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首页> 外文期刊>Acta Pharmacologica Sinica >Anticarcinogenic and antioxidant activity of diindolylmethane derivatives
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Anticarcinogenic and antioxidant activity of diindolylmethane derivatives

机译：二吲哚基甲烷衍生物的抗癌和抗氧化活性

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摘要

AIM: To investigate the synthesis methods and the bioactivity of diindolylmethane (DIM) derivatives. METHODS: 1) A 30-Quantitative Structure-Active Relationships (QSAR) Comparative Molecular Field Analysis (CoMFA) study of 14 DIM derivatives was investigated to predict their anticarcinogenic activity. 2) Based on CoMFA model, a series of new derivatives of DIM were designed and synthesized. 3) Their free radical scavenging and antioxidant potentials were tested using in-vitro DPPH radical scavenging and β-carotene antioxidant models. 4) The anticarcinogenic activities of some compounds were tested by using microculture tetrazolium assay (MTT) and sulforhodamine B (SRB) proteochromosomic assays. RESULTS: 1) The CoMFA model derived from DIM analogues proved a good predictive ability with q~2 value of 0.827. 2) New designed compounds 3c and 4c exhibited 3-fold more potent radical scavenging activity than reference substance Vitamin E in DPPH model expressed by IC_(50) values. 3) The primary antitumor screening essay showed that some DIM derivatives designed exhibited the inhibitory activities to some tumor cell growth at relatively high concentration, and DIM was the most effective among them. CONCLUSION: DIM's 3D-QSAR model is reliable. According to it, eleven DIM derivatives were synthesized, and two derivatives of them possess potent radical scavenging activities and some showed the inhibitory activities in primary anticancer assay in vitro.
机译：目的：研究二吲哚基甲烷（DIM）衍生物的合成方法和生物活性。方法：1）研究了14种DIM衍生物的30定量构效关系（QSAR）比较分子场分析（CoMFA）研究，以预测其抗癌活性。 2）基于CoMFA模型，设计并合成了一系列新的DIM衍生物。 3）使用体外DPPH自由基清除和β-胡萝卜素抗氧化剂模型测试它们的自由基清除和抗氧化能力。 4）通过使用微培养四唑鎓测定（MTT）和磺基若丹明B（SRB）蛋白染色体测定来测试某些化合物的抗癌活性。结果：1）DIM类似物衍生的CoMFA模型具有良好的预测能力，q〜2值为0.827。 2）新设计的化合物3c和4c在清除自由基方面的活性比参考物质维生素E高3倍，用IC_（50）值表示。 3）初步的抗肿瘤筛选研究表明，设计的一些DIM衍生物在较高浓度下对某些肿瘤细胞的生长具有抑制活性，其中DIM最有效。结论：DIM的3D-QSAR模型是可靠的。据此，合成了11种DIM衍生物，其中2种衍生物具有有效的自由基清除活性，有些在体外原发性抗癌试验中显示出抑制活性。

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