RESUMO
The article reports the chemical composition, antioxidant, six key enzymes inhibitory and antimicrobial activities of two solvent extracts (water and methanol) of leaves and stem bark of Uapaca togoensis. For chemical composition, methanol extract of stem bark exhibited significant higher total phenolic (129.86â mg GAE/g) and flavanol (10.44â mg CE/g) contents. Methanol extract of leaves and water extract of stem bark showed high flavonoids (20.94â mg RE/g) and phenolic acid (90.40â mg CAE/g) content, respectively. In addition, HPLC-ESI-TOF-MS analysis revealed that U. togoensis was rich in procyanidins. The methanol and water extracts of stem bark had overall superior antioxidant activity; however, only methanol extract of stem bark showed higher inhibition of cholinesterase (AChE: 2.57â mg GALAE/g; BChE: 4.69â mg GALAE/g), tyrosinase (69.53â mg KAE/g) and elastase (2.73â mmol CE/g). Potent metal chelating ability was showed by water extract of leaves (18.94â mg EDTAE/g), higher inhibition of amylase was detected for water extracts of leaves (0.94â mmol ACAE/g) and stem bark (0.92â mmol ACAE/g). The tested extracts have shown wide-spectrum antibacterial properties and these effects have shown to be more effective against Aspergillus ochraceus, Penicillium funiculosum, Trichoderma viride, Bacillus cereus, Escherichia coli and Pseudomonas aeruginosa. The results revealed that the antioxidant, enzyme inhibitory and antimicrobial activities depended on the extraction solvents and the parts of plant. Bioinformatics analysis on the 17 major compounds showed modulation of pathway associated with cancer. In brief, U. togoensis might be valuable as potential source of natural agents for therapeutic application.
Assuntos
Biflavonoides/química , Catequina/química , Biologia Computacional/métodos , Inibidores Enzimáticos/química , Magnoliopsida/química , Extratos Vegetais/química , Proantocianidinas/química , Amilases/antagonistas & inibidores , Amilases/metabolismo , Anti-Infecciosos/química , Anti-Infecciosos/isolamento & purificação , Anti-Infecciosos/farmacologia , Antioxidantes/química , Biflavonoides/isolamento & purificação , Biflavonoides/metabolismo , Biflavonoides/farmacologia , Catequina/isolamento & purificação , Catequina/metabolismo , Catequina/farmacologia , Cromatografia Líquida de Alta Pressão , Análise por Conglomerados , Inibidores Enzimáticos/isolamento & purificação , Inibidores Enzimáticos/metabolismo , Inibidores Enzimáticos/farmacologia , Fungos/efeitos dos fármacos , Bactérias Gram-Negativas/efeitos dos fármacos , Bactérias Gram-Positivas/efeitos dos fármacos , Magnoliopsida/metabolismo , Testes de Sensibilidade Microbiana , Monofenol Mono-Oxigenase/antagonistas & inibidores , Monofenol Mono-Oxigenase/metabolismo , Casca de Planta/química , Casca de Planta/metabolismo , Folhas de Planta/química , Folhas de Planta/metabolismo , Proantocianidinas/isolamento & purificação , Proantocianidinas/metabolismo , Proantocianidinas/farmacologia , Espectrometria de Massas por Ionização por ElectrosprayRESUMO
The chemical and pharmacological profiles of essential oils (EOs) hydrodistilled in yields of 0.03-0.77 % (w/w) from three exotic (Cinnamomum camphora, Petroselinum crispum, and Syzygium samarangense) and two endemic (Pittosporum senacia subsp. senacia and Syzygium coriaceum) medicinal plants were studied. GC-MS/GC-FID analysis of the EOs identified the most dominant components to be myristicin (40.3 %), myrcene (62.2 %), 1,8-cineole (54.0 %), ß-pinene (21.3 %) and (E)-ß-ocimene (24.4 %) in P. crispum, P. senacia and C. camphora, S. samarangense and S. coriaceum EOs, respectively. All EOs were found to possess anti-amylase (0.70-1.50â mM ACAE/g EO) and anti-tyrosinase (109.35-158.23â mg KAE/g) properties, whereas no glucosidase inhibition was displayed. Only Syzygium EOs acted as dual inhibitors of both acetyl- and butyryl-cholinesterases, while P. senacia and C. camphora EOs inhibited acetylcholinesterase selectively and P. crispum EO was inactive (AChE: 4.64-4.96â mg GALAE/g; BChE: 5.96 and 7.10â mg GALAE/g). Molecular docking revealed 1,8-cineole to present the best binding affinities with butyrylcholinesterase, amylase and tyrosinase, while both myristicin and ß-pinene with acetylcholinesterase and finally ß-pinene with glucosidase. In vitro antioxidant potency was also demonstrated in different assays (DPPH: 13.52-53.91â mg TE/g, ABTS: 5.49-75.62â mg TE/g; CUPRAC: 45.38-243.21â mg TE/g, FRAP: 42.49-110.64â mg TE/g; and phosphomolybdenum assay: 82.61-160.93â mM TE/g). Principal component analysis revealed the EOs to differ greatly in their bioactivities due to their chemodiversity. This study has unveiled some interesting preliminary pharmacological profiles of the EOs that could be explored for their potential applications as phytotherapeutics.
