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姜黄素葡糖醛酸苷:评估对人类细胞系的增殖活性

Curcumin glucuronides: assessing the proliferative activity against human cell lines.

作者信息

Pal Ashutosh, Sung Bokyung, Bhanu Prasad Basvoju A, Schuber Paul T, Prasad Sahdeo, Aggarwal Bharat B, Bornmann William G

机构信息

Department of Experimental Therapeutics, The University of Texas M.D. Anderson Cancer Center, Houston, TX 77030, USA.

Department of Experimental Therapeutics, The University of Texas M.D. Anderson Cancer Center, Houston, TX 77030, USA.

出版信息

Bioorg Med Chem. 2014 Jan 1;22(1):435-9. doi: 10.1016/j.bmc.2013.11.006. Epub 2013 Nov 12.

Abstract

A gram scale synthesis of the glucuronide metabolites of curcumin were completed in four steps. The newly synthesized curcumin glucuronide compounds 2 and 3 along with curcumin 1 were tested and their anti-proliferative effects against KBM-5, Jurkat cell, U266, and A549 cell lines were reported. Biological data revealed that as much as 1 μM curcumin 1 exhibited anticancer activity and almost 100% cell kill was noted at 10 μM on two out of four cell lines; while curcumin mono-glucuronide 2 as well as di-glucuronide 3 displayed no suppression of cell proliferation.

摘要

姜黄素葡糖醛酸代谢物的克级合成通过四个步骤完成。对新合成的姜黄素葡糖醛酸化合物2和3以及姜黄素1进行了测试,并报道了它们对KBM - 5、Jurkat细胞、U266和A549细胞系的抗增殖作用。生物学数据显示,高达1 μM的姜黄素1表现出抗癌活性,在10 μM时,四种细胞系中的两种出现了几乎100%的细胞死亡;而姜黄素单葡糖醛酸2以及双葡糖醛酸3均未显示出对细胞增殖的抑制作用。

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