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1.
Int J Pharm ; 644: 123323, 2023 Sep 25.
Artigo em Inglês | MEDLINE | ID: mdl-37597596

RESUMO

Herein we report the synthesis of transition-metal-free potassium borophosphate glasses and their application as bactericidal and bacteriostatic material. The antimicrobial activity was achieved through a simple change in the molar ratio of boron and phosphorus atoms, making borophosphate glass soluble in water. The glasses were analyzed by X-ray powder diffraction, Raman spectroscopy, laser-induced breakdown spectroscopy, and water absorption. The addition of a boron compound is required to obtain potassium-based phosphate glasses. Moreover, the change in the phosphorus and boron molar ratio (P/B), 2, 1 or 0.5 affects the glass solubilization in water, which increases with the phosphorus content. The glass materials were submitted to tests of biological activity against the bacteria Staphylococcus aureus, Escherichia coli, and Pseudomonas aeruginosa. These water-soluble borophosphate glasses were employed in the development of hydrogel formulations using Carbopol®. Phosphorous-rich samples at a concentration of 15 % (w/w) in hydrogel showed better antimicrobial activity against S. aureus and E. coli, when compared to other samples, including commercial alcohol hand sanitizer gel, with an average size of the inhibition halo of 24.02±1.43 and 19.24±1.63mm, respectively.


Assuntos
Anti-Infecciosos , Boro , Escherichia coli , Staphylococcus aureus , Hidrogéis , Fósforo , Potássio
2.
Bioorg Med Chem Lett ; 47: 128206, 2021 09 01.
Artigo em Inglês | MEDLINE | ID: mdl-34146704

RESUMO

Acetylcholinesterase (AChEis) inhibitors are used to treat neurodegenerative diseases like Alzheimer's disease (AD). l-Hypaphorine (l-HYP) is a natural indole alkaloid that has been shown to have effects on the central nervous system (CNS). The goal of this research was to synthesize l-HYP and d-HYP and test their anticholinesterasic properties in rat brain regions. l-HYP suppressed acetylcholinesterase (AChE) activity only in the cerebellum, whereas d-HYP inhibited AChE activity in all CNS regions studied. No cytotoxic effect on normal human cells (HaCaT) was observed in the case of l-HYP and d-HYP although an increase in cell proliferation. Molecular modeling studies revealed that d-HYP and l-HYP have significant differences in their binding mode positions and interact stereospecifically with AChE's amino acid residues.


Assuntos
Acetilcolinesterase/metabolismo , Encéfalo/enzimologia , Inibidores da Colinesterase/farmacologia , Indóis/farmacologia , Animais , Encéfalo/patologia , Inibidores da Colinesterase/química , Relação Dose-Resposta a Droga , Indóis/química , Estrutura Molecular , Ratos , Relação Estrutura-Atividade
3.
ChemMedChem ; 15(5): 449-458, 2020 03 05.
Artigo em Inglês | MEDLINE | ID: mdl-31834975

RESUMO

Organosulfur compounds show cytotoxic potential towards many tumor cell lines. Disulfides and thiosulfonates act through apoptotic processes, inducing proteins associated with apoptosis, endoplasmic reticulum stress, and the unfolded protein response. Three p-substituted symmetric diaryl disulfides and three diaryl thiosulfonates were synthesized and analyzed for inhibition of tubulin polymerization and for human cancer cell cytotoxic activity against seven tumor cell lines and a non-tumor cell line. S-(4-methoxyphenyl)-4-methoxybenzenesulfonothioate (6) exhibited inhibition of tubulin polymerization and showed the best antiproliferative potential, especially against the 786-0 cell line, being six times more selective as compared with the non-tumor cell line. In addition, compound 6 was able to activate caspase-3 after 24 and 48 h treatments of the 786-0 cell line and induced cell-cycle arrest in the G2/M stage at the highest concentration evaluated at 24 and 48 h. Compound 6 was able to cause complete inhibition of proliferation, inducing the death of 786-0 cells, by increasing the number of cells at G2/M and greater activation of caspase-3.