Assuntos
Antioxidantes/farmacologia , Inibidores Enzimáticos/farmacologia , Óleos Voláteis/farmacologia , Análise de Componente Principal , Acetilcolinesterase/metabolismo , Amilases/antagonistas & inibidores , Amilases/metabolismo , Antioxidantes/química , Antioxidantes/isolamento & purificação , Benzotiazóis/antagonistas & inibidores , Compostos de Bifenilo/antagonistas & inibidores , Butirilcolinesterase/metabolismo , Cinnamomum camphora/química , Relação Dose-Resposta a Droga , Avaliação Pré-Clínica de Medicamentos , Inibidores Enzimáticos/química , Inibidores Enzimáticos/isolamento & purificação , Cromatografia Gasosa-Espectrometria de Massas , Maurício , Simulação de Acoplamento Molecular , Estrutura Molecular , Monofenol Mono-Oxigenase/antagonistas & inibidores , Monofenol Mono-Oxigenase/metabolismo , Óleos Voláteis/química , Óleos Voláteis/isolamento & purificação , Petroselinum/química , Picratos/antagonistas & inibidores , Rosales/química , Relação Estrutura-Atividade , Ácidos Sulfônicos/antagonistas & inibidores , Syzygium/químicaRESUMO
Lagochilus species are mainly distributed in Central Asia and widely used in folk medicine as a sedative and haemostatic. The present investigation reports on the extraction by hydrodistillation and the chemical composition of three Lagochilus species (L. gypsaceus, L. inebrians and L. setulosus) essential oils from Uzbekistan. The chemical composition of these essential oils was determined by GC-MS. The results showed that the studied essential oils are made up mainly of linalool (11.97%), ß-ionone (11.75%), trans-chrysanthenyl acetate (7.15%), α-terpineol (7.40%) for L. gypsaceus; trans-chrysanthenyl acetate (9.40%), eugenol (7.01%), trans-verbenol (3.85%), bicyclo[3.1.1]hept-3-en-2-one (3.76%), pinocarvone (3.43%) for L. inebrians; and finally 2,4-bis(1,1-dimethylethyl)phenol (19.78%), bicyclo[3.1.1]hept-2-en-4-ol (5.43%), hexadecanoic acid (5.39%), limonene (5.19%), 2-hexenal (5.03%) for L. setulosus. The best antioxidant and tyrosinase inhibitory activity was observed for the essential oil of L. inebrians. However, L. setulosus essential oil exhibited the strongest inhibitory effect against amylase.
Assuntos
Lamiaceae/química , Óleos Voláteis , Amilases/antagonistas & inibidores , Antioxidantes/isolamento & purificação , Antioxidantes/farmacologia , Cromatografia Gasosa-Espectrometria de Massas , Limoneno , Monofenol Mono-Oxigenase/antagonistas & inibidores , Óleos Voláteis/farmacologia , Compostos Fitoquímicos/isolamento & purificação , Compostos Fitoquímicos/farmacologia , UzbequistãoRESUMO
BACKGROUND: This study provides an insight into the impact of ultrasound-assisted extraction with water as solvent (UAEW) and extraction by supercritical carbon dioxide (SC-CO2 ) with 5% EtOH on antioxidant and enzyme inhibitory activity in regard to the chemical profile of the edible and medicinal mushroom, Pleurotus pulmonarius. RESULTS: Extraction efficiency was between 0.36% and 63.32%, depending on the extraction technique. The main compounds in the extracts were fatty acids. Supercritical CO2 extraction with co-solvent was the most suitable method for obtaining extracts that were rich in ergosterol content, reaching a value of 40.1 mg g-1 . The UAEW of crude mushroom powder ensured the highest yield, as well as the extracts with best antioxidative activity. The measurements of enzyme inhibitory activity revealed that all types of investigated extracts exhibited only tyrosinase and amylase inhibition at a significant level. CONCLUSION: Based on our results, the extraction methods significantly affected the chemical profile and bioactivity of P. pulmonarius. © 2020 Society of Chemical Industry.
Assuntos
Amilases/antagonistas & inibidores , Cromatografia com Fluido Supercrítico/métodos , Inibidores Enzimáticos/isolamento & purificação , Monofenol Mono-Oxigenase/antagonistas & inibidores , Extratos Vegetais/isolamento & purificação , Pleurotus/química , Amilases/química , Inibidores Enzimáticos/química , Ergosterol/química , Ergosterol/isolamento & purificação , Humanos , Monofenol Mono-Oxigenase/química , Extratos Vegetais/química , UltrassomRESUMO
BACKGROUND: Medicinal plants are widely used in many cultures, traditions, and civilizations worldwide. Plants with high contents of the valuable biological compounds can efficiently cure many diseases. This study is aimed at assessing, for the first time, the anti-α-amylase, antilipase, antimicrobial, and cytotoxic activities of Nonea obtusifolia (Willd.) DC. of five extracts from Palestine. METHODS: The antimicrobial activity was estimated using well diffusion method for N. obtusifolia plant of five extracts against eight ATCC (American Type Culture Collection) and clinical isolates. The cytotoxic effects for these extracts were evaluated against HeLa (cervical) carcinoma cells using MTS (3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2H-tetrazolium) assay. Moreover, the lipase and α-amylase inhibitory properties were determined using standard biomedical assays. RESULTS: The acetone extract of N. obtusifolia plant showed a more potent α-amylase inhibitory compared with acarbose with IC50 values of 25.7 ± 0.08 and 28.18 ± 1.22 µg/ml, respectively. Additionally, the acetone and methanol extracts revealed moderate antilipase activity compared to orlistat with IC50 values of 30.19 ± 0.11, 33.11 ± 0.13, and 12.3 ± 0.35 µg/ml, respectively. The methylene chloride extract was found to inhibit the growth of all the tested bacterial and fungal strains and also found to have potential cytotoxic effect against HeLa cancer cell line. CONCLUSION: This research work reports for the first time the biological activity of N. obtusifolia from Palestine, and the results were promising indicating that N. obtusifolia extracts contain valuable bioactive molecules that have a potential anti-α-amylase, antilipase, antibacterial, and antifungal cytotoxic potentials. Therefore, N. obtusifolia could have a medical significance in the future.
