Tipton C L, Shih M, Magat W J
Department of Biochemistry and Biophysics, Iowa State University, Ames 50011.
J Lipid Res. 1991 Sep;32(9):1403-8.
A series of cholesterol hydroperoxides has been prepared and tested as inactivators of calmodulin. Two previously undescribed compounds, tentatively identified as 20-(R)-25-dihydroperoxy-5-cholesten-3 beta-ol and its 20-(S) isomer inactivate calmodulin with 50% loss of activity at 5-10 microM. Cholesterol derivatives with a single hydroperoxy group at C-20 or C-25 are less effective, while 7 alpha-hydroperoxy-cholesterol and 25-hydroxy-cholesterol are inactive. The side-chain hydroperoxide compounds were isolated from a mixture shown earlier to suppress formation of fatty streaks in aortas of rabbits fed a diet supplemented with cholesterol.
已制备出一系列胆固醇氢过氧化物，并作为钙调蛋白的灭活剂进行了测试。两种先前未描述的化合物，暂定为20-(R)-25-二氢过氧-5-胆甾烯-3β-醇及其20-(S)异构体，在5-10微摩尔浓度下可使钙调蛋白失活，活性丧失50%。在C-20或C-25处带有单个氢过氧基的胆固醇衍生物效果较差，而7α-氢过氧胆固醇和25-羟基胆固醇则无活性。侧链氢过氧化物化合物是从先前显示可抑制喂食添加胆固醇饮食的兔子主动脉中脂肪条纹形成的混合物中分离出来的。
