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新型大环内酯类抗生素麦迪霉素在小鼠和猴子体内的抗疟活性谱

Spectrum of the antimalarial activity of a new macrolide antibiotic midecamycin in mice and monkeys.

作者信息

Puri S K, Dutta G P

机构信息

Division of Microbiology, Central Drug Research Institute, Lucknow, India.

出版信息

Chemotherapy. 1989;35(3):187-92. doi: 10.1159/000238669.

DOI:10.1159/000238669
PMID:2766859
Abstract

The antimalarial activity of a new macrolide antibiotic, midecamycin, has been evaluated against a sensitive strain of Plasmodium berghei, a chloroquine-resistant strain of P. yoelii nigeriensis and a simian parasite, P. cynomolgi B. The ED50 and ED90 values of this antibiotic administered in two divided daily doses were found to be 37.15 +/- 3.51 and 100.84 +/- 7.54 mg/kg, respectively, against P. berghei and 362.34 +/- 85.33 and 878.04 +/- 10.02 mg/kg, respectively, against P. yoelii nigeriensis. Doses above 45 mg/kg for 4 days significantly extended the mean survival time of treated mice infected with either of the two parasites. However, no appreciable blood schizontocidal (at 100 mg/kg X 7 days), anti-relapse (at 100 mg/kg X 7 days) or causal prophylactic activities (at 200 mg/kg X 3 days) were observed against P. cynomolgi infection in rhesus monkeys.

摘要

一种新型大环内酯类抗生素麦迪霉素对伯氏疟原虫敏感株、约氏疟原虫尼日尔亚种氯喹耐药株以及猴疟原虫食蟹猴疟原虫B的抗疟活性进行了评估。该抗生素每日分两次给药,对伯氏疟原虫的半数有效剂量(ED50)和90%有效剂量(ED90)分别为37.15±3.51毫克/千克和100.84±7.54毫克/千克,对约氏疟原虫尼日尔亚种的ED50和ED90分别为362.34±85.33毫克/千克和878.04±10.02毫克/千克。45毫克/千克以上剂量连续给药4天可显著延长感染上述两种疟原虫之一的治疗小鼠的平均存活时间。然而,对于恒河猴感染食蟹猴疟原虫,未观察到明显的血内裂殖体杀灭作用(100毫克/千克×7天)、抗复发作用(100毫克/千克×7天)或病因性预防作用(200毫克/千克×3天)。

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