Analgesic potential of marrubiin derivatives, a bioactive diterpene present in Marrubium vulgare (Lamiaceae)

C. Meyre-Silva , R.A. Yunes , V. Schlemper , F. Campos-Buzzi , V. Cechinel-Filho
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引用次数: 90

Abstract

Marrubiin, a furane labdane diterpene, is the main analgesic compound present in Marrubium vulgare, a medicinal plant used in Brazil and other countries to treat several ailments. Considering its important pharmacological action, as well as its high yield, some structural modifications were performed in order to obtain more active compounds. Success was obtained in reducing the lactonic function, in the formation of marrubiinic acid and two esterified derivatives, which exhibited significant analgesic effect against the writhing test in mice. Marrubiinic acid showed better activity and excellent yield, and its analgesic effect was confirmed in other experimental models of pain in mice, suggesting its possible use as a model to obtain new and potent analgesic agents.

马芦比素衍生物的镇痛潜力——马芦比素是马芦比科一种生物活性二萜
Marrubiin是一种呋喃二萜,是存在于Marrubium vulgare中的主要镇痛化合物,Marrubium vulgare是巴西和其他国家用于治疗几种疾病的药用植物。考虑到其重要的药理作用和较高的产率,为了获得更有效的化合物,对其进行了一些结构修饰。成功地降低了内压功能,形成了马芦比酸和两种酯化衍生物,在小鼠扭体实验中表现出明显的镇痛作用。马鲁比酸表现出较好的活性和优良的产率,其镇痛作用在其他小鼠疼痛实验模型中得到证实,提示其有可能作为获得新型强效镇痛药的模型。
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