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Published on: June 20, 2014
Synthesis and biological activity of halophenols as potent antioxidant and cytoprotective agents
Wanyi Zhao1, Xiue Feng, Shurong Ban
1School of Pharmaceutical Science, Shanxi Medical University, Taiyuan 030001, China.
Abstract:
A series of new bromophenols and chlorophenols were prepared by a practical route. The in vitro antioxidative activity of the halophenols was evaluated by the 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical-scavenging assay, and their cytoprotective activity was also tested on hydrogen peroxide (H(2)O(2))-induced injury in human umbilical vein endothelial cells (HUVEC). All halophenols tested displayed moderate to good DPPH radical-scavenging activity, and two bromophenols, 2,3'-dibromo-4,5,6'-trihydroxydiphenylmethanone (16c) and 2,3-dibromo-4,5-dihydroxydiphenylmethanone (17c) exhibited high protective activity against H(2)O(2)-induced injury in HUVEC with EC(50) values of 0.4 and 0.8 microM, respectively. The preliminary structure-activity relationships of these compounds were also investigated in order to determine the essential structures required for their bioactivities.
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