title: The mode of inhibitory action of alpha-mangostin, a novel inhibitor, on the sarcoplasmic reticulum Ca(2+)-pumping ATPase from rabbit skeletal muscle.
abstract: alpha-Mangostin, the principal ingredient of the fruit hull of Garcinia mangostana, caused a concentration-dependent decrease in the activities of both Ca(2+)-ATPase and Ca(2+)-transport of the sarcoplasmic reticulum from rabbit skeletal muscle with an IC50 value of 5 microM. Neither Ca2+ release nor other enzyme activities were affected by alpha-mangostin. Kinetic analysis of the inhibitory effects of alpha-mangostin on Ca(2+)-ATPase suggests that the inhibition of the ATPase is a noncompetitive-type with respect to ATP or Ca2+. alpha-Mangostin may become a useful pharmacological tool for clarifying the physiological functions of Ca(2+)-pumping ATPase and sarcoplasmic reticulum.
authors.affiliation: Department of Pharmaceutical Molecular Biology, Faculty of Pharmaceutical Sciences, Tohoku University, Sendai, Japan.
authors.forename: K
authors.initials: K
authors.lastname: Furukawa
authors.forename: K
authors.initials: K
authors.lastname: Shibusawa
authors.forename: N
authors.initials: N
authors.lastname: Chairungsrilerd
authors.forename: T
authors.initials: T
authors.lastname: Ohta
authors.forename: S
authors.initials: S
authors.lastname: Nozoe
authors.forename: Y
authors.initials: Y
authors.lastname: Ohizumi
mesh_terms: D000255:Adenosine Triphosphate / Q000378:metabolism; D000818:Animals; D002118:Calcium / Q000378:metabolism; D004305:Dose-Response Relationship, Drug; D018482:Muscle, Skeletal / Q000187:drug effects*; D011494:Protein Kinases / Q000494:pharmacology*; D011817:Rabbits; D012519:Sarcoplasmic Reticulum / Q000187:drug effects; D014966:Xanthenes / Q000494:pharmacology*; D044004:Xanthones
chemical_list: D014966:Xanthenes; D044004:Xanthones; D000255:Adenosine Triphosphate; D011494:Protein Kinases; D002118:Calcium; C021053:mangostin