Department of Biological and Biomedical Sciences, Aga Khan University Medical College, Karachi, Pakistan.
Pharm Biol. 2011 Aug;49(8):821-5. doi: 10.3109/13880209.2010.550056. Epub 2011 Apr 18.
The present study describes the spasmogenic and spasmolytic activities of Daphne oleoides Schreb. (Thymelaeaceae), exploring the possible underlying pharmacological mechanisms.
Pharmacological investigation of Daphne oleoides to provide evidence for its therapeutic application in gastrointestinal motility disorders.
Methanol crude extract of Daphne oleoides (Do.Cr) was studied in gastrointestinal isolated tissues.
In spontaneously contracting rabbit jejunum preparations, Do.Cr at 0.3-3.0 mg/mL caused moderate stimulation, followed by relaxant effect at the next higher concentrations (5.0-10 mg/mL). In presence of atropine, spasmogenic effect was blocked and the relaxation was emerged, suggesting that the spasmogenic effect of Daphne oleoides is mediated through activation of muscarinic receptors. When tested against the high K+ (80 mM)-induced contractions, Do.Cr (0.3-5.0 mg/mL), like verapamil, inhibited the induced contractions, suggesting Ca++ channel blockade (CCB) effect. The CCB effect was further confirmed when pre-treatment of the tissue with Do.Cr shifted the Ca++ concentration-response curves to the right, similar to that caused by verapamil.
These results indicate that Daphne oleoides exhibits gut excitatory and inhibitory effects, occurred via cholinergic and Ca++ antagonistic pathways, respectively.
本研究描述了瑞香科瑞香属植物（Daphne oleoides Schreb.）的痉挛和松弛活性，探索了其潜在的药理学机制。
对 Daphne oleoides 进行药理学研究，为其在胃肠道动力障碍治疗中的应用提供依据。
研究了 Daphne oleoides 的甲醇粗提物（Do.Cr）对胃肠道分离组织的作用。
在自发收缩的兔空肠标本中，Do.Cr 在 0.3-3.0 mg/mL 浓度下引起中度刺激，随后在更高浓度（5.0-10 mg/mL）下产生松弛作用。在阿托品存在的情况下，痉挛作用被阻断，出现松弛作用，表明 Daphne oleoides 的痉挛作用是通过激活毒蕈碱受体介导的。当测试 Do.Cr 对高钾（80 mM）诱导的收缩作用时，Do.Cr（0.3-5.0 mg/mL）与维拉帕米一样，抑制诱导的收缩，表明存在钙通道阻断（CCB）作用。Do.Cr 预处理组织可使钙浓度-反应曲线右移，与维拉帕米引起的变化相似，进一步证实了 CCB 作用。
这些结果表明，Daphne oleoides 表现出肠道兴奋和抑制作用，分别通过胆碱能和钙拮抗途径发生。
