Eur J Pharmacol
November 2024
Introduction: Pancreatic ductal adenocarcinoma (PDAC) is a highly aggressive cancer with limited treatment options. This study explores the potential of novel 5-nitro-thiophene-thiosemicarbazone derivatives as therapeutic agents for PDAC.
Methods: We evaluated the cytotoxicity of seven derivatives in peripheral blood mononuclear cells (PBMCs) and PDAC cell lines.
Mol Biochem Parasitol
December 2024
The study aimed to conduct in vitro biological assessments of hydantoin and thiohydantoin compounds against mature Schistosoma mansoni worms, evaluate their cytotoxic effects and predict their pharmacokinetic parameters using computational methods. The compounds showed low in vitro cytotoxicity and were not considered hemolytic. Antiparasitic activity against adult S.
View Article and Find Full Text PDFAn Acad Bras Cienc
June 2024
Cancer is a complex and multifactorial disease characterized by uncontrolled cell growth and is one of the main causes of death in the world. This work aimed to evaluate a small series of 10 different indole-thiosemicarbazone compounds as potential antitumor agents. This is a pioneering study.
View Article and Find Full Text PDFAn Acad Bras Cienc
May 2024
Thiosemicarbazones are promising classes of compounds with antitumor activity. For this study, six 2,4-dihydroxy-benzylidene-thiosemicarbazones compounds were synthesized. These compounds were submitted to different assays in silico, in vitro and in vivo to evaluate the toxicological, antioxidant and antitumor effects.
View Article and Find Full Text PDFParasitol Res
February 2024
The objective of the study was to evaluate the in vitro and in vivo schistosomicidal activity of sanguinarine (SA) on Schistosoma mansoni and its in silico pharmacokinetic parameters. ADMET parameters and oral bioavailability were evaluated using the PkCSM and SwissADME platforms, respectively. The activity of SA in vitro, at the concentrations of 1.
View Article and Find Full Text PDFAn Acad Bras Cienc
December 2023
In this work, an in silico study and evaluation of the cytotoxicity of 4-(4-chlorophenyl)thiazole compounds against mouse splenocytes and the chloroquine-sensitive Plasmodium falciparum 3D7 strain are reported. The in silico results showed that the compounds have important pharmacokinetic properties for compounds with potential drug candidates. Regarding cytotoxicity assays against splenocytes, the compounds have low cytotoxicity.
View Article and Find Full Text PDFUnlabelled: Ruiz & Pav is a neotropical species found in humid forests from southern Mexico to southern Brazil. There are few studies related to the ethnopharmacological use of . Our objective was to evaluate the hydroalcoholic extract of as a potential antiparasitic agent.
View Article and Find Full Text PDFInt J Biol Macromol
October 2023
In this context, the objective of this work was to isolate an alkaline lignin from the leaves of C. ferrea, in addition to investigating different biological activities and its use in the production of releasing tablets in vitro. Initially, the analysis of the composition of the leaves was performed, the contents were: cellulose (33.
View Article and Find Full Text PDFActa Trop
September 2023
The present work aimed to carry out in vitro biological assays of thiazole compounds against adult worms of Schistosoma mansoni, as well as the in silico determination of pharmacokinetic parameters to predict the oral bioavailability of these compounds. In addition to presenting moderate to low cytotoxicity against mammalian cells, thiazole compounds are not considered hemolytic. All compounds were initially tested at concentrations ranging from 200 to 6.
View Article and Find Full Text PDFNeglected tropical diseases are a diverse group of communicable pathologies that mainly prevail in tropical and subtropical regions. Thus, the objective of this work was to evaluate the biological potential of eight 4-(4-chlorophenyl)thiazole compounds. Tests were carried out in silico to evaluate the pharmacokinetic properties, the antioxidant, cytotoxic activities in animal cells and antiparasitic activities were evaluated against the different forms of Leishmania amazonensis and Trypanosoma cruzi in vitro.
View Article and Find Full Text PDF3 Biotech
April 2023
The objective of this work was to isolate a polysaccharide similar to pectin from leaves, not yet reported in the literature, and to evaluate its antioxidant, cytotoxic and immunomodulatory profile. Pectin was extracted from the leaves in three stages, organic solvent followed by acidified water and ethanol precipitation. With the pectin obtained, the physicochemical characterization of the molecule was carried out using high-performance liquid chromatography, Fourier-transform infrared spectroscopy, nuclear magnetic resonance (C and H) and different thermal and elemental analysis.
