Antispasmodic activity of licochalcone A, a species-specific ingredient of Glycyrrhiza inflata roots

Licochalcone A, a species-specific and characteristic retrochalcone ingredient of Glycyrrhiza inflata root, has been shown to possess multiple bioactive properties. However, its muscle relaxant activity has not been reported previously. Licochalcone A showed a concentration-dependent relaxant effect...

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Bibliographic Details
Published inJournal of pharmacy and pharmacology Vol. 59; no. 10; p. 1421
Main Authors Nagai, Hidemasa, He, Ju-Xiu, Tani, Tadato, Akao, Teruaki
Format Journal Article
LanguageEnglish
Published England 01.10.2007
Subjects
1-Methyl-3-isobutylxanthine - pharmacology
Animals
Chalcones - administration & dosage
Chalcones - isolation & purification
Chalcones - pharmacology
Dose-Response Relationship, Drug
Glycyrrhiza - chemistry
In Vitro Techniques
Jejunum - drug effects
Jejunum - metabolism
Magnetic Resonance Spectroscopy
Male
Mice
Mice, Inbred ICR
Muscle Contraction - drug effects
Parasympatholytics - administration & dosage
Parasympatholytics - isolation & purification
Parasympatholytics - pharmacology
Phytotherapy
Plant Extracts - chemistry
Plant Extracts - pharmacology
Plant Roots
Plants, Medicinal
Spasm - drug therapy
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Summary:Licochalcone A, a species-specific and characteristic retrochalcone ingredient of Glycyrrhiza inflata root, has been shown to possess multiple bioactive properties. However, its muscle relaxant activity has not been reported previously. Licochalcone A showed a concentration-dependent relaxant effect on the contraction induced by carbachol (50% effective concentration (EC50) = 5.64 +/- 1.61 microM), KCl (EC50 5.12 +/- 1.68 microM), BaCl2 (EC50 1.97 +/- 0.48 microM) and A23187 (EC50 2.63 +/- 2.05 microM). Pretreatment with licochalcone A enhanced the relaxant effect of forskolin, an adenylyl cyclase activator, on the contraction in a similar manner to 3-isobutyl-1-methylxanthine (IBMX), a phosphodiesterase (PDE) inhibitor. Furthermore, the IC50 (22.1 +/- 10.9 microM) of licochalcone A against cAMP PDE was similar to that of IBMX (26.2 +/- 7.4 microM). These results indicated that licochalcone A may have been responsible for the relaxant activity of G. inflata root and acted through the inhibition of cAMP PDE.
ISSN:0022-3573
2042-7158
DOI:10.1211/jpp.59.10.0013