A5036633970- Research on Leishmaniasis Studies
- Trypanosoma species research and implications
- Phytochemistry Medicinal Plant Applications
- Enzyme function and inhibition
- Enzyme Production and Characterization
- Phytochemicals and Antioxidant Activities
- Essential Oils and Antimicrobial Activity
- Traditional and Medicinal Uses of Annonaceae
- Animal Genetics and Reproduction
- Biomedical Research and Pathophysiology
- Synthesis and Biological Evaluation
- Toxin Mechanisms and Immunotoxins
- Botanical Research and Applications
- Biochemical and Molecular Research
- Phenothiazines and Benzothiazines Synthesis and Activities
- Phytochemistry and Bioactivity Studies
- Insect Pest Control Strategies
- Phytochemical compounds biological activities
- Science and Education Research
- Insect and Pesticide Research
- Polyamine Metabolism and Applications
- Chronic Kidney Disease and Diabetes
- Genetics, Aging, and Longevity in Model Organisms
- Cancer Treatment and Pharmacology
- Microencapsulation and Drying Processes
Universidade de São Paulo
2013-2025
Southwest Bahia State University
2019
Fundação de Estudo e Pesquisa em Medicina Veterinária e Zootecnia
2019
Universidade Estadual de Campinas (UNICAMP)
2016
Universidade Luterana do Brasil
2008
Fisetin, quercetin, luteolin and 7,8-hydroxyflavone show high activity in Leishmania cultures present low toxicity to mammalian cells. In this work, the structural aspects of 13 flavonoids were analyzed for their inhibition arginase enzyme from (Leishmania) amazonensis. A higher potency was observed with fisetin, which four ten times greater than that quercetin luteolin, respectively. These data hydroxyl group at position 3 contributed significantly inhibitory arginase, while 5 did not. The...
Epigallocatechin-3-gallate (EGCG), a dietary polyphenol (flavanol) from green tea, possesses leishmanicidal and antitrypanosomal activity. Mitochondrial damage was observed in Leishmania treated with EGCG, it contributed to the lethal effect. However, molecular target has not been defined. In this study, (+)-catechin (−)-epicatechin were tested against recombinant arginase amazonensis (ARG-L) rat liver (ARG-1). The compounds inhibit ARG-L ARG-1 but are more active parasite enzyme. Enzyme...
Many species of plants in the Brazilian cerrado (savanna) are widely used ethnomedicine. However, safety and effectiveness medicinal communities with little or no access to manufactured drugs should be evaluated. Evaluate antimicrobial cytotoxic activities extracts from eight plant species, obtained using cachaça as extractor liquid. The were tested against Bacillus subtilis, Staphylococcus aureus, Escherichia coli, Pseudomonas aeruginosa, Candida albicans, parapsilosis, promastigote forms...
Verbascoside (1) is a phenylethanoid glycoside that has antileishmanial activity against Leishmania infantum and donovani. In this study, we verified the of 1 on amazonensis arginase inhibition. Compound showed an EC50 19 μM L. promastigotes competitive inhibitor (Ki = 0.7 μM). Docking studies were performed to assess interaction with at molecular level. Arginase enzyme polyamine biosynthesis pathway important parasite infectivity, results our study suggest could be useful develop new...
Arginase is a glycosomal enzyme in Leishmania that involved polyamine and trypanothione biosynthesis. The central role of arginase (Leishmania) amazonensis was demonstrated by the generation two mutants: one with an lacking addressing signal which arginase-coding gene knocked out. Both these mutants exhibited decreased infectivity. Thus, seems to be potential drug target for treatment. In attempt search inhibitors, 29 derivatives [1,2,4]triazolo[1,5-a]pyrimidine system were tested against...
Taxifolin, quercetin glucuronide and glucosides inhibit arginase from <italic>Leishmania amazonensis</italic>.
