Isosteviol as a potassium channel opener to lower intracellular calcium concentrations in cultured aortic smooth muscle cells

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Title:	Isosteviol as a potassium channel opener to lower intracellular calcium concentrations in cultured aortic smooth muscle cells
Authors:	Wong, KL;Yang, HY;Chan, P;Cheng, TH;Liu, JC;Hsu, FL;Liu, IM;Cheng, YW;Cheng, JT
Contributors:	附設醫院麻醉部;Taipei Med Univ, Wan Fang Hosp, Div Cardiovasc Med, Dept Med, Taipei 117, Taiwan;Taipei Med Univ, Grad Inst Med Sci, Taipei, Taiwan;Taipei Med Univ, Grad Sch Pharmacol, Taipei, Taiwan;Tajen Inst Technol, Dept Pharmacol, Yen Pou, Ping Tung Provi, Taiwan;Natl Cheng Kung Univ, Coll Med, Dept Pharmacol, Tainan 70101, Taiwan;China Med Univ Hosp, Dept Anesthesia, Taichung, Taiwan
Date:	2004
Issue Date:	2010-09-24 14:51:33 (UTC+8)
Publisher:	GEORG THIEME VERLAG KG
Abstract:	Scutellariae Radix (SR), the root of Scutellaria baicalensis (Labiatae), is widely used in clinical Chinese medicine. In order to investigate the effect of SR on the absorption and disposition of cyclosporine, rats were administered with cyclosporine orally (in the form of the microemulsion Neoral(R)) and intravenously with and without coadministration of SR decoction in randomized cross-over designs, respectively. Furthermore, the effects of the major constituents, e.g., baicalin and its aglycone baicalein on cyclosporine pharmacokinetics were also investigated in rats. A specific monoclonal fluorescence polarization immunoassay was used to determine the blood concentration of cyclosporine. Our results indicated that coadministration of SR decoction at doses of 1 g/kg and 2 g/kg significantly decreased the C-max of cyclosporine by 62.9% and 79.6% and reduced the AUC(0-540) by 55.2 % and 82.0 %, respectively. On the contrary, coadministration of baicalin and baicalein at doses of 112 mumol/kg markedly elevated the C-max of cyclosporine by 408.1% and 87.5% and increased the AUC(0-540) by 685.3 % and 150.2%, respectively. Nevertheless, SR decoction did not alter the pharmacokinetics of intravenous cyclosporine. These results indicate that a profound interaction between SR decoction and cyclosporine occurred at the absorption site. In order to ensure the efficacy and safety of cyclosporine, the coadministration of SR and its preparations with oral cyclosporine should be avoided.
Relation:	PLANTA MEDICA 70(2):108-112
Appears in Collections:	[China Medical University Hospital] Jurnal articles

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