- 作者: Hsiu-Jen Wang, Alexis G Martin, Po-Kuan Chao, Rhett A Reichard, Adam L Martin, Yue-wern Huang, Ming-Huan Chan and Robert S Aronstam
- 作者服務機構: Department of Biological Sciences, Missouri University of Science & Technology, 400 W. 11th St, Rolla MO 65409, USA
- 中文摘要: --
- 英文摘要:
Background: Honokiol, a cell-permeable phenolic compound derived from the bark of magnolia trees and present in Asian herbal teas, has a unique array of pharmacological actions, including the inhibition of multiple autonomic responses. We determined the effects of honokiol on calcium signaling underlying transmission mediated by human M3 muscarinic receptors expressed in Chinese hamster ovary (CHO) cells. Receptor binding was determined in radiolabelled ligand binding assays; changes in intracellular calcium concentrations were determined using a fura-2 ratiometric imaging protocol; cytotoxicity was determined using a dye reduction assay.
Results: Honokiol had a potent (EC50 [almost equal to] 5 mumol/l) inhibitory effect on store operated calcium entry (SOCE) that was induced by activation of the M3 receptors. This effect was specific, rapid and partially reversible, and was seen at concentrations not associated with cytotoxicity, inhibition of IP3 receptor-mediated calcium release, depletion of ER calcium stores, or disruption of M3 receptor binding.
Conclusions: It is likely that an inhibition of SOCE contributes to honokiol disruption of parasympathetic motor functions, as well as many of its beneficial pharmacological properties. - 中文關鍵字: --
- 英文關鍵字: Honokiol, Calcium signaling, Store operated calcium entry (SOCE), Inositol trisphosphate(IP3), Muscarinic acetylcholine receptor, Phospholipase Cβ