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

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20 Citations (Scopus)


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
Issue number5
Publication statusPublished - 2006 Apr 1

All Science Journal Classification (ASJC) codes

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


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