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中国精品科技期刊2020
赵雪淞, 李盛钰, 杨旭, 周义发. 甾体糖苷抗肿瘤活性构效关系研究[J]. 华体会体育, 2016, (11): 345-349. DOI: 10.13386/j.issn1002-0306.2016.11.063
引用本文: 赵雪淞, 李盛钰, 杨旭, 周义发. 甾体糖苷抗肿瘤活性构效关系研究[J]. 华体会体育, 2016, (11): 345-349. DOI: 10.13386/j.issn1002-0306.2016.11.063
ZHAO Xue-song, LI Sheng-yu, YANG Xu, ZHOU Yi-fa. Structure- antineoplastic activity relationships of steroid glycosides[J]. Science and Technology of Food Industry, 2016, (11): 345-349. DOI: 10.13386/j.issn1002-0306.2016.11.063
Citation: ZHAO Xue-song, LI Sheng-yu, YANG Xu, ZHOU Yi-fa. Structure- antineoplastic activity relationships of steroid glycosides[J]. Science and Technology of Food Industry, 2016, (11): 345-349. DOI: 10.13386/j.issn1002-0306.2016.11.063

甾体糖苷抗肿瘤活性构效关系研究

Structure- antineoplastic activity relationships of steroid glycosides

  • 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 assess the roles of the carbohydrate side chain and aglycon part of steroid glycosides in influencing antineoplastic activities of these compounds,the antiproliferative activities against human cervical carcinoma( Hela),liver cancer( H7402) and mouse fibroblast( L929) cells of a series of structurally related individual compounds including dioscin,gracillin,solamargine,solasonine and chaconine,were examined using a microculture tetrazolium( MTT) assay. And then,the antiproliferative activities against human colonic cancer( HCT-8) cells of a series of chemically modified steroid glycosides including 6-O-sulfated chaconine,6,6'-di-O-sulfated solanine and per-O-acetyled chaconine were examined using a MTT assay.The results showed that the antiproliferative activity of the chacotriose-containing steroid glycosides dioscin,chaconine and solamargine was higher significantly than other trisaccharide-containing steroid glycosides solasonine and gracillin. The effectiveness against the human carcinoma cells was greater than against the mouse fibroblast cells.6-O-sulfated chaconine,6,6'-di-O-sulfated solanine and per-O-acetyled chaconine shown no antiproliferative activity against human HCT-8 cells. Structure-activity relationship studies indicated that the F ring structure of the aglycon unit influence biological activity; the composition,nature and the order of attachment of the sugars in the oligosaccharide associated with the steroid glycosides,were important in the antineoplastic properties; the-OH group of the sugar molecules seem to be an vital factor related to antineoplastic activity.

     

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