【摘要】：為研究甾體糖苷的苷元和糖鏈結構對其抗腫瘤活性的影響,采用噻唑藍(MTT)比色法測定了五種結構相關的甾體糖苷薯蕷皂苷、纖細皂苷、邊緣茄堿、澳洲茄堿和查茄堿對人宮頸癌細胞(Hela細胞)、人肝癌細胞(H7402細胞)和小鼠成纖維細胞(L929細胞)增殖的影響,隨后測定了化學修飾的6-O-雙硫酸茄堿、6-O-硫酸查茄堿和全乙酰化查茄堿對人結腸癌細胞(HCT-8細胞)增殖的影響。結果發(fā)現,以查茄三糖為糖鏈的薯蕷皂苷、邊緣茄堿和查茄堿抗增殖活性明顯高于以其它三糖為糖鏈的纖細皂苷和澳洲茄堿;甾體糖苷對人源癌細胞的抑制作用更強;6-O-雙硫酸茄堿、6-O-硫酸查茄堿和全乙酰化查茄堿無抗增殖活性。構效關系分析表明,苷元"F"環(huán)結構對活性有一定影響,糖鏈的單糖組成和結構對抗腫瘤活性有顯著影響;糖鏈上的羥基在甾體糖苷的抗腫瘤活性中發(fā)揮關鍵作用。
[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.
【作者單位】： 遼寧工程技術大學礦業(yè)學院;吉林省農業(yè)科學院農產品加工研究所/國家乳品加工技術研發(fā)分中心;東北師范大學生命科學學院;
【基金】：高等學校博士學科點專項科研基金(20070200004)
【分類號】：R96

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