Pinto Michelle F S, Silva Osmar N, Viana Juliane C, Porto William F, Migliolo Ludovico, B da Cunha Nicolau, Gomes Nelson, Fensterseifer Isabel C M, Colgrave Michelle L, Craik David J, Dias Simoni C, Franco Octavio L
Centro de Análises Proteômicas e Bioquímicas, Programa de Pós-Graduação em Ciências Genômicas e Biotecnologia, Universidade Católica de Brasília , Brasília-DF, Brazil.
Faculdade Anhanguera de Ciências e Tecnologia de Brasília , Brasília-DF, Brazil.
J Nat Prod. 2016 Nov 23;79(11):2767-2773. doi: 10.1021/acs.jnatprod.6b00270. Epub 2016 Nov 3.
The extraction and purification of parigidin-br3, a cyclotide analogue belonging to the "bracelet" subfamily, from Palicourea rigida leaves is discussed. Unlike conventional cyclotides, parigidin-br3 has free N- and C-termini, as identified by MALDI-TOF/TOF analysis and confirmed by gene structure elucidation, and is one of a small number of acyclotides discovered during recent years. Parigidin-br3 showed cytotoxic activity against MCF-7 (breast cancer) and CACO2 (colorectal adenocarcinoma) cells, with IC values of ∼2.5 μM and less than 10% hemolytic activity. Overall, parigidin-br3 is a promising new molecule with cytotoxic properties against tumor cell lines and, unlike many synthetic acyclic analogues, demonstrates that cytotoxic activity is not limited to conventional (i.e., cyclic) cyclotides.
本文讨论了从硬叶帕利草叶中提取和纯化帕里吉丁-br3的方法，帕里吉丁-br3是一种属于“手镯”亚家族的环肽类似物。与传统环肽不同，经基质辅助激光解吸电离飞行时间串联质谱（MALDI-TOF/TOF）分析鉴定并通过基因结构解析确认，帕里吉丁-br3具有游离的N端和C端，是近年来发现的少数无环肽之一。帕里吉丁-br3对MCF-7（乳腺癌）和CACO2（结肠直肠腺癌）细胞显示出细胞毒性活性，IC值约为2.5 μM，溶血活性小于10%。总体而言，帕里吉丁-br3是一种有前景的新分子，对肿瘤细胞系具有细胞毒性特性，并且与许多合成无环类似物不同，表明细胞毒性活性不限于传统（即环状）环肽。
