Your browser doesn't support javascript.
loading
Mostrar: 20 | 50 | 100
Resultados 1 - 6 de 6
Filtrar
Mais filtros











Base de dados
Intervalo de ano de publicação
1.
PeerJ ; 12: e15638, 2024.
Artigo em Inglês | MEDLINE | ID: mdl-38188145

RESUMO

A novel Artemisinin/Quercetin/Zinc (Art/Q/Zn) mixed ligand complex was synthesized, tested for its antiviral activity against coronavirus (SARS-CoV-2), and investigated for its effect against toxicity and oxidative stress induced by acrylamide (Acy), which develops upon cooking starchy foods at high temperatures. The synthesized complex was chemically characterized by performing elemental analysis, conductance measurements, FT-IR, UV, magnetic measurements, and XRD. The morphological surface of the complex Art/Q/Zn was investigated using scanning and transmission electron microscopy (SEM and TEM) and energy dispersive X-ray analysis (XRD). The in vitro antiviral activity of the complex Art/Q/Zn against SARS-CoV-2 and its in vivo activity against Acy-induced toxicity in hepatic and pulmonary tissues were analyzed. An experimental model was used to evaluate the beneficial effects of the novel Art/Q/Zn novel complex on lung and liver toxicities of Acy. Forty male rats were randomly divided into four groups: control, Acy (500 mg/Kg), Art/Q/Zn (30 mg/kg), and a combination of Acy and Art/Q/Zn. The complex was orally administered for 30 days. Hepatic function and inflammation marker (CRP), tumor necrosis factor, interleukin-6 (IL-6), antioxidant enzyme (CAT, SOD, and GPx), marker of oxidative stress (MDA), and blood pressure levels were investigated. Histological and ultrastructure alterations and caspase-3 variations (immunological marker) were also investigated. FT-IR spectra revealed that Zn (II) is able to chelate through C=O and C-OH (Ring II) which are the carbonyl oxygen atoms of the quercetin ligand and carbonyl oxygen atom C=O of the Art ligand, forming Art/Q/Zn complex with the chemical formula [Zn(Q)(Art)(Cl)(H2O)2]⋅3H2O. The novel complex exhibited a potent anti-SARS-CoV-2 activity even at a low concentration (IC50 = 10.14 µg/ml) and was not cytotoxic to the cellular host (CC50 = 208.5 µg/ml). Art/Q/Zn may inhibit the viral replication and binding to the angiotensin-converting enzyme-2 (ACE2) receptor and the main protease inhibitor (MPro), thereby inhibiting the activity of SARS-CoV-2 and this proved by the molecular dynamics simulation. It alleviated Acy hepatic and pulmonary toxicity by improving all biochemical markers. Therefore, it can be concluded that the novel formula Art/Q/Zn complex is an effective antioxidant agent against the oxidative stress series, and it has high inhibitory effect against SARS-CoV-2.


Assuntos
Artemisininas , COVID-19 , Masculino , Animais , Ratos , Antioxidantes/farmacologia , Quercetina/farmacologia , SARS-CoV-2 , Zinco/farmacologia , Ligantes , Espectroscopia de Infravermelho com Transformada de Fourier , Artemisininas/farmacologia , Antivirais/farmacologia , Acrilamida/toxicidade , Oxigênio
2.
Antibiotics (Basel) ; 11(7)2022 Jul 19.
Artigo em Inglês | MEDLINE | ID: mdl-35884222

RESUMO

In this study, metal cefotaxime complexes of Ca(II), Cr(III), Cu(II), Zn(II), and Se(VI) were synthesized and characterized by elemental analysis, conductance measurements, IR, electronic spectra, magnetic measurements, 1HNMR, and XRD, as well as by scanning electron microscopy (SEM) and transmission electron microscopy (TEM). The lower values for molar conductance refer to the nonelectrolyte nature of the complexes. The FTIR and 1H-NMR spectra for the metal complexes of cefotaxime proved that the free cefotaxime antibiotic ligand acted as a monoanionic tridentate ligand through the oxygen atoms of lactam carbonyl, the carboxylate group, and the nitrogen atoms of the amino group. From the magnetic measurements and electronic spectral data, octahedral structures were proposed for the Cr(III) and Se(VI) complexes, while the Cu(II) complex had tetragonal geometry. This study aimed to investigate the effects of cefotaxime and cefotaxime metal complexes on oxidative stress using antioxidant assays including DPPH, ORAC, FARAB, and ABTS, a metal chelation assay, as well as the inhibition of the viability of cancer cells (HepG-2). Regarding the antibacterial activity, the cefotaxime metal complexes were highly effective against both Bacillus subtilis and Escherichia coli. In conclusion, the cefotaxime metal complexes exhibited highly antioxidant activities. The cefotaxime metal complexes with Zn and Se inhibited HepG-2 cellular viability. Thus, the cefotaxime metal complexes elicited promising results as potent antioxidant and anticancer agents against HepG-2, with potent antibacterial activities at a much lower concentration.

