6-Tridecylresorcylic acid, a novel ATPase inhibitor that blocks the contractile apparatus of skeletal muscle proteins.
6-Tridecylresorcylic acid (TRA) isolated from a primula Lysimachia japonica Thunb. inhibited contraction of myofibrils, superprecipitation of myosin B, and ATPase activities of myosin and actomyosin prepared from rabbit skeletal muscle in a dose-dependent manner. The IC50 values in molarity of TRA were as follows: myosin (K+,EDTA)-ATPase, 3.5 X 10(-6); myosin Ca2+-ATPase, 3.5 X 10(-5); and actomyosin Mg2+-ATPase, 1.6 X 10(-5). The inhibition of ATPase activity of myofibrils by TRA was virtually reversed by washing with the fresh saline solution. Kinetic analysis of inhibitory effects of TRA suggests that the inhibition of (K+,EDTA)-ATPase activity of myosin or subfragment-1 is parabolic noncompetitive. TRA had no effect on alkaline phosphatase and choline acetyltransferase activities. TRA may provide a useful chemical tool for the study of the molecular mechanisms of actin-myosin contractile systems.
D000205:Actomyosin / Q000037:antagonists & inhibitors; D000251:Adenosine Triphosphatases / Q000037:antagonists & inhibitors*; D000818:Animals; D062385:Hydroxybenzoates / Q000494:pharmacology*; D007700:Kinetics; D009119:Muscle Contraction / Q000187:drug effects*; D009132:Muscles / Q000187:drug effects / Q000502:physiology; D009210:Myofibrils / Q000187:drug effects* / Q000502:physiology; D009218:Myosins / Q000037:antagonists & inhibitors / Q000302:isolation & purification; D010944:Plants; D011817:Rabbits
D062385:Hydroxybenzoates; C042674:6-tridecylresorcylic acid; D000205:Actomyosin; D000251:Adenosine Triphosphatases; D009218:Myosins