View Article and Find Full Text PDFExp Parasitol
May 2023
In this work, 13 thiosemicarbazones (1a - m) and 16 thiazoles (2a - p) were obtained, which were properly characterized by spectroscopic and spectrometric techniques. The pharmacokinetic properties obtained in silico revealed that the derivatives are in accordance with the parameters established by lipinski and veber, showing that such compounds have good bioavailability or permeability when administered orally. In assays of antioxidant activity, thiosemicarbazones showed moderate to high antioxidant potential when compared to thiazoles.
View Article and Find Full Text PDF3 Biotech
March 2023
Unlabelled: This work aimed to isolate and characterize xylans from branches and leaves of , in addition to evaluating its in vitro biological and prebiotic potential. The results showed that the chemical structure of the obtained polysaccharides is similar being classified as homoxylans. The xylans presented an amorphous structure, in addition to being thermally stable and presenting a molecular weight close to 36 g/mol.
View Article and Find Full Text PDFInt J Biol Macromol
April 2023
In this work we will discuss the antiproliferative evaluation and the possible mechanisms of action of indole-thiosemicarbazone compounds LTs with anti-inflammatory activity, previously described in the literature. In this perspective, some analyzes were carried out, such as the study of binding to human serum albumin (HSA) and to biological targets: DNA and human topoisomerase IIα (topo). Antiproliferative study was performed with DU-145, Jukart, MCF-7 and T-47D tumor lines and J774A.
View Article and Find Full Text PDFInt J Biol Macromol
March 2023
The Amazon rainforest is considered the largest tropical timber reserve in the world. The management of native forests in the Amazon is one of the most sensitive geopolitical issues today, given its national and international dimension. In this work, we obtained and characterized physicochemical lignins extracted from branches and leaves of Protium puncticulatum and Scleronema micranthum.
View Article and Find Full Text PDFInt J Biol Macromol
October 2022
In this work, we investigated in vitro different biological activities of alkaline lignins extracted from the species Buchenavia viridiflora, a tree from the Amazon rainforest used as a wood product. The chemical composition results for the twig and leaves were, respectively (%): cellulose (30.88 and 24.
View Article and Find Full Text PDFInt J Biol Macromol
December 2021
In this work, we investigated in vitro the antioxidant, cytotoxic and anti-leishmanial activities of a lignin extracted from the leaves of Morinda citrifolia. Initially, an analysis of the composition of the sheets was performed, then the lignin was obtained by alkaline delignification and characterized by different techniques: elemental analysis, FT-R, UV-vis, HSQC-NMR, thermal analysis, Py-GC/MS and by GPC. The results showed that the leaves had in their composition cellulose (31.
View Article and Find Full Text PDFInt J Biol Macromol
November 2020
Caesalpinia pulcherrima is a shrub with worldwide distribution used as an ornamental plant. In this study, we extracted a lignin from the C. pulcherrima leaves and investigated its biological functions.
View Article and Find Full Text PDFNat Prod Res
December 2021
The leaves of were subjected to physicochemical analysis, such as ion content, extractives, and structural molecules. The hexanic, ethanolic and ethyl acetate extracts were submitted to phytochemical analyzes by GC-MS, HPLC-MS, and spectrophotometry. In addition, antioxidant (DPPH, ABTS and TAA methods) potential, antimicrobial (MIC method) action, cytotoxicity and immunostimulant activity (flow cytometry analysis) were performed.
View Article and Find Full Text PDFIn this work, we investigated the antioxidant and immunomodulatory activities of a lignin isolated from Conocarpus erectus leaves. The lignin was characterized by FTIR, H NMR, C NMR and gel permeation chromatography analysis as well as ultraviolet/visible absorption spectra. The lignin was evaluated for total antioxidant activity (TAA), DPPH and ABTS scavenging abilities, and by a lipid peroxidation inhibition assay.
View Article and Find Full Text PDFAn Acad Bras Cienc
May 2019
Currently, the research of new natural compounds with biological potential demonstrates great ethnopharmacological importance. In this study, we evaluated the biological properties promoted by saline extract from Malpighia emarginata DC leaves, whose objective is to evaluate the antioxidant, antimicrobial and cytotoxicity potential. Phytochemical characterization was performed by UPLC-MS chromatography to identify the chemical compounds.
View Article and Find Full Text PDFInt J Biol Macromol
February 2019
Opuntia fícus-indica and Opuntia cochenillifera are species of Cactaceae, found in the arid regions of the planet. They present water, cellulose, hemicellulose, pectins, extractives, ashes and lignins. Here we aimed to study the immunomodulatory action of lignins from these two species against mice splenocytes, since no study for this purpose has yet been reported.
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