benzofurans and tetrahydropalmatine

In this present study, a sensitive and rapid UPLC-MS/MS method was developed for simultaneous quantification of paeoniflorin, albiflorin, ferulic acid, tetrahydropalmatine, protopine, typhaneoside and senkyunolide I in Beagle dog plasma after oral administration of the Shao-Fu-Zhu-Yu Decoction. Chloramphenicol and clarithromycin were used as internal standards. Plasma samples were processed by protein precipitation with methanol. The separation was performed on an Acquity BEH C18 column (100mm×2.1mm, 1.7μm) at a flow-rate of 0.4mL/min, using 0.1% formic acid-acetonitrile as mobile phase. Method validation was performed as per Food and Drug Administration guidelines and the results met the acceptance criteria. After validation, this method was successfully applied to a pharmacokinetic study. The results showed that the apparent plasma clearance of paeoniflorin, albiflorin, typhaneoside and senkyunolide I were significantly higher than others. Double peak was observed in plasma concentration curves of tetrahydropalmatine, the ferulic acid had a good absorption in Beagle dog plasma, and senkyunolide I was detected in plasma from the first blood sampling time (15min) and rapidly reached Tmax. The compound of typhaneoside has a low bioavailability according to the results.

Topics: Administration, Oral; Animals; Benzofurans; Benzophenanthridines; Berberine Alkaloids; Bridged-Ring Compounds; Chromatography, High Pressure Liquid; Coumaric Acids; Dogs; Drugs, Chinese Herbal; Female; Glucosides; Glycosides; Monoterpenes; Tandem Mass Spectrometry

To observe the effects of the separate and joint use of salvianolic acid B (SalB) and tetrahydropalmatine (THP) on the L-type calcium channel of rat ventricular myocytes.. Single isolated ventricular myocytes of rats were obtained using acute enzymolysis separation. The current of the L-type calcium channel was recorded using whole-cell patch clamp technique. Changes of the current peak value of the calcium channel (the vertical distance between the peak value point after activation of the calcium electric current and the electric current track after complete inactivation) were observed before and after medication.. The inhibition rate of using SalB (at the dose of 1, 10, and 100 micromol/L) alone on the current peak value of the calcium channel was respectively (25.3 +/- 16.4)% (n=4), (44.6 +/- 24.0)% (n=6), and (86.0 +/- 20.4)% (n =4). That of using THP (at the dose of 10, 30, and 100 micromol/L) alone on the current peak value of the calcium channel was respectively (22.2 +/- 6.4)% (n=5), (27.4 +/- 1.6)% (n= 3), and (51.0 +/- 23.0)% (n=9). The inhibition potency of joint use of SalB (1 micromol/L) and THP (10 micromol/L) on the current peak value of the calcium channel was stronger than using SalB (1 micromol/L) alone or THP (10 micromol/L) alone, showing statistical difference ( P< 0.05). Atropine hydrochloric acid (14 mmol/L) could reverse the inhibition of THP on the L-type calcium channel, while strengthening the inhibition of SalB.. Both SalB and THP showed inhibition on the L-type calcium channel of rat ventricular myocytes. They could generate synergistic effects. Besides, their action mechanisms for regulating the L-type calcium channel were different.

Topics: Animals; Benzofurans; Berberine Alkaloids; Calcium Channels, L-Type; Heart Ventricles; Male; Myocytes, Cardiac; Patch-Clamp Techniques; Rats; Rats, Sprague-Dawley