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1.
J Fluoresc ; 2024 Sep 17.
Artigo em Inglês | MEDLINE | ID: mdl-39287722

RESUMO

In this research, CNDs were prepared by a green and cost effective method using Cinnamomum Tamala (bay leaf) as carbon sources. TEM, UV, FTIR, ZETA Potential, PL and Fluorescence methods were used to characterize the produced CNDs and the average particle size is 3.42 nm. This research was conducted on the development of fluorescent sensors for various metal ions, including Fe3+, Cu2+, Zn2+, Ni2+, Pb2+, Cr3+, Mg2+, Na+ 1 and Cd2+. The CNDs demonstrated selective sensing of biologically important Fe+ 3 and Cu+ 2 metal ions. The CNDs antioxidant assay was tasked with DPPH• radical scavenging properties. CNDs made from Cinnamomum Tamala had the highest DPPH free radical scavenging activity at 100 mg/L (42.06%) with the IC50 of 130.68 mg/L. The outcome implies that Indian spices are among the best materials for optical metal ion detection and sensing, and they also have therapeutic benefits.

2.
Environ Res ; 242: 117767, 2024 Feb 01.
Artigo em Inglês | MEDLINE | ID: mdl-38029826

RESUMO

The anti-dermatophytic (Proteus vulgaris, Klebsiella pneumoniae, Enterobacter aerogenes, Propionibacterium acnes, Staphylococcus aureus, and Streptococcus pyogenes) and nephroprotective activities of methanol and aqueous extracts obtained from Lannea coromandelica fruit were investigated through in-vitro (agar well diffusion method) and in-vivo (animal model) study. The methanol extract showed considerable antibacterial activity against selective bacterial pathogens at increased concentration (15.0 mg mL-1) in the following order P. vulgaris (35.2 ± 1.6 mm) > E. aerogenes (32.1 ± 2.1 mm) > K. pneumoniae (29.3±2 mm) > P. acnes (28.2 ± 2.4 mm) > S. aureus (25.5 ± 2.4 mm) > S. pyogenes (24.3 ± 2.1 mm) than aqueous extract. The MIC values of this methanol and aqueous extract was found as 2.5-7.5 mg mL-1 and 5.0 to 1.0 mg mL-1 respectively. Different treatment sets (A-E) on a rat-based animal model study revealed that the methanol extract has excellent antioxidant and nephroprotective activity, as well as favorable effects on essential biochemical substances involved in active metabolic activities. As demonstrated by histopathological and microscopic examination, the biologically active chemical present in methanol extract had a positive effect on serum markers, enzyme, and non-enzyme-based antioxidant activities, as well as lowering the toxicity caused by EG in the rat (as nephroprotective activity) renal cells.


Assuntos
Anacardiaceae , Antioxidantes , Ratos , Animais , Antioxidantes/farmacologia , Extratos Vegetais/farmacologia , Extratos Vegetais/química , Metanol/farmacologia , Frutas , Staphylococcus aureus , Testes de Sensibilidade Microbiana , Antibacterianos/toxicidade , Antibacterianos/química , Água
3.
Mol Divers ; 2024 Mar 11.
Artigo em Inglês | MEDLINE | ID: mdl-38466554

RESUMO

The conventional one-drug-one-disease theory has lost its sheen in multigenic diseases such as Alzheimer's disease (AD). Propolis, a honeybee-derived product has ethnopharmacological evidence of antioxidant, anti-inflammatory, antimicrobial and neuroprotective properties. However, the chemical composition is complex and highly variable geographically. So, to leverage the potential of propolis as an effective treatment modality, it is essential to understand the role of each phytochemical in the AD pathophysiology. Therefore, the present study was aimed at investigating the anti-Alzheimer effect of bioactive in Indian propolis (IP) by combining LC-MS/MS fingerprinting, with network-based analysis and experimental validation. First, phytoconstituents in IP extract were identified using an in-house LC-MS/MS method. The drug likeness and toxicity were assessed, followed by identification of AD targets. The constituent-target-gene network was then constructed along with protein-protein interactions, gene pathway, ontology, and enrichment analysis. LC-MS/MS analysis identified 16 known metabolites with druggable properties except for luteolin-5-methyl ether. The network pharmacology-based analysis revealed that the hit propolis constituents were majorly flavonoids, whereas the main AD-associated targets were MAOB, ESR1, BACE1, AChE, CDK5, GSK3ß, and PTGS2. A total of 18 gene pathways were identified to be associated, with the pathways related to AD among the topmost enriched. Molecular docking analysis against top AD targets resulted in suitable binding interactions at the active site of target proteins. Further, the protective role of IP in AD was confirmed with cell-line studies on PC-12, in situ AChE inhibition, and antioxidant assays.

