Sadraei H, Ghanadian M, Asghari G, Sharifian R
Department of Pharmacology and Toxicology, Isfahan Pharmaceutical Sciences Research Centre, School of Pharmacy and Pharmaceutical Sciences, Isfahan University of Medical Sciences, Isfahan, I.R. Iran.
Department of Pharmacognosy, Isfahan Pharmaceutical Sciences Research Centre, School of Pharmacy and Pharmaceutical Sciences, Isfahan University of Medical Sciences, Isfahan, I.R. Iran.
Res Pharm Sci. 2015 Jan-Feb;10(1):52-8.
Bioassay monitoring of hydroalcoholic extract from the aerial part of Pyconcycla spinosa revealed that it contains components with spasmolytic activity in vitro. In addition, P. spinosa extract at oral dose of 1-5 mg/kg inhibits diarrhoea in animal models. Pharmacological screening of pure compounds isolated from P. spinosa hydroalcoholic extract led to the identification of 3,7,10,14,15-pentaacetyl-5-butanoyl-13,17-epoxy-8-myrsinene (PABEM) which is a new diterpene. In this research, we have investigated antispasmodic and antidiarrheal effects of PABEM for comparison with P. spinosa extract. Aerial parts of P. spinosa were extracted with ethanol. For antispasmodic studies, rat isolated ileum was suspended in Tyrode's solution in an organ bath. The ileum was contracted by acetylcholine (ACh, 0.5 μM), serotonin (5-HT, 5 μM) or electrical field stimulation (EFS). P. spinosa extract in a concentration dependent manner (10-640 μg/ml) inhibited ileum contractions induced by ACh, 5-HT or EFS. The new compound isolated form P. spinosa extract "PABEM" in a similar manner inhibited the contractile response to ACh, 5-HT and EFS. However, the inhibitory effects of PABEM were observed at much lower bath concentrations. The relaxation effect of PABEM was started at 40 ng/ml bath concentration and with 2.5 μg/ml PABEM in the bath, the contractile responses of ileum were completely abolished. Both hydroalcoholic extract of P. spinosa and PABEM reduced intestinal meal transit and castor oil and MgSO4 induced diarrhoea in mice. However, PABEM was about 10 times more potent than its parent extract. This research shows that PABEM is probably the main component responsible for antispasmodic and antidiarrheal actions of P. spinosa extract.
对刺环菊地上部分水醇提取物的生物测定监测表明，其含有在体外具有解痉活性的成分。此外，刺环菊提取物以1 - 5毫克/千克的口服剂量可抑制动物模型中的腹泻。对从刺环菊水醇提取物中分离出的纯化合物进行药理筛选，鉴定出一种新的二萜类化合物3,7,10,14,15 - 五乙酰基 - 5 - 丁酰基 - 13,17 - 环氧 - 8 - 肉豆蔻烯（PABEM）。在本研究中，我们研究了PABEM的抗痉挛和止泻作用，以便与刺环菊提取物进行比较。刺环菊的地上部分用乙醇提取。在抗痉挛研究中，将大鼠离体回肠悬挂在器官浴中的台氏液中。回肠通过乙酰胆碱（ACh，0.5 μM）、5 - 羟色胺（5 - HT，5 μM）或电场刺激（EFS）收缩。刺环菊提取物以浓度依赖性方式（10 - 640微克/毫升）抑制由ACh、5 - HT或EFS诱导的回肠收缩。从刺环菊提取物中分离出的新化合物“PABEM”以类似方式抑制对ACh、5 - HT和EFS的收缩反应。然而，在低得多的浴液浓度下就观察到了PABEM的抑制作用。PABEM的松弛作用在浴液浓度为40纳克/毫升时开始，当浴液中含有2.5微克/毫升PABEM时，回肠的收缩反应完全被消除。刺环菊水醇提取物和PABEM均减少了小鼠的肠内容物转运以及蓖麻油和硫酸镁诱导的腹泻。然而，PABEM的效力约为其母提取物的10倍。这项研究表明，PABEM可能是刺环菊提取物抗痉挛和止泻作用的主要成分。
