Antileishmanial activity of 3,4,5-trisubstituted isoxazoles by interaction with Leishmania amazonensis plasma membrane

2022 ◽  
Vol 1249 ◽  
pp. 131604
Author(s):  
Lais Alonso ◽  
Karlos Eduardo Pianoski ◽  
Antonio Alonso ◽  
Fernanda Andreia Rosa
Keyword(s):  
Plasma Membrane ◽  
Leishmania Amazonensis ◽  
Antileishmanial Activity

scholarly journals Tamoxifen alters cell membrane properties in Leishmania amazonensis promastigotes

2018 ◽  
Vol 4 ◽  
Author(s):  
Juliana Q. Reimão ◽  
Silvia R. B. Uliana
Keyword(s):  
Plasma Membrane ◽  
Membrane Potential ◽  
Oestrogen Receptor ◽  
Morphological Analysis ◽  
Experimental Models ◽  
Leishmania Amazonensis ◽  
Antileishmanial Activity ◽  
Membrane Properties ◽  
Membrane Disruption ◽  
Receptor Modulator

Abstract The treatment of leishmaniasis relies primarily on highly toxic, parenterally administered drugs. Therefore, the search for more effective and safer drugs is considered a priority for leishmaniasis’ control. The antileishmanial activity of the oestrogen receptor modulator tamoxifen was previously described in experimental models of leishmaniasis. However, the mechanisms responsible for the antileishmanial activity of tamoxifen remain unknown. Since tamoxifen has been shown to affect plasma and intracellular membranes in tumour cells, the aim of this study was to investigate the activity of the drug on Leishmania amazonensis membranes. Through morphological analysis and labelling with propidium iodide and DiSBAC2(3), we demonstrated that tamoxifen led to plasma membrane depolarization without general membrane disruption or permeabilization. Tamoxifen also caused mitochondrial damage, with loss of membrane potential, as shown by Rhodamine 123 accumulation. Mitochondrial swelling followed, signalling the mitochondrial dysfunction. Therefore, the effect of tamoxifen on Leishmania is mediated, at least in part, by disorder in parasite's membranes. These alterations are sufficient to trigger a series of lethal events.

Selective in vitro antileishmanial activity of Mimosa caesalpiniifolia stem barks and its main constituent betulinic acid against Leishmania amazonensis

2021 ◽  
Vol 140 ◽  
pp. 68-75
Author(s):  
Lucas Moreira Brito ◽  
Michel Muálem de Moraes Alves ◽  
Adriana Cunha Souza ◽  
Thaynara Parente de Carvalho ◽  
José Henrique Furtado Campos ◽  
...  
Keyword(s):  
Betulinic Acid ◽  
Leishmania Amazonensis ◽  
Antileishmanial Activity ◽  
Main Constituent

scholarly journals Antileishmanial activity and mechanism of action from a purified fraction of Zingiber officinalis Roscoe against Leishmania amazonensis

2016 ◽  
Vol 166 ◽  
pp. 21-28 ◽  
Author(s):  
Mariana C. Duarte ◽  
Grasiele S.V. Tavares ◽  
Diogo G. Valadares ◽  
Daniela P. Lage ◽  
Tatiana G. Ribeiro ◽  
...  
Keyword(s):  
Mechanism Of Action ◽  
Leishmania Amazonensis ◽  
Antileishmanial Activity

scholarly journals In vitro antileishmanial activity of Anacardium othonianum and isolated compounds against Leishmania amazonensis

2021 ◽  
Vol 5 (1) ◽  
pp. 44
Author(s):  
Tavane Aparecida Alvarenga ◽  
Osvaine Júnior Alvarenga Alves ◽  
Mariana Cintra Pagotti ◽  
Wilson Roberto Cunha ◽  
Márcio Luís Andrade e Silva ◽  
...  
Keyword(s):  
High Resolution Mass Spectrometry ◽  
Leishmania Amazonensis ◽  
Antileishmanial Activity ◽  
Anacardic Acid ◽  
Array Detector ◽  
Preparative Hplc ◽  
Moderate Activity ◽  
Phytochemical Study ◽  
Phenol Derivatives