4.
Crit Rev Food Sci Nutr ; : 1-15, 2023 Aug 13.
Artigo em Inglês | MEDLINE | ID: mdl-37574586

RESUMO

Functional foods and their by-products contain a wide range of bioactive components with an array of health benefits and were proposed to improve public health, well-being, and others. To achieve a circular economy, the processing and extraction of flavonoids, phenolic compounds, and others from functional food and agri-food wastes will require the use of environmentally friendly, sustainable, and a low-cost solution. Extraction methods that can eliminate the use of organic solvents, suitable for use in the laboratory and production of extracts will be covered. This will include subcritical water extraction (SBE), pressurized hot water extraction (PHWE), supercritical fluid extraction (SFE), and others. Based on the selected analytical methods, the determination of the marker or bioactive compounds and chemical fingerprints will provide the control measures to identify the batch-to-batch variation of the composition of the functional food products obtained. The combination of chemical standardization with antioxidant assay, such as DPPH and ABTS+ will provide further information on the quality of the extracts. Lastly, to ascertain the biological and physiological relevance of the antioxidant properties of the target sample, treatment of the antioxidant compounds or extracts was carried out using cellular models, and validated using other experimental endpoints, such as metabolomics.

5.
Arch Insect Biochem Physiol ; 112(4): e21994, 2023 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-36567513

RESUMO

In this study, we have demonstrated, for the first time, the muscular protective effects of Piranhea trifoliata bark extract against Paraquat (PQ)-induced oxidative stress in Drosophila melanogaster. Exposure of D. melanogaster (Canton Special) to PQ caused oxidative stress, as evidenced by protein carbonyl and elevated acetylcholinesterase (AChE) activity levels. However, a diet supplemented with the P. trifoliata extracts (0.1 mg/ml) for 10 days ameliorates protein carbonyl levels and enzymatic activities of AChE and citrate synthase to prevent PQ damage. Also, P. trifoliata bark extracts showed in phytochemical assays the presence of phenols, at 46.06 mg EAG/g extract of total phenolic compounds, and a 40% 2,2-diphenyl-1-picryl-hydrazyl scavenging effect. The study showed the muscular protective function of the P. trifoliata extracts in D. melanogaster exposed to PQ. On the basis of the results, we contemplate that the bark of P. trifoliata might prevent and ameliorate human diseases caused by oxidative stress. The muscular action of the P. trifoliata extract can be attributed to the antioxidant constituents, while the precise mechanism of its action needs further investigation.


Assuntos
Drosophila melanogaster , Paraquat , Animais , Humanos , Paraquat/toxicidade , Acetilcolinesterase/metabolismo , Antioxidantes/farmacologia , Antioxidantes/metabolismo , Estresse Oxidativo , Extratos Vegetais/farmacologia , Extratos Vegetais/metabolismo , Fenóis/metabolismo , Fenóis/farmacologia
6.
Molecules ; 28(22)2023 Nov 09.
Artigo em Inglês | MEDLINE | ID: mdl-38005217

RESUMO

The number of patients with Alzheimer's disease (AD) continues to rise and, despite the efforts of researchers, there are still no effective treatments for this multifaceted disease. The main objective of this work was the search for multifunctional and more effective anti-Alzheimer agents. Herein, we report the evaluation of a library of quercetin-1,2,3-triazole hybrids (I-IV) in antioxidant, hydrogen peroxide-induced oxidative stress protection, and cholinesterases (AChE and BuChE) inhibitory activities. Hybrids IIf and IVa-d showed potent in vitro inhibitory activity on eqBuChE (IC50 values between 11.2 and 65.7 µM). Hybrid IIf, the best inhibitor, was stronger than galantamine, displaying an IC50 value of 11.2 µM for eqBuChE, and is also a competitive inhibitor. Moreover, toxicity evaluation for the most promising hybrids was performed using the Artemia salina toxicity assay, showing low toxicity. Hybrids IIf, IVb, and IVd did not affect viability at 12.5 µM and also displayed a protective effect against oxidative stress induced by hydrogen peroxide in cell damage in MCF-7 cells. Hybrids IIf, IVb, and IVd act as multifunctional ligands in AD pathologies.


