Department of Pharmaceutical Products, Pharmacy Faculty, Federal University of Minas Gerais, 6627 Antônio Carlos AVE, 31270-901, Belo Horizonte, Minas Gerais, Brazil.
Department of Foods, Pharmacy Faculty, Federal University of Minas Gerais, 6627 Antônio Carlos AVE, 31270-901, Belo Horizonte, Minas Gerais, Brazil.
J Mol Graph Model. 2019 Jan;86:106-112. doi: 10.1016/j.jmgm.2018.10.007. Epub 2018 Oct 12.
The antioxidant potential of a series of thiazolylhydrazone derivatives was investigated using three different methods namely DPPH, ABTS and FRAP assays. In general, the tested compounds showed higher or comparable activity to that of curcumin, used as positive control. Chemometric analyses demonstrated that the presence of hydrazone moiety is required for the activity of this class of compounds. From these results, compound 4 was identified as the most promising molecule and was then selected for further studies. The antiproliferative effect of compound 4 was evaluated, being active in three (T47D, MDA-MB-231 and SKMEL) of the six cancer cell lines tested, with IC values ranging from 15.9 to 31.3 μM. Compound 4 exhibited no detectable cytotoxic effect on peripheral blood mononuclear cells (PBMC) when tested at a concentration of 100 μM, demonstrating good selectivity. From these results, it is possible to infer that there is a correlation between antioxidant capacity and anticancer effects.
采用 DPPH、ABTS 和 FRAP 三种方法研究了一系列噻唑基腙衍生物的抗氧化能力。一般来说，测试的化合物表现出比用作阳性对照的姜黄素更高或相当的活性。化学计量学分析表明，腙部分的存在是此类化合物活性所必需的。从这些结果中，确定化合物 4 是最有前途的分子，然后选择用于进一步研究。评估了化合物 4 的抗增殖作用，在测试的六种癌细胞系中的三种（T47D、MDA-MB-231 和 SKMEL）中表现出活性，IC 值范围为 15.9 至 31.3 μM。当在 100 μM 的浓度下测试时，化合物 4 对外周血单核细胞（PBMC）没有可检测的细胞毒性作用，显示出良好的选择性。从这些结果可以推断，抗氧化能力和抗癌作用之间存在相关性。