Assuntos
Antineoplásicos/farmacologia , Carcinoma de Células Renais/tratamento farmacológico , Neoplasias Renais/tratamento farmacológico , Animais , Antineoplásicos/síntese química , Antineoplásicos/química , Carcinoma de Células Renais/metabolismo , Carcinoma de Células Renais/patologia , Linhagem Celular , Proliferação de Células/efeitos dos fármacos , Ensaios de Seleção de Medicamentos Antitumorais , Humanos , Neoplasias Renais/metabolismo , Neoplasias Renais/patologia , Camundongos , Simulação de Acoplamento Molecular , Estrutura Molecular , Polimerização/efeitos dos fármacos , Tubulina (Proteína)/metabolismo
4.
J Colloid Interface Sci ; 533: 216-226, 2019 Jan 01.
Artigo em Inglês | MEDLINE | ID: mdl-30165299

RESUMO

The development of self-healing materials opens perspectives to fabricate devices with unprecedented lifetimes and recyclability that can be integrated with flexible electronics. However, the timescale at which these materials operate remains an important challenge to overcome. This article describes the fast self-healing behavior of aluminum/iron polyphosphate metallo-gels and their hybrids with polyaniline and gives a detailed investigation of their electrical behaviors. The samples can be cut, molded and healed by manual handling. The rebuilding process is mediated by water uptake and was directly observed by environmental scanning electron microscopy. Metallo-gels with and without polyaniline can be mixed to give homogeneous samples, where the conducting polymer is uniformly distributed within the inorganic matrix. Cyclic voltammetry experiments showed that polyaniline behaves within the metallo-gel in the same manner as it does in aqueous electrolytes. Furthermore, polyaniline adds electronic conductivity to the originally ion-conducting polyphosphate metallo-gel, as demonstrated by impedance spectroscopy. The ionic and electronic conductivities are 1.3-1.7 × 10-2 S·cm-1 and 5.2 × 10-4 S·cm-1, respectively. Such properties result from the "free" and "bound" water within the hydrogel network and the dynamic nature of the aluminum-phosphate interactions within the supramolecular network. The features presented here make these materials good candidates to be used as moldable electroactive binders in carbon-based electrodes and in all-solid-state flexible separators for repairable electrochemical capacitors and batteries.

6.
ACS Appl Mater Interfaces ; 10(9): 8077-8085, 2018 Mar 07.
Artigo em Inglês | MEDLINE | ID: mdl-29462559

RESUMO

Plastic debris is a major environmental concern, and to find effective ways to reuse polystyrene (PS) presents major challenges. Here, it is demonstrated that polystyrene foams impregnated with SnO2 are easily generated from plastic debris and can be applied to photocatalytic degradation of dyes. SnO2 nanoparticles were synthesized by a polymeric precursor method, yielding specific surface areas of 15 m2/g after heat treatment to 700 °C. Crystallinity, size, and shape of the SnO2 particles were assessed by X-ray diffraction (XRD) and transmission electron microscopy (TEM), demonstrating the preparation of crystalline spherical nanoparticles with sizes around 20 nm. When incorporated into PS foams, which were generated using a thermally induced phase separation (TIPS) process, the specific surface area increased to 48 m2/g. These PS/SnO2 nanofoams showed very good efficiency for photodegradation of rhodamine B, under UV irradiation, achieving up to 98.2% removal. In addition the PS/SnO2 nanofoams are shown to retain photocatalytic activity for up to five reuse cycles.

7.
Chem Commun (Camb) ; 49(27): 2765-7, 2013 Apr 07.
Artigo em Inglês | MEDLINE | ID: mdl-23443740

RESUMO

Dicationic magnetic ionic liquids with heteroanionic anions allow for tunability of physicochemical properties while retaining magnetic susceptibility.

8.
Langmuir ; 27(15): 9277-84, 2011 Aug 02.
Artigo em Inglês | MEDLINE | ID: mdl-21739956

RESUMO

A new class of photoreactive surfactants (PRSs) is presented here, consisting of amphiphiles that can also act as reagents in photochemical reactions. An example PRS is cobalt 2-ethylhexanoate (Co(EH)(2)), which forms reverse micelles (RMs) in a hydrocarbon solvent, as well as mixed reversed micelles with the standard surfactant Aerosol-OT (AOT). Small-angle neutron scattering (SANS) data show that mixed AOT/PRS RMs have a spherical structure and size similar to that of pure AOT micelles. Excitation of the ligand-to-metal charge transfer (LMCT) band in the PRSs promotes electron transfer from PRS to associated metal counterions, leading to the generation of metal and metal-oxide nanoparticles inside the RMs. This work presents proof of concept for employing PRSs as precursors to obtain nearly monodisperse inorganic nanoparticles: here both Co(3)O(4) and Bi nanoparticles have been synthesized at high metal concentration (10(-2) M) by simply irradiating the RMs. These results point toward a new approach of photoreactive self-assembly, which represents a clean and straightforward route to the generation of nanomaterials.

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