Assuntos
Amilases/antagonistas & inibidores , Anti-Infecciosos/farmacologia , Boraginaceae/química , Lipase/antagonistas & inibidores , Extratos Vegetais/farmacologia , Acetona/química , Animais , Antibacterianos/farmacologia , Antioxidantes/farmacologia , Difusão , Células HeLa , Humanos , Concentração Inibidora 50 , Lipase/química , Lipídeos/química , Cloreto de Metileno/química , Testes de Sensibilidade Microbiana , Orlistate/farmacologia , Pâncreas/enzimologia , Compostos Fitoquímicos/farmacologia , Folhas de Planta/química , Plantas Medicinais/química , Suínos , alfa-Amilases/químicaRESUMO
The purpose of current study was green synthesis of silver nanoparticles (AgNPs) from seeds and wild Silybum plants in comparison with their respective extracts followed by characterization and biological potency. The biologically synthesized AgNPs were subjected to characterization using techniques like XRD, FTIR, TEM, HPLC and SPE. Highly crystalline and stable NPs were obtained using Silybum wild plant (NP1) and seeds (NP3) with size range between 18.12 and 13.20 nm respectively. The synthesized NPs and their respective extracts revealed a vast range of biological applications showing antibacterial, antioxidant, anti-inflammatory, cytotoxic and anti-aging potencies. The highest antioxidant activity (478.23 ± 1.9 µM, 176.91 ± 1.3 µM, 83.5 ± 1.6% µgAAE/mg, 156.32 ± 0.6 µgAAE/mg) for ABTS, FRAP, FRSA, TRP respectively was shown by seed extract (NP4) followed by highest value of (117.35 ± 0.9 µgAAE/mg) for TAC by wild extract (NP2). The highest antifungal activity (13 mm ± 0.76) against Candida albicans was shown by NP3 while antibacterial activity of (6 mm against Klebsiella pneumonia) was shown by NP3 and NP4. The highest anti-inflammatory activity (38.56 ± 1.29 against COX1) was shown by NP2. Similarly, the high value of (48.89 ± 1.34 against Pentosidine-Like AGEs) was shown by NP4. Also, the high anti-diabetic activity (38.74 ± 1.09 against α-amylase) was shown by NP4. The extracts and the synthesized NPs have shown activity against hepato-cellular carcinoma (HepG2) human cells. The HPLC analysis revealed that the highest value of silymarin component (silybin B 2289 mg/g DW) was found for NP4. Silydianin is responsible for capping. Among the green synthesized AgNPs and the extracts used, the effect of NP4 was most promising for further use.
Assuntos
Nanopartículas Metálicas/química , Extratos Vegetais/química , Prata/química , Silybum marianum/química , Amilases/antagonistas & inibidores , Amilases/metabolismo , Animais , Anti-Infecciosos/síntese química , Anti-Infecciosos/química , Anti-Infecciosos/farmacologia , Anti-Inflamatórios/síntese química , Anti-Inflamatórios/química , Anti-Inflamatórios/farmacologia , Antidiuréticos/química , Antidiuréticos/metabolismo , Antioxidantes/química , Candida albicans/efeitos dos fármacos , Bovinos , Sobrevivência Celular/efeitos dos fármacos , Ciclo-Oxigenase 1/metabolismo , Química Verde , Células Hep G2 , Humanos , Klebsiella pneumoniae/efeitos dos fármacos , Silybum marianum/metabolismo , Sementes/química , Sementes/metabolismoRESUMO
This study aimed to compare the effects of four solvent extractions on the physicochemical properties, antioxidant and hypoglycemic activities of polysaccharides from Mentha haplocalyx (MHPs). The solvent extractions included hot water, citric acid (pH 3.0), 5% NaOH/0.05% NaBH4 and 0.9% NaCl. Four corresponding MHPs named as MHP-W, MHP-C, MHP-A and MHP-S were obtained, respectively. The experimental results showed that the extraction yields, basic chemical components, monosaccharide contents, molecular weights, antioxidant and hypoglycemic activities of four MHPs were significantly different. However, their thermal stabilities, preliminary structural characteristics and monosaccharide types were similar. MHP-A possessed the highest extraction yield of 9.37 ± 0.24% and the smallest molecular weight. MHP-W had the highest uronic acid content and the largest molecular weight. More specifically, MHP-C exhibited the highest sugar content, the most remarkable antioxidant abilities of DPPH radical scavenging activity and ferric reducing power, and the strongest inhibitory activities on α-glucosidase and α-amylase. The above results indicated that MHP-C extracted with citric acid could be served as a promising bioactive substance for applications in the functional food and medicine industries.
