Vasorelaxant effects of cardamonin and alpinetin from Alpinia henryi K. Schum.
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AbstractThe vascular effects of cardamonin and alpinetin from Alpinia henryi K. Schum. were examined in the rat isolated mesenteric arteries. H-1 and C-13 nuclear magnetic resonance spectra showed that cardamonin is present in trans-form, and single-crystal radiographic structure revealed that alpinetin is present in S configuration. Both cardamonin and alpinetin produced a rightward shift in the concentration-response curve for phenylephrine in a noncompetitive manner, and they induced relaxation of phenylephrine-preconstricted arteries with respective mean inhibitory concentrations (IC50) of 9.3 +/- 0.6 muM and 17.5 +/- 2.8 muM. Both compounds also relaxed arteries preconstricted by endothelin I or U46619, Their relaxant effects were decreased in endothelium-removed rings. Pretreatment with N-G-nitro-L-arginine methyl ester or methylene blue inhibited relaxation induced by both agents, and pretreatment with L-arginine reversed the effect of N-G-nitro-L-arginine methyl ester on cardamonin-induced endothelium-dependent relaxation. The relaxant effects of cardamonin and alpinetin were unaffected by indomethacin (3 muM). Cardamonin and alpinetin inhibited 60 mM K+-induced contraction with respective IC50 of 11.5 +/- 0.3 muM and 37.9 +/- 3.6 muM. In addition, both agents inhibited the transient contraction induced by 3 muM phenylephrine or by 10 mM caffeine in Ca2+-free Krebs solution, Finally, these two agents also concentration dependently relax the arteries preconstricted by 1 muM phorbol 12,13-diacetate in Ca2+-free Krebs solution. These results indicate that purified cardamonin and alpinetin from A. henryi K, Schum, relaxed rat mesenteric arteries through multiple mechanisms. They induced both endothelium-dependent and -independent relaxation; the former is likely mediated by nitric oxide whereas the latter is probably mediated through nonselective inhibition of Ca2+ influx and intracellular Ca2+ release and inhibition of the protein kinase C-dependent contractile mechanism.
All Author(s) ListWang ZT, Lau CW, Chan FL, Yao XQ, Chen ZY, He ZD, Huang Y
Journal nameJournal of Cardiovascular Pharmacology
Volume Number37
Issue Number5
Pages596 - 606
LanguagesEnglish-United Kingdom
Keywordsalpinetin; Alpinia henryi; Ca2+ channels; cardamonin; endothelium; mesenteric artery; nitric oxide; rat; vasorelaxation
Web of Science Subject CategoriesCardiac & Cardiovascular Systems; CARDIAC & CARDIOVASCULAR SYSTEMS; Cardiovascular System & Cardiology; Pharmacology & Pharmacy; PHARMACOLOGY & PHARMACY

Last updated on 2021-24-09 at 01:07