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用香豆素(-)mammea A/BB 对感染利什曼原虫的感染小鼠的皮肤利什曼病病变进行肌内和局部治疗。

Intramuscular and topical treatment of cutaneous leishmaniasis lesions in mice infected with Leishmania amazonensis using coumarin (-) mammea A/BB.

机构信息

Programa de Pós-Graduação em Ciências Farmacêuticas, Universidade Estadual de Maringá, Maringá, Paraná, Brazil.

出版信息

Phytomedicine. 2012 Oct 15;19(13):1196-9. doi: 10.1016/j.phymed.2012.08.001. Epub 2012 Sep 4.

Abstract

Treatment of cutaneous leishmaniasis remains limited to a few available options. Recent studies showed in vitro antileishmanial activity of (-) mammea A/BB, a coumarin isolated from leaves of Calophyllum brasiliense. Moreover, the dichloromethane crude extract and hexane fraction from this plant demonstrated in vivo activity in mice infected with Leishmania amazonensis. We evaluated the antileishmanial activity of (-) mammea A/BB in the L. amazonensis BALB/c mice model. The animals were given intramuscular and topical treatment with (-) mammea A/BB for 30 consecutive days. The results demonstrated that 18mg/kg/d intramuscularly or 0.2% topically of (-) mammea A/BB significantly reduced the size of skin lesions in footpads of mice compared with those in the control group (p<0.05). The activity of Glucantime(®) (corresponding to 27mg/kg/d of pentavalent antimony) administered intramuscularly was similar to that of (-) mammea A/BB (p<0.05) by both routes of administration. The histopathological evaluation showed no changes in the organs analyzed. These results indicate that the coumarin obtained from C. brasiliense is the antileishmanially active compound and can be used to control the development of cutaneous leishmaniasis lesions caused by L. amazonensis.

摘要

皮肤利什曼病的治疗仍然局限于少数几种可用的选择。最近的研究表明,(-)mammea A/BB 对利什曼原虫具有体外抗利什曼原虫活性,(-)mammea A/BB 是从巴西厚壳桂的叶子中分离出来的一种香豆素。此外,这种植物的二氯甲烷粗提物和正己烷馏分在感染了莱什曼原虫亚马逊亚种的小鼠体内表现出活性。我们评估了(-)mammea A/BB 在 L. amazonensis BALB/c 小鼠模型中的抗利什曼原虫活性。动物接受肌肉内和局部注射(-)mammea A/BB 治疗,连续 30 天。结果表明,与对照组相比,肌肉内注射 18mg/kg/d 或局部应用 0.2%(-)mammea A/BB 显著减少了小鼠足垫皮肤损伤的大小(p<0.05)。肌肉内注射葡甲胺(®)(相当于 27mg/kg/d 的五价锑)的活性与(-)mammea A/BB 相似(p<0.05),两种给药途径均如此。组织病理学评估显示,所分析的器官没有变化。这些结果表明,从巴西厚壳桂中获得的香豆素是具有抗利什曼原虫活性的化合物,可用于控制由 L. amazonensis 引起的皮肤利什曼病病变的发展。

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