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柏子仁治疗胃肠和呼吸道机能亢奋症的药理学解释。

Pharmacological explanation for the medicinal use of Juniperus excelsa in hyperactive gastrointestinal and respiratory disorders.

机构信息

Natural Products Research Unit, Department of Biological and Biomedical Sciences, Aga Khan University Medical College, Karachi 74800, Pakistan.

出版信息

J Nat Med. 2012 Apr;66(2):292-301. doi: 10.1007/s11418-011-0605-z. Epub 2011 Dec 3.

Abstract

Crude extract of Juniperus excelsa (JeExt), which tested positive for the presence of anthraquinone, flavonoids, saponins, sterols, terpenes and tannin, exhibited a protective effect against castor oil-induced diarrhoea in mice at 100-1000 mg/kg. In rabbit jejunum preparations, JeExt (0.01-1.0 mg/mL) caused relaxation of spontaneous and K(+) (80 mM)-induced contractions at similar concentrations to papaverine, whereas verapamil was relatively more potent against K(+). JeExt (0.03-0.3 mg/mL) shifted Ca(2+) concentration-response curves to the right, like papaverine or verapamil. JeExt (0.003-0.01 mg/mL) caused a leftward shift of isoprenaline-induced inhibitory concentration-response curves, similar to papaverine. JeExt (1.0-30 mg/kg) caused suppression of carbachol (CCh, 100 μg/kg)-induced increase in inspiratory pressure of anaesthetized rats. In guinea-pig trachea, JeExt (0.001-3.0 mg/mL) relaxed CCh (1 μM)- and high K(+)-induced contractions and shifted isoprenaline-induced inhibitory curves to the left. This study suggests that Juniperus excelsa possibly exhibits a combination of Ca(2+) antagonist and phosphodiesterase inhibitory effects, which provides a pharmacological basis for its traditional use in disorders of gut and airways hyperactivity, such as diarrhoea, colic and asthma.

摘要

沙枣粗提物(JeExt)经检测含有蒽醌、类黄酮、皂苷、甾体、萜类化合物和单宁,在 100-1000mg/kg 剂量下对蓖麻油诱导的小鼠腹泻具有保护作用。在兔空肠制剂中,JeExt(0.01-1.0mg/mL)在与罂粟碱相似的浓度下引起自发性和 K+(80mM)诱导收缩的松弛,而维拉帕米对 K+的作用相对更强。JeExt(0.03-0.3mg/mL)使 Ca2+浓度-反应曲线右移,与罂粟碱或维拉帕米相似。JeExt(0.003-0.01mg/mL)引起异丙肾上腺素抑制性浓度-反应曲线向左移位,与罂粟碱相似。JeExt(1.0-30mg/kg)抑制麻醉大鼠的 carbachol(CCh,100μg/kg)诱导的吸气压力增加。在豚鼠气管中,JeExt(0.001-3.0mg/mL)松弛 CCh(1μM)和高 K+诱导的收缩,并使异丙肾上腺素诱导的抑制曲线向左移位。本研究表明,沙枣可能具有钙拮抗剂和磷酸二酯酶抑制作用的组合,为其在胃肠道和呼吸道过度活跃性紊乱(如腹泻、绞痛和哮喘)的传统用途提供了药理学基础。

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