Assuntos
Inibidores de Glicosídeo Hidrolases , Mentha/química , Extratos Vegetais/química , Polissacarídeos , Amilases/antagonistas & inibidores , Antioxidantes/química , Antioxidantes/isolamento & purificação , Inibidores de Glicosídeo Hidrolases/química , Inibidores de Glicosídeo Hidrolases/isolamento & purificação , Estrutura Molecular , Polissacarídeos/química , Polissacarídeos/isolamento & purificação , SolventesRESUMO
Pile-fermentation is the most important process of producing ripened pu-erh tea. To study the chemical changes of tea leaves during pile-fermentation (PF), liquid chromatography coupled with tandem mass spectrometry (LC-MS) was used. Untargeted metabolomics analysis revealed that the first stage of PF is crucial in transforming the original secondary metabolites, whereas the contents of flavan-3-ols and gallic acid were decreased after long-term PF. Targeted metabolomics analysis indicated that the levels of puerins (N-ethyl-2-pyrrolidinone substituted gallocatechin and catechin) were significant increased after the first stage of PF, but after long-term PF the levels of flavonol glycosides, procyanidins and galloylated flavan-3-ols were significantly decreased. Accordingly, long-term PF also decreased the inhibition of α-amylase and α-glucosidase activities of the extracts. As a conclusion, pile-fermentation is an important step of changing the polyphenols and bioactivities of pu-erh tea.
Assuntos
Camellia/metabolismo , Metabolômica , Amilases/antagonistas & inibidores , Amilases/metabolismo , Camellia/química , Análise por Conglomerados , Fermentação , Flavonóis/metabolismo , Ácido Gálico/metabolismo , Glicosídeos/metabolismo , Análise dos Mínimos Quadrados , Extratos Vegetais/química , Extratos Vegetais/metabolismo , Folhas de Planta/química , Folhas de Planta/metabolismo , Análise de Componente Principal , Proantocianidinas/metabolismoRESUMO
Olive waste was used as a sustainable resource because it contained a variety of valuable compounds. The polyphenols active fraction from enrichment by microporous resin and extraction with ethyl acetate were analysed by different chromatographic methods. A total of 14 polyphenolic compounds were isolated and identified by structure elucidation. Based on the above obtained compounds, tyrosol was selected as a characteristic polyphenol and participated in transesterification reaction to synthesise ß-ketoester using Yb(OTf)3. Then the Biginelli reaction with benzaldehyde, urea and ketoester (1:1.2:1.2) was performed at 90 °C for 3.0 h under the acidic condition. In addition, the ß-ketoester prepared using tyrosol with benzyl had a greater inhibitory effect on α-glucosidase and α-amylase, and the inhibition of enzyme activity for 3, 4-dihydropyrimidinone derivatives prepared using abovementioned ß-ketoester was improved significantly. Meanwhile, fluorine-containing dihydropyrimidinone derivatives were considerable inhibitors for both enzymes.
Assuntos
Inibidores de Glicosídeo Hidrolases/isolamento & purificação , Olea/química , Extratos Vegetais/química , Polifenóis/isolamento & purificação , alfa-Amilases/antagonistas & inibidores , Amilases/antagonistas & inibidores , Inibidores de Glicosídeo Hidrolases/farmacologia , Polifenóis/análise , alfa-Glucosidases/efeitos dos fármacosRESUMO
Bunium species have been reported to be used both as food and in traditional medicines. The scientific community has attempted to probe into the pharmacological and chemical profiles of this genus. Nonetheless, many species have not been investigated fully to date. In this study, we determined the phenolic components, antimicrobial, antioxidant, and enzyme inhibitory activities of aerial parts of four Bunium species (B. sayai, B. pinnatifolium, B. brachyactis and B. macrocarpum). Results showed that B. microcarpum and B. pinnatifolium were strong antioxidants as evidenced in the DPPH, ABTS, CUPRAC, and FRAP assays. B. brachyactis was the most effective metal chelator, and displayed high enzyme inhibition against cholinesterase, tyrosinase, amylase, glucosidase, and lipase. The four species showed varied antimicrobial activity against each microorganism. Overall, they showed high activity against P. mirabilis and E. coli (MIC and MBC <1â¯mg mL-1). B. brachyactis was more effective against Aspergillus versicolor compared to the standard drug ketoconazole. B. brachyactis was also more effective than both ketoconazole and bifonazole against Trichoderma viride. B. sayai was more effective than ketoconazole in inhibiting A. fumigatus. B. sayai was most non-toxic to HEK 293 (cellular viabilityâ¯=â¯117%) and HepG2 (cellular viabilityâ¯=â¯104%). The highest level of TPC was observed in B. pinnatifolium (35.94â¯mg GAE g-1) while B. microcarpum possessed the highest TFC (39.21 mg RE g-1). Seventy four compounds were detected in B. microcarpum, 70 in B. brachyactis, 66 in B. sayai, and 51 in B. pinnatifolium. Quinic acid, chlorogenic acid, pantothenic acid, esculin, isoquercitrin, rutin, apigenin, and scopoletin were present in all the four species. This study showed that the four Bunium species are good sources of biologically active compounds with pharmaceutical and nutraceutical potential.
