游离B环黄酮类化合物作为结肠癌治疗的潜在先导化合物。
Free-B-Ring flavonoids as potential lead compounds for colon cancer therapy.
作者信息
Ibrahim Ahmed, Sobeh Mohamed, Ismail Aya, Alaa Ahmed, Sheashaa Hussein, Sobh Mohamed, Badria Farid
机构信息
Department of Biochemistry, Faculty of Pharmacy, Mansoura University, Mansoura 35516, Egypt.
Medical Experimental Research Center, Faculty of Medicine, Mansoura University, Mansoura 35516, Egypt.
出版信息
Mol Clin Oncol. 2014 Jul;2(4):581-585. doi: 10.3892/mco.2014.278. Epub 2014 Apr 16.
Although flavonoids have been identified as a versatile source of anticancer agents, to the best of our knowledge, no study has yet investigated their anticolon cancer activity in depth. Therefore, the aim of this study was to investigate the association between the structural characteristics of flavonoids and their anticolon cancer activity in the Caco-2 human colon cancer cell line. Our findings demonstrated that the hydroxylation of C5 and C7 in ring A significantly enhanced the anticolon cancer activity of flavonoids over that of 5-fluorouracil, the classic reference cytotoxic agent. By contrast, the glycosylation or the presence of hydroxyl groups in ring B significantly decreased flavonoid anticancer activity. Collectively, these findings suggest a novel, rational design of flavonoid-related compounds that may improve the treatment of colorectal cancer.
尽管黄酮类化合物已被确认为抗癌剂的多种来源，但据我们所知，尚未有研究对其抗结肠癌活性进行深入调查。因此，本研究的目的是在Caco-2人结肠癌细胞系中研究黄酮类化合物的结构特征与其抗结肠癌活性之间的关联。我们的研究结果表明，A环中C5和C7的羟基化显著增强了黄酮类化合物的抗结肠癌活性，超过了经典参考细胞毒性剂5-氟尿嘧啶。相比之下，B环中的糖基化或羟基的存在显著降低了黄酮类化合物的抗癌活性。总体而言，这些发现提示了一种可能改善结直肠癌治疗的黄酮类相关化合物的新型合理设计。
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