| Literature DB >> 27623316 |
Gaurav Gupta1,2, Kevin J Peine3,4, Dalia Abdelhamid5,6, Heidi Snider1, Andrew B Shelton7, Latha Rao7, Sainath R Kotha7, Andrew C Huntsman5, Sanjay Varikuti1, Steve Oghumu1, C Benjamin Naman5, Li Pan5, Narasimham L Parinandi7, Tracy L Papenfuss8,9, A Douglas Kinghorn5, Eric M Bachelder10,4, Kristy M Ainslie10,4, James R Fuchs5, Abhay R Satoskar1.
Abstract
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.Entities:
Keywords: antileishmanial; liposome; novel sterol synthesis; visceral leishmaniasis
Year: 2015 PMID: 27623316 PMCID: PMC5730984 DOI: 10.1021/acsinfecdis.5b00081
Source DB: PubMed Journal: ACS Infect Dis ISSN: 2373-8227 Impact factor: 5.084