甾体糖苷抗肿瘤活性构效关系研究

发布时间：2018-12-13 01:10

【摘要】：为研究甾体糖苷的苷元和糖链结构对其抗肿瘤活性的影响,采用噻唑蓝(MTT)比色法测定了五种结构相关的甾体糖苷薯蓣皂苷、纤细皂苷、边缘茄碱、澳洲茄碱和查茄碱对人宫颈癌细胞(Hela细胞)、人肝癌细胞(H7402细胞)和小鼠成纤维细胞(L929细胞)增殖的影响,随后测定了化学修饰的6-O-双硫酸茄碱、6-O-硫酸查茄碱和全乙酰化查茄碱对人结肠癌细胞(HCT-8细胞)增殖的影响。结果发现,以查茄三糖为糖链的薯蓣皂苷、边缘茄碱和查茄碱抗增殖活性明显高于以其它三糖为糖链的纤细皂苷和澳洲茄碱;甾体糖苷对人源癌细胞的抑制作用更强;6-O-双硫酸茄碱、6-O-硫酸查茄碱和全乙酰化查茄碱无抗增殖活性。构效关系分析表明,苷元"F"环结构对活性有一定影响,糖链的单糖组成和结构对抗肿瘤活性有显著影响;糖链上的羟基在甾体糖苷的抗肿瘤活性中发挥关键作用。
[Abstract]:In order to study the effect of glycoside and carbohydrate structure of steroidal glycoside on its antitumor activity, five steroidal glycoside diosgenin, slender saponins and marginal solanine were determined by thiazolyl blue (MTT) colorimetry. The proliferation of human cervical cancer cells (Hela cells), human liver cancer cells (H7402 cells) and mouse fibroblasts (L929 cells) was affected by Australian and Chaga alkaloids. Effects of 6-O _ 2SO _ 4 on the proliferation of human colon cancer cells (HCT-8). The results showed that the antiproliferative activities of diosgenin, marginal solanine and chamaetin were significantly higher than those of other trisaccharides and Australian solanine, and steroidal glycosides had stronger inhibitory effect on human cancer cells. 6-O-bissulphate, 6-O-sulfate and total acetylated solanine have no anti-proliferative activity. The structure-activity relationship analysis showed that the structure of glycoside "F" ring had a certain influence on the activity, the monosaccharide composition and structure of the sugar chain had a significant effect on the antitumor activity, and the hydroxyl group on the carbohydrate chain played a key role in the antitumor activity of steroidal glycosides.
【作者单位】：辽宁工程技术大学矿业学院;吉林省农业科学院农产品加工研究所/国家乳品加工技术研发分中心;东北师范大学生命科学学院;
【基金】：高等学校博士学科点专项科研基金(20070200004)
【分类号】：R96

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