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Tetrandrine inhibits Ca2+-activated chloride channel in cultured human umbilical vein endothelial cells

  
@article{APS7890,
	author = {Qi-zhi FANG and Ning ZHONG and Yi ZHANG and Zhao-nian ZHOU},
	title = {Tetrandrine inhibits Ca2+-activated chloride channel in cultured human umbilical vein endothelial cells},
	journal = {Acta Pharmacologica Sinica},
	volume = {25},
	number = {3},
	year = {2016},
	keywords = {},
	abstract = {AIM:
To characterize the electrophysiological and kinetic properties of Ca2+-activated chloride channel (CaCC) in cultured human umbilical vein endothelial cell line (HUVEC), and test the inhibitory effects of tetrandrine (Tet) on CaCC.
METHODS:
Ca2+-activated Cl- currents (I(Cl,Ca)) were recorded by patch-clamp whole cell configurations. [Ca2+]i was measured via intracellular Fura-2 fluorescence intensities.
RESULTS:
I(Cl,Ca) was activated by increasing [Ca2+]i via direct elevation of intracellular calcium. I(Cl,Ca) showed an apparent outward rectification properties, and it was activated in a voltage- and calcium-dependent mode. Tet dose-dependently inhibited I(Cl,Ca), the IC50 was (5.2+/-0.4) micromol/L (n=8 cells). Tet suppressed both voltage-dependent and calcium-dependent activation of I(Cl,Ca). The activation time constant was (326+/-12) ms [in the presence of 10 micromol/L Tet, compared to control (175+/-17) ms, at +100 mV], and Ca2+ concentration for half maximal activation was (387+/-61) nmol/L for Tet (compared to control (287+/-36) nmol/L.
CONCLUSIONS:
Tet effectively blocked I(Cl,Ca), and such effects might be due to its inhibitory effects on the activation process of Ca2+-activated chloride channel.},
	issn = {1745-7254},	url = {http://www.chinaphar.com/article/view/7890}
}