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1.
Curr Issues Mol Biol ; 46(9): 9639-9658, 2024 Sep 01.
Artigo em Inglês | MEDLINE | ID: mdl-39329925

RESUMO

Oxidative stress is a key factor that activates several transcription factors and mediators involved in the inflammatory pathways responsible for the pathogenesis of many chronic diseases. Targeting the expression of these mediators represents a promising approach to preventing these diseases. Cassinopsis ilicifolia leaf infusion is traditionally used for treating conditions such as inflammation and pain relief. Thus, the present study assessed the antioxidant and anti-inflammatory activities of the hydroethanolic leaf extract of C. ilicifolia using in vitro and cell-based assays. As a result, C. ilicifolia extract exhibited the highest DPPH• and ABTS•+ radical scavenging potential. At the same time, it weakly scavenged the Fe3+-TPTZ radical up to 200 µg/mL, thus suggesting a different antioxidant mechanism triggered during each assay. Additionally, C. ilicifolia extract inhibited NO production and 15-LOX activity with IC50 values of 21.10 µg/mL and 40.28 µg/mL, respectively. Further, C. ilicifolia extract was found to strongly inhibit ROS production in LPS-activated RAW 264.7 cells, and the study of its mechanism of action showed that it exerts its anti-inflammatory effect by downregulating the expression of inflammatory mediators such as IL-1ß, TNF-α, and COX-2. Overall, C. ilicifolia extract showed consistent potency in all assays, and the analysis of its phytochemical profile led to the identification of 30 compounds, among which the most abundant were secologanic acid (1), chlorogenic acid (3CQA) (2), monotropein (3), chlorogenic acid (5CQA) (4), geniposidic acid (5), rutin (6), quercetin 3-galactoside (7), astragalin-7-rhamnoside (8), and minecoside (9) that are possibly responsible for its anti-inflammatory and antioxidant activities. Therefore, our findings suggested the potential use of C. ilicifolia as an alternative source for developing plant-based products against oxidative stress and inflammation-related conditions.

2.
PeerJ ; 12: e17698, 2024.
Artigo em Inglês | MEDLINE | ID: mdl-39071122

RESUMO

Despite their overlooked status, weeds are increasingly recognized for their therapeutic value, aligning with historical reliance on plants for medicine and nutrition. This study investigates the medicinal potential of native weed species in Bangladesh, specifically pigments, antioxidants, and free radical scavenging abilities. Twenty different medicinal weed species were collected from the vicinity of Khulna Agricultural University and processed in the Crop Botany Department Laboratory. Pigment levels were determined using spectrophotometer analysis, and phenolics, flavonoids, and DPPH were quantified accordingly. Chlorophyll levels in leaves ranged from 216.70 ± 9.41 to 371.14 ± 28.67 µg g-1 FW, and in stems from 51.98 ± 3.21 to 315.89 ± 17.19 µg g-1 FW. Flavonoid content also varied widely, from 1,624.62 ± 102.03 to 410.00 ± 115.58 mg CE 100 g-1 FW in leaves, and from 653.08 ± 32.42 to 80.00 ± 18.86 mg CE 100 g-1 FW in stems. In case of phenolics content Euphorbia hirta L. displaying the highest total phenolic content in leaves (1,722.33 ± 417.89 mg GAE 100 g-1 FW) and Ruellia tuberosa L. in stems (977.70 ± 145.58 mg GAE 100 g-1 FW). The lowest DPPH 2.505 ± 1.028 mg mL-1was found in Heliotropium indicum L. leaves. Hierarchical clustering links species with pigment, phenolic/flavonoid content, and antioxidant activity. PCA, involving 20 species and seven traits, explained 70.07% variability, with significant PC1 (14.82%) and PC2 (55.25%). Leaves were shown to be superior, and high-performing plants such as E. hirta and H. indicum stood out for their chemical composition and antioxidant activity. Thus, this research emphasizes the value of efficient selection while concentrating on the therapeutic potential of native weed species.