This study analyzes the antileishmanial activity of the crude ethanol extract, fractions, and isolated compounds of A. othonianum nuts. Antileishmanial activity was evaluated against Leishmania amazonensis promastigotes in vitro. The phytochemical study was performed by high-performance liquid chromatography-high-resolution mass spectrometry-diode array detector (HPLC-HRMS-DAD) and by preparative HPLC. HPLC-HRMS-DAD analysis of the bioactive extract confirmed the presence of ten alkyl phenol derivatives that had previously been isolated from A. occidentale. Bioassay-guided isolation afforded cardanol triene, cardanol diene, cardanol monoene, cardol triene, anacardic acid triene, anacardic acid diene, and anacardic acid monoene. Cardol triene gave an IC50 of 80.66 µM. The obtained data suggest that the evaluated extract, fractions, and cardol triene had moderate activity against L. amazonensis promastigotes. This is the first description of alkyl phenols in A. othonianum.

Antileishmanial activity of verbascoside: Selective arginase inhibition of intracellular amastigotes of Leishmania (Leishmania) amazonensis with resistance induced by LPS plus IFN-γ

2017 ◽  
Vol 127 ◽  
pp. 28-33 ◽  
Author(s):  
Claudia do Carmo Maquiaveli ◽  
Arina Lázaro Rochetti ◽  
Heidge Fukumasu ◽  
Paulo Cezar Vieira ◽  
Edson Roberto da Silva
Keyword(s):  
Leishmania Amazonensis ◽  
Antileishmanial Activity ◽  
Intracellular Amastigotes ◽  
Ifn Γ

scholarly journals Antileishmanial activity of Melampodium divaricatum and Casearia sylvestris essential oils on Leishmania amazonensis

2019 ◽  
Vol 61 ◽  
Author(s):  
Raquel Regina Duarte Moreira ◽  
André Gonzaga dos Santos ◽  
Flavio Alexandre Carvalho ◽  
Caio Humberto Perego ◽  
Eduardo José Crevelin ◽  
...  
Keyword(s):  
Essential Oils ◽  
Leishmania Amazonensis ◽  
Antileishmanial Activity ◽  
Casearia Sylvestris

scholarly journals Acyclic Sesquiterpenes from the Fruit Pericarp of Sapindus saponaria Induce Ultrastructural Alterations and Cell Death in Leishmania amazonensis

2017 ◽  
Vol 2017 ◽  
pp. 1-11 ◽  
Author(s):  
Amanda Louzano Moreira ◽  
Débora Botura Scariot ◽  
Bruna Luíza Pelegrini ◽  
Greisiele Lorena Pessini ◽  
Tânia Ueda-Nakamura ◽  
...  
Keyword(s):  
Electron Microscopy ◽  
Flow Cytometry ◽  
Hemolytic Activity ◽  
Solid Phase ◽  
Reversed Phase ◽  
Leishmania Amazonensis ◽  
Antileishmanial Activity ◽  
Ultrastructural Changes ◽  
Phosphatidylserine Exposure ◽  
Sapindus Saponaria