Assuntos
Doença de Alzheimer , Fármacos Neuroprotetores , Humanos , Inibidores da Colinesterase/farmacologia , Inibidores da Colinesterase/uso terapêutico , Quercetina/farmacologia , Quercetina/uso terapêutico , Peróxido de Hidrogênio , Doença de Alzheimer/tratamento farmacológico , Galantamina , Acetilcolinesterase/metabolismo , Relação Estrutura-Atividade , Desenho de Fármacos , Fármacos Neuroprotetores/farmacologia , Fármacos Neuroprotetores/uso terapêutico
7.
Molecules ; 28(2)2023 Jan 04.
Artigo em Inglês | MEDLINE | ID: mdl-36677546

RESUMO

This study presents modeling and optimization of ultrasound-assisted extraction (UAE) of Melastoma malabathricum with the objective of evaluating its phytochemical properties. This one-factor-at-a-time (OFAT) procedure was conducted to screen for optimization variables whose domains included extraction temperature (XET), ultrasonic time (XUT), solvent concentration (XSC), and sample-to-liquid ratio (XSLR). Response surface methodology (RSM) coupled with Box-Behnken design (BBD) was applied to establish optimum conditions for maximum antioxidant extraction. Modeling and optimization conditions of UAE at 37 kHz, XET 32 °C for XUT 16 min and dissolved in an XSC 70% ethanol concentration at a XSLR 1:10 ratio yielded scavenging effects on 2,2-diphenyl-1-picryl-hydrazyl (DPPH) at 96% ± 1.48 and recorded values of total phenolic content (TPC) and total flavonoid content (TFC) at 803.456 ± 32.48 mg GAE (gallic acid equivalents)/g, and 102.972 ± 2.51 mg QE (quercetin equivalents)/g, respectively. The presence of high flavonoid compounds was verified using TWIMS-QTOFMS. Chromatic evaluation of phytochemicals using gas chromatography-mass spectrometry (GC-MS) revealed the presence of 14 phytocompounds widely documented to play significant roles in human health. This study provides a comparative evaluation with other studies and may be used for validation of the species' potential for its much-acclaimed medicinal and cosmeceutical uses.


Assuntos
Antioxidantes , Fenóis , Humanos , Antioxidantes/farmacologia , Antioxidantes/química , Fenóis/química , Flavonoides/química , Solventes , Extratos Vegetais/química , Etanol/química
8.
Molecules ; 27(11)2022 Jun 01.
Artigo em Inglês | MEDLINE | ID: mdl-35684500

RESUMO

Antioxidants have drawn the attention of the scientific community due to being related to the prevention of various degenerative diseases. The antioxidant capacity has been extensively studied in vitro, and different methods have been used to assess its activity. However, the main issues related to studying natural antioxidants are evaluating whether these antioxidants demonstrate a key role in the biological system and assessing their bioavailability in the organism. The majority of outcomes in the literature are controversial due to a lack of method standardization and their proper application. Therefore, this study aims to compile the main issues concerning the natural antioxidant field of study, comparing the most common in vitro methods to evaluate the antioxidant activity of natural compounds, demonstrating the antioxidant activity in biological systems and the role of the main antioxidant enzymes of redox cellular signaling and explaining how the bioavailability of bioactive compounds is evaluated in animal models and human clinical trials.


Assuntos
Antioxidantes , Animais , Antioxidantes/metabolismo , Antioxidantes/farmacologia , Disponibilidade Biológica , Oxirredução
9.
Bioorg Chem ; 106: 104465, 2021 01.
Artigo em Inglês | MEDLINE | ID: mdl-33229119

RESUMO

A new series of pyrrole analogs were developed via the microwave irradiation synthesis. Consequently, got a high yield of the products. As pyrroles are familiar for showing various biological properties, all obtained compounds were screened for their antioxidant properties, most of the compounds showing significant activity. In fact, the motifs 5e, 5g, 5h and 5m showed outstanding antioxidant properties. Further, to enlighten the biologically energetic behavior underlying the antioxidant activity, compounds DFT studies were performed. Noteworthy results have been attained and the structure activity relationship (SAR) was discussed with the support of this results. It was found that highly biological active compounds exhibited a low HOMO-LUMO energy gap (Eg) and the high Eg value compounds show very low/negligible or inactive antioxidant activities. In other cases, compounds containing high HOMO energy levels also provide high antioxidant activity. The thought-provoking point of our results is that theoretical descriptors of the HOMO-LUMO energy gap and the highest occupied molecular orbital energy are important descriptors in the bioorganic research to support the biological experiments.


