title: Activation of muscarinic M-1 cholinoceptors by curcumin to increase contractility in urinary bladder isolated from Wistar rats.
abstract: Curcumin is an active principle contained in rhizome of Curcuma longa, and it has been recently mentioned to show affinity to muscarinic M-1 cholinoceptors (M(1)-mAChR). In the present study, we found that curcumin caused a concentration-dependent increase of muscle tone in urinary bladder isolated from Wistar rats. This action was inhibited by pirenzepine at concentration enough to block M(1)-mAChR. In radioligand-binding assay, specific binding of [(3)H]-oxotremorine (OXO-M) in the rat bladder homogenates was also displaced by curcumin in a concentration-dependent manner. In the presence of inhibitors for PLC-PKC pathway, either U73122 (phospholipase C inhibitor) or chelerythrine (protein kinase C inhibitor), curcumin-stimulated contraction in urinary bladder was markedly reduced. In conclusion, the obtained results suggest that curcumin can activate M(1)-mAChR at concentrations lower than to scavenge free radicals to increase of muscle tone in urinary bladder through PLC-PKC pathway.
authors.affiliation: Department of Urology and Department of Medical Research, Chi-Mei Medical Center, Yong Kang City, Taiwan, ROC.
authors.forename: Tse-Chou
authors.initials: TC
authors.lastname: Cheng
authors.forename: Chih-Cheng
authors.initials: CC
authors.lastname: Lu
authors.forename: Hsien-Hui
authors.initials: HH
authors.lastname: Chung
authors.forename: Chih-Chieh
authors.initials: CC
authors.lastname: Hsu
authors.forename: Nozomi
authors.initials: N
authors.lastname: Kakizawa
authors.forename: Shizuo
authors.initials: S
authors.lastname: Yamada
authors.forename: Juei-Tang
authors.initials: JT
authors.lastname: Cheng
mesh_terms: D000818:Animals; D053119:Benzophenanthridines / Q000494:pharmacology; D003474:Curcumin / Q000494:pharmacology*; D004963:Estrenes / Q000494:pharmacology; D066298:In Vitro Techniques; D008297:Male; D018721:Muscarinic Agonists / Q000494:pharmacology*; D009119:Muscle Contraction; D009130:Muscle, Smooth / Q000187:drug effects / Q000502:physiology; D011493:Protein Kinase C / Q000037:antagonists & inhibitors / Q000502:physiology; D011760:Pyrrolidinones / Q000494:pharmacology; D011869:Radioligand Assay; D051381:Rats; D017208:Rats, Wistar; D043643:Receptor, Muscarinic M1 / Q000502:physiology*; D010738:Type C Phospholipases / Q000037:antagonists & inhibitors / Q000502:physiology; D001743:Urinary Bladder / Q000187:drug effects* / Q000502:physiology
chemical_list: D053119:Benzophenanthridines; D004963:Estrenes; D018721:Muscarinic Agonists; D011760:Pyrrolidinones; D043643:Receptor, Muscarinic M1; C060229:1-(6-((3-methoxyestra-1,3,5(10)-trien-17-yl)amino)hexyl)-1H-pyrrole-2,5-dione; C016299:chelerythrine; D011493:Protein Kinase C; D010738:Type C Phospholipases; D003474:Curcumin