A5025870096- Research on Leishmaniasis Studies
- Synthesis and Biological Evaluation
- Organoselenium and organotellurium chemistry
- Synthesis and biological activity
- Trypanosoma species research and implications
- Toxin Mechanisms and Immunotoxins
- Insect Pest Control Strategies
- Quinazolinone synthesis and applications
- Insect and Pesticide Research
- Parasites and Host Interactions
- Selenium in Biological Systems
- Food composition and properties
- Metal complexes synthesis and properties
- Urticaria and Related Conditions
- Microbial Metabolites in Food Biotechnology
- Cholinesterase and Neurodegenerative Diseases
- Reproductive System and Pregnancy
- Advancements in Transdermal Drug Delivery
- Organometallic Compounds Synthesis and Characterization
- Synthesis and Characterization of Heterocyclic Compounds
- Garlic and Onion Studies
- Phenothiazines and Benzothiazines Synthesis and Activities
- Nanoparticle-Based Drug Delivery
- Chemical synthesis and pharmacological studies
- Beetle Biology and Toxicology Studies
Universidad de Navarra
2015-2024
Navarre Institute of Health Research
2015-2023
Fraunhofer Institute for Applied Polymer Research
2023
Al-Azhar University
2023
Instituto de Salud Pública de Navarra
2014-2022
Universidad Autónoma del Estado de Hidalgo
2015-2021
Valencia Catholic University Saint Vincent Martyr
2018
Weatherford College
2014
ABSTRACT A series of new selenocyanates and diselenides bearing interesting bioactive scaffolds (quinoline, quinoxaline, acridine, chromene, furane, isosazole, etc.) was synthesized, their in vitro leishmanicidal activities against Leishmania infantum amastigotes along with cytotoxicities human THP-1 cells were determined. Interestingly, most tested compounds active the low micromolar range led us to identify four lead (1h, 2d, 2e, 2f) 50% effective dose (ED 50 ) values ranging from 0.45...
Berberine (BER)-an anti-inflammatory quaternary isoquinoline alkaloid extracted from plants-has been reported to have a variety of biologic properties, including antileishmanial activity. This work addresses the preparation BER-loaded liposomes with aim prevent its rapid liver metabolism and improve drug selective delivery infected organs in visceral leishmaniasis (VL). BER (LP-BER) displayed mean size 120 nm, negative Z-potential -38 mV loaded 6 nmol/μmol lipid. In vitro, loading enhanced...
Nowadays, oxidative cell damage is one of the common features cancer and Alzheimer’s disease (AD), Se-containing molecules, such as ebselen, which has demonstrated strong antioxidant activity, have well-established preventive effects against both diseases. In this study, a total 39 Se-derivatives were synthesized, purified, spectroscopically characterized by NMR. Antioxidant ability was tested using DPPH assay, while antiproliferative activity screened in breast, lung, prostate, colorectal...
Abstract A novel series of fourteen substituted selenadiazoles has been synthesized and the compounds tested for their in vitro antiproliferative cytotoxic activities. The tests were carried out against leukemia (CCRF‐CEM), colon (HT‐29), lung (HTB‐54), breast (MCF‐7) cancer cells. In order to assess selectivity under investigation assays also on two non‐tumoral lines – one mammary (184B5) bronchial epithelium (BEAS‐2B) cell line. Assay‐based activity studies revealed that seven derivatives...
A novel series of thirty-one N-substituted urea, thiourea, and selenourea derivatives containing diphenyldiselenide entities were synthesized, fully characterized by spectroscopic analytical methods, screened for their in vitro leishmanicidal activities. The cytotoxic activity these was tested against Leishmania infantum axenic amastigotes, selectivity assessed human THP-1 cells.