Assuntos
Sequestradores de Radicais Livres/química , Maleimidas/química , Teoria da Densidade Funcional , Sequestradores de Radicais Livres/síntese química , Sequestradores de Radicais Livres/efeitos da radiação , Anidridos Maleicos/química , Anidridos Maleicos/efeitos da radiação , Maleimidas/síntese química , Maleimidas/efeitos da radiação , Micro-Ondas , Modelos Químicos , Estrutura Molecular , Fenilenodiaminas/química , Fenilenodiaminas/efeitos da radiação , Relação Estrutura-Atividade
10.
Bioorg Chem ; 107: 104535, 2021 02.
Artigo em Inglês | MEDLINE | ID: mdl-33341280

RESUMO

With the rapid development of nanotechnology, much has been anticipated with silver nanoparticles (AgNPs) due to their extensive industrial and commercial applications. However, it has raised concerns over environmental safety and human health effects. In this study, AgNPs were bio-fabricated using aqueous extract of Microchaete and their medical applications like antioxidant, anti-proliferative, and apoptosis were done. The biosynthesis of AgNPs was continuously followed by UV-vis spectrophotometric analysis. The physiochemical properties like shape, size, crystallinity, and polydispersity of the nanoparticles were determined by Scanning Electron Microscopy (SEM) along with EDX, Transmission Electron Microscope (TEM), Atomic Force Microscope (AFM), dynamic light scattering (DLS), and X-Ray Diffraction (XRD). Biosynthesized 7.0 nm sized AgNPs with the crystalline structure (crystalline size 4.8 nm) having a hydrodynamic diameter of 38.74 ± 2.6 nm was achieved due to the involvement of reducing agents present in the cyanobacterial extract. The IC50 values of the AgNPs were evaluated as 75 µg/ml and 79.41 µg/ml with HepG2 and MCF-7 cell lines. Different in-vitro cellular assays investigated in the present study exhibited antioxidant, anti-proliferative, and apoptotic activities. Probably delayed apoptosis in HepG2 and MCF-7 is due to better antioxidant activities of Microchaete based AgNPs.


Assuntos
Antineoplásicos/farmacologia , Antioxidantes/química , Apoptose/efeitos dos fármacos , Nanopartículas Metálicas/química , Prata/química , Antineoplásicos/síntese química , Antineoplásicos/química , Linhagem Celular Tumoral , Cianobactérias/química , Cianobactérias/metabolismo , Química Verde , Humanos , Peróxido de Hidrogênio/química , Nanopartículas Metálicas/toxicidade , Estresse Oxidativo/efeitos dos fármacos
11.
Metab Brain Dis ; 36(4): 571-579, 2021 04.
Artigo em Inglês | MEDLINE | ID: mdl-33559804

RESUMO

Epilepsy has been associated with several behavioral changes such as depression and anxiety while some antiepileptic drugs can precipitate psychiatric conditions in patients. This study evaluated the ameliorative effect of creatine on seizure severity and behavioral changes in pentylenetetrazole (PTZ) kindled mice. Mice were kindled by administering sub-convulsive doses of PTZ (35 mg/kg i.p.) at interval of 48 h. The naïve group (n = 7) constituted group 1, while successfully kindled mice were randomly assigned to five groups (n = 7). Group II served as vehicle treated group; groups III-V were treated with creatine 75, 150, and 300 mg/kg/day, p.o; Group V was given 25 mg/kg/day of phenytoin p.o. The treatment was for 15 consecutive days. The intensity of convulsion was scored according to a seven-point scale ranging from stage 0-7. Tail suspension test (TST) and Elevated plus maze (EPM) were utilized to assess depression and anxiety-like behavior respectively. After behavioral evaluation on day 15th, their brain was isolated and assayed for catalase, superoxide dismutase, reduced glutathione, and malondialdehyde. There was a significant (p < 0.05) reduction in the seizure scores, anxiety and depression-like behaviors in mice from the 5th day of treatment. The antioxidant assays revealed significant (p < 0.05) increase in catalase and reduced glutathione, and significant (p < 0.05) reduction in lipid peroxidation in treated mice. This study provides evidence for the seizure reducing property of creatine and its ameliorating potential on anxiety and depressive-like behaviors that follows seizure episodes.