Assuntos
Apiaceae/química , Apiaceae/classificação , Amilases/antagonistas & inibidores , Amilases/metabolismo , Animais , Anti-Infecciosos/análise , Anti-Infecciosos/farmacologia , Antioxidantes/análise , Antioxidantes/farmacologia , Apigenina/análise , Apigenina/metabolismo , Ácido Clorogênico/análise , Ácido Clorogênico/farmacologia , Inibidores da Colinesterase/análise , Inibidores da Colinesterase/farmacologia , Enterobacter cloacae/efeitos dos fármacos , Enterobacter cloacae/metabolismo , Inibidores Enzimáticos/análise , Inibidores Enzimáticos/farmacologia , Escherichia coli/efeitos dos fármacos , Escherichia coli/metabolismo , Esculina/análise , Esculina/farmacologia , Glucosidases/antagonistas & inibidores , Glucosidases/metabolismo , Células HEK293 , Células Hep G2 , Humanos , Lipase/antagonistas & inibidores , Lipase/metabolismo , Camundongos , Testes de Sensibilidade Microbiana , Monofenol Mono-Oxigenase/antagonistas & inibidores , Monofenol Mono-Oxigenase/metabolismo , Ácido Pantotênico/análise , Ácido Pantotênico/farmacologia , Fenóis/análise , Fenóis/farmacologia , Extratos Vegetais/análise , Extratos Vegetais/farmacologia , Proteus mirabilis/efeitos dos fármacos , Proteus mirabilis/metabolismo , Pseudomonas aeruginosa/efeitos dos fármacos , Pseudomonas aeruginosa/metabolismo , Quercetina/análogos & derivados , Quercetina/análise , Quercetina/farmacologia , Ácido Quínico/análise , Ácido Quínico/farmacologia , Células RAW 264.7 , Rutina/análise , Rutina/farmacologiaRESUMO
This study aimed to reveal chemical profiles and biological activities of ethyl acetate (EA), methanol (MeOH), and water extracts of Lotus corniculatus. Ethnobotanical reports have indicated the importance of phytochemical properties of the genus Lotus. In this study, the effects of medicinal plant extracts on antioxidant (DPPH, ABTS, CUPRAC, FRAP, phosphomolybdenum, and metal chelating assays), enzyme inhibitory (on cholinesterase, tyrosinase, a-amylase and a-glucosidase), DNA protection and anticancer properties (including anti-proliferative, cell death and telomerase activity marker gene analysis, apoptotic DNA fragmentation analysis, cell migration test) were evaluated. According to chemical analysis, quercetin derivatives geraldol, isorhamnetin and kaempferol-O-coumaroylhexoside-O-deoxyhexoside isomers were dominant in the extracts. MeOH extracts showed the highest total flavonoids capacity with 21.13â¯mg RE/g. EA extract showed the strongest anti-amylase activity among the tested extracts. Water extract had the most protective activity against plasmid DNA. To indicate cell survival, MTT test was performed against human MCF-7 and MDA-MB-231 breast cancer cells. Half-maximal inhibitory concentration for cells were calculated and used for detection of mechanisms behind the cancer cell death. EA extract showed up-regulation of Bax proapoptotic gene and apoptotic DNA fragmentation activity on highly invasive MDA-MB-231 cells. Beclin-1 and LC3-II autophagy genes were higly expressed after treatment of MCF-7 cells with EA extracts. EA and MeOH extracts inhibited cell migration ability of both cancer cells. Linoleamide, was dominant component in EA extract and caused apoptosis on MDA-MB-231 breast cancer cells via increasing intranuclear Ca²+. The detailed mechanism behind the anticancer properties should be further investigated.
Assuntos
Antineoplásicos Fitogênicos/farmacologia , Apoptose , Autofagia , Neoplasias da Mama/tratamento farmacológico , Lotus/química , Extratos Vegetais/farmacologia , Acetatos/química , Amilases/antagonistas & inibidores , Animais , Antioxidantes/farmacologia , Linhagem Celular Tumoral , Fragmentação do DNA , Ensaios de Seleção de Medicamentos Antitumorais , Feminino , Flavonoides/análise , Flavonoides/farmacologia , Humanos , Células MCF-7 , Melanoma Experimental , Metanol/química , Camundongos , Estresse Oxidativo , Água/químicaRESUMO
Certain food properties (ex.: pH, polyphenolic composition) can inhibitdigestive amylases and thereby slow down starch digestion. Our aim was twofold. (1) To determine the impact of21 beverages and condiments (coffees, teas, wines, vinegars and lemon juice)on salivary and pancreatic amylolysis: inhibition ranged from 10% to 100%in our experimental conditions. (2) To investigate the effect of one black tea and lemon juice (selected for their strong inhibitory capacity) on starch hydrolysis during dynamicoro-gastro-intestinal digestion of bread. Compared to water (control), the effect of black tea was limited to a ≈20% reduction of released oligosaccharides during the intestinal phase. Lemon juice had a remarkable effect, completely interrupting gastric amylolysis by salivary amylase via a preliminary acidification of gastric contents. These results provide a strong biochemical rationale for the development of dietary strategies to improve the glycaemic impact of starch-rich meals which could be tested in vivo.
Assuntos
Amilases/metabolismo , Camellia sinensis/química , Sucos de Frutas e Vegetais/análise , Amido/metabolismo , Chá/química , Amilases/antagonistas & inibidores , Pão/análise , Camellia sinensis/metabolismo , Humanos , Hidrólise , Pâncreas/enzimologia , Saliva/enzimologia , Chá/metabolismoRESUMO
Heracleum sphondylium L. subsp. ternatum (Velen.) Brummitt. commonly known as "hogweed" is traditionally used to manage several human ailments. This investigation assessed, for the first time, the enzyme inhibitory properties, antioxidant activity, phytochemical profile, antimutagenic, and antimicrobial potential of the ethyl acetate, methanol, and water extracts of H. sphondylium. We also established the possible interactions of identified phenolic compounds with cholinesterases, amylase, glucosidase, and tyrosinase using in silico docking studies. Chlorogenic acid was found in high amounts in the methanol extract of H. sphondylium. The methanol extract was an effective inhibitor of acetylcholinesterase (1.70 mg galantamine equivalent (GALAE)/g extract) while the ethyl acetate extract showed pronounced inhibitory action against butyrylcholinesterase (1.77 mg GALAE/g extract). The extracts exhibited low inhibition against amylase (0.12-0.84 mmol acarbose equivalent (ACAE)/g extract) and a more pronounced inhibition against glucosidase (2.29-3.65 mmol ACAE/g extract). In silico results showed that rutin and quercetin (-70.4 and -72.2 Kcal/mol, for rutin and quercetin respectively) docked to the enzymatic cavity of acetylcholinesterase but these phenolic compounds showed less affinity with butyrylcholinesterase (-15.0 and -5.2 Kcal/mol, for rutin and quercetin respectively). The extracts did not induce any mutations on the bacterial strains, while they have excellent antimutagenic capacity against well-known mutagens (inhibition values 98%, 97% and 96%). The methanol extract (0.78 mg/ml) showed moderate antifungal activity while the ethyl acetate extract (0.78-3.12 mg/ml) showed weak to moderate antimicrobial activity. This study provides valuable baseline data which might serve for the development of future pharmacophores for the management of human ailments.
