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首页> 美国卫生研究院文献>Antimicrobial Agents and Chemotherapy >Efficacy of Orally Administered 2-Substituted Quinolines in Experimental Murine Cutaneous and Visceral Leishmaniases
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Efficacy of Orally Administered 2-Substituted Quinolines in Experimental Murine Cutaneous and Visceral Leishmaniases

机译：口服给药的2-取代喹啉在实验性小鼠皮肤和内脏利什曼病中的功效

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We report in this study the in vivo efficacy of nine 2-substituted quinolines on the Leishmania amazonensis cutaneous infection murine model and on the Leishmania infantum and Leishmania donovani visceral infection murine models. In the case of the L. amazonensis model, quinolines were administered orally at 25 mg/kg twice daily for 15 days. Quinolines 1, 2, 3, and 7 reduced by 80 to 90% the parasite burdens in the lesion, whereas N-methylglucamine antimoniate (Glucantime), administered by subcutaneous injections at 100 mg [28 mg Sb(V)] per kg of body weight daily, reduced the parasite burdens by 98%. In visceral leishmaniasis due to L. infantum, mice treated orally at 25 mg/kg daily for 10 days with quinolines 1, 4, 5, and 6 showed a significant reduction of parasite burdens in the liver and spleen. These quinolines were significantly more effective than meglumine antimoniate to reduce the parasite burden in both the liver and spleen. Also, the oral in vivo activity of three quinolines (quinolines 4, 5, and 2-n-propylquinoline) were determined against L. donovani (LV 9) at 12.5 and 25 mg/kg for 10 days. Their activity was compared with that of miltefosine at 7.5 mg/kg. Miltefosine, 2-n-propylquinoline, and quinoline 5 at 12.5 mg/kg significantly reduced the parasite burdens in the liver by 72, 66, and 61%, respectively. From the present study, quinoline 5 is the most promising compound against both cutaneous and visceral leishmaniasis. The double antileishmanial and antiviral activities of these compounds suggest that this series could be a potential treatment for coinfection of Leishmania-human immunodeficiency virus.
机译：我们在这项研究中报告了九个2-取代喹啉在亚马逊利什曼原虫皮肤感染鼠模型以及婴儿利什曼原虫和多形利什曼原虫内脏感染鼠模型中的体内疗效。在亚马逊乳杆菌模型的情况下，喹啉以25 mg / kg的剂量每天口服两次，持续15天。喹啉1、2、3和7将病灶中的寄生虫负担减少了80％至90％，而N-甲基葡萄糖胺锑酸盐（Glucantime）通过皮下注射每公斤体重100 mg [28 mg Sb（V）]每天的体重减少了98％的寄生虫负担。在由于范氏乳杆菌引起的内脏利什曼病中，每天口服25 mg / kg喹啉1、4、5和6处理10天的小鼠，肝脏和脾脏的寄生虫负担显着降低。这些喹啉在减轻肝脏和脾脏寄生虫负担方面比葡甲胺锑酸盐明显更有效。另外，测定了三种喹啉（喹啉4、5和2-正丙基喹啉）在12.5和25 mg / kg下对多诺氏乳杆菌（LV 9）的口服体内活性，持续10天。将其活性与7.5 mg / kg的米替福辛进行了比较。浓度为12.5 mg / kg的Miltefosine，2-n-丙基喹啉和quinoline 5分别将肝脏中的寄生虫负担降低了72％，66％和61％。从目前的研究来看，喹啉5是对抗皮肤和内脏利什曼病的最有希望的化合物。这些化合物具有双重抗疟疾和抗病毒活性，表明该系列药物可能是利什曼原虫-人类免疫缺陷病毒合并感染的潜在治疗方法。

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