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Activation of iberiotoxin-sensitive, Ca 2+-activated K + channels of porcine isolated left anterior descending coronary artery by diosgenin
Au A.L.S.2; Kwok C.C.2; Lee A.T.C.2; Kwan Y.W.2; Lee M.M.S.1; Zhang R.-Z.1; Ngai S.M.1; Lee S.M.Y.1; He G.-W.1; Fung K.P.1
2004-10-11
Source PublicationEuropean Journal of Pharmacology
ISSN00142999
Volume502Issue:1-2Pages:123-133
Abstract

The objective of this study was to determine the vasodilating effect of 3β-hydroxy-5-spirostene (diosgenin), a phytoestrogen found in wild yams, using porcine resistance left anterior descending coronary artery. In 5-hydroxytryptamine (3 μM) pre-contracted preparation, diosgenin caused a concentration-dependent (0.01 to 1 μM), endothelium-independent relaxation, with a maximum relaxation of ∼72% at 1 μM. No apparent effect was observed with 17β-oestradiol and progesterone with concentrations ≤0.3 μM, and a relaxation of ∼15% and ∼23% caused by 17β-oestradiol (1 μM) and progesterone (1 μM), respectively. Diosgenin-elicited relaxation was not altered by 7α,17β-[9[(4,4,5,5,5-pentafluoropentyl) sulfinyl]nonyl]estra-1,3,5(10)-triene-3,17-diol (ICI 182,780), mifepristone, (+)-bicuculline, cis-N-(2-phenylcyclopentyl)azacyclotridec-1-en-2-amine (MDL 12330A), glibenclamide and scavengers of reactive oxygen species. The iberiotoxin-sensitive, Ca -activated K (BK ) current of single vascular myocytes recorded, using patch-clamp techniques, was markedly enhanced by diosgenin, 17β-oestradiol and progesterone. Application of (9S, 10R, 12R)-2,3,9,10,11,12-hexahydro-10-methoxy-2,9-dimethyl- 1-oxo-9,12-epoxy-1H-diindolo[1,2,3-fg:3′,2′,1′-kl]pyrrolo[3, 4-i][1,6]benzodiazocine-10-carboxylic acid methyl ester (KT 5823, 300 nM) eradicated the enhancement of BK amplitude. Diosgenin, 17β-oestradiol and progesterone did not affect whereas phloretin, biochanin A and zearalanone (1 μM each) significantly suppressed [Ca ] -induced contraction. In oestrogen competition essay using human breast cancer cell (MCF-7 cells), diosgenin (0.001 nM to 10 μM) did not interact with oestrogen receptor-α, and no displacement of [ H]17β-oestradiol was observed. In oestrogen receptor α- and β-fluorescence polarization competitor assay, diosgenin (100 μM) demonstrated a greater competition with the β-isoform of oestrogen receptor. These results suggest that diosgenin caused an acute, endothelium-independent coronary artery relaxation via protein kinase G signalling cascade and an activation of BK channel of arterial smooth muscle cells. The oestrogen receptor (α and β-isoforms) and progesterone receptor are probably not involved. © 2004 Elsevier B.V. All rights reserved.

KeywordCa 2+-activated k + (Bk Ca) Channel Diosgenin Iberiotoxin-sensitive Oestrogen Receptor Porcine Coronary Artery
DOI10.1016/j.ejphar.2004.08.045
URLView the original
Indexed BySCI
WOS Research AreaPharmacology & Pharmacy
WOS SubjectPharmacology & Pharmacy
WOS IDWOS:000224448900015
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被引频次[WOS]:37   [WOS记录]     [WOS相关记录]
Document TypeJournal article
专题Institute of Chinese Medical Sciences
Affiliation1.Chinese University of Hong Kong
2.Fac. Med.
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GB/T 7714
Au A.L.S.,Kwok C.C.,Lee A.T.C.,et al. Activation of iberiotoxin-sensitive, Ca 2+-activated K + channels of porcine isolated left anterior descending coronary artery by diosgenin[J]. European Journal of Pharmacology,2004,502(1-2):123-133.
APA Au A.L.S..,Kwok C.C..,Lee A.T.C..,Kwan Y.W..,Lee M.M.S..,...&Fung K.P..(2004).Activation of iberiotoxin-sensitive, Ca 2+-activated K + channels of porcine isolated left anterior descending coronary artery by diosgenin.European Journal of Pharmacology,502(1-2),123-133.
MLA Au A.L.S.,et al."Activation of iberiotoxin-sensitive, Ca 2+-activated K + channels of porcine isolated left anterior descending coronary artery by diosgenin".European Journal of Pharmacology 502.1-2(2004):123-133.
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