The in vitro leishmanicidal activities of a series 48 recently synthesized selenium derivatives against Leishmania infantum and braziliensis parasites were tested using promastigotes intracellular amastigote forms. cytotoxicity the compounds for J774.2 macrophage cells was also measured order to establish their selectivity. Six (compounds 8, 10, 11, 15, 45, 48) showed selectivity indexes higher than those reference drug, meglumine antimonate (Glucantime), both species; case L. braziliensis,...
We report for the first time a novel series of tellurides bearing sulfonamide as selective and potent inhibitors β-class carbonic anhydrase (CA; EC 4.2.1.1) enzyme expressed in Leishmania donovani protozoa. Such derivatives showed high activity against axenic amastigotes, among them, compound 5g (4-(((3,4,5-trimethoxyphenyl)tellanyl)methyl)benzenesulfonamide) an IC50 0.02 μM being highly parasites over THP-1 cells with selectivity index 300. The vitro vivo toxicity experiments to possess...
The generation of new antileishmanial drugs has become a priority. Selenium and its derivatives stand out as having promising leishmanicidal activity. In fact, some parasites express selenoproteins metabolize selenium. Recently, selenium have shown the potential to reduce parasitemia, clinical manifestations, mortality in parasite-infected mice. this paper, after selecting four candidates according drug similarity parameters, we observed that two them, called compounds 2b...
Bisacylimidoselenocarbamate derivatives (BSC) are potent anticancer agents with a strong cytotoxic activity against different types of tumour cells. Based in phosphatidylserine exposure on the cell membranes we show that BSC treatment resulted enhanced death leukaemia CCRF-CEM DNA fragmentation detection breast adenocarcinoma MCF-7 cells showed triggered is concentration and time dependent. We also two these compounds, 3g 3n, cause cell-cycle arrest late G2/M Consistent this, reduction CDK1...
Chagas disease is a tropical infection caused by the protozoan parasite Trypanosoma cruzi and global public health concern. It paradigmatic example of chronic without an effective treatment. Current treatments targeting T. are limited to two obsolete nitroheterocyclic drugs, benznidazole nifurtimox, which lead serious drawbacks. Hence, new, more effective, safer, affordable drugs urgently needed. Selenium their derivatives have emerged as interesting strategy for treatment different...
The lack of safe and cost-effective treatments against leishmaniasis highlights the urgent need to develop improved leishmanicidal agents. Antimicrobial peptides (AMPs) are an emerging category therapeutics exerting a wide range biological activities such as anti-bacterial, anti-fungal, anti-parasitic anti-tumoral. In present study, approach repurposing AMPs antileishmanial drugs was applied. activity two synthetic anti-lipopolysaccharide (SALPs), so-called 19-2.5 19-4LF characterized in...
The oral administration of dapsone (DAP) for the treatment cutaneous leishmaniasis (CL) is effective, although serious hematological side effects limit its use. In this study, we evaluated drug topical CL. As efficacy depends on potency and skin penetration, first determined antileishmanial activity (IC50 = 100 μM) selectivity index in vitro against Leishmania major-infected macrophages. order to evaluate penetration ex vivo, compared an O/W cream containing DAP that had been micronized with...
Leishmaniasis urgently needs new oral treatments, as it is one of the most important neglected tropical diseases that affects people with poor resources. The drug discovery pipeline for administration currently discards entities aqueous solubility and permeability (class IV compounds in Biopharmaceutical Classification System, BCS) such diselenide 2m, a trypanothione reductase (TR) inhibitor. This work was assisted by glyceryl palmitostearate diethylene glycol monoethyl ether-based...
Currently, cancer, leishmaniasis and bacterial infections represent a serious public health burden worldwide. Six cinnamyl benzodioxyl derivatives incorporating selenium (Se) as selenocyanate, diselenide, or selenide were designed synthesized through nucleophilic substitution and/or reduction using hydrides. Ferrocene was also incorporated by Friedel-Crafts acylation. All the compounds screened in vitro for their antiproliferative, antileishmanial, antibacterial properties. Their capacity to...