Assuntos
Antibacterianos/farmacologia , Antifúngicos/farmacologia , Inibidores Enzimáticos/farmacologia , Heracleum/química , Extratos Vegetais/farmacologia , Acetilcolinesterase/metabolismo , Amilases/antagonistas & inibidores , Amilases/metabolismo , Antibacterianos/química , Antibacterianos/isolamento & purificação , Antifúngicos/química , Antifúngicos/isolamento & purificação , Bactérias/efeitos dos fármacos , Butirilcolinesterase/metabolismo , Inibidores Enzimáticos/química , Inibidores Enzimáticos/isolamento & purificação , Fungos/efeitos dos fármacos , Humanos , Testes de Sensibilidade Microbiana , Simulação de Acoplamento Molecular , Estrutura Molecular , Extratos Vegetais/química , Extratos Vegetais/isolamento & purificaçãoRESUMO
The genus Scrophularia has received much interest with regards to its traditional uses against eczema, psoriasis, and mastitis. Yet, the medicinal properties of some species still need to be scientifically validated. The present study was designed to investigate into the biological properties of various solvent extracts (ethyl acetate, methanol, and aqueous) of the roots and aerial parts of Scrophularia lucida based on its antioxidant, anti-inflammatory, and enzyme inhibitory activities together with phytochemical screening. Our results revealed that the solvent extracts differed in their biological effectiveness. The root ethyl acetate extract showed the highest ABTS scavenging, FRAP, CUPRAC, and inhibitory activity against AChE and α-glucosidase. The ethyl acetate extract of the aerial parts displayed the highest BChE and α-amylase inhibition and antioxidant effect in the phosphomolybdenum assay, while the methanol extracts of both parts were the most effective DPPH⢠scavengers and tyrosinase inhibitors. The methanol extracts of the root and aerial parts also inhibited NO production in lipopolysaccharide (LPS)-stimulated murine leukemic monocyte-macrophage cell (4.99% and 10.77%, respectively), at 31.25 µg/mL concentration. The highest TPC (34.98 mg GAE/g extract) and TFC (48.33 mg RE/g extract) were observed in the ethyl acetate extract of the root and aerial parts, respectively. The most abundant compounds in the root ethyl acetate extract were luteolin (852 µg/g extract), rosmarinic acid (522 µg/g extract), and hesperidin (394 µg/g extract) while kaempferol was most abundant in the ethyl acetate extract of the aerial parts (628 µg/g extract). In silico experiments were conducted on tyrosinase and the higher docking values were observed for rosmarinic acid and hesperidin. The present findings provide base line information which tend to support the potential use of S. lucida in the management of several chronic diseases, including Alzheimer's disease and diabetes mellitus.
Assuntos
Anti-Inflamatórios/farmacologia , Antioxidantes/farmacologia , Cromatografia Líquida de Alta Pressão , Simulação por Computador , Inibidores Enzimáticos/farmacologia , Extratos Vegetais/farmacologia , Scrophularia/química , Acetatos/química , Amilases/antagonistas & inibidores , Amilases/metabolismo , Animais , Anti-Inflamatórios/isolamento & purificação , Antioxidantes/química , Antioxidantes/isolamento & purificação , Inibidores da Colinesterase/isolamento & purificação , Inibidores da Colinesterase/farmacologia , Cinamatos/isolamento & purificação , Cinamatos/farmacologia , Depsídeos/isolamento & purificação , Depsídeos/farmacologia , Inibidores Enzimáticos/química , Inibidores Enzimáticos/isolamento & purificação , Inibidores de Glicosídeo Hidrolases/isolamento & purificação , Inibidores de Glicosídeo Hidrolases/farmacologia , Hesperidina/isolamento & purificação , Hesperidina/farmacologia , Quempferóis/isolamento & purificação , Quempferóis/farmacologia , Luteolina/isolamento & purificação , Luteolina/farmacologia , Macrófagos/efeitos dos fármacos , Macrófagos/metabolismo , Metanol/química , Camundongos , Simulação de Acoplamento Molecular , Simulação de Dinâmica Molecular , Estrutura Molecular , Monofenol Mono-Oxigenase/antagonistas & inibidores , Monofenol Mono-Oxigenase/metabolismo , Óxido Nítrico/metabolismo , Componentes Aéreos da Planta/química , Extratos Vegetais/química , Extratos Vegetais/isolamento & purificação , Raízes de Plantas/química , Células RAW 264.7 , Scrophularia/classificação , Solventes/química , Relação Estrutura-Atividade , Ácido RosmarínicoRESUMO
The toxicity and safety associated with the use of medicinal plants remains a major concern. In this study, the antidiabetic properties of the dichloromethane (DCM) fraction of C. volubile leaves were investigated in vitro. Its cytotoxic effect and mechanism of toxicity were also investigated in Human Embryonic Kidney (HEK293) cells. The fraction was subjected to in vitro antioxidant assays using the 2,2'-diphenyl-1-picrylhydrazyl (DPPH) scavenging and Ferric reducing antioxidant power (FRAP) protocols. Its enzyme-inhibitory properties were investigated on α-glucosidase and α-amylase activities. Gas Chromatography Mass Spectroscopy (GCMS) and Fourier Transform Infrared (FTIR) spectroscopic analysis were used to identify its phytoconstituents. Cytotoxicity was determined via MTT assay. The treated cells were assayed for reduced glutathione (GSH), non-protein thiol, nitric oxide and malondialdehyde (MDA) levels, as well as Superoxide Dismutase (SOD), catalase, myeloperoxidase and ATPase activities. Cell apoptosis and/or morphological changes were determined using the acridine orange and ethidium bromide (AO/EB) dual staining method. The fraction showed significant (pâ¯<â¯0.05) antioxidant and enzyme-inhibitory activity. It showed significant (pâ¯<â¯0.05) cytotoxic effect against HEK293 cells with concomitant depletion of antioxidative and elevation of proinflammatory biomarkers. Morphological changes were examined in the cells with an apoptotic index of 0.84. 