Assuntos
Ansiedade/tratamento farmacológico , Creatina/uso terapêutico , Depressão/tratamento farmacológico , Pentilenotetrazol/toxicidade , Convulsões/tratamento farmacológico , Índice de Gravidade de Doença , Animais , Ansiedade/induzido quimicamente , Ansiedade/metabolismo , Convulsivantes/toxicidade , Creatina/farmacologia , Depressão/induzido quimicamente , Depressão/metabolismo , Relação Dose-Resposta a Droga , Glutationa/metabolismo , Peroxidação de Lipídeos/efeitos dos fármacos , Peroxidação de Lipídeos/fisiologia , Malondialdeído/metabolismo , Camundongos , Convulsões/induzido quimicamente , Convulsões/metabolismo
12.
Biomed Chromatogr ; 35(12): e5215, 2021 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-34269469

RESUMO

Contents of total flavonoids (TFc), total phenolics (TPc), and total crude polysaccharide (TCPc) in licorice from different origins were determined by optimized colorimetric methods, whereas five monomer ingredients (liquiritin [LQ], isoliquiritin [ILQ], liquiritigenin [LQG], isoliquiritigenin [ILQG], and glycyrrhizic acid [GA]) were simultaneously identified and quantified by HPLC-MS and HPLC. The results indicated that the contents of chemical compounds in licorice showed significant difference in different origins. Hierarchical cluster analysis and principal component analysis further proved that producing area indeed affected the quality including compounds and pharmacological activity in licorice. Licorice from Inner Mongolia exhibited the excellent DPPH assay, whereas samples from Gansu and Xinjiang showed high scavenging capacity to OH and ABTS free radicals. Meanwhile, α-Glu inhibitory activity of licorice samples was four times higher than the antioxidant activity. Correlation analysis made clear that TFc and TCPc both strongly contribute to DPPH scavenge capacity at P < 0.01 level, whereas TCPc contributed to α-Glu inhibitory activity at P < 0.05 level. This study would contribute to the comprehensive quality evaluation based on the compounds and pharmacological activity of licorice, and provide a reference for the choice of producing area to ensure the quality of licorice as a medicine.


Assuntos
Antioxidantes , Inibidores de Glicosídeo Hidrolases , Glycyrrhiza/química , Extratos Vegetais , Antioxidantes/análise , Antioxidantes/química , Antioxidantes/farmacologia , Quimiometria , Cromatografia Líquida de Alta Pressão , Flavonoides , Inibidores de Glicosídeo Hidrolases/análise , Inibidores de Glicosídeo Hidrolases/química , Inibidores de Glicosídeo Hidrolases/farmacologia , Espectrometria de Massas , Extratos Vegetais/análise , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Reprodutibilidade dos Testes
13.
Molecules ; 26(4)2021 Feb 16.
Artigo em Inglês | MEDLINE | ID: mdl-33669321

RESUMO

This study was aimed at preparing and characterizing solid lipid nanoparticles loading rutin (RT-SLNs) for the treatment of oxidative stress-induced diseases. Phospholipon 80H® as a solid lipid and Polysorbate 80 as surfactant were used for the SLNs preparation, using the solvent emulsification/diffusion method. We obtained spherical RT-SLNs with low sizes, ranging from 40 to 60 nm (hydrodynamic radius) for the SLNs prepared starting from 2% and 5% (w/w) theoretical amount. All prepared formulations showed negative zeta-potential values. RT was efficiently encapsulated within SLNs, obtaining high encapsulation efficiency and drug content percentages, particularly for SLNs prepared with a 5% theoretical amount of RT. In vitro release profiles and analysis of the obtained data applying different kinetic models revealed Fickian diffusion as the main mechanism of RT release from the SLNs. The morphology of RT-SLNs was characterized by scanning electron microscopy (SEM), whereas the interactions between RT and the lipid matrix were investigated by Raman spectroscopy, evidencing spectral modifications of characteristic bands of RT due to the establishment of new interactions. Finally, antioxidant activity assay on human glioblastoma astrocytoma (U373) culture cells showed a dose-dependent activity for RT-SLNs, particularly at the highest assayed dose (50 µM), whereas the free drug showed the lesser activity.


