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Cinnamic acids derived compounds with antileishmanial activity target Leishmania amazonensis arginase
Chemical Biology & Drug Design ( IF 3 ) Pub Date : 2018-10-10 , DOI: 10.1111/cbdd.13391
Edson Roberto da Silva 1 , Simone Brogi 2 , Alessandro Grillo 2 , Giuseppe Campiani 2 , Sandra Gemma 2 , Paulo Cezar Vieira 3 , Claudia do Carmo Maquiaveli 4
Affiliation  

This study describes the activity of five natural hydroxycinnamic acids and derived compound: caffeic (1), rosmarinic (2), chlorogenic (3), and cryptochlorogenic (4), acids and isoverbascoside (5). All compounds inhibited Leishmania amazonensis arginase with IC50 —in range of 1.5—11 μM. Compounds 2 and 5 also showed activity against promastigotes of L. amazonensis with IC50 = 61 (28–133) μM and IC50 = 14 (9–24) μM, respectively. Further computational studies applying molecular docking simulations were performed on the competitive inhibitors to gain insight into the molecular basis for arginase inhibition and could be exploited to the development of new antileishmanials drug targeting parasite arginase.

中文翻译:

肉桂酸衍生的具有抗疟原虫活性的化合物靶向亚马逊利什曼原虫精氨酸酶

这项研究描述了五种天然羟基肉桂酸及其衍生化合物的活性:咖啡因(1),迷迭香(2),绿原(3)和隐绿原(4),酸和异山bas苷(5)。所有化合物均以1.5〜11μM的IC 50抑制亚马逊利什曼原虫精氨酸酶。化合物25对的前鞭毛体也显示出活性亚马逊利什曼原虫与IC 50  = 61(28-133)μM和IC 50 分别为14(9–24)μM。对竞争性抑制剂进行了应用分子对接模拟的进一步计算研究,以深入了解精氨酸酶抑制的分子基础,并可用于开发针对寄生虫精氨酸酶的新抗疟药。
更新日期:2018-10-10
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