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高良姜中黄酮衍生物的合成及抗K562增殖活性研究 被引量:1

Study on synthesis of flavone derivatives in rhizoma and anti-proliferative activity of K562 cells
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摘要 在对高良姜素(AO-1)结构修饰研究的基础上,对高良姜主要成分山柰素-4'-甲醚(AO-2)和高良姜素-3-甲醚(AO-3)进行结构修饰,期望得到抑制K562细胞增殖活性更好的高良姜衍生物,并总结构效关系。以AO-2和AO-3为母核进行结构修饰得到了9个衍生物,其中有8个为新化合物。采用MTT法测定了山柰素-4'-甲醚、高良姜素-3-甲醚及其衍生物在不同浓度下对K562细胞的抑制率。化合物B-1、B-3、B-4、B-5、B-6活性良好,其中B-1、B-3、B-4在浓度为100μM时对K562细胞的抑制率均在50%左右;B-6活性是最好的,当浓度在30μM,100μM时的抑制率可以分别达到56.9%,72.5%,其对K562细胞的抑制率很高,活性最佳,其IC50为36.2μmol/L。通过本研究发现在山奈素-4'甲醚3位羟基引入肉桂酸衍生物,当肉桂酸的苯环对位上为苄基时,活性最强。说明肉桂酸的4位取代基对活性有较大影响,而肉桂酸的3位取代基对活性影响不大。将适当修饰的肉桂酸衍生物引入山柰素-4'-甲醚的3位羟基可以提高它的抗K562细胞增殖活性,这为接下来SAR(构效关系)的研究和发现活性更好的抑制K562增殖的抗肿瘤药物奠定了基础。 In this paper,based on the study of the structural modification of galangin(AO-1),structure modification of kaempferol-4'-methyl ether(AO-2)and galangin-3-methyl ether(AO-3)from Alpinia officinarum was carried out,it is expected to find better anti-proliferation of K562cells derivatives and summary of structure-activity relationship.9derivatives were obtained from AO-2and AO-3,8of which were new compounds.The compounds’inhibition rates of K562cells were determined by MTT assay.B-1,B-3,B-4,B-5and B-6showed good activities.The inhibitory rates of B-1,B-3and B-4at100μM on K562cells were approximately50%;B-6showed the strongest activities,and when the concentration was30μM,100μM,its inhibition rate could reach56.9%and72.5%,respectively.The inhibition rate of K562cells was high and the activity was the best.Its IC50was36.2μmol/L.From the study,it was found that the Benzyl group on the para-position of the cinnamic acid at the3-position of kaempferol-4'-methyl ether had the strongest activity.It indicated that the para-position substituents of cinnamic acid had great influence on the activities,while the3-position of cinnamic acid had little influence.Kaempferol-4'-methyl ether at the3-position introduce suitably modified cinnamic acid derivatives could greatly enhance the anti-K562cell proliferation activities,which settled firmly foundation for further studyonSAR(structure-activity relationship)and discovery of antitumor drugs.
作者 薛稳来 赵耀鑫 费强 赵玲 XUE Wenlai;ZHAO Yaoxin;FEI Qiang;ZHAO Ling(School of Biology and Pharmaceutical Engineering,Wuhan Polytechnic University,Wuhan 430023,China)
出处 《武汉轻工大学学报》 2017年第4期5-11,23,共8页 Journal of Wuhan Polytechnic University
基金 武汉轻工大学校立项目(2016y32)
关键词 高良姜 山柰素-4′-甲醚 结构修饰 K562细胞 alpinia officinarum kaempferol-4'-methyl ether structural modification k562 cells
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