Othman R, Ibrahim H, Mohd M A, Mustafa M R, Awang K
Department of Pharmacy, Faculty of Medicine, University of Malaya, 50603 Kuala Lumpur, Malaysia.
Phytomedicine. 2006 Jan;13(1-2):61-6. doi: 10.1016/j.phymed.2004.07.004. Epub 2005 Jun 27.
Bioassay-guided fractionation was performed on a crude dichloromethane extract of Kaempferia galanga L. using chromatography techniques. Screening of the extract for biological activity started with the brine shrimp lethality bioassay, followed by the study of its antihypertensive activity on anaesthetized rats, which involved monitoring of the extract's effect on mean arterial blood pressure. The components of the fractions obtained from the separation procedures were analyzed using gas chromatography (GC). The yield of the CH(2)Cl(2) extract was 0.29% of the crude plant extract. Analysis of the data for brine shrimp lethality test using the Finney computer program showed that this extract exhibited potent bioactivity with an ED(50) value of 7.92+/-0.13 microgml(-1). Intravenous administration of the extract induced a dose-related reduction of basal mean arterial pressure (MAP) (130+/-5 mmHg) in the anaesthetized rat, with maximal effects seen after 5-10 min of injection. The gas chromatogram showed that the common compound in the active fractions obtained from the bioassay-guided fractionation of the CH(2)Cl(2) extract was ethyl cinnamate. This vasorelaxant active compound, ethyl cinnamate, was isolated as a colorless oil. Ethyl p-methoxycinnamic acid was also isolated as white needles but did not exhibit any relaxant effect on the precontracted thoracic rat aorta.
采用色谱技术对山柰的二氯甲烷粗提物进行生物活性导向分离。提取物的生物活性筛选始于卤虫致死生物测定,随后研究其对麻醉大鼠的降压活性,这涉及监测提取物对平均动脉血压的影响。使用气相色谱(GC)分析分离过程中得到的各馏分的成分。二氯甲烷提取物的得率为粗植物提取物的0.29%。使用芬尼计算机程序分析卤虫致死试验数据表明,该提取物表现出强大的生物活性,半数致死剂量(ED50)值为7.92±0.13μg/ml(-1)。静脉注射该提取物可使麻醉大鼠的基础平均动脉压(MAP)(130±5 mmHg)呈剂量依赖性降低,注射后5 - 10分钟出现最大效应。气相色谱图显示,从二氯甲烷提取物的生物活性导向分离中获得的活性馏分中的常见化合物为肉桂酸乙酯。这种血管舒张活性化合物肉桂酸乙酯被分离为无色油状物。对甲氧基肉桂酸乙酯也被分离为白色针状物,但对预先收缩的大鼠胸主动脉未表现出任何舒张作用。