Assuntos
Lipídeos/química , Nanopartículas/química , Rutina/farmacologia , Antioxidantes/farmacologia , Bioensaio , Linhagem Celular Tumoral , Sobrevivência Celular/efeitos dos fármacos , Liberação Controlada de Fármacos , Humanos , Hidrodinâmica , Nanopartículas/ultraestrutura , Análise de Regressão , Análise Espectral Raman , Eletricidade Estática
14.
Chem Biodivers ; 17(8): e2000285, 2020 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-32478439

RESUMO

Tyrosinase is a type 3 copper enzyme responsible for skin pigmentation disorders, skin cancer, and enzymatic browning of vegetables and fruits. In the present article, 12 small molecules of 2-benzylidenehydrazine-1-carbothioamide were designed, synthesized and evaluated for their anti-tyrosinase activities followed by molecular docking and pharmacophore-based screening. Among synthesized thiosemicarbazone derivatives, one compound, (2E)-2-[(4-nitrophenyl)methylidene]hydrazine-1-carbothioamide, is the strongest inhibitor of mushroom tyrosinase with IC50 of 0.05 µM which demonstrated a 128-fold increase in potency compared to the positive control. Kinetic studies also revealed mix type inhibition by this compound. Docking studies confirmed the complete fitting of the synthesized compounds into the tyrosinase active site. The results underline the potential of 2-benzylidenehydrazine-1-carbothioamides as potent pharmacophore to extend the tyrosinase inhibition in drug discovery.


Assuntos
Compostos de Benzilideno/farmacologia , Inibidores Enzimáticos/farmacologia , Hidrazinas/química , Monofenol Mono-Oxigenase/antagonistas & inibidores , Tioamidas/química , Compostos de Benzilideno/química , Relação Dose-Resposta a Droga , Inibidores Enzimáticos/síntese química , Inibidores Enzimáticos/química , Cinética , Simulação de Acoplamento Molecular , Relação Estrutura-Atividade
15.
J Food Sci Technol ; 57(10): 3852-3863, 2020 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-32903995

RESUMO

The leaves of Ocimum sanctum were extracted in methanol (OsM) and sequentially fractionated with n-hexane (OsH), ethylacetate (OsE) and butanol (OsB) to find the best extraction solvent for antioxidants from the herb known for its medicinal values. OsB was rich in both total polyphenolic content (TPC) (212.26 ± 6.3 mg GAE/g extract) and total flavonoid contents (TFC) (54.51 ± 3.5 mg QE/g extract). OsE also had significantly high TPC (202.71 ± 5.5 mg GAE/g extract). The EC50 based on DPPH (3.91 ± 0.3 µg/ml), ABTS (1.6 ± 0.1 µg/ml) and phosphomolybdate (2.31 ± 0.1 µg/ml) for OsB; hydroxyl (5.3 ± 0.4 µg/ml), superoxide (7.32 ± 0.9 µg/ml) radicals for OsM and DPPH (8.61 ± 0.6 µg/ml), phosphomolybdate (2.43 ± 0.1 µg/ml) and ABTS (5.3 ± 0.4 µg/ml) for OsE were lower than ascorbic acid showing potential antioxidant properties. EC50 values of different fractions for DPPH anion, ABTS cation free radical scavenging and phosphomolybdate reducing property were significantly and positively correlated with TPC and TFC. LC-MS analysis of OsB and OsE showed the presence of luteolin, apigenin, rosmarinic, chlorogenic, caffeic acid and their derivatives. Quercetin is extracted in ethylacetate fraction. Overall data revealed that O. sanctum leaf extracts in butanol and ethylacetate with high polyphenolics and flavonoids, had strong antioxidant potential.

16.
Molecules ; 24(19)2019 Sep 26.
Artigo em Inglês | MEDLINE | ID: mdl-31561628

RESUMO

A series of 7-halogeno- (X = F, Cl, Br) and 7-methoxy-substituted acetylated 6-iodo-3-O-flavonol glycosides were prepared, and evaluated for inhibitory effect in vitro against acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) activities. 7-Bromo-2-(4-chlorophenyl)-6-iodo-4H-chromen-4-one-3-O-2,3,4,6-O-tetraacetyl-ß-d-glucopyranoside (2k) and 7-bromo-6-iodo-2-(4-methoxyphenyl)-4H-chromen-4-one-3-O-2,3,4,6-O-tetraacetyl-ß-d-glucopyranoside (2l) exhibited significant inhibitory effect against AChE activity when compared to the activity of the reference standard, donepezil. Compound 2k was found to be selective against AChE and to exhibit reduced inhibitory effect against BChE activity. 6-Iodo-7-methoxy-2-(4-methoxyphenyl)-4H-chromen-4-one-3-O-2,3,4,6-O-tetraacetyl-ß-d-glucopyranoside (2p) was found to exhibit increased activity against BChE, more so than the activity of donepezil. The most active compounds were also evaluated for inhibitory effect against ß-secretase activity and for potential radical scavenging activities. The experimental data were complemented with molecular docking (in silico) studies of the most active compounds into the active sites of these enzymes.


