Kohno H, Inoue H, Seyama Y, Yamashita S, Akasu M
Department of Clinical Chemistry, Hoshi College of Pharmacy, Tokyo, Japan.
Nihon Yakurigaku Zasshi. 1987 Oct;90(4):205-11. doi: 10.1254/fpj.90.205.
Cepharanthine, a biscouclaurine alkaloid of Stephania cepharantha, has been used for various clinical purposes. Cepharanthine was known to inhibit histamine release from mast cells obtained from sensitized animals. In vitro studies suggested that the mechanism of action of cepharanthine may be ascribed to the membrane stabilizing action. The membrane stabilization may be attained by reducing the elasticity of the membrane. However, in vivo mechanisms of the anti-allergic action of cepharanthine have not been examined. In the present in vivo study, the anti-allergic action of cepharanthine was examined using experimental allergic rhinitis in rats. The locally administered cepharanthine solution (0.1 mg/ml), by perfusing the nasal cavity, inhibited the dye leakage and an increase in lysosomal enzyme activity due to antigen stimulation. This is the reason for the membrane stabilization by cepharanthine. In the metyrapone (20 mg/kg, s.c., 5 days) pretreated rats of the rhinitis models, the anti-allergic action of cepharanthine was weaker. On the other hand, the effect of ketotifen was not altered by such an effect. The experimental results suggest that the anti-allergic mechanism of cepharanthine might be exerted by its membrane stabilizing action and by stimulation of the pituitary-adrenotropic function.
千金藤素是千金藤属植物头花千金藤中的一种双苄基异喹啉生物碱，已被用于多种临床用途。已知千金藤素能抑制从致敏动物获得的肥大细胞释放组胺。体外研究表明，千金藤素的作用机制可能归因于其膜稳定作用。膜稳定作用可能通过降低膜的弹性来实现。然而，千金藤素抗过敏作用的体内机制尚未得到研究。在本体内研究中，使用大鼠实验性变应性鼻炎来研究千金藤素的抗过敏作用。通过鼻腔灌注局部给予千金藤素溶液（0.1毫克/毫升），可抑制由于抗原刺激引起的染料渗漏和溶酶体酶活性增加。这就是千金藤素具有膜稳定作用的原因。在鼻炎模型的甲吡酮（20毫克/千克，皮下注射，5天）预处理大鼠中，千金藤素的抗过敏作用较弱。另一方面，酮替芬的作用不受这种影响的改变。实验结果表明，千金藤素的抗过敏机制可能是通过其膜稳定作用以及刺激垂体 - 肾上腺功能来发挥的。
