Rao M R, Shen X H, Zou X
Department of Cardiovascular Pharmacology, Nanjing Medical College, China.
Eur J Pharmacol. 1988 Oct 18;155(3):293-6. doi: 10.1016/0014-2999(88)90516-x.
Praeruptorin C and E isolated from Peucedanum praeruptorum Dunn. decreased the maximum contractile effect of Ca2+ in potassium-depolarized swine coronary strips and shifted the concentration-response curve to the right in a non-parallel manner. The calcium antagonistic activity of praeruptorin C and E expressed as pD'2 value was 5.7 and 5.2, respectively. Nifedipine, with a pD'2 value of 6.88, was used as a known calcium antagonistic drug to compare the potency of the drugs studied. The relaxation induced by praeruptorin C was concentration-dependent and the IC50 value was 79 microM. Praeruptorin C also reduced the maximum contractile response and shifted the concentration-response curve for calcium to the right in a non-parallel manner in potassium-depolarized guinea-pig left atria (pD'2 = 5.52) but its potency was much less than that of nifedipine (pD'2 = 7.19). The results suggest that praeruptorin C and E relaxed swine coronary artery and decreased contractility in guinea-pig left atria. These effects are similar in many respects to those displayed by drugs that have calcium entry blocking activity.
从白花前胡中分离得到的白花前胡丙素和白花前胡乙素可降低钾离子去极化的猪冠状动脉条中Ca2+的最大收缩效应，并使浓度-反应曲线非平行右移。以pD'2值表示的白花前胡丙素和白花前胡乙素的钙拮抗活性分别为5.7和5.2。硝苯地平的pD'2值为6.88，用作已知的钙拮抗药物以比较所研究药物的效力。白花前胡丙素诱导的舒张呈浓度依赖性，IC50值为79 microM。白花前胡丙素还降低了钾离子去极化的豚鼠左心房的最大收缩反应，并使钙的浓度-反应曲线非平行右移（pD'2 = 5.52），但其效力远低于硝苯地平（pD'2 = 7.19）。结果表明，白花前胡丙素和白花前胡乙素可舒张猪冠状动脉并降低豚鼠左心房的收缩力。这些作用在许多方面与具有钙通道阻滞活性的药物所表现出的作用相似。