Assuntos
Secretases da Proteína Precursora do Amiloide/antagonistas & inibidores , Antioxidantes/farmacologia , Inibidores da Colinesterase/farmacologia , Glicosídeos/farmacologia , Secretases da Proteína Precursora do Amiloide/química , Antioxidantes/química , Sítios de Ligação , Inibidores da Colinesterase/química , Relação Dose-Resposta a Droga , Ativação Enzimática/efeitos dos fármacos , Flavonóis/química , Glicosídeos/química , Concentração Inibidora 50 , Cinética , Modelos Moleculares , Conformação Molecular , Estrutura Molecular , Ligação Proteica , Relação Estrutura-Atividade
17.
Anal Biochem ; 555: 59-66, 2018 08 15.
Artigo em Inglês | MEDLINE | ID: mdl-29908862

RESUMO

The development of simple, fast and reproducible techniques that provide information about the antioxidant activity (AA) of different compounds is essential to screen and discover new molecules with potential applications in the therapeutic, cosmetic, toxicological and food fields. Here, a novel and simple colorimetric method ("BCB assay") is proposed for measuring the AA of chemical compounds by protection of the reporter dye Brilliant Cresyl Blue (BCB) from loss of color due to oxidation by hypochlorite (a physiological oxidant). The decay in BCB blue color (λmax = 634 nm) in the presence of hypochlorite occurred in only 5 min and was used to track the AA of different molecules. Particularly, the AA of monoterpenes was demonstrated and used to quantify them at milimolar concentrations. Natural antioxidants like vitamins C and E, resveratrol, dithiothreitol, N-actyl-l-cysteine and glutathione were used as controls to validate the assay. Linalool, geraniol and 1,8-cineole were tested and showed in vitro AA in a concentration-dependent manner. The monoterpene concentrations providing 50% protection against oxidation (AA50) were 2.3, 36.2 and 135.0 mM for linalool, geraniol and 1,8-cineole respectively, suggesting interesting AA. The method provides a useful, fast, simple and low-cost tool to determine the in vitro AA of different molecules.


Assuntos
Antioxidantes/análise , Monoterpenos/análise , Oxazinas/química , Colorimetria/métodos , Oxirredução
18.
Bioorg Med Chem ; 26(8): 1511-1522, 2018 05 01.
Artigo em Inglês | MEDLINE | ID: mdl-29429576

RESUMO

Alzheimer's disease (AD) is a progressive neurodegenerative disorder with multiple factors associated with its pathogenesis. Our strategy against AD involves design of multi-targeted 2-substituted-4,5-diphenyl-1H-imidazole analogues which can interact and inhibit AChE, thereby, increasing the synaptic availability of ACh, inhibit BuChE, relieve induced oxidative stress and confer a neuroprotective role. Molecular docking was employed to study interactions within the AChE active site. In silico ADME study was performed to estimate pharmacokinetic parameters. Based on computational studies, some analogues were synthesized and subjected to pharmacological evaluation involving antioxidant activity, toxicity and memory model studies in animals followed by detailed mechanistic in vitro cholinesterase inhibition study. Amongst the series, analogue 13 and 20 are the most promising multi-targeted candidates which can potentially increase memory, decrease free radical levels and protect neurons against cognitive deficit.


