화학공학소재연구정보센터
Biochemical and Biophysical Research Communications, Vol.341, No.2, 357-362, 2006
Synthetic heteroprostanoids of A- and E-types as novel non-comprehensive inhibitors of adenylyl cyclase in rat hepatocytes
Treatment of rat hepatocyte plasma membranes with five novel synthetic heteroprostanoids of A- and E-types significantly decreased basal activity of adenylyl cyclase. Inhibition of forskolin-Stimulated activity of the enzyme was seen as well. The maximal effective concentration for all substances tested was found at approximately 5 X 10(-6)-1 X 10(-5) M. The values of half maximal concentration (IC50) for all prostanoids were at the region of 0.7-1.1 mu M. Prostanoids belonging to cyclopentenone group A (U-39 U-26) were less active than analogs of 11-deoxy-PGE(1) (TA-227, TA-280, and TA-239). The strongest inhibitory effect of adenylyl cyclase activity (more than 3 times) was determined in the presence of prostanoid TA-227 possessing hydrophobic 15-phenyl ring and isoxazol group in omega-chain. The investigation of AC activity in the presence of different concentrations of prostanoids and varying concentrations of Mg-ATP has demonstrated that a non-comprehensive mechanisin With P,particular effect takes place ill case of AC inhibition by the heteroprostanoids. (c) 2006 Elsevier Inc. All rights reserved.