1,1-Dodecanediol, diacetate was identified as the most predominant compound, while aromatics and amines as the most functional groups present in the fraction. These results suggest the antidiabetic and cytotoxic effects of C. volubile leaves. The toxicity can be attributed to induced oxidative stress and proinflammation with concomitant depletion of ATP leading to apoptosis of the cells.
Assuntos
Clerodendrum , Diabetes Mellitus Tipo 2/tratamento farmacológico , Inibidores Enzimáticos/toxicidade , Células Epiteliais/efeitos dos fármacos , Hipoglicemiantes/toxicidade , Inflamação/induzido quimicamente , Estresse Oxidativo/efeitos dos fármacos , Extratos Vegetais/farmacologia , Trifosfato de Adenosina/metabolismo , Amilases/antagonistas & inibidores , Amilases/metabolismo , Apoptose/efeitos dos fármacos , Biomarcadores/metabolismo , Glicemia/efeitos dos fármacos , Glicemia/metabolismo , Sobrevivência Celular/efeitos dos fármacos , Clerodendrum/química , Diabetes Mellitus Tipo 2/sangue , Diabetes Mellitus Tipo 2/enzimologia , Relação Dose-Resposta a Droga , Inibidores Enzimáticos/isolamento & purificação , Células Epiteliais/metabolismo , Células Epiteliais/patologia , Inibidores de Glicosídeo Hidrolases/toxicidade , Células HEK293 , Humanos , Hipoglicemiantes/isolamento & purificação , Mediadores da Inflamação/metabolismo , Lipase/antagonistas & inibidores , Lipase/metabolismo , Extratos Vegetais/isolamento & purificação , Folhas de PlantaRESUMO
Methanol-aqueous extracts from the aerial parts of Gypsophila glomerata (GGE), G. trichotoma (GTE) and G. perfoliata (GPE) were investigated for antioxidant potential using different in vitro models, as well as for phenolic and flavonoid contents. The possible anti-cholinesterase, anti-tyrosinase, anti-amylase and anti-glucosidase activities were also tested. The flavonoid variability was analyzed using ultra high-performance liquid chromatography (UHPLC) coupled with hybrid quadrupole-Orbitrap high resolution mass spectrometry (HRMS). Eleven C-glycosyl flavones and 4 O-glycosyl flavonoids, including 2"-O-pentosyl-6-C-hexosyl-apigenin/methylluteolin, as well as their mono(di)-acetyl derivatives were found in GGE. Both GGE and GTE shared 2"-pentosyl-6-C-hexosyl-luteolin together with the common saponarin, homoorientin, orientin, isovitexin and vitexin, while di C-glycosyl flavones were evidenced only in GPE. The highest radical scavenging in both ABTS and DPPH assays was noted in GPE, as well as ferric and cupric reducing abilities. However, GTE had the strongest metal chelating activity (17.44⯱â¯0.51â¯mg EDTAE/g extract). GPE and GGE were more potent as acetylcholinesterases inhibitors witnessed by 2.09⯱â¯0.02â¯mg GALAE/g extract and 1.59⯱â¯0.09 mgGALAE/g extract, respectively. All flavonoids were found in G. glomerata for the first time. Therefore, further isolation and structural elucidation of newly described acetylated flavonoids are needed in order to determine their relevance in the beneficial properties of the plant.
Assuntos
Caryophyllaceae/química , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Amilases/antagonistas & inibidores , Antioxidantes/química , Antioxidantes/farmacologia , Inibidores da Colinesterase/química , Inibidores da Colinesterase/farmacologia , Cromatografia Líquida de Alta Pressão/métodos , Flavonas/química , Flavonas/farmacologia , Glucosidases/antagonistas & inibidores , Espectrometria de Massas/métodos , Monofenol Mono-Oxigenase/antagonistas & inibidores , Fenóis/química , Fenóis/farmacologiaRESUMO
The importance of postprandial hyperglycemia in the treatment of diabetes has been recognized recently. Tea products, such as tea polyphenols (TP), epigallocatechin gallate (EGCG), matcha, and instant tea, were chosen as constituents of tea-flour food, aimed at regulating the release of glucose from starchy foods in the postprandial period. Six starches were chosen for internal composition analysis and hydrolysis studies in vitro. Corn starch, wheat starch, and lily root flour appeared to have higher resistant starch content, slower digestion profiles, and lower kinetic constants, implying sustained release of glucose in the gastrointestinal tract. The effect of tea products on starch digestion was determined in order to get a desired formulation of dietary product for patients with hyperglycemia. Compared with macha and instant tea, TP and EGCG exerted greater inhibition of amylase and amyloglucosidase, especially for corn starch with 0.5% TP or 0.5% EGCG.
