从草酸青霉中分离得到的细胞毒 1,3-噻唑和 1,2,4-噻二唑生物碱：结构阐明和全合成。

Cytotoxic 1,3-Thiazole and 1,2,4-Thiadiazole Alkaloids from Penicillium oxalicum: Structural Elucidation and Total Synthesis.

机构信息

Hubei Key Laboratory of Natural Products Research and Development, College of Biological and Pharmaceutical Sciences, China Three Gorges University, Yichang 443002, China.

China Three Gorges University People's Hospital & Yichang First People's Hospital, Yichang 443000, China.

出版信息

Molecules. 2016 Feb 26;21(3):232. doi: 10.3390/molecules21030232.

DOI:10.3390/molecules21030232

PMID:26927049

原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC6273271/

Abstract

Two new thiazole and thiadiazole alkaloids, penicilliumthiamine A and B (2 and 3), were isolated from the culture broth of Penicillium oxalicum, a fungus found in Acrida cinerea. Their structures were elucidated mainly by spectroscopic analysis, total synthesis and X-ray crystallographic analysis. Biological evaluations indicated that compound 1, 3a and 3 exhibit potent cytotoxicity against different cancer cell lines through inhibiting the phosphorylation of AKT/PKB (Ser 473), one of important cancer drugs target.

摘要

从中华稻蝗中分离得到的草酸青霉发酵液中分离得到两个新的噻唑和噻二唑生物碱penicilliumthiamine A 和 B（2 和 3）。它们的结构主要通过光谱分析、全合成和 X 射线晶体学分析来阐明。生物评价表明，化合物 1、3a 和 3 通过抑制 AKT/PKB（Ser 473）的磷酸化，一种重要的癌症药物靶点，对不同的癌细胞系表现出强烈的细胞毒性。