Assuntos
Antioxidantes , Sequestradores de Radicais Livres , Plantas Daninhas , Plantas Medicinais , Bangladesh , Antioxidantes/química , Antioxidantes/análise , Antioxidantes/farmacologia , Plantas Daninhas/química , Sequestradores de Radicais Livres/química , Plantas Medicinais/química , Folhas de Planta/química , Flavonoides/análise , Flavonoides/química , Fenóis/análise , Fenóis/química , Extratos Vegetais/química , Pigmentos Biológicos/química , Pigmentos Biológicos/análise , Clorofila/análise
3.
Future Med Chem ; 14(21): 1507-1526, 2022 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-36268762

RESUMO

Background: To discover novel lead molecules against diabetes, Alzheimer's disease and oxidative stress, a library of arylated pyrazole-fused pyran derivatives, 1-20, were synthesized in a one-pot reaction. Materials & methods:1H-NMR spectroscopic and electron ionization mass spectrometry techniques were used to characterize the synthetic hybrid molecules 1-20. Analogs were screened against four indispensable therapeutic targets, including α-amylase, α-glucosidase, acetylcholinesterase and butyrylcholinesterase enzymes. Results: Except for derivatives 17 and 18, all other compounds exhibited varying degrees of inhibitory activities against target enzymes. The kinetic studies revealed that the synthetic molecules followed a competitive-type mode of inhibition for α-amylase and acetylcholinesterase enzymes, as well as a non-competitive mode of inhibition for α-glucosidase and butyrylcholinesterase enzymes. In addition, molecular docking studies identified crucial binding interactions of ligands with the enzyme's active site. Conclusion: These molecules may serve as a potential drug candidate to cure diabetes, Alzheimer's disease and oxidative stress in the future.


Assuntos
Doença de Alzheimer , Diabetes Mellitus , Humanos , Butirilcolinesterase/metabolismo , Acetilcolinesterase/metabolismo , Doença de Alzheimer/tratamento farmacológico , Simulação de Acoplamento Molecular , Inibidores da Colinesterase/química , alfa-Glucosidases/metabolismo , Piranos/uso terapêutico , Cinética , alfa-Amilases/metabolismo , Pirazóis/uso terapêutico , Relação Estrutura-Atividade , Estrutura Molecular
4.
Food Res Int ; 126: 108683, 2019 12.
Artigo em Inglês | MEDLINE | ID: mdl-31732040

RESUMO

Geopropolis is a stingless bee product compose mainly by soil, presenting complex composition geopropolis has bioactive compounds that will depend on geographical characteristics as well bee species, changing their chemical and biological properties. Thus the study aims to evaluate the solubility and chemical stability of geopropolis extracts, through radical capture capacity and reducing capacity. Besides, analysis of free and bonded phenolic compounds, and mineral composition. Geopropolis samples of Melipona mondury, Melipona quadrifasciata, Melipona scutellaris, Melipona seminigra and Tetragonisca angustula were analyzed. Both reducing compounds with a maximum of 2.96% GAE and free radical scavenging potential with a maximum of 5.84% AAE and 8.58% TE increases over 30 days of storage time. Also, methanolic extracts released at least 51% more reducing compounds and exhibited at least 27% more free radical scavenging potential in comparison to ethanolic extracts. The polyphenolic profile shows 31 compounds after acid and alkaline hydrolysis as cinnamic acid, ferulic acid, p-coumaric acid, aromadendrin, vanillin. For the mineral composition, sixteen minerals were found among essential and non-essential, differentiating each sample by chemometric PCA and HCA analysis according to geographic region. Geopropolis is a potential source of natural compounds that could enhance food quality, increasing the bioactive content and preventing oxygen damages in foods, likewise for pharmacological application for healthcare.