Caffeic acid phenethyl ester (CAPE) is a polyphenol produced by many plants and found in red green propolis. Here, we evaluated the antileishmanial activity of this natural product against Leishmania amazonensis. CAPE exhibited IC50 values 8.07 µM (95% CI, 6.79–9.62 µM) 13.51 10.71–17.16 L. amazonensis promastigotes intracellular amastigotes, respectively. Additionally, inhibited arginase non-competitive manner with Ki value 1.51 ± 0.04 µM. These results highlight potential as promising lead...
Abstract This study describes the activity of five natural hydroxycinnamic acids and derived compound: caffeic ( 1 ), rosmarinic 2 chlorogenic 3 cryptochlorogenic 4 isoverbascoside 5 ). All compounds inhibited Leishmania amazonensis arginase with IC 50 —in range 1.5—11 μM. Compounds also showed against promastigotes L. = 61 (28–133) μM 14 (9–24) μM, respectively. Further computational studies applying molecular docking simulations were performed on competitive inhibitors to gain insight into...
Caffeic acid and related natural compounds were previously described as Leishmania amazonensis arginase (L-ARG) inhibitors, against the whole parasite in vitro. In this study, we tested cinnamides that synthesized to target human arginase. The compound caffeic phenethyl amide (CAPA), a weak inhibitor of (IC50 = 60.3 ± 7.8 μM) was found have 9-fold more potency L-ARG 6.9 0.7 μM). other did not inhibit characterized L-ARG, showing an IC50 between 1.3–17.8 μM, where most active 15 1.3 0.1 All...
The plant Cecropia pachystachya Trécul has been used in Brazilian folk medicine to treat hypertension, bladder and kidney inflammation renal diseases. aim of this study was evaluate the potential aqueous fraction from ethanolic extract (FCP) management progressive disease rats submitted 5/6 nephrectomy.Thirty male Wistar nephrectomy (5/6 NE) were untreated (NE) or treated (NE+FCP) with FCP (0.5g/kg/day). treatment started 15 days after surgery, followed for a period 60 days. Systolic blood...
Searching for new substances with antileishmanial activity, we synthesized and evaluated a series of α,α-difluorohydrazide α,α-difluoramides against Leishmania amazonensis arginase (LaArg). Four derivatives showed activity LaArg Ki in the range 1.3–26 μM. The study kinetics inhibition that these might act via different inhibitory mechanisms or even by combination these. compounds were tested L. promastigotes best result was obtained to compound 4 (EC50 12.7 ± 0.3 μM). In addition, order...
Background Lung tumors are the leading cause of cancer deaths worldwide and paclitaxel has proven to be useful for patients with lung cancer, however, acquired resistance is a major problem. To overcome this problem, one promising option use Constitutive Androstane Receptor (CAR) ligands in combination chemotherapeutics against cells. Therefore, we wish elucidate effects CAR on antineoplastic efficacy Methodology/Principal Findings Our results from cell viability assays exposing agonist or...
Targeting self-renewal and tumorigenicity has been proposed as a potential strategy against cancer stem cells (CSCs). Epigenetic proteins are key modulators of gene expression development contributing to regulation maintenance tumorigenicity. Here, we have screened small-molecule epigenetic inhibitor library using 3D in vitro models order determine targets associated with Canine Mammary Cancer (CMC) cells. We identified inhibition BET promising inhibit CMC colonies tumorspheres formation....
Arginase is a metalloenzyme that plays central role in Leishmania infections. Previously, rosmarinic and caffeic acids were described as antileishmanial agents amazonensis arginase inhibitors. Here, we describe the inhibition of L. by acid analogs (1-7) new acid-derived amides (8-10). Caffeic esters produced means an engineered synthesis E. coli tested against arginase. New (8-10) biosynthesized cultured with 2 mM different combinations feeding substrates. The most potent inhibitors showed...
In this present work simulation models were obtained in order to develop tools for early stages of design a new strain gauge by numerical modeling. The deformation was extracted FEM simulation. Moreover, correlation with experimental results established understand the efficiency results. It observed that finite element method is an adequate methodology evaluate strain-stress behavior printed flexible structure. found be suitable technology applied boards. Therefore, it could as direct...