Activation of muscarinic M-1 cholinoceptors by curcumin to increase contractility in urinary bladder isolated from Wistar rats.
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.
Cheng
Tse-Chou
TC
Department of Urology and Department of Medical Research, Chi-Mei Medical Center, Yong Kang City, Taiwan, ROC.
Lu
Chih-Cheng
CC
Chung
Hsien-Hui
HH
Hsu
Chih-Chieh
CC
Kakizawa
Nozomi
N
Yamada
Shizuo
S
Cheng
Juei-Tang
JT
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
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