Department of Urology and Department of Medical Research, Chi-Mei Medical Center, Yong Kang City, Taiwan, ROC.
Neurosci Lett. 2010 Apr 5;473(2):107-9. doi: 10.1016/j.neulet.2010.02.029. Epub 2010 Feb 19.
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.
姜黄素是姜黄根茎中的一种活性成分,最近有研究表明它对毒蕈碱 M1 型胆碱能受体(M1-mAChR)具有亲和力。在本研究中,我们发现姜黄素可引起 Wistar 大鼠离体膀胱肌肉张力呈浓度依赖性增加,该作用可被哌仑西平所抑制,其抑制浓度足以阻断 M1-mAChR。在放射性配体结合实验中,姜黄素可呈浓度依赖性置换大鼠膀胱匀浆中[3H]-oxotremorine(OXO-M)的特异性结合。在 PLC-PKC 通路抑制剂存在的情况下,无论是 U73122(PLC 抑制剂)还是Chelerythrine(PKC 抑制剂),均可明显减少姜黄素引起的膀胱收缩。结论:研究结果提示,姜黄素可在低于清除自由基的浓度下激活 M1-mAChR,通过 PLC-PKC 通路增加膀胱肌肉张力。