Synthesis and Antitumor Activity of Biotin Curcumin Derivatives
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维普
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为进一步开发安全有效的抗口腔癌药物,利用酰基化法及羧氨缩合法制备一系列姜黄素类衍生物,采用药物拼合原理,使姜黄素连接具有一定抗肿瘤活性及靶向性的生物素,合成一系列姜黄素-生物素偶联物(目标化合物2、4、5),其结构经1 H NMR、13 C NMR和HR-MS(ESI)确证.采用四甲基偶氮唑蓝(MTT)法检测目标化合物对人口腔表皮样癌细胞(KB细胞)增殖的抑制作用.结果显示:化合物2 在作用24h及48h时对KB细胞的IC50分别是40.82 μmol/L和26.23 μmol/L,提示其抗肿瘤活性优于姜黄素.化合物4 在作用24h及48h时对KB细胞的IC50分别是39.83 μmol/L和51.24 μmol/L,提示在作用24h时,其抗肿瘤活性优于原药姜黄素.
In order to further develop safe and effective anti-oral cancer drugs,firstly,a series of cur-cumin derivatives were prepared using acylation and carboxamide condensation methods,and the prin-ciple of drug combination was used to connect curcumin to biotins with certain anti-tumor activity and targeting properties,thus synthesizing a series of curcumin-biotin conjugates(target compounds 2,4,and 5).Its structure was confirmed by 1 H NMR,13 C NMR,and HR-MS(ESI).Secondly,methyl th-iazolyl tetrazolium(MTT)method was used to detect inhibitory effect of the target compound on the proliferation of human oral epidermoid carcinoma cells(KB cells).The results showed that the IC50 of compound 2 on KB cells at 24 h and 48 h were 40.82 μmol/L and 26.23 μmol/L,respectively,indi-cating that its antitumor activity is superior to curcumin;the IC50 of compound 4 on KB cells at 24 h and 48 h were 39.83 μmol/L and 51.24 μmol/L,respectively,indicating that its antineoplastic activ-ity is superior to the original drug curcumin after 24 hours.
curcuminbiotinprinciple of drug combinationconjugatemethyl thiazolyl tetrazoliumantineoplastic activity
维普
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