Effects of nitro-heterocyclic derivatives against Leishmania (Leishmania) infantum promastigotes and intracellular amastigotes. 2016

Simone Carolina Soares Petri e Silva, and Fanny Palace-Berl, and Leoberto Costa Tavares, and Sandra Regina Castro Soares, and José Angelo Lauletta Lindoso
Laboratório de Soroepidemiologia e Imunobiologia, do Instituto de Medicina Tropical da, Universidade de São Paulo, Brazil.

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 showed to be promising as an anti-Leishmania drug, in in vitro studies.

UI MeSH Term Description Entries
D007898 Leishmaniasis, Visceral A chronic disease caused by LEISHMANIA DONOVANI and transmitted by the bite of several sandflies of the genera Phlebotomus and Lutzomyia. It is commonly characterized by fever, chills, vomiting, anemia, hepatosplenomegaly, leukopenia, hypergammaglobulinemia, emaciation, and an earth-gray color of the skin. The disease is classified into three main types according to geographic distribution: Indian, Mediterranean (or infantile), and African. Black Fever,Kala-Azar,Fever, Black,Kala Azar,Visceral Leishmaniasis
D008264 Macrophages The relatively long-lived phagocytic cell of mammalian tissues that are derived from blood MONOCYTES. Main types are PERITONEAL MACROPHAGES; ALVEOLAR MACROPHAGES; HISTIOCYTES; KUPFFER CELLS of the liver; and OSTEOCLASTS. They may further differentiate within chronic inflammatory lesions to EPITHELIOID CELLS or may fuse to form FOREIGN BODY GIANT CELLS or LANGHANS GIANT CELLS. (from The Dictionary of Cell Biology, Lackie and Dow, 3rd ed.) Bone Marrow-Derived Macrophages,Monocyte-Derived Macrophages,Macrophage,Macrophages, Monocyte-Derived,Bone Marrow Derived Macrophages,Bone Marrow-Derived Macrophage,Macrophage, Bone Marrow-Derived,Macrophage, Monocyte-Derived,Macrophages, Bone Marrow-Derived,Macrophages, Monocyte Derived,Monocyte Derived Macrophages,Monocyte-Derived Macrophage
D009000 Monocytes Large, phagocytic mononuclear leukocytes produced in the vertebrate BONE MARROW and released into the BLOOD; contain a large, oval or somewhat indented nucleus surrounded by voluminous cytoplasm and numerous organelles. Monocyte
D009569 Nitric Oxide A free radical gas produced endogenously by a variety of mammalian cells, synthesized from ARGININE by NITRIC OXIDE SYNTHASE. Nitric oxide is one of the ENDOTHELIUM-DEPENDENT RELAXING FACTORS released by the vascular endothelium and mediates VASODILATION. It also inhibits platelet aggregation, induces disaggregation of aggregated platelets, and inhibits platelet adhesion to the vascular endothelium. Nitric oxide activates cytosolic GUANYLATE CYCLASE and thus elevates intracellular levels of CYCLIC GMP. Endogenous Nitrate Vasodilator,Mononitrogen Monoxide,Nitric Oxide, Endothelium-Derived,Nitrogen Monoxide,Endothelium-Derived Nitric Oxide,Monoxide, Mononitrogen,Monoxide, Nitrogen,Nitrate Vasodilator, Endogenous,Nitric Oxide, Endothelium Derived,Oxide, Nitric,Vasodilator, Endogenous Nitrate
D009574 Nitro Compounds Compounds having the nitro group, -NO2, attached to carbon. When attached to nitrogen they are nitramines and attached to oxygen they are NITRATES. Nitrated Compounds
D010718 Phosphatidylserines Derivatives of PHOSPHATIDIC ACIDS in which the phosphoric acid is bound in ester linkage to a SERINE moiety. Serine Phosphoglycerides,Phosphatidyl Serine,Phosphatidyl Serines,Phosphatidylserine,Phosphoglycerides, Serine,Serine, Phosphatidyl,Serines, Phosphatidyl
D002460 Cell Line Established cell cultures that have the potential to propagate indefinitely. Cell Lines,Line, Cell,Lines, Cell
D004305 Dose-Response Relationship, Drug The relationship between the dose of an administered drug and the response of the organism to the drug. Dose Response Relationship, Drug,Dose-Response Relationships, Drug,Drug Dose-Response Relationship,Drug Dose-Response Relationships,Relationship, Drug Dose-Response,Relationships, Drug Dose-Response
D005434 Flow Cytometry Technique using an instrument system for making, processing, and displaying one or more measurements on individual cells obtained from a cell suspension. Cells are usually stained with one or more fluorescent dyes specific to cell components of interest, e.g., DNA, and fluorescence of each cell is measured as it rapidly transverses the excitation beam (laser or mercury arc lamp). Fluorescence provides a quantitative measure of various biochemical and biophysical properties of the cell, as well as a basis for cell sorting. Other measurable optical parameters include light absorption and light scattering, the latter being applicable to the measurement of cell size, shape, density, granularity, and stain uptake. Cytofluorometry, Flow,Cytometry, Flow,Flow Microfluorimetry,Fluorescence-Activated Cell Sorting,Microfluorometry, Flow,Cell Sorting, Fluorescence-Activated,Cell Sortings, Fluorescence-Activated,Cytofluorometries, Flow,Cytometries, Flow,Flow Cytofluorometries,Flow Cytofluorometry,Flow Cytometries,Flow Microfluorometries,Flow Microfluorometry,Fluorescence Activated Cell Sorting,Fluorescence-Activated Cell Sortings,Microfluorimetry, Flow,Microfluorometries, Flow,Sorting, Fluorescence-Activated Cell,Sortings, Fluorescence-Activated Cell
D006571 Heterocyclic Compounds Cyclic compounds that include atoms other than carbon in their ring structure. Heterocyclic Compound,Compound, Heterocyclic,Compounds, Heterocyclic

