Freire S M, Torres L M, Souccar C, Lapa A J
Universidade Federal de São Paulo, Escola Paulista de Medicina, Department of Pharmacology, São Paulo, SP, Brazil.
J Pharm Pharmacol. 1996 Jun;48(6):624-8. doi: 10.1111/j.2042-7158.1996.tb05985.x.
The herb Scoparia dulcis L. is used in Brazilian folk medicine to treat bronchitis, gastric disorders, haemorrhoids, insect bites and skin wounds, and in oriental medicine to treat hypertension. A previous study has shown that extracts of S. dulcis have analgesic and anti-inflammatory properties; in this work the sympathomimetic activity of an ethanolic extract of Scoparia dulcis L. has been investigated in rodent preparations in-vivo and in-vitro. Administration of the extract (0.5-2 mg kg-1, i.v.) to anaesthetized rats produced dose-related hypertension blocked by the alpha-adrenoceptor antagonist prazosin (1 mg kg-1). Partition of the extract in chloroform-water yielded an aqueous phase 20 times more potent than the extract; this produced hypertension in either reserpine-treated or pithed rats. In untreated and reserpine-treated rats the same fraction (1-3 x 10(3) micrograms mL-1) produced concentration-dependent contractions of the vas deferens musculature parallel to those obtained with noradrenaline (10(-8)-10(-4)M). Prazosin (10(-7)M) reduced the maximum contractile effect of the aqueous fraction, and shifted the concentration-response curves for noradrenaline to the right. The aqueous fraction (25 and 50 micrograms mL-1) increased the inotropism of electrically driven left atria of rats, the effect being blocked by propranolol (0.4 microgram mL-1). In preparations of guinea-pig tracheal rings the aqueous fraction (1-3 x 10(3) micrograms mL-1) relaxed the muscle contraction induced by histamine (10(-4) M) in proportion to the concentration. The effect was antagonized competitively by propranolol (1.5 microM). High-performance liquid-chromatographic analysis of the aqueous fraction revealed the presence of both noradrenaline and adrenaline in the plant extract. The results indicated that both catecholamines may account for the hypertensive and inotropic effects obtained after parenteral administration of S. dulcis extracts. This sympathomimetic activity is, however, unrelated to the previously reported analgesic and anti-inflammatory properties of the plant extract, but may explain its effectiveness upon topical application in the healing of mucosal and skin wounds.
甜地丁草在巴西民间医学中用于治疗支气管炎、胃部疾病、痔疮、昆虫叮咬和皮肤伤口,在东方医学中用于治疗高血压。先前的一项研究表明,甜地丁草提取物具有镇痛和抗炎特性;在这项工作中,对甜地丁草乙醇提取物在啮齿动物体内和体外制剂中的拟交感神经活性进行了研究。给麻醉大鼠静脉注射提取物(0.5 - 2 mg kg-1)会产生剂量相关的高血压,该作用可被α-肾上腺素能受体拮抗剂哌唑嗪(1 mg kg-1)阻断。提取物在氯仿 - 水体系中的分配产生了一个水相,其效力比提取物高20倍;这在利血平处理的大鼠或去脑大鼠中都会引起高血压。在未处理和利血平处理的大鼠中,相同部分(1 - 3×10(3) μg mL-1)产生与去甲肾上腺素(10(-8) - 10(-4)M)平行的输精管肌肉组织浓度依赖性收缩。哌唑嗪(10(-7)M)降低了水相部分的最大收缩效应,并使去甲肾上腺素的浓度 - 反应曲线右移。水相部分(25和50 μg mL-1)增加了大鼠电驱动左心房的收缩力,该作用被普萘洛尔(0.4 μg mL-1)阻断。在豚鼠气管环制剂中,水相部分(1 - 3×10(3) μg mL-1)按浓度比例松弛组胺(10(-4) M)诱导的肌肉收缩。该作用被普萘洛尔(1.5 μM)竞争性拮抗。对水相部分的高效液相色谱分析表明植物提取物中同时存在去甲肾上腺素和肾上腺素。结果表明,这两种儿茶酚胺可能是甜地丁草提取物经肠胃外给药后产生高血压和正性肌力作用的原因。然而,这种拟交感神经活性与先前报道的植物提取物的镇痛和抗炎特性无关,但可能解释了其在局部应用于黏膜和皮肤伤口愈合时的有效性。