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首页> 外文期刊>Ukrainian Biochemical Journal >Effect of dihydropyrrol and maleimide derivatives on the state of the liver and colon in normal rats and those with colorectal carcinogenesis induced by dimethylhydrazine
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Effect of dihydropyrrol and maleimide derivatives on the state of the liver and colon in normal rats and those with colorectal carcinogenesis induced by dimethylhydrazine

机译:二氢吡咯和马来酰亚胺衍生物对正常大鼠及二甲基肼诱发结直肠癌的大鼠肝脏和结肠状态的影响

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No liver and colon alterations in rats, caused by cytostatic compounds 5-amino-4-(1,3-benzothyazol-2-yl)-1-(3-methoxyphenyl)-1,2-dihydro-3Н-pyrrol-3-one (D1) and 1-(4-Cl-benzyl)-3-Cl-4-(CFsub3/sub-phenylamino)-1H-pyrrol-2,5-dione (MI-1) when administered over a long time were found, as evidenced by the histopathological data and the data of activity of transaminases, alkaline phosphatase and lactate dehydrogenase in the blood serum. D1 and MI-1 in vivo decrease the total area of DMH-induced colon tumors in rats by 46-60%. Furthermore, D1 and MI-1 partially protect the liver and colon mucosa from toxic effects caused by 1,2-dimethylhydrazine (DMH) reducing DNA oxidative modifications, as evidenced by urine 8-hydroxydeoxyguanosine level. The effects of both compounds are similar, but MI-1 is less toxic for the liver and colon of intact animals possessing more pronounced antitumor activity and protective properties in the setting of chemically induced carcinogenesis.
机译:抑制细胞生长的化合物5-氨基-4-(1,3-苯并噻唑-2-基)-1-(3-甲氧基苯基)-1,2-二氢-3Н-吡咯-3-引起的大鼠肝和结肠无变化(D1)和1-(4-Cl-苄基)-3-Cl-4-(CF 3 -苯氨基)-1H-吡咯-2,5-二酮(MI-1)时从组织病理学数据以及血清中转氨酶,碱性磷酸酶和乳酸脱氢酶的活性数据可以证明,长期服用这种药物非常有效。体内D1和MI-1使DMH诱导的大鼠结肠肿瘤的总面积减少46-60%。此外,D1和MI-1部分保护肝脏和结肠黏膜免受1,2-二甲基肼(DMH)引起的降低DNA氧化修饰的毒性作用,尿液中的8-羟基脱氧鸟苷水平证明了这一点。两种化合物的作用相似,但MI-1对完整动物的肝脏和结肠毒性较小,在化学诱导的癌变过程中具有更明显的抗肿瘤活性和保护特性。

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