prod Res. 2021 Feb;35(4):593-599. doi: 10.1080/14786419.2019.1590709. Epub 2019 Mar 31.

Abstract

is distributed in America and Asia where is widely used in traditional medicine. This study describes the bioguided fractionation of the methanol extract (ME) obtained from the fruit that showed activity against ; assay was used to determine toxicity; and the purified compound was computationally analysed to obtain its absorption-distribution-metabolism-excretion-and-toxicity properties (ADMET). The ME and its fractions were more active than praziquantel (PZQ), and the purified compound was characterized as -malonyl-(+)tryptophan (NMT). Parasites treated with NMT showed shorter paralysis and death times (5 and 7 min) than those treated with PZQ (15 and 30 min), both used at 20 mg/mL. Toxicity and ADMET prediction results supported the slight-hazardousness and efficacy of the assayed fractions/compound. This is the first report of the antiparasitary activity of both the ME and NMT, showing their potential to treat human infections.

摘要

在美洲和亚洲均有分布,在传统医学中被广泛应用。本研究描述了从 果实的甲醇提取物(ME)的生物导向分离,该提取物显示出对 的活性; 测定用于测定毒性;并对纯化的化合物进行计算分析以获得其吸收分布代谢排泄和毒性(ADMET)特性。ME 及其馏分比吡喹酮(PZQ)更具活性,而纯化的化合物被表征为 - 丙二酰基 -(+)色氨酸(NMT)。用 NMT 处理的寄生虫的麻痹和死亡时间(5 和 7 分钟)比用 PZQ 处理的寄生虫(15 和 30 分钟)短,两者均以 20 mg/mL 使用。毒性和 ADMET 预测结果支持所测馏分/化合物的轻度危害性和功效。这是 ME 和 NMT 的抗寄生虫活性的首次报道,表明它们有潜力治疗人类 感染。

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