文摘
In order to better understand the antioxidant behavior of a series of polyphenolic 2¡ä-hydroxychalcones, we describe the results of several chemical and biological studies, m>in?vitrom> and m>in?vivom>. Single crystal X-ray methods elucidated their molecular structures and important intermolecular interactions such as H-bonding and molecular stacking in the crystal structures that contribute to our knowledge in explaining antioxidant activity. The results of experiments using the 1,1-diphenyl-2-dipicrylhydrazyl (DPPH) UV-vis spectroscopic method indicate that a hydroxyl group in position 5¡ä induces the highest antioxidant activity. Consequently, 2,2¡ä,5¡ä-trihydroxychalcone was selected for further study m>in?vitrom> towards ROS scavenging in L-6 myoblasts and THP-1 human monocytes, where it shows an excellent antioxidant activity in a concentration range lower than that reported by most studies of related molecules. In addition, this chalcone shows a very selective activity: it inhibits the proliferation of leukemic cells, but it does not affect the normal L-6 myoblasts and human fibroblasts. In studying 2,2¡ä,5¡ä-trihydroxychalcone's effect on weight gain and serum glucose and insulin levels in Zucker m>fattym> (m>fam>?/m>fam>?) rats we found that supplementing the diet with a 10?mg/kg dose of this chalcone (3 times weekly) blunted the increase in glucose that co-occurs with weight gain over the 6-week treatment period. It is concluded that 2,2¡ä,5¡ä-trihydroxychalcone has the potential to serve as a protective agent for some debilitating diseases.
