Gupta Gaurav, Peine Kevin J, Abdelhamid Dalia, Snider Heidi, Shelton Andrew B, Rao Latha, Kotha Sainath R, Huntsman Andrew C, Varikuti Sanjay, Oghumu Steve, Naman C Benjamin, Pan Li, Parinandi Narasimham L, Papenfuss Tracy L, Kinghorn A Douglas, Bachelder Eric M, Ainslie Kristy M, Fuchs James R, Satoskar Abhay R
Department of Pathology, The Wexner Medical Center, The Ohio State University , 320 West 10th Avenue, Columbus, Ohio 43210, United States.
Department of Biochemistry and Immunology, School of Medicine of Ribeirão Preto, University of Sao Paulo , Av. Bandeirantes 3900, 14049-900 Ribeirão Preto, Brazil.
ACS Infect Dis. 2015 Oct 9;1(10):497-506. doi: 10.1021/acsinfecdis.5b00081. Epub 2015 Sep 21.
Visceral leishmaniasis (VL), caused by the protozoan parasite Leishmania donovani, is a global health problem affecting millions of people worldwide. Treatment of VL largely depends on therapeutic drugs such as pentavalent antimonials, amphotericin B, and others, which have major drawbacks due to drug resistance, toxicity, and high cost. In this study, for the first time, we have successfully demonstrated the synthesis and antileishmanial activity of the novel sterol pentalinonsterol (PEN), which occurs naturally in the root of a Mexican medicinal plant, Pentalinon andrieuxii. In the experimental BALB/c mouse model of VL induced by infection with L. donovani, intravenous treatment with liposome-encapsulated PEN (2.5 mg/kg) led to a significant reduction in parasite burden in the liver and spleen. Furthermore, infected mice treated with liposomal PEN showed a strong host-protective TH1 immune response characterized by IFN-γ production and formation of matured hepatic granulomas. These results indicate that PEN could be developed as a novel drug against VL.
内脏利什曼病(VL)由原生动物寄生虫杜氏利什曼原虫引起,是一个影响全球数百万人的全球性健康问题。VL的治疗很大程度上依赖于五价锑剂、两性霉素B等治疗药物,但由于耐药性、毒性和高成本,这些药物存在主要缺点。在本研究中,我们首次成功证明了新型甾醇喷他诺甾醇(PEN)的合成及其抗利什曼活性,该甾醇天然存在于墨西哥药用植物安氏喷他诺(Pentalinon andrieuxii)的根部。在由杜氏利什曼原虫感染诱导的实验性BALB/c小鼠VL模型中,用脂质体包裹的PEN(2.5mg/kg)静脉治疗导致肝脏和脾脏中的寄生虫负荷显著降低。此外,用脂质体PEN治疗的感染小鼠表现出以产生IFN-γ和形成成熟肝肉芽肿为特征的强烈的宿主保护性TH1免疫反应。这些结果表明PEN可被开发为一种抗VL的新型药物。