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甘草查尔酮A对感染硕大利什曼原虫的小鼠及感染杜氏利什曼原虫的仓鼠的抗利什曼原虫活性。

Antileishmanial activity of licochalcone A in mice infected with Leishmania major and in hamsters infected with Leishmania donovani.

作者信息

Chen M, Christensen S B, Theander T G, Kharazmi A

机构信息

Department of Clinical Microbiology, National University Hospital (Rigshospitalet), Copenhagen, Denmark.

出版信息

Antimicrob Agents Chemother. 1994 Jun;38(6):1339-44. doi: 10.1128/AAC.38.6.1339.

Abstract

This study was designed to examine the antileishmanial activity of the oxygenated chalcone licochalcone A in mice and hamsters infected with Leishmania parasites. Intraperitoneal administration of licochalcone A at doses of 2.5 and 5 mg/kg of body weight per day completely prevented lesion development in BALB/c mice infected with Leishmania major. Treatment of hamsters infected with L. donovani with intraperitoneal administration of licochalcone A at a dose of 20 mg/kg of body weight per day for 6 consecutive days resulted in a > 96% reduction of parasite load in the liver and the spleen compared with values for untreated control animals. The [3H]thymidine uptake by the parasites isolated from the treated hamsters was only about 1% of that observed in parasites isolated from the controls. Oral administration of licochalcone A at concentrations of 5 to 150 mg/kg of body weight per day for 6 consecutive days resulted in > 65 and 85% reductions of L. donovani parasite loads in the liver and the spleen, respectively, compared with those of untreated control hamsters. These data clearly demonstrate that licochalcone A is a promising lead for the development of a new drug against leishmaniases.

摘要

本研究旨在检测氧化查耳酮甘草查耳酮A对感染利什曼原虫的小鼠和仓鼠的抗利什曼活性。每天以2.5和5毫克/千克体重的剂量腹腔注射甘草查耳酮A,可完全防止感染硕大利什曼原虫的BALB/c小鼠出现病变。每天以20毫克/千克体重的剂量连续6天腹腔注射甘草查耳酮A,治疗感染杜氏利什曼原虫的仓鼠,与未治疗的对照动物相比,肝脏和脾脏中的寄生虫载量降低了> 96%。从治疗后的仓鼠中分离出的寄生虫对[3H]胸苷的摄取量仅为从对照中分离出的寄生虫的约1%。每天以5至150毫克/千克体重的浓度连续6天口服甘草查耳酮A,与未治疗的对照仓鼠相比,肝脏和脾脏中的杜氏利什曼原虫载量分别降低了> 65%和85%。这些数据清楚地表明,甘草查耳酮A是开发抗利什曼病新药的一个有前景的先导化合物。

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