Assuntos
Acetilcolinesterase/metabolismo , Doença de Alzheimer/tratamento farmacológico , Butirilcolinesterase/metabolismo , Inibidores da Colinesterase/farmacologia , Imidazóis/farmacologia , Fármacos Neuroprotetores/farmacologia , Doença de Alzheimer/metabolismo , Animais , Inibidores da Colinesterase/síntese química , Inibidores da Colinesterase/química , Modelos Animais de Doenças , Relação Dose-Resposta a Droga , Electrophorus , Feminino , Cavalos , Imidazóis/síntese química , Imidazóis/química , Masculino , Aprendizagem em Labirinto/efeitos dos fármacos , Transtornos da Memória/tratamento farmacológico , Transtornos da Memória/metabolismo , Camundongos , Estrutura Molecular , Fármacos Neuroprotetores/síntese química , Fármacos Neuroprotetores/química , Relação Estrutura-Atividade
19.
Sensors (Basel) ; 18(1)2018 Jan 11.
Artigo em Inglês | MEDLINE | ID: mdl-29324685

RESUMO

Since an unbalanced excess of reactive oxygen/nitrogen species (ROS/RNS) causes various diseases, determination of antioxidants that can counter oxidative stress is important in food and biological analyses. Optical/electrochemical nanosensors have attracted attention in antioxidant activity (AOA) assessment because of their increased sensitivity and selectivity. Optical sensors offer advantages such as low cost, flexibility, remote control, speed, miniaturization and on-site/in situ analysis. Electrochemical sensors using noble metal nanoparticles on modified electrodes better catalyze bioelectrochemical reactions. We summarize the design principles of colorimetric sensors and nanoprobes for food antioxidants (including electron-transfer based and ROS/RNS scavenging assays) and important milestones contributed by our laboratory. We present novel sensors and nanoprobes together with their mechanisms and analytical performances. Our colorimetric sensors for AOA measurement made use of cupric-neocuproine and ferric-phenanthroline complexes immobilized on a Nafion membrane. We recently designed an optical oxidant/antioxidant sensor using N,N-dimethyl-p-phenylene diamine (DMPD) as probe, from which ROS produced colored DMPD-quinone cationic radicals electrostatically retained on a Nafion membrane. The attenuation of initial color by antioxidants enabled indirect AOA estimation. The surface plasmon resonance absorption of silver nanoparticles as a result of enlargement of citrate-reduced seed particles by antioxidant addition enabled a linear response of AOA. We determined biothiols with Ellman reagent-derivatized gold nanoparticles.


Assuntos
Microscopia Eletroquímica de Varredura , Antioxidantes , Análise de Alimentos , Ouro , Nanopartículas Metálicas , Nanoestruturas , Oxirredução , Prata , Espectrofotometria
20.
Z Naturforsch C J Biosci ; 74(1-2): 17-23, 2018 Dec 19.
Artigo em Inglês | MEDLINE | ID: mdl-30500781

RESUMO

The current study was conducted to evaluate the antimicrobial, antioxidant, antileishmanial and cytotoxic potential of designed derivatives of 1,1'-(1,3-phenylenebis(methylene))bis(3-alkyl/aryl-1H-benzimidazol-3-ium) salts. The antibacterial potential of the test compounds was investigated against Staphylococcus aureus, Pseudomonas aeruginosa and two methicillin-resistant S. aureus (MRSA) strains (MRSA10, MRSA11), where compound 6 showed the best results. For brine shrimp lethality bioassay (BSLB), compound 6 again showed up to 100% mortality at 200 µg/mL and 56.7% mortality at 6.25 µg/mL. Antileishmanial assay was performed against Leishmania tropica at 20 µg/mL dosage, where 6 showed the most promising activity with 16.26% survival (83.74% mortality; IC50=14.63 µg/mL). The anticancer potential of the selected benzimidazole derivatives was evaluated against two selected cell lines (human colorectal cancer, HCT-116 and breast adenocarcinoma, MCF-7) using sulforhodamine B (SRB) assay. Compound 6 was found to be the most effective cytotoxic compound with 75% inhibition of HCT-116 proliferation at 1 mg/mL concentration. Succinctly, 6 exhibited impressive pharmacological potential that might be attributed to its higher lipophilic character owing to the longer N-substituted alkyl chains when compared to the other test compounds.


Assuntos
Anti-Infecciosos/química , Antineoplásicos/química , Antioxidantes/química , Benzimidazóis/química , Compostos Heterocíclicos/química , Anti-Infecciosos/farmacologia , Antineoplásicos/farmacologia , Benzimidazóis/farmacologia , Candida albicans/efeitos dos fármacos , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Compostos Heterocíclicos/farmacologia , Humanos , Leishmania/efeitos dos fármacos , Staphylococcus aureus Resistente à Meticilina/efeitos dos fármacos , Testes de Sensibilidade Microbiana , Sais/química , Staphylococcus aureus/efeitos dos fármacos
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