Assuntos
Digestão , Amido/química , Amido/metabolismo , Chá/química , Amilases/antagonistas & inibidores , Amilases/metabolismo , Catequina/análogos & derivados , Catequina/química , Catequina/metabolismo , Farinha , Alimentos Fortificados , Glucana 1,4-alfa-Glucosidase/antagonistas & inibidores , Glucana 1,4-alfa-Glucosidase/metabolismo , Glucose/metabolismo , Humanos , Hidrólise , Polifenóis/química , Polifenóis/metabolismo , Período Pós-Prandial/fisiologia , Triticum/química , Triticum/metabolismo , Zea mays/químicaRESUMO
Stem lettuce is widely consumed as a vegetable in China. It is also used as a traditional Chinese medicine for a long time. Up to now, no information is available for stem lettuce polysaccharide (SLP). In this study, extraction optimization, characterization, and antioxidant activity of SLP was investigated.The maximum SLP yield of 20.89% was obtained under the optimal extraction conditions as follows: extraction temperature 95°C, extraction time 3.3h and ratio of water to material 25mL/g. The sulfate content of SLP was 5.82% and the main monosaccharides were GalA, Gal, and Ara with a mole ratio of 49.2: 23.3: 22.9. FT-IR spectrum and HPGPC result further indicated that SLP is a sulfated polydisperse heterpolysaccharide. Congo-red test and AFM scan indicated that SLP might be branching and intertwining structure with triple helix conformation. Moreover, SLP exhibited potent antioxidant activity and α-amylase inhibitory activity, hence it could be used as a potential natural antioxidant and hypoglycemic agent in medicine or functional food fields.
Assuntos
Fracionamento Químico/métodos , Lactuca/química , Polissacarídeos/isolamento & purificação , Polissacarídeos/farmacologia , Água/química , Amilases/antagonistas & inibidores , Antioxidantes/química , Antioxidantes/isolamento & purificação , Antioxidantes/farmacologia , Inibidores Enzimáticos/química , Inibidores Enzimáticos/isolamento & purificação , Inibidores Enzimáticos/farmacologia , Monossacarídeos/análise , Polissacarídeos/química , Solubilidade , Sulfatos/químicaRESUMO
BACKGROUND: Diabetes mellitus is one of the most common endocrinal disorders and medicinal plants continue to play an important role in the management of this disease. In this study, Rosa canina was investigated for the antioxidant and α-amylase inhibition activities. MATERIALS AND METHODS: Methanolic extract of Rosa canina was investigated for its potential antioxidant activity. The extracts' total phenolic and flavonoid contents and scavenging capacity for free radicals were evaluated. The α-amylase inhibition assay was also carried. RESULTS: Rosa canina extract exhibits a total Phenolic and flavonoid levels respectively (21.918 mg GAE/g and 2.647mg ER/g). The free radical scavenging activity was found to be prominent against DPPH with an IC50 of 0.668 mg/ml and against ABTS with an IC50 of 0.467 mg/ml. Extract showed a significant ferric ion reducing activities with an IC50 of4.962 mg/ml. CONCLUSION: Rosa canina exerted a higher inhibitory activity against α-amylase. The obtained results support the antidiabetic use of rosa canina.
Assuntos
Amilases/antagonistas & inibidores , Antioxidantes/farmacologia , Flavonoides/farmacologia , Hipoglicemiantes/farmacologia , Fenóis/farmacologia , Extratos Vegetais/farmacologia , Rosa/química , Benzotiazóis/metabolismo , Compostos de Bifenilo/metabolismo , Diabetes Mellitus/enzimologia , Flavonoides/análise , Fenóis/análise , Picratos/metabolismo , Extratos Vegetais/química , Ácidos Sulfônicos/metabolismoRESUMO
Representatives of the Achillea genus are widely used as foods or nutraceuticals. Considering the increasing demand for herbal dietary supplements with health promoting effects, the objective of this research was to evaluate the biological and chemical profiles of different extracts (ethyl acetate, methanol and water) obtained from three Achillea species (A. biebersteinii, A. millefolium and A. teretifolia). The antioxidant (free radical scavenging (DPPH and ABTS), reducing power (CUPRAC and FRAP), metal chelating and phosphomolybdenum), enzyme inhibitory (anti-cholinesterase, anti-tyrosinase, anti-amylase and anti-glucosidase) and antimicrobial (antibacterial and antifungal) effects were assessed to investigate their biological profiles. Moreover, the total phenolic and flavonoid contents were determined and LC-MS analysis was performed for the chemical profile of the investigated extracts. The LC-MS analysis revealed the presence of several caffeoylquinic acids in these extracts. Generally, the methanol and water extracts exhibited stronger antioxidant abilities, which correlated with the higher levels of phenolic compounds when compared to the ethyl acetate extracts. In addition, the best antimicrobial activities were obtained for the ethyl acetate and methanolic extracts. However, the ethyl acetate extract had remarkable enzyme inhibitory potential. On the basis of our results, Achillea species may be promoted as promising sources of natural agents and used for the development of nutraceuticals or functional food ingredients.