【摘要】：為研究甾體糖苷的苷元和糖鏈結(jié)構(gòu)對(duì)其抗腫瘤活性的影響,采用噻唑藍(lán)(MTT)比色法測(cè)定了五種結(jié)構(gòu)相關(guān)的甾體糖苷薯蕷皂苷、纖細(xì)皂苷、邊緣茄堿、澳洲茄堿和查茄堿對(duì)人宮頸癌細(xì)胞(Hela細(xì)胞)、人肝癌細(xì)胞(H7402細(xì)胞)和小鼠成纖維細(xì)胞(L929細(xì)胞)增殖的影響,隨后測(cè)定了化學(xué)修飾的6-O-雙硫酸茄堿、6-O-硫酸查茄堿和全乙�；榍褖A對(duì)人結(jié)腸癌細(xì)胞(HCT-8細(xì)胞)增殖的影響。結(jié)果發(fā)現(xiàn),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(xì)皂苷和澳洲茄堿;甾體糖苷對(duì)人源癌細(xì)胞的抑制作用更強(qiáng);6-O-雙硫酸茄堿、6-O-硫酸查茄堿和全乙�；榍褖A無抗增殖活性。構(gòu)效關(guān)系分析表明,苷元"F"環(huán)結(jié)構(gòu)對(duì)活性有一定影響,糖鏈的單糖組成和結(jié)構(gòu)對(duì)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(guān)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(shù)大學(xué)礦業(yè)學(xué)院;吉林省農(nóng)業(yè)科學(xué)院農(nóng)產(chǎn)品加工研究所/國(guó)家乳品加工技術(shù)研發(fā)分中心;東北師范大學(xué)生命科學(xué)學(xué)院;
【基金】：高等學(xué)校博士學(xué)科點(diǎn)專項(xiàng)科研基金(20070200004)
【分類號(hào)】：R96

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