| 大黄素三甲氧基衍生物合成及体外抗肿瘤活性试验 |
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| 引用本文： | 金丹婷,钟梁,刘北忠,袁佩,刘畅,王翀,王春光,朱丹,吴燕. 大黄素三甲氧基衍生物合成及体外抗肿瘤活性试验[J]. 中国医院药学杂志, 2010, 0(5) |
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| 作者姓名： | 金丹婷 钟梁 刘北忠 袁佩 刘畅 王翀 王春光 朱丹 吴燕 |
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| 作者单位： | 重庆医科大学医学检验系临床检验诊断学教育部重点实验室;重庆医科大学医药研究所; |
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| 基金项目： | 国家自然科学基金(No.30300449); 国家中医药管理局(No.02-03ZP52); 重庆医科大学校级课题(No.XBYB2007104,XBYB2007108) |
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| 摘 要： | 目的:以天然存在的大黄素为原料合成了甲基化衍生物三甲氧基大黄素,并进行体外抗肿瘤活性的研究。方法:利用硫酸二甲酯/丙酮甲基化组合合成目标化合物1,3,8-三甲氧基-6-甲基蒽醌;通过常规方法,对其理化性质进行鉴定。采用HPLC及ESI-MS对其结构进行表征;通过MTT比色法与流式细胞术检测其对K562细胞增殖及细胞周期分布的影响。结果:三甲氧基大黄素为淡黄色粉末,mp:226～227℃,溶于氯仿等有机溶剂。其结构经HPLC及ESI-MS检测得到确证;浓度依赖性地抑制K562细胞的增殖,并使G0/G1期的细胞比例增加。结论:以大黄素为原料,成功合成了其新的衍生物。三甲氧基大黄素具有抑制K562细胞增殖及阻滞细胞周期由G0/G1期向S期移行的抗肿瘤活性。
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| 关 键 词： | 大黄素 大黄素衍生物 合成 抗肿瘤活性 |
Synthesis of trimethoxy derivatives of emdoin and its anti-tumor activities test in vitro |
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| JIN Dan-ting,ZHONG Liang,LIU Bei-zhong,YUAN Pei,LIU Chang,WANG Chong,WANG Chun-guang,ZHU Dan,WU Yan. Synthesis of trimethoxy derivatives of emdoin and its anti-tumor activities test in vitro[J]. Chinese Journal of Hospital Pharmacy, 2010, 0(5) |
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| Authors: | JIN Dan-ting ZHONG Liang LIU Bei-zhong YUAN Pei LIU Chang WANG Chong WANG Chun-guang ZHU Dan WU Yan |
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| Affiliation: | JIN Dan-ting1,ZHONG Liang1,LIU Bei-zhong1,YUAN Pei2,LIU Chang1,WANG Chong1,WANG Chun-guang1,ZHU Dan1,WU Yan1(1. Key Laboratory of Laboratory Medical Diagnostics of Ministry of Education,Faculty of Laboratory Medicine in Chongqing Medical University,Chongqing 400016,China,2. The Institute of Medicine in Chongqing Medical University,China) |
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| Abstract: | OBJECTIVE To synthesize emodin derivatives and evaluate its anti-tumor activities in vitro.METHODS A new emodin trimethoxy derivatives were synthesized from emodin with (Me)2SO4. The physicochemical property of the new derivatives was identified with routine methods. And its structure was characterized by HPLC and ESI-MS spectra. The effect of the new derivatives on K562 cell proliferation was detected by MTT, as well as the cell cycle by flow cytometry.RESULTS Emodin derivatives were slight yellow powder w... |
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| Keywords: | emodin emodin derivatives synthesis anti-tumor activitve |
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