多羟基姜黄素类化合物的合成与生物学评价

Synthesis and biological evaluation of polyhydroxycurcuminoids.

作者信息

Venkateswarlu Somepalli, Ramachandra Marellapudi S, Subbaraju Gottumukkala V

机构信息

Laila Impex Research Centre, Unit 1, Phase III, Jawahar Autonagar, Vijayawada, India.

出版信息

Bioorg Med Chem. 2005 Dec 1;13(23):6374-80. doi: 10.1016/j.bmc.2005.06.050. Epub 2005 Aug 19.

DOI:10.1016/j.bmc.2005.06.050

PMID:16112582

Abstract

A series of curcumin analogs (1-3, 5a-5t) was synthesized through the condensation of appropriately protected hydroxybenzaldehydes with acetylacetone, followed by deprotection. The antioxidant activity of these analogs was determined by superoxide free radical nitroblue tetrazolium and DPPH free radical scavenging methods and the polyhydroxycurcuminoids (5l-5s) displayed excellent antioxidant activity. These analogs showed cytotoxicity to lymphocytes and promising tumor-reducing activity on Dalton's lymphoma ascites tumor cells.

摘要

通过适当保护的羟基苯甲醛与乙酰丙酮缩合，然后脱保护，合成了一系列姜黄素类似物（1-3、5a-5t）。通过超氧阴离子自由基氮蓝四唑法和DPPH自由基清除法测定了这些类似物的抗氧化活性，多羟基姜黄素类化合物（5l-5s）表现出优异的抗氧化活性。这些类似物对淋巴细胞显示出细胞毒性，并对道尔顿淋巴瘤腹水肿瘤细胞具有良好的肿瘤抑制活性。