Abstract:
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 ≈ 5 μmol/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.
journal_name
J Biomed Scijournal_title
Journal of biomedical scienceauthors
Wang HJ,Martin AG,Chao PK,Reichard RA,Martin AL,Huang YW,Chan MH,Aronstam RSdoi
10.1186/1423-0127-20-11subject
Has Abstractpub_date
2013-02-23 00:00:00pages
11eissn
1021-7770issn
1423-0127pii
1423-0127-20-11journal_volume
20pub_type
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