某些苯并咪唑衍生物对特定肿瘤细胞系的抗氧化活性

I. Goshev, A. Mavrova, B. Mihaylova, D. Wesselinova
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引用次数: 3

摘要

一组双(苯并咪唑-2-酰基)胺已经在体外对人类结直肠癌细胞系HT-29、乳腺癌细胞MDA-MB-231和正常脾细胞进行了细胞毒性评估,其中两种(B1和B2)已被用于我们目前的研究。从第二组1,3-二取代-2,3-二氢-2-亚胺苯并咪唑化合物中选择了两种物质(B3和B4),因为它们对人结直肠癌细胞系HT-29、乳腺癌细胞MDA-MB-231和正常脾细胞具有最明显的抗增殖作用,使用体外增殖mts试验。重要的是要估计这种抑制活性的化合物的原因。我们认为这可能是由于它们的抗氧化能力。采用HORAC和ORAC方法检测了这些物质对羟基和过氧基自由基的抗氧化活性,结果显示出相当大的抗氧化能力。B2对羟基自由基的清除能力最强,其次是B1。据估计,B2对氧自由基的清除能力最大,被测细胞释放的氧自由基由大到小依次为B1、B3和B4。观察到的差异可以认为是它们的结构对Me2- heling活性和有效h原子给予的影响。观察到特定物质的结构与表达的抗氧化电位之间存在相关性。后者也与对肿瘤细胞系的影响相关。这一结果意味着肿瘤细胞伴随着可测量的ROS排放,这可能通过适当应用抗氧化剂来调节。
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Antioxidant activity of some benzimidazole derivatives to definite tumor cell lines
A group of bis(benzimidazol-2-yl) amines have been already evaluated for cytotoxicity in vitro to human colorectal cancer cell line HT-29, breast cancer cells MDA-MB-231 and normal spleen cells and two of them (B1 and B2) have been taken for the purposes of our present investigations. From the second group of compounds representing 1,3-disubstituted-2,3-dihydro-2-iminobenzimidazoles two substances (B3 and B4) have been chosen because of their most pronounced anti-proliferative effect to human colorectal cancer cell line HT-29, breast cancer cells MDA-MB-231 and normal spleen cells, using the in vitro proliferative MTS-test. It was important to estimate the cause for this suppressive activity of the compounds. We proposed that this could be due to their antioxidant capacity. The substances were examined for antioxidant activity against hydroxyl and peroxyl radicals, applying the HORAC and ORAC methods and showed considerable capacity. The scavenging capacity of B2 towards hydroxyl radicals is the highest, followed by B1. It was estimated that B2 has the greatest scavenger capacity of oxygen radicals, emitted by the examined cells followed in descending order by B1, B3 and B4. The observed differences can be considered as impact of their structure on the Me2-helating activity and effective H-atom donation. A correlation was observed between the structure of the particular substance and the expressed antioxidant potential. The latter correlated also with the effect on the tested tumor cell lines. This result means that tumor cells are accompanied by a measurable emission of ROS which might be regulated by a proper application of antioxidants.
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