胍腙衍生物抗增殖活性的初步体外评估

Preliminary in vitro evaluation of the anti-proliferative activity of guanylhydrazone derivatives.

作者信息

França Paulo H B, Da Silva-Júnior Edeildo F, Aquino Pedro G V, Santana Antônio E G, Ferro Jamylle N S, De Oliveira Barreto Emiliano, Do Ó Pessoa Cláudia, Meira Assuero Silva, De Aquino Thiago M, Alexandre-Moreira Magna S, Schmitt Martine, De Araújo-Júnior João X

出版信息

Acta Pharm. 2016 Mar;66(1):129-37. doi: 10.1515/acph-2016-0015.

DOI:10.1515/acph-2016-0015

PMID:26959549

Abstract

Guanylhydrazones have shown promising antitumor activity in preclinical tumor models in several studies. In this study, we aimed at evaluating the cytotoxic effect of a series of synthetic guanylhydrazones. Different human tumor cell lines, by including HCT-8 (colon carcinoma), MDA-MB-435 (melanoma) and SF-295 (glioblastoma) were continuous exposed to guanylhydrazone derivatives for 72 hours and growth inhibition of tumor cell lines and macrophages J774 was measured using tetrazolium salt (MTT) assay. Compounds 7, 11, 16 and 17 showed strong cytotoxic activity with IC50 values lower than 10 μmol L(-1) against four tumor cell lines. Among them, 7 was less toxic to non-tumor cells. Finally, obtained data suggest that guanylhydrazones may be regarded as potential lead compounds for the design of novel anticancer agents.

摘要

在多项研究的临床前肿瘤模型中，胍基腙已显示出有前景的抗肿瘤活性。在本研究中，我们旨在评估一系列合成胍基腙的细胞毒性作用。将包括HCT-8（结肠癌）、MDA-MB-435（黑色素瘤）和SF-295（胶质母细胞瘤）在内的不同人类肿瘤细胞系连续暴露于胍基腙衍生物72小时，并使用四唑盐（MTT）法测定肿瘤细胞系和巨噬细胞J774的生长抑制情况。化合物7、11、16和17表现出较强的细胞毒性活性，对四种肿瘤细胞系的IC50值低于10 μmol L(-1)。其中，7对非肿瘤细胞的毒性较小。最后，所得数据表明胍基腙可被视为设计新型抗癌药物的潜在先导化合物。