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链霉菌 CB01388 产生的除草霉素具有抗隐孢子虫活性。

Herbicidins from Streptomyces sp. CB01388 Showing Anti- Cryptosporidium Activity.

机构信息

Department of Chemistry , The Scripps Research Institute , Jupiter , Florida 33458 , United States.

California Institute for Biomedical Research , La Jolla , California 92037 , United States.

出版信息

J Nat Prod. 2018 Apr 27;81(4):791-797. doi: 10.1021/acs.jnatprod.7b00850. Epub 2018 Feb 22.

Abstract

A high-content imaging assay was used to screen the fraction collection of the Natural Product Library at The Scripps Research Institute for inhibitors of Cryptosporidium parvum. A chemical investigation of one strain, Streptomyces sp. CB01388, resulted in the isolation of six herbicidins (1-6), one of which is new (herbicidin L, 1). Five of the six herbicidins (1-3, 5, 6) showed moderate inhibitory activity against C. parvum, with 1 and 6 comparable to the FDA-approved drug nitazoxanide, and 2-6 showed no toxicity to the host HCT-8 cells and human HEK293T and HepG2 cells. These findings highlight the herbicidin scaffold for anti- Cryptosporidium drug development.

摘要

高内涵成像分析方法被用于筛选斯克里普斯研究所天然产物库的馏分,以寻找隐孢子虫的抑制剂。对一株链霉菌 CB01388 的化学研究导致了六种除草菌素(1-6)的分离,其中一种是新的(除草菌素 L,1)。六种除草菌素中的五种(1-3、5、6)对隐孢子虫表现出中等抑制活性,其中 1 和 6 可与美国食品和药物管理局批准的药物硝唑尼特相媲美,而 2-6 对宿主 HCT-8 细胞、人 HEK293T 和 HepG2 细胞没有毒性。这些发现突出了除草菌素骨架在抗隐孢子虫药物开发中的应用。

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