Assuntos
Polifenóis/análise , Própole/química , Oligoelementos/análise , Animais , Antioxidantes/análise , Abelhas , Brasil , Própole/análise
5.
Nat Prod Res ; 28(17): 1328-34, 2014.
Artigo em Inglês | MEDLINE | ID: mdl-24697259

RESUMO

The flavonoid-rich natural products exert a wide range of pharmacological properties. This investigation aimed at obtaining extracts from tobacco cultivars and waste enriched with flavonoids and purified from nicotine and phenolic acids, and evaluating their radical scavenging potential. Extraction with a mixture of ethyl acetate-methanol (1:1, v/v) was employed resulting in 100% yield for flavonoids and 36% yield for phenolic acids. The crude extracts were purified using preparative column chromatography on silica gel. The content of flavonoids in the purified extracts varied from 8.8 ± 1.1% to 14.3 ± 1.8%. Nicotine was not detected in amounts higher than 0.3 µg mL(-1). The content of phenolic acids was lower than 1.0%. The radical scavenging potential of extracts from tobacco cultivars exhibited values from IC50 = 35.0 ± 3.1 to 64.6 ± 7.5 µg mL(-1). The extracts obtained by the proposed procedure are enriched with flavonoids with high radical scavenging potential and are purified from nicotine and phenolic acids. They can be regarded as potential biopharmaceuticals.


Assuntos
Flavonoides/isolamento & purificação , Flavonoides/farmacologia , Sequestradores de Radicais Livres/isolamento & purificação , Sequestradores de Radicais Livres/farmacologia , Nicotiana/química , Algoritmos , Bulgária , Flavonoides/análise , Sequestradores de Radicais Livres/análise , Hidroxibenzoatos/análise , Concentração Inibidora 50 , Fenóis/análise , Extratos Vegetais/química , Folhas de Planta/química
6.
Indian J Pharm Sci ; 74(5): 481-6, 2012 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-23716882

RESUMO

A series of new 1,3-dihydro-3-hydroxy-3-(2-phenyl-2-oxoethyl)-2H-indol-2-ones (1a-g) and 1,3-dihydro-3-(2-phenyl-2-oxoethylidene)-2H-indol-2-ones (2a-g) were synthesised by Knoevenagel condensation of substituted indole-2,3-diones (isatins) with various acetophenones. The synthesised compounds were characterised by their physical data, elemental, IR, (1)H NMR, (13)C NMR and mass spectral analyses and their in vitro antioxidant activity was determined by 2,2-diphenyl-1-picrylhydrazyl free radical scavenging assay. These compounds showed moderate to good antioxidant activities as compared with the standard, ascorbic acid. The antioxidant potential of 3-hydroxy-3-substituted oxindoles (1a-g) increased in a concentration-dependent manner from 10 to 500 µg/ml with 5-fluoro and 5-methyl analogues showing maximum activity. Of 3-aroyl methylene indol-2-ones (2a-g), majority of compounds with halogen substitution at position 5 of isatin ring exhibited good antioxidant activity within a concentration range of 5-100 µg/ml and the maximum activity was observed at 20 and 25 µg/ml concentrations. Thus, our study provides evidence that some newly synthesised isatin derivatives exhibit substantial antioxidant activity at low concentrations.

7.
Indian J Pharm Sci ; 72(5): 644-9, 2010 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-21695001

RESUMO

Antioxidant potential of fruits of Artemisia nilagirica was studied using different in vitro models like 1,1-diphenyl-2-picryl hydrazyl, 2,2-azinobis-(3-ethylbenzothizoline-6-sulphonate), nitric oxide, superoxide, hydroxyl radical and lipid peroxidation. Both the ethanol and aqueous extracts of A. nilagirica fruits at 500 µg/ml showed maximum scavenging activity (89.33% and 89.14%) in quenching 1,1-diphenyl-2-picryl hydrazyl radical. The ethanol extract showed better scavenging activity (69.78%) of 1,1-diphenyl-2-picryl hydrazyl radical followed by the scavenging of nitric oxide radical (73.25%) compared to aqueous extract. In contrast, hydroxyl and superoxide radicals were effectively scavenged by aqueous extract. Total antioxidant capacity of ethanol and aqueous extracts at 500 µg/ml concentration was found to be 56.21 and 62.78 mg ascorbic acid equivalents, respectively. However, both the extracts showed only moderate lipid peroxidation inhibition activity. They were also found to contain considerable total phenols and flavonoids suggesting their role as an effective free radical scavenger. These findings suggest that phenolics and flavonoids in the fruits provide substantial antioxidant activity.

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