Diosgenin, a plant-derived sapogenin, stimulates Ca2+-activated K+ current in human cortical HCN-1A neuronal cells

Ya Jean Wang, Yen-Chin Liu, Han Dong Chang, Sheng-Nan Wu

Research output: Contribution to journalArticle

18 Citations (Scopus)

Abstract

The effects of diosgenin (3β-hydroxy-5-spirostene), a plant-derived sapogenin, on ion currents in human cortical neurons (HCN-1A) were investigated. In the whole-cell configuration, diosgenin (0.3-30 μM) increased the amplitude of K+ outward current (IK). Diosgenin-stimulated IK was sensitive to inhibition by paxilline (1 μM), but not by apamin (200 nM) or glibenclamide (10 μM). In the cell-attached configuration, diosgenin applied to the bath increased the activity of large-conductance Ca2+-activated K+ (BKCa) channels without altering single-channel conductance. Diosgenin enhanced BKCa-channel activity with an EC50 value of 25 μM. However, in inside-out patches, diosgenin applied to the intracellular surface had no effect on BK Ca-channel activity, while cilostazol or caffeic acid phenethyl ester increased it. As shown with the aid of intracellular Ca2+ measurements, diosgenin elevated intracellular Ca2+ in HCN-1A cells. Western blotting also revealed the presence of the α-subunit of BK Ca channels in these cells. The sustained stimulation of I K arises primarily from the diosgenin-induced Ca2+ influx across the cell membrane. The effect of diosgenin on these channels may affect the functional activity of cortical neurons.

Original languageEnglish
Pages (from-to)430-436
Number of pages7
JournalPlanta Medica
Volume72
Issue number5
DOIs
Publication statusPublished - 2006 Apr 1

Fingerprint

Diosgenin
Sapogenins
Large-Conductance Calcium-Activated Potassium Channels
Neurons
Apamin
Calcium-Activated Potassium Channels
Glyburide
Cell membranes
Baths
Western Blotting
Cell Membrane
Ions

All Science Journal Classification (ASJC) codes

  • Analytical Chemistry
  • Molecular Medicine
  • Pharmacology
  • Pharmaceutical Science
  • Drug Discovery
  • Complementary and alternative medicine
  • Organic Chemistry

Cite this

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title = "Diosgenin, a plant-derived sapogenin, stimulates Ca2+-activated K+ current in human cortical HCN-1A neuronal cells",
abstract = "The effects of diosgenin (3β-hydroxy-5-spirostene), a plant-derived sapogenin, on ion currents in human cortical neurons (HCN-1A) were investigated. In the whole-cell configuration, diosgenin (0.3-30 μM) increased the amplitude of K+ outward current (IK). Diosgenin-stimulated IK was sensitive to inhibition by paxilline (1 μM), but not by apamin (200 nM) or glibenclamide (10 μM). In the cell-attached configuration, diosgenin applied to the bath increased the activity of large-conductance Ca2+-activated K+ (BKCa) channels without altering single-channel conductance. Diosgenin enhanced BKCa-channel activity with an EC50 value of 25 μM. However, in inside-out patches, diosgenin applied to the intracellular surface had no effect on BK Ca-channel activity, while cilostazol or caffeic acid phenethyl ester increased it. As shown with the aid of intracellular Ca2+ measurements, diosgenin elevated intracellular Ca2+ in HCN-1A cells. Western blotting also revealed the presence of the α-subunit of BK Ca channels in these cells. The sustained stimulation of I K arises primarily from the diosgenin-induced Ca2+ influx across the cell membrane. The effect of diosgenin on these channels may affect the functional activity of cortical neurons.",
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Diosgenin, a plant-derived sapogenin, stimulates Ca2+-activated K+ current in human cortical HCN-1A neuronal cells. / Wang, Ya Jean; Liu, Yen-Chin; Chang, Han Dong; Wu, Sheng-Nan.

In: Planta Medica, Vol. 72, No. 5, 01.04.2006, p. 430-436.

Research output: Contribution to journalArticle

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AU - Wang, Ya Jean

AU - Liu, Yen-Chin

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AB - The effects of diosgenin (3β-hydroxy-5-spirostene), a plant-derived sapogenin, on ion currents in human cortical neurons (HCN-1A) were investigated. In the whole-cell configuration, diosgenin (0.3-30 μM) increased the amplitude of K+ outward current (IK). Diosgenin-stimulated IK was sensitive to inhibition by paxilline (1 μM), but not by apamin (200 nM) or glibenclamide (10 μM). In the cell-attached configuration, diosgenin applied to the bath increased the activity of large-conductance Ca2+-activated K+ (BKCa) channels without altering single-channel conductance. Diosgenin enhanced BKCa-channel activity with an EC50 value of 25 μM. However, in inside-out patches, diosgenin applied to the intracellular surface had no effect on BK Ca-channel activity, while cilostazol or caffeic acid phenethyl ester increased it. As shown with the aid of intracellular Ca2+ measurements, diosgenin elevated intracellular Ca2+ in HCN-1A cells. Western blotting also revealed the presence of the α-subunit of BK Ca channels in these cells. The sustained stimulation of I K arises primarily from the diosgenin-induced Ca2+ influx across the cell membrane. The effect of diosgenin on these channels may affect the functional activity of cortical neurons.

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