(±)-Naringenin 是一种天然的类黄酮。它通过激活肌细胞中 BKCa通道发挥对内皮剥脱血管的舒张作用。
产品描述
(±)-Naringenin is a natural product. It displays vasorelaxant effect on endothelium-denuded vessels via the activation of BKCa channels in myocytes.
体内活性
(+/-)-Naringenin induced concentration-dependent relaxation in endothelium-denuded rat aortic rings pre-contracted with either 20 mM KCl or noradrenaline (pIC(50) values of 4.74 and 4.68, respectively).?Tetraethylammonium, iberiotoxin, 4-aminopyridine and 60 mM KCl antagonised (+/-)-naringenin-induced vasorelaxation, while glibenclamide did not produce any significant antagonism.?Naringin [(+/-)-naringenin 7-beta-neohesperidoside] caused a concentration-dependent relaxation of rings pre-contracted with 20 mM KCl, although its potency and efficacy were significantly lower than those of (+/-)-naringenin.?In rat tail artery myocytes, (+/-)-naringenin increased large conductance Ca(2+)-activated K(+) (BK(Ca)) currents in a concentration-dependent manner;?this stimulation was iberiotoxin-sensitive and fully reversible upon drug wash-out.?(+/-)-Naringenin accelerated the activation kinetics of BK(Ca) current, shifted, by 22 mV, the voltage dependence of the activation curve to more negative potentials, and decreased the slope of activation.?(+/-)-Naringenin-induced stimulation of BK(Ca) current was insensitive either to changes in the intracellular Ca(2+) concentration or to the presence, in the pipette solution, of the fast Ca(2+) chelator BAPTA.?However, such stimulation was diminished when the K(+) gradient across the membrane was reduced.
细胞实验
Naringenin is dissolved in DMSO and diluted in cell culture medium. The cells are rinsed with PBS and grown in a medium containing various concentrations of naringenin (50, 100, 150, 200, 250, 300 μM). The solvent DMSO treated cells are served as control. After 24 hrs of treatment, the medium is removed and replaced by another medium containing MTT. Cell viability is measured using the MTT assay[1].
Cas No.
67604-48-2
分子式
C15H12O5
分子量
272.256
别名
Naringenine;柚皮素;Naringenin;(±)-柚皮素;Salipurpol;(±)-Naringenin
储存和溶解度
H2O:< 0.1 mg/mL (insoluble)
DMSO:120 mg/mL (440.77 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years