Related Publications

Simone Carolina Soares Petri e Silva, and Fanny Palace-Berl, and Leoberto Costa Tavares, and Sandra Regina Castro Soares, and José Angelo Lauletta Lindoso
April 2017, Parasitology international,
Simone Carolina Soares Petri e Silva, and Fanny Palace-Berl, and Leoberto Costa Tavares, and Sandra Regina Castro Soares, and José Angelo Lauletta Lindoso
May 2005, International journal for parasitology,
Simone Carolina Soares Petri e Silva, and Fanny Palace-Berl, and Leoberto Costa Tavares, and Sandra Regina Castro Soares, and José Angelo Lauletta Lindoso
February 2005, International journal of antimicrobial agents,
Simone Carolina Soares Petri e Silva, and Fanny Palace-Berl, and Leoberto Costa Tavares, and Sandra Regina Castro Soares, and José Angelo Lauletta Lindoso
April 2013, European journal of medicinal chemistry,
Simone Carolina Soares Petri e Silva, and Fanny Palace-Berl, and Leoberto Costa Tavares, and Sandra Regina Castro Soares, and José Angelo Lauletta Lindoso
September 2017, Acta parasitologica,
Simone Carolina Soares Petri e Silva, and Fanny Palace-Berl, and Leoberto Costa Tavares, and Sandra Regina Castro Soares, and José Angelo Lauletta Lindoso
December 2012, Experimental parasitology,
Simone Carolina Soares Petri e Silva, and Fanny Palace-Berl, and Leoberto Costa Tavares, and Sandra Regina Castro Soares, and José Angelo Lauletta Lindoso
December 2015, The Journal of parasitology,
Simone Carolina Soares Petri e Silva, and Fanny Palace-Berl, and Leoberto Costa Tavares, and Sandra Regina Castro Soares, and José Angelo Lauletta Lindoso
May 2001, Acta tropica,
Simone Carolina Soares Petri e Silva, and Fanny Palace-Berl, and Leoberto Costa Tavares, and Sandra Regina Castro Soares, and José Angelo Lauletta Lindoso
August 2007, Planta medica,
Simone Carolina Soares Petri e Silva, and Fanny Palace-Berl, and Leoberto Costa Tavares, and Sandra Regina Castro Soares, and José Angelo Lauletta Lindoso
July 2011, The Journal of antibiotics,
Copied contents to your clipboard!