A5059226120- Research on Leishmaniasis Studies
- Trypanosoma species research and implications
- Synthesis and Biological Evaluation
- Insect and Pesticide Research
- Parasites and Host Interactions
- Phytochemical compounds biological activities
- Venomous Animal Envenomation and Studies
- N-Heterocyclic Carbenes in Organic and Inorganic Chemistry
- Insect Pest Control Strategies
- Helminth infection and control
- Metal complexes synthesis and properties
- Insect symbiosis and bacterial influences
- Urticaria and Related Conditions
- Antimicrobial Peptides and Activities
- Click Chemistry and Applications
- Heme Oxygenase-1 and Carbon Monoxide
- Traditional and Medicinal Uses of Annonaceae
- Malaria Research and Control
- Synthesis and Characterization of Heterocyclic Compounds
- Toxin Mechanisms and Immunotoxins
- Synthesis and biological activity
- Microbial Natural Products and Biosynthesis
- HIV/AIDS drug development and treatment
- Pesticide Exposure and Toxicity
- Synthetic Organic Chemistry Methods
Universidade Estadual de Campinas (UNICAMP)
2016-2025
Universidad Tecnológica Indoamérica
2023
Fundação Oswaldo Cruz
2020
Universidad Católica Cecilio Acosta
2020
University of Wisconsin–Platteville
2020
Universidade de São Paulo
2007-2018
University of Maryland, College Park
2012-2017
Universidade Federal do Rio Grande do Sul
2010
Universidade Brasil
2010
This study was performed to investigate the activity of tamoxifen, an antioestrogen widely used in treatment breast cancer, against Leishmania. Drug assessed vitro axenically grown promastigotes and amastigotes through cell counting or by measuring cleavage MTT, intracellular treating infected macrophage cultures evaluating number parasites. Intravacuolar pH changes induced inside parasitophorous vacuoles Leishmania (Leishmania) amazonensis-infected macrophages were evaluated using...
Trypanosomatid protozoan parasites lack a functional heme biosynthetic pathway, so must acquire from the environment to survive. However, molecular pathway responsible for acquisition by these organisms is unknown. Here we show that L. amazonensis LHR1, homolog of C. elegans plasma membrane transporter HRG-4, functions in transport. Tagged LHR1 localized and endocytic compartments, both mammalian cells. Heme deprivation increased transcript levels, promoted uptake fluorescent analog ZnMP,...
Leishmania parasites infect macrophages, cells that play an important role in organismal iron homeostasis. By expressing ferroportin, a membrane protein specialized export, macrophages release stored intracellularly into the circulation. Iron is essential for intracellular replication of Leishmania, but how compete with export function their host cell unknown. Here, we show infection amazonensis inhibits ferroportin expression macrophages. In TLR4-dependent manner, infected upregulated...
Leishmaniasis chemotherapy remains very challenging. The high cost of active drugs, along with the severity their side effects and increasing failure rate current therapeutic schemes, calls for discovery new drugs schemes treatment. use combination therapy has gained much attention in recent years as a possible strategy overcoming various shortcomings present arsenal. We recently described effectiveness tamoxifen murine models leishmaniasis, here, we investigated interactions between...
The aim of this study was to evaluate the efficacy tamoxifen in vivo experimental models cutaneous (CL) and visceral leishmaniasis (VL) caused by Leishmania braziliensis chagasi, respectively.Drug activity assessed against intracellular amastigotes treating infected macrophage cultures evaluating number cells. In tested L. braziliensis-infected BALB/c mice chagasi-infected hamsters. Treatment with 20 mg/kg/day administered for 15 days intraperitoneal route. Efficacy evaluated through...
Resistance of Leishmania parasites to specific chemotherapy has become a well-documented problem in the Indian subcontinent recent years but only few studies have focused on susceptibility American isolates. Our assays meglumine antimoniate were performed against intracellular amastigotes after standardizing an vitro model macrophage infection appropriate for (Viannia) braziliensis For determination promastigote amphotericin B, we developed simplified MTT-test. The sensitivity and B 13...