Previous studies reported antiprotozoal activities of Sapindus saponaria L. The aim of this work was the evaluation of antileishmanial activity and mechanism of action of extract and fractions of S. saponaria L. Hydroethanolic extract (EHA) obtained from fruit pericarps was fractionated using solid-phase extraction in a reversed phase, resulting in fractions enriched with saponins (SAP fraction) and acyclic sesquiterpene oligoglycosides (OGSA fraction). The activities of EHA, SAP, and OGSA were evaluated by antiproliferative assays with promastigote and intracellular amastigote forms. Cytotoxicity on macrophages and hemolytic activity were also analyzed. Morphological and ultrastructural changes in Leishmania amazonensis promastigotes were evaluated by electron microscopy. Flow cytometry was used to investigate mitochondrial dysfunction and phosphatidylserine exposure. OGSA was more selective for parasites than mammalian J774A1 macrophage cells, with selectivity indices of 3.79 and 7.35, respectively. Our results showed that only the OGSA fraction did not present hemolytic activity at its IC50 for promastigote growth. Electron microscopy revealed changes in parasite flagellum, cell body shape, and organelle size, mainly mitochondria. Flow cytometry analysis indicated mitochondrial membrane and cell membrane dysfunction. OGSA showed antileishmanial activity, resulting in several changes to protozoa cells, including mitochondrial depolarization and early phosphatidylserine exposure, suggesting a possible apoptotic induction.

Screening of selected essential oils for their in vitro antileishmanial activity against Leishmania amazonensis

Planta Medica ◽  
2010 ◽  
Vol 76 (12) ◽  
Author(s):  
A Crotti ◽  
F Dos Santos ◽  
L Magalhães ◽  
K Wakabayashi ◽  
G Aguiar ◽  
...  
Keyword(s):  
Essential Oils ◽  
Leishmania Amazonensis ◽  
Antileishmanial Activity

scholarly journals Effect of DODAB Nano-Sized Cationic Bilayer Fragments against Leishmania amazonensis

Molecules ◽  
2020 ◽  
Vol 25 (23) ◽  
pp. 5741
Author(s):  
Thalita C. S. Ferreira ◽  
Ismael P. Sauter ◽  
Lina Borda-Samper ◽  
Enyd Bentivoglio ◽  
Jarina P. DaMata ◽  
...  
Keyword(s):  
Zeta Potential ◽  
Control Strategies ◽  
Cationic Lipid ◽  
Leishmania Amazonensis ◽  
Antileishmanial Activity ◽  
Plasma Membrane Permeability ◽  
Life Cycle Stages ◽  
Bacteria And Fungi ◽  
Reported Data ◽  
Median Effective Concentration

The dioctadecyldimethylammonium bromide (DODAB) is a double-chained cationic lipid with potent bactericide and fungistatic activities; however, its toxicity on protozoan parasites is still unknown. Here, we show the antileishmanial activity of DODAB nano-sized cationic bilayer fragments on stationary-phase promastigotes and amastigotes of Leishmania amazonensis, the causative agent of cutaneous leishmaniasis. Upon treatment with DODAB, we analyzed the parasite surface zeta-potential, parasite viability, cellular structural modifications, and intracellular proliferation. The DODAB cytotoxic effect was dose-dependent, with a median effective concentration (EC50) of 25 µM for both life-cycle stages, comparable to the reported data for bacteria and fungi. The treatment with DODAB changed the membrane zeta-potential from negative to positive, compromised the parasite’s morphology, affected the cell size regulation, caused a loss of intracellular organelles, and probably dysregulated the plasma membrane permeability without membrane disruption. Moreover, the parasites that survived after treatment induced small parasitophorous vacuoles and failed to proliferate inside macrophages. In conclusion, DODAB displayed antileishmanial activity, and it remains to be elucidated how DODAB acts on the protozoan membrane. Understanding this mechanism can provide insights into the development of new parasite-control strategies.

scholarly journals Leishmania amazonensis hijacks host cell lysosomes involved in plasma membrane repair to induce invasion in fibroblasts

2019 ◽  
Vol 132 (6) ◽  
pp. jcs226183 ◽  
Author(s):  
Victor Soares Cavalcante-Costa ◽  
Mariana Costa-Reginaldo ◽  
Thamires Queiroz-Oliveira ◽  
Anny C. S. Oliveira ◽  
Natália Fernanda Couto ◽  
...  
Keyword(s):  
Plasma Membrane ◽  
Host Cell ◽  
Leishmania Amazonensis ◽  
Membrane Repair ◽  
Plasma Membrane Repair
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