3.
Antioxidants (Basel) ; 11(7)2022 Jun 23.
Artigo em Inglês | MEDLINE | ID: mdl-35883718

RESUMO

Exposure to cadmium chloride (CdCl2) causes an imbalance in the oxidant status of the body by triggering the release of reactive oxygen species (ROS). This study investigated the effect of Rosa damascena (R. damascena) extract on oxidative stress, hepatotoxicity, and the injured cardiac tissue of male rats exposed to CdCl2. Forty male Wistar albino rats were divided into four groups: the vehicle control (1 mg/kg normal saline), the CdCl2-treated group (5 mg/kg), the R. damascena extract group (100 mg Kg), and the combination of CdCl2 and R. damascena extract group. Male rats exposed to CdCl2 showed multiple significant histopathological changes in the liver and heart, including inflammatory cell infiltration and degenerative alterations. Successive exposure to CdCl2 elevated the levels of hepatic and cardiac reactive oxygen species (ROS), malondialdehyde (MDA), tumour necrosis factor-alpha) (TNF-α) and interleukin -6 (IL-6) and decreased antioxidant defences. The extracts significantly increased the levels of glutathione, superoxide dismutase (SOD), and catalase (CAT), whereas it dramatically decreased the levels of lipid peroxidation (LPO), alanine aminotransferase (ALT), aspartate aminotransferase (AST), and the mRNA of TNF-α and IL-6. R. damascena administration prevented liver and heart injury; suppressed excessive ROS generation, LPO, and inflammatory responses; and enhanced antioxidant defences. In addition, R. damascena upregulated the mRNA of TNF-α and IL-6 in CdCl2-administered male rats. In conclusion, R. damascena modulated the oxidative stress and inflammation induced by CdCl2. The hepatic and cardiac tissue damage and histopathological alterations resulting from the CdCl2-induced oxidative stress were counteracted by the administration of R. damascena extracts. R. damascena enhanced antioxidant defence enzymes in male rats.

4.
PLoS One ; 16(3): e0246265, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-33661932

RESUMO

Medicinal uses and applications of metals and their complexes are of increasing clinical and commercial importance. The ligation behavior of quercetin (Q), which is a flavonoid, and its Zn (II) (Q/Zn) complex were studied and characterized based on elemental analysis, molar conductance, Fourier-transform infrared (FTIR) spectra, electronic spectra, proton nuclear magnetic resonance (1H-NMR), thermogravimetric analysis, and transmission electron microscopy (TEM). FTIR spectral data revealed that Q acts as a bidentate ligand (chelating ligand) through carbonyl C(4) = O oxygen and phenolic C(3)-OH oxygen in conjugation with Zn. Electronic, FTIR, and 1H-NMR spectral data revealed that the Q/Zn complex has a distorted octahedral geometry, with the following chemical formula: [Zn(Q)(NO3)(H2O)2].5H2O. Diabetes was induced by streptozotocin (STZ) injection. A total of 70 male albino rats were divided into seven groups: control, diabetic untreated group and diabetic groups treated with either MSCs and/or Q and/or Q/Zn or their combination. Serum insulin, glucose, C-peptide, glycosylated hemoglobin, lipid profile, and enzymatic and non-enzymatic antioxidant levels were determined. Pancreatic and lung histology and TEM for pancreatic tissues in addition to gene expression of both SOD and CAT in pulmonary tissues were evaluated. MSCs in combination with Q/Zn therapy exhibited potent protective effects against STZ induced hyperglycemia and suppressed oxidative stress, genotoxicity, glycometabolic disturbances, and structural alterations. Engrafted MSCs were found inside pancreatic tissue at the end of the experiment. In conclusion, Q/Zn with MSC therapy produced a synergistic effect against oxidative stress and genotoxicity and can be considered potential ameliorative therapy against diabetes with pulmonary dysfunction, which may benefit against COVID-19.


