Aida Y, Kasama T, Takeuchi N, Chiba M, Tobinaga S
Nippon Hoechst Marion Roussel, Tokyo, Japan.
Methods Find Exp Clin Pharmacol. 1998 May;20(4):343-51. doi: 10.1358/mf.1998.20.4.485689.
The spasmolytic and antiallergic effects of AA and BB, compounds isolated from Peucedanum japonicum THUNB. (P. japonicum THUNB.) and Peucedanum praeruptorium DUNN. (P. praeruptorium DUNN.), were investigated in isolated smooth muscle and rat PCA. AA and BB showed noncompetitive antagonistic effects on Ach- and histamine-induced contraction in the isolated guinea pig ileum. Both AA and BB at 10(-6) g/ml caused a slight shift to the right of the dose-response curve for Ca2+ in isolated guinea pig ileum, and a concentration up to 3 x 10(-6) g/ml displayed noncompetitive antagonistic effects. The Ba2+ (3 x 10(-4) g/ml)-induced contraction in ileum and the histamine (10(-3) g/ml)-induced contraction in trachea were obtained to relaxation by AA and BB in a concentration-dependent fashion. AA and BB showed noncompetitive antagonist action on serotonin-induced contraction of the rat uterus excised 24-48 h after subcutaneous injection of female rats with estradiol. But, AA and BB were found to have hardly any inhibitory effect on rabbit thoracic aorta contractions induced by epinephrine (3 x 10(-6) g/ml). When the effect of oral administration of 40 mg/kg dose of BB was tested on the rat homologous PCA using anti-egg albumin mouse serum dilutions (1:100, 1:250, 1:500 and 1:750), it inhibited the 1:750 serum reaction 42.6%, but the inhibition rates for the other dilutions were 12-20%. Thus, based on the results of testing AA and BB, compounds isolated from P. japonicum THUNB. and P. praeruptorium DUNN. were confirmed to possess a spasmolytic effect on different types of smooth muscle and a mild antiallergic effect. These findings are of interest in regard to the medical uses of P. japonicum THUNB. and P. praeruptorium DUNN. as a herbal drug for bronchial asthma, spasmolytic effect, etc.
从日本前胡（Peucedanum japonicum THUNB.）和白花前胡（Peucedanum praeruptorium DUNN.）中分离得到的化合物AA和BB的解痉和抗过敏作用，在离体平滑肌和大鼠被动皮肤过敏反应（PCA）实验中进行了研究。AA和BB对豚鼠离体回肠中乙酰胆碱和组胺诱导的收缩呈现非竞争性拮抗作用。在豚鼠离体回肠中，AA和BB在10⁻⁶ g/ml时均使Ca²⁺剂量-反应曲线轻度右移，浓度高达3×10⁻⁶ g/ml时呈现非竞争性拮抗作用。AA和BB能使回肠中Ba²⁺（3×10⁻⁴ g/ml）诱导的收缩以及气管中组胺（10⁻³ g/ml）诱导的收缩呈浓度依赖性松弛。在皮下注射雌二醇24 - 48小时后的雌性大鼠切除子宫中，AA和BB对5-羟色胺诱导的收缩呈现非竞争性拮抗作用。但是，AA和BB对肾上腺素（3×10⁻⁶ g/ml）诱导的兔胸主动脉收缩几乎没有抑制作用。当用抗卵清蛋白小鼠血清稀释液（1:100、1:250、1:500和1:750）在大鼠同源PCA实验中测试口服40 mg/kg剂量BB的效果时，它对1:750血清反应的抑制率为42.6%，但对其他稀释液的抑制率为12 - 20%。因此，基于对AA和BB的测试结果，证实从日本前胡和白花前胡中分离得到的化合物对不同类型的平滑肌具有解痉作用，并具有轻度抗过敏作用。这些发现对于日本前胡和白花前胡作为治疗支气管哮喘等疾病的草药的医学用途具有重要意义。
