Yang S, Miao Y S, Han Q, Jiang M H, Jin G Z
Department of Pharmacology, School of Pharmacy, Shanghai Medical University, China.
Zhongguo Yao Li Xue Bao. 1993 May;14(3):235-7.
The relaxant effects of (-)-stepholidine ((-)-SPD) and tetrahydroberberine (THB) on rat aorta were studied in vitro. (-)-SPD IC50 18.1 (95% confidence limits 11.1-29.5) mumol.L-1 and THB IC50 18.6 (95% confidence limits 9.2-37.9) mumol.L-1 inhibited the contractions caused by KCl (100 mmol.L-1) concentration-dependently. Both (-)-SPD and THB markedly inhibited the 160 mmol.L-1 KCl-stimulated 45Ca influx. The inhibitions by (-)-SPD 10 mumol.L-1 and 100 mumol.L-1 were 18 +/- 13% (P > 0.05) and 47.0 +/- 2.8% (P < 0.01), respectively. The inhibitions by THB 10 mumol.L-1 and 100 mumol.L-1 were 36 +/- 9% (P < 0.01) and 43 +/- 8% (P < 0.05), respectively. The results showed that the effective concentrations of the 2 drugs inhibiting high KCl-induced contraction and 45Ca transmembrane influx in rat thoracic aorta were at a similar level, and that they were nearly 1/100 and 1/10 of those of verapamil respectively, indicating that (-)-SPD and THB had similar calcium channel blocking effect on rat artery, but were weaker than verapamil.
在体外研究了(-)-千金藤啶碱((-)-SPD)和四氢小檗碱(THB)对大鼠主动脉的舒张作用。(-)-SPD的IC50为18.1(95%置信限为11.1 - 29.5)μmol·L-1，THB的IC50为18.6(95%置信限为9.2 - 37.9)μmol·L-1，它们浓度依赖性地抑制由KCl(100 mmol·L-1)引起的收缩。(-)-SPD和THB均显著抑制160 mmol·L-1 KCl刺激的45Ca内流。10 μmol·L-1和100 μmol·L-1的(-)-SPD抑制率分别为18±13%(P>0.05)和47.0±2.8%(P<0.01)。10 μmol·L-1和100 μmol·L-1的THB抑制率分别为36±9%(P<0.01)和43±8%(P<0.05)。结果表明，这两种药物抑制大鼠胸主动脉高KCl诱导的收缩和45Ca跨膜内流的有效浓度处于相似水平，且分别约为维拉帕米的1/100和1/10，表明(-)-SPD和THB对大鼠动脉具有相似的钙通道阻滞作用，但比维拉帕米弱。