Assuntos
Diabetes Mellitus Experimental/terapia , Hipoglicemiantes/uso terapêutico , Transplante de Células-Tronco Mesenquimais , Quercetina/uso terapêutico , Zinco/uso terapêutico , Animais , Glicemia/análise , Glicemia/metabolismo , Peptídeo C/sangue , Peptídeo C/metabolismo , Células Cultivadas , Complexos de Coordenação/química , Complexos de Coordenação/uso terapêutico , Diabetes Mellitus Experimental/sangue , Diabetes Mellitus Experimental/metabolismo , Diabetes Mellitus Experimental/patologia , Hemoglobinas Glicadas/análise , Hemoglobinas Glicadas/metabolismo , Hiperglicemia/sangue , Hiperglicemia/metabolismo , Hiperglicemia/patologia , Hiperglicemia/terapia , Hipoglicemiantes/química , Insulina/sangue , Insulina/metabolismo , Pulmão/efeitos dos fármacos , Pulmão/metabolismo , Pulmão/patologia , Masculino , Estresse Oxidativo/efeitos dos fármacos , Quercetina/análogos & derivados , Ratos , Zinco/química
5.
Future Med Chem ; 10(14): 1693-1704, 2018 07 01.
Artigo em Inglês | MEDLINE | ID: mdl-29957063

RESUMO

AIM: Melatonin (MLT) is a major hormone secreted by the pineal gland. In this study, a gold(III) MLT (Au+3/MLT) complex has been synthesized and investigating its protective effects against testicular damage. METHODOLOGY: The structural features of the complex were investigated. For biological assessment, 30 male rats were divided into three groups for 30 days. The first control group, the second received MLT and the third received Au+3/MLT complex. RESULTS: The Au+3/MLT complex was found to be nonelectrolytic with formula (Au[MLT]2[Cl][H2O]). The ligand is monodentate and adopt square-planar geometry. Its particles range in diameter from 35 to 100 nm. MLT affords slight oxidative stress protection. The Au+3/MLT complex significantly decreases TNF-α and IL-1ß levels but elevates antioxidant enzyme capacities, reducing lipid peroxidation markers and improving testicular histological structure. CONCLUSION: The Au+3/MLT complex improves the anti-inflammatory actions of MLT, exhibits potent antioxidant activity and enhances reproductive capacity.


Assuntos
Anti-Inflamatórios/síntese química , Complexos de Coordenação/farmacologia , Ouro/química , Melatonina/química , Nanoestruturas/química , Testículo/efeitos dos fármacos , Animais , Anti-Inflamatórios/química , Anti-Inflamatórios/farmacologia , Antioxidantes/metabolismo , Catalase/metabolismo , Complexos de Coordenação/síntese química , Complexos de Coordenação/química , Interleucina-1beta/metabolismo , Magnetismo , Masculino , Modelos Animais , Ratos , Ratos Wistar , Superóxido Dismutase/metabolismo , Testículo/metabolismo , Testículo/patologia , Fator de Necrose Tumoral alfa/metabolismo
6.
Chem Biol Interact ; 220: 169-80, 2014 Sep 05.
Artigo em Inglês | MEDLINE | ID: mdl-24998638

RESUMO

A new silver-carbocysteine (Ccy-Ag) complex [Ag2(Ccy)2(H2O)2] has been synthesized and characterized by using a combination of FTIR, Raman, molar conductivity, (1)H NMR, electronic spectra, thermal analyses, X-ray powder diffraction (XRD) and scanning electron microscopy (SEM). The infrared spectrum of Ccy-Ag complex in comparison with carbocysteine ligand prove that Ccy behaves as monobasic bidentate chelate to the silver metal ions via the deprotonated carboxylate O atom. The assessments of Ccy and its complexation with Ag(+) in treating COPD, evaluating immune activities through measuring IL-8, TGF-ß1, VEGF and TNF-α, antioxidant activities of (Ccy-Ag) complex by measuring SOD, MDA and GPX and bronchial asthma were discussed.


Assuntos
Carbocisteína/química , Carbocisteína/farmacologia , Complexos de Coordenação , Pulmão/efeitos dos fármacos , Prata/química , Prata/farmacologia , Animais , Antioxidantes/síntese química , Antioxidantes/química , Antioxidantes/farmacologia , Complexos de Coordenação/síntese química , Complexos de Coordenação/farmacologia , Interleucina-8/metabolismo , Pulmão/patologia , Masculino , Microscopia Eletrônica de Varredura , Oxirredução/efeitos dos fármacos , Ratos , Fator de Necrose Tumoral alfa/metabolismo
SELEÇÃO DE REFERÊNCIAS
DETALHE DA PESQUISA