机构地区:[1]Institute of Pharmacy & Pharmacology, University of South China, Hengyang 421001, P. R. China, [2]Suzhou Academy of Wumen Chinese Medicine, Suzhou Hospital of Traditional Chinese Medieine, Suzhou 215003, P. R. China [3]Soochow University Affiliated Children's Hospital, Suzhou 215003, P. R. China [4]Institute of Chemistry & Chemical Engineering, University of South China, Hengyang 421001, P. R. China
出 处:《Chemical Research in Chinese Universities》2014年第6期925-930,共6页高等学校化学研究(英文版)
摘 要:Two series of 7-O-modified chrysin derivatives were prepared from 7-O-carboxymethy! chrysin(2a), 7-O-carboxypropylchrysin(2b) and short-chain alcohols by using 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide hydrochloride(EDCI), N-hydroxybenzotriazole(HOBt) and 4-dimethylamiopryidine(DMAP) as coupling reagents. Taking cisplatin as a reference substance, their anti-proliferative activities in vitro against human gastric carcinoma MGC-803 cells were evaluated by the standard 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-2H-tetrazolium bromide (MTT) method. The results show that among the compounds tested, hepty 4-(5-hydroxy-4-oxo-2-phenyl-4H- chromen-7-yloxy) acetate(3f) displayed the most potent growth-inhibitory effect on MGC-803 cells with half maximal inhibitory concentration(ICso) value of 3.23 pmol/L. The preliminary mechanism of inhibitory effect of compound 3f was also detected by flow cytometry(FCM), and the compound exerted anti- cancer activity via inducing the apoptosis of MGC-803 cells in a dose dependent manner, which suggested that compound 3f would be a potential anti-cancer agent.Two series of 7-O-modified chrysin derivatives were prepared from 7-O-carboxymethy! chrysin(2a), 7-O-carboxypropylchrysin(2b) and short-chain alcohols by using 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide hydrochloride(EDCI), N-hydroxybenzotriazole(HOBt) and 4-dimethylamiopryidine(DMAP) as coupling reagents. Taking cisplatin as a reference substance, their anti-proliferative activities in vitro against human gastric carcinoma MGC-803 cells were evaluated by the standard 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-2H-tetrazolium bromide (MTT) method. The results show that among the compounds tested, hepty 4-(5-hydroxy-4-oxo-2-phenyl-4H- chromen-7-yloxy) acetate(3f) displayed the most potent growth-inhibitory effect on MGC-803 cells with half maximal inhibitory concentration(ICso) value of 3.23 pmol/L. The preliminary mechanism of inhibitory effect of compound 3f was also detected by flow cytometry(FCM), and the compound exerted anti- cancer activity via inducing the apoptosis of MGC-803 cells in a dose dependent manner, which suggested that compound 3f would be a potential anti-cancer agent.
关 键 词:7-O-Modified chrysin Anti-proliferative effect Apoptotic effect Flavanoid
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