title: Inhibition of calmodulin-dependent protein kinase II by cyclic and linear peptide alkaloids from Zizyphus species.
abstract: The effects of sedative peptide alkaloids from Zizyphus species on calmodulin- dependent protein kinase II were investigated. Protein kinase II activity was assayed on the basis of its ability to activate tryptophan 5-monooxygenase as its substrate in the presence of calmodulin. All thirteen alkaloids tested were stronger inhibitors than chlorpromazine (IC50, 98 microM) on calmodulin-dependent protein kinase II. Among them, the most potent inhibitor was daechuine S27 (IC50 2.95 microM), which was stronger than pimozide (IC50, 15.0 microM).
authors.affiliation: Natural Products Research Institute, College of Pharmacy, Seoul National University, Seoul 110-460, Korea. snake@snu.ac.kr
authors.forename: Yong Nam
authors.initials: YN
authors.lastname: Han
authors.forename: Keum Hee
authors.initials: KH
authors.lastname: Hwang
authors.forename: Byung Hoon
authors.initials: BH
authors.lastname: Han
mesh_terms: D000470:Alkaloids / Q000494:pharmacology*; D000818:Animals; D001933:Brain Stem / Q000187:drug effects / Q000201:enzymology; D054732:Calcium-Calmodulin-Dependent Protein Kinase Type 2; D017871:Calcium-Calmodulin-Dependent Protein Kinases / Q000037:antagonists & inhibitors*; D066298:In Vitro Techniques; D010455:Peptides / Q000494:pharmacology*; D051381:Rats; D017207:Rats, Sprague-Dawley; D013329:Structure-Activity Relationship; D014365:Tryptophan Hydroxylase / Q000378:metabolism; D031957:Ziziphus / Q000737:chemistry*
chemical_list: D000470:Alkaloids; D010455:Peptides; D014365:Tryptophan Hydroxylase; D054732:Calcium-Calmodulin-Dependent Protein Kinase Type 2; D017871:Calcium-Calmodulin-Dependent Protein Kinases