Al-Abdely H M, Graybill J R, Bocanegra R, Najvar L, Montalbo E, Regen S L, Melby P C
Division of Infectious Diseases, Department of Medicine, The University of Texas Health Science Center at San Antonio, San Antonio, Texas 78284, USA.
Antimicrob Agents Chemother. 1998 Oct;42(10):2542-8. doi: 10.1128/AAC.42.10.2542.
Current therapy for leishmaniasis is unsatisfactory because parenteral antimonial salts and pentamidine are associated with significant toxicity and failure rates. We examined the efficacy of KY62, a new, water-soluble, polyene antifungal, against cutaneous infection with Leishmania amazonensis and against visceral infection with Leishmania donovani in susceptible BALB/c mice. Mice were infected with L. amazonensis promastigotes in the ear pinna and in the tail and were treated with KY62 or amphotericin B. The cutaneous lesions showed a remarkable response to therapy with KY62 at a dose of 30 mg per kg of body weight per day. At this dose, the efficacy of KY62 was equivalent to or better than that of amphotericin B at 1 to 5 mg/kg/day. Mice infected intravenously with 10(7) L. donovani promastigotes and treated with KY62 showed a 4-log reduction in the parasite burden in the liver and spleen compared to untreated mice. These studies indicate potent activity of KY62 against experimental cutaneous leishmaniasis caused by L. amazoniensis and against experimental visceral leishmaniasis caused by L. donovani.
目前用于治疗利什曼病的疗法并不令人满意,因为肠胃外使用的锑盐和喷他脒具有显著的毒性且存在失败率。我们研究了一种新型水溶性多烯抗真菌药KY62对易感的BALB/c小鼠皮肤感染亚马逊利什曼原虫以及内脏感染杜氏利什曼原虫的疗效。小鼠在耳廓和尾巴处感染亚马逊利什曼原虫前鞭毛体,并用KY62或两性霉素B进行治疗。皮肤病变对每天每千克体重30毫克剂量的KY62治疗表现出显著反应。在此剂量下,KY62的疗效等同于或优于每天1至5毫克/千克的两性霉素B。静脉注射10(7)个杜氏利什曼原虫前鞭毛体并接受KY62治疗的小鼠,与未治疗的小鼠相比,其肝脏和脾脏中的寄生虫负荷降低了4个对数级。这些研究表明KY62对由亚马逊利什曼原虫引起的实验性皮肤利什曼病以及由杜氏利什曼原虫引起的实验性内脏利什曼病具有强大的活性。