| 4-(4-羟基-3-甲氧基苯甲基)姜黄素合成及其抗肿瘤活性 |
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| 引用本文： | 刘洋,陈纯,李娜,许建华.4-(4-羟基-3-甲氧基苯甲基)姜黄素合成及其抗肿瘤活性[J].中国医院药学杂志,2011(14). |
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| 作者姓名： | 刘洋 陈纯 李娜 许建华 |
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| 作者单位： | 福建医科大学药学院药物化学系;福建医科大学药学院药理学系;福建医科大学附属协和医院药剂科; |
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| 基金项目： | 国家自然科学基金(编号:30873101); 福建省科技重点项目(编号:2009Y0025); 福建省教育厅项目(编号:JA10150) |
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| 摘 要： | 目的:合成4-(4-羟基-3-甲氧基苯甲基)姜黄素(C086),并对其体内外抗肿瘤活性进行评价。方法:以芳香醛、乙酰丙酮为原料,Knovenagel缩合、氢化还原、Claisen-Schmidt缩合三步反应制备目标化合物。以姜黄素为对照,MTT法考察目标化合物对人慢性粒细胞白血病急变细胞株K562、人急性髓系白血病细胞株HL-60、人肝肿瘤细胞株HepG2、小鼠黑色素瘤细胞株B-16、人结肠癌细胞株SW480、人神经母细胞瘤细胞株SH-SY5Y、人胰腺癌细胞株Bxpc-3、人胃癌细胞株MGC80-3的抑制活性。考察目标化合物体内抑制人结肠癌SW480裸鼠移植性肿瘤活性。结果:目标化合物结构经核磁和质谱确证,对上述细胞株的IC50值依次为2.90,4.11,4.11,3.55,4.78,7.92,18.8,17.1μmol.L-1,均明显比姜黄素强,100mg.kg-1.d-1灌胃给药对人结肠癌SW480裸鼠移植性肿瘤的抑瘤率为40.7%,小鼠的体质量无明显减轻。结论:合成了4-(4-羟基-3-甲氧基苯甲基)姜黄素,体外对多种肿瘤细胞抑制活性明显强于Cur,体内能明显抑制结肠癌移植瘤的生长。
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| 关 键 词： | 姜黄素 姜黄素类似物 抗肿瘤活性 |
Study on the synthesis and antitumor activity of 4-(4-hydroxy-3-methoxybenzyl)curcumin |
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| LIU Yang,CHEN Chun,LI Na,XU Jian-hua.Study on the synthesis and antitumor activity of 4-(4-hydroxy-3-methoxybenzyl)curcumin[J].Chinese Journal of Hospital Pharmacy,2011(14). |
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| Authors: | LIU Yang CHEN Chun LI Na XU Jian-hua |
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| Institution: | LIU Yang1,CHEN Chun2,LI Na3,XU Jian-hua2(1.Department of medical chemistry,School of Pharmacy,Fujian Medical University,Fujian Fuzhou 350004,China,2.Department of Pharmacology,3.Department of Pharmacy,The Affiliated union Hospital,Fujian Fuzhou 350001,China) |
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| Abstract: | OBJECTIVE To synthesize 4-(4-hydroxy-3-methoxybenzyl)curcumin(C086) and to test its antitumor activity.METHODS 4-(4-hydroxy-3-methoxybenzyl)curcumin was synthesized from vanillin and acetylacetone by Knovenagel condensation,hydrogenation and Claisen-Schmidt condensation.The antiproliferative activities in vitro were tested with eight cancer cell lines including K562,HL-60,HepG2,B16,SW480,SH-SY5Y,Bxpc-3 and MGC80-3 by MTT assay.Curcumin was used for comparative purpose.C086 was tested for in vivo inhibition ... |
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| Keywords: | curcumin curcumin analogs antitumor activity |
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