Chemotherapy is still a critical issue in the management of leishmaniasis. Until recently, pentavalent antimonials, amphotericin B or pentamidine compounded classical arsenal treatment. All these drugs are toxic and have to be administered by parenteral route. Tamoxifen has been used as an antiestrogen treatment prevention breast cancer for many years. Its safety pharmacological profiles well established humans. We shown that tamoxifen active antileishmanial compound vitro, this paper we...
The protozoan parasite Leishmania amazonensis is a heme auxotroph and must acquire this essential factor from the environment. Previous studies showed that L. incorporates through transmembrane protein LHR1 (Leishmania Heme Response 1). LHR1-null promastigotes were not viable, suggesting transporter for survival. Here, we compared growth, differentiation, infectivity macrophages mice of wild-type, LHR1-single-knockout (LHR1/Δlhr1), LHR1-complemented (LHR1/Δlhr1 plus LHR1) strains. LHR1/Δlhr1...
Leishmaniasis is one of the leading globally neglected diseases, affecting millions people worldwide. Leishmania infection depends on ability insect-transmitted metacyclic promastigotes to invade mammalian hosts, differentiate into amastigotes, and replicate inside macrophages. To counter hostile oxidative environment macrophages, these protozoans contain anti-oxidant systems that include iron-dependent superoxide dismutases (SODs) in mitochondria glycosomes. Increasing evidence suggests...
The isolation and identification of a series new pseudoceratidine (1) derivatives from the sponge Tedania brasiliensis enabled evaluation their antiparasitic activity against Plasmodium falciparum, Leishmania (Leishmania) amazonensis, infantum, Trypanosoma cruzi, causative agents malaria, cutaneous leishmaniasis, visceral Chagas disease, respectively. 3-debromopseudoceratidine (4), 20-debromopseudoceratidine (5), 4-bromopseudoceratidine (6), 19-bromopseudoceratidine (7),...
Background The treatment of leishmaniasis relies mostly on parenteral drugs with potentially serious adverse effects. Additionally, parasite resistance in the has been demonstrated for majority available, making search more effective and less toxic regimens a priority control leishmaniasis. aims this study were to evaluate antileishmanial activity raloxifene vitro vivo investigate its mechanism action against Leishmania amazonensis. Methodology/Principal Findings Raloxifene was shown possess...
Phospholipase A2 toxins present in snake venoms interact with biological membranes and serve as structural models for the design of small peptides anticancer, antibacterial antiparasitic properties. Oligoarginine are capable increasing cell membrane permeability (cell penetrating peptides), this reason interesting delivery systems compounds pharmacological interest. Inspired by these two families bioactive molecules, we have synthesized 13-mer potential antileishmanial leads gaining insights...
A series of mononuclear coordination or organometallic AuI /AuIII complexes (1-9) have been comparatively studied in vitro for their antileishmanial activity against promastigotes and amastigotes, the clinically relevant parasite form, Leishmania amazonensis braziliensis. One cationic bis-N-heterocyclic carbenes (3) has low EC50 values (ca. 4 μM) cells no toxicity host macrophages. Together with two other AuIII (6 7), compound is also extremely effective intracellular amastigotes from L....
Leishmania spp. are trypanosomatid parasites that replicate intracellularly in macrophages, causing serious human morbidity and mortality throughout the world. Trypanosomatid protozoa cannot synthesize heme, so must acquire this essential cofactor from their environment. Earlier studies identified LHR1 as a amazonensis transmembrane protein mediates heme uptake. Null mutants of not viable single knockout strains have reduced virulence, but very little is known about properties directly...
SUMMARY The aims of the present work were to test effect tamoxifen administered topically and therapeutic efficacy pentavalent antimonial combinations in an experimental model cutaneous leishmaniasis. BALB/c mice infected with a luciferase expressing line Leishmania amazonensis treated topical two different formulations (ethanol or oil-free cream) as monotherapy co-administration antimonial. Treatment was evaluated by lesion size parasite burden, quantified through luminescence, at end...