[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].

H. Kuznietsova, O. Lynchak, M. O. Danylov, I. Kotliar, V. K. Rybal'chenko
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引用次数: 19

Abstract

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-3H-pyrrol-3-one (D1) and 1-(4-Cl-benzyl)-3-Cl-4-(CF3-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.
[二氢吡咯和马来酰亚胺衍生物对正常大鼠和二甲肼致结直肠癌大鼠肝脏和结肠状态的影响]。
组织病理学数据和血清转氨酶、碱性磷酸酶、乳酸脱氢酶活性数据均证实,长期给药细胞抑制剂5-氨基-4-(1,3-苯并噻唑-2-基)-1-(3-甲氧基苯基)-1,2-二氢- 3h -吡咯-3-酮(D1)和1-(4- cl -苄基)-3- cl -4-(cf3 -苯胺)- 1h -吡咯-2,5-二酮(MI-1)对大鼠肝脏和结肠无明显影响。体内D1和MI-1可使dmh诱导的大鼠结肠肿瘤总面积减少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)减少DNA氧化修饰引起的毒性作用,这一点可以通过尿8-羟基脱氧鸟苷水平得到证实。这两种化合物的作用是相似的,但MI-1对完整动物的肝脏和结肠的毒性较小,在化学诱导致癌的环境中具有更明显的抗肿瘤活性和保护特性。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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