Effects of (1R,9S)-β-Hydrastine on Intracellular Calcium Concentration in PC12 Cells(Analytical Biochemistry)

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(1R,9S)-β-Hydrastine (BHS) decreases the basal intracellular Ca^<2+> concentration ([Ca^<2+>]_i) in PC12 cells. This study examined the effects of (1R,9S)-BHS on [Ca^<2+>]_i in PC12 cells. (1R,9S)-BHS at 10-100 μM in combination with a high extracellular K^+ level (56 mM) inhibited the release of dopamine in a concentration-dependent manner with an IC_<50> value of 66.5 μM. BHS at 100 μM inhibited the sustained increase in [Ca^<2+>]_i induced by a high K^+ level (56 mM), and had an inhibitory effect on the 2 μM nifedipine-induced blockage of the K^+-stimulated sustained increase in [Ca^<2+>]_i. In addition, (1R,9S)-BHS at 100 μM prevented the rapid and sustained increase in [Ca^<2+>]_i elicited by 20 mM caffeine, but did not have an effect on the increase induced by 1 μM thapsigargin, in the presence of external Ca^<2+>. These results suggest that the active sites of (1R,9S)-BHS are mainly L-type Ca^<2+> channels and caffeine-sensitive Ca^<2+>-permeable channels in PC12 cells.
公益社団法人日本薬学会の論文
2007-08-01