Abstract
Leishmaniasis is an overlooked tropical disease affecting approximately 1 million people in several countries. Clinical manifestation depends on the interaction between Leishmania and the host's immune response. Currently available treatment options for leishmaniasis are limited and induce severe side effects. In this research, we tested nitro-heterocyclic compounds (BSF series) as a new alternative against Leishmania. Its activity was measured in Leishmania (Leishmania) infantum promastigotes and intracellular amastigotes using MTT colorimetric assay. Additionally, we assessed the phosphatidylserine exposure by promastigotes, measured by flow cytometry, as well as nitric oxide production, measured by Griess' method. The nitro-heterocyclic compounds (BSF series) showed activity against L. (L.) infantum promastigotes, inducting the phosphatidylserine exposition by promastigotes, decreasing intracellular amastigotes and increasing oxide nitric production. The selectivity index was more prominent to Leishmania than to macrophages. Compared to amphotericin b, our compounds presented higher IC50, however the selectivity index was more specific to parasite than to amphotericin b. In conclusion, these nitro-heterocyclic compounds show...Continue Reading
References
Mar 15, 1989·European Journal of Biochemistry·M C Jockers-ScherüblR L Krauth-Siegel
Apr 20, 2002·Current Opinion in Infectious Diseases·J A Urbina
May 7, 2002·Memórias do Instituto Oswaldo Cruz·José Rodriques Coura, Solange L de Castro
Apr 24, 2003·Parasitology Research·R Luise Krauth-Siegel, Oliver Inhoff
Aug 24, 2004·The Journal of Biological Chemistry·Tim J VickersAlan H Fairlamb
Jan 20, 2005·Angewandte Chemie·R Luise Krauth-SiegelR Heiner Schirmer
Feb 14, 2006·Bioelectrochemistry·J ArgüelloJ A Squella
Feb 28, 2006·Brazilian Journal of Medical and Biological Research = Revista Brasileira De Pesquisas Médicas E Biológicas·P R T RomãoF Q Cunha
Mar 24, 2009·Bioorganic & Medicinal Chemistry·Fávero Reisdorfer PaulaLeoberto Costa Tavares
Apr 10, 2009·The Journal of Biological Chemistry·Manjusha M KulkarniBradford S McGwire
Nov 7, 2009·Revista Do Instituto De Medicina Tropical De São Paulo·José Angelo L Lindoso, Ana Angélica B P Lindoso
Feb 25, 2011·The Journal of Biological Chemistry·Belinda S HallShane R Wilkinson
May 4, 2011·Memórias do Instituto Oswaldo Cruz·Aretha Molina SesanaElenice Moreira Lemos
Feb 17, 2015·TheScientificWorldJournal·Shyam SundarMadhukar Rai
Feb 19, 2015·FASEB Journal : Official Publication of the Federation of American Societies for Experimental Biology·Ayan K GhoshPradeep Das
Mar 15, 2015·Journal of Natural Products·Fernanda Fonseca-SilvaElmo E Almeida-Amaral
Apr 4, 2015·PLoS Neglected Tropical Diseases·Emiliano LuceroKoert Ritmeijer
Apr 8, 2015·Chemical Biology & Drug Design·Edson R da SilvaTalita H da Costa
Apr 22, 2015·The American Journal of Tropical Medicine and Hygiene·Harparkash KaurSimon L Croft
Apr 29, 2015·Türkiye parazitolojii dergisi·Yavuz YeşilovaAhmet Özbilgin
May 6, 2015·Pharmacotherapy·Niyati H VakilPunit J Shah
Citations
May 28, 2019·The Journal of Venomous Animals and Toxins Including Tropical Diseases·Daiane Barros Dias MendonçaJose Angelo Lauletta Lindoso
Nov 4, 2020·Drug Development Research·Christina KannigaduDavid D N'Da
Jan 23, 2021·RSC Medicinal Chemistry·Sushobhan MukhopadhyaySanjay Batra