Warsaw University of Life Sciences, Faculty of Veterinary Medicine, Department of Preclinical Sciences, Division of Pharmacology and Toxicology, 8 Ciszewskiego Street, 02-786 Warsaw, Poland.
J Ethnopharmacol. 2013 Mar 7;146(1):423-6. doi: 10.1016/j.jep.2012.12.023. Epub 2012 Dec 26.
The dry extract of Hedera helix leaves, due to its secretolytic and antispasmodic effects, is commonly used to produce pharmaceuticals applied in case of cough and other respiratory symptoms. The results of some in vitro studies as well as the clinical signs of poisoning caused by Hedera helix suggest however strong contractile effect on smooth muscle. In order to clarify the impact of α-hederin (the main active agent of ivy extract) on smooth muscle, the origin of activated calcium involved in α-hederin-induced contraction of gastric smooth muscle preparations was studied.
The study was carried out on rat isolated stomach corpus and fundus strips, under isotonic conditions. The effect of α-hederin (100 μM) on smooth muscle preparations was measured before and after the treatment with verapamil during the incubation in modified Krebs-Henseleit solution (M K-HS). Besides, the effect of saponin was measured during the incubation of preparation in Ca2+-free modified Krebs-Henseleit solution or Ca2+-free EGTA-containing modified Krebs-Henseleit solution.
The obtained results revealed that the application of verapamil significantly inhibited the reaction evoked by α-hederin. The incubation of stomach strips in calcium-free modified Krebs-Henseleit solution did not change the force of the observed contraction in comparison to the reaction of the preparations incubated in regular incubation solution (M K-HS). In contrary, the replacement of M K-HS by calcium-free chelator-containing solution inhibited totally the reaction to α-hederin.
The results indicated that α-hederin-induced contraction results from the influx of calcium which is located in intercellular spaces or bound to the outside of the cell membrane. The Ca2+ influx occurs predominantly through voltage-dependent calcium channels of L-type.
由于具有化痰和平喘作用,常春藤干叶提取物被用于生产治疗咳嗽和其他呼吸道症状的药物。然而,一些体外研究结果以及常春藤中毒的临床迹象表明,常春藤对平滑肌有很强的收缩作用。为了阐明α-常春藤苷(常春藤提取物的主要活性成分)对平滑肌的影响,研究了参与α-常春藤苷诱导胃平滑肌收缩的激活钙的来源。
在等张条件下,对大鼠分离的胃体和胃底条带进行研究。在改良 Krebs-Henseleit 溶液(M K-HS)孵育过程中,用维拉帕米处理后,测量 100 μM α-常春藤苷对平滑肌制剂的作用。此外,在无钙改良 Krebs-Henseleit 溶液或无钙含 EGTA 的改良 Krebs-Henseleit 溶液孵育过程中,测量皂素的作用。
研究结果表明,维拉帕米的应用显著抑制了由α-常春藤苷引起的反应。与在常规孵育溶液(M K-HS)中孵育的制剂的反应相比,在无钙改良 Krebs-Henseleit 溶液中孵育胃条带并没有改变观察到的收缩力。相反,用不含钙的螯合剂溶液代替 M K-HS 完全抑制了对α-常春藤苷的反应。
结果表明,α-常春藤苷诱导的收缩是由位于细胞间隙或与细胞膜外结合的钙内流引起的。钙内流主要通过 L 型电压依赖性钙通道发生。