RESUMO
Fully ripe fruits and mature leaves of Elaeagnus angustifolia were harvested and analyzed by means of analytical and biological tests to better comprehend the chemical composition and therapeutic/nutraceutical potential of this plant. Fruits and leaves were dried and the obtained powders were analyzed to study their color character and (via headspace gas chromatography) describe the chemical profile. Subsequently, they were submitted to a chloroform-methanol extraction, to a hydroalcoholic extraction procedure assisted or not by microwaves, and to an extraction with supercritical CO2, assisted or not by ethanol as the co-solvent, to detect the polyphenolic and the volatile content. The resulting extracts were evaluated in terms of chlorophyll and carotenoid content, polyphenolic content, volatile fraction, total phenolic content, total flavonoid content, antioxidant activity, radical scavenging activity, and enzymatic inhibition activity. The results confirmed the correlation between the chemical composition and the high antioxidant potential of leaf extracts compared to the fruit extracts in terms of the phenolic and pigment content. A promising effect against tyrosinase emerged for all the extracts, suggesting a therapeutic/nutraceutical use for this plant. Conversely, the volatile content from both natural matrices was similar.
Assuntos
Antioxidantes/análise , Carotenoides/análise , Elaeagnaceae/química , Flavonoides/análise , Frutas/química , Extratos Vegetais/análise , Folhas de Planta/química , Polifenóis/análise , Antioxidantes/química , Carotenoides/química , Clorofórmio/química , Clorofila/análise , Cromatografia Gasosa , Cromatografia Líquida de Alta Pressão , Cor , Flavonoides/química , Espectroscopia de Ressonância Magnética , Espectrometria de Massas , Metanol/química , Micro-Ondas , Monofenol Mono-Oxigenase/antagonistas & inibidores , Fenóis/análise , Fenóis/química , Extratos Vegetais/química , Polifenóis/química , Pós , Solventes/químicaRESUMO
The genus Rubus (Rosaceae) has great potential for and a history of use as natural agents in several traditional folk remedies. Based on this concept, this study focused on the antioxidant activities and enzyme inhibitory effects of extracts and fractions from Rubus caesius. Different chemical assays were performed to detect antioxidant capacity, namely, free radical scavenging (ABTS and DPPH assays), reducing power (CUPRAC and FRAP), phosphomolybdenum and metal chelating. Enzyme inhibitory effects were tested towards cholinesterases (AChE and BChE), tyrosinase, α-amylase and α-glucosidase. In addition, total amounts of phenolics and flavonoids were detected by colorimetric assays. Among the samples, the ethyl acetate fraction exhibited the strongest antioxidant potential with its higher concentration of total phenolics. The highest AChE and α-amylase inhibitory activities were observed in the diethyl ether fraction, while the n-butanol fraction had the strongest anti-tyrosinase inhibitor ability. The present study demonstrated that R. caesius may be considered a source of biologically active compounds to develop novel functional products or drugs in the pharmaceutical field.
Assuntos
Antioxidantes/química , Inibidores da Colinesterase/química , Inibidores de Glicosídeo Hidrolases/química , Monofenol Mono-Oxigenase/antagonistas & inibidores , Extratos Vegetais/química , Rubus/química , alfa-Amilases/antagonistas & inibidores , Flavonoides/análise , Fenóis/análise , Folhas de Planta/químicaRESUMO
The multicomponent pattern and biological characterization of plant material are essential for pharmaceutical field, in the food supplements quality control procedures and to all plant-based products. These nutrients often show valuable effects related to their consumption due to the occurrence of secondary metabolites that show useful properties on health. In this framework, researches performed on this topic play a central role for human health and drug development process. The aim of this study was to compare phenolics and free anthraquinones multicomponent pattern of two wild Turkish species: Asphodeline anatolica and Potentilla speciosa using validated high-performance liquid chromatography-photogiode array (HPLC-PDA) assays, coupled to biological evaluation. Even if some variances related to biological and enzymatic inhibition activities can be ascribed to other phytochemicals, the reported data support traditional use of Asphodeline anatolica and Potentilla speciosa roots as valuable natural font for the development of novel natural-derived drug formulations and/or food supplements with health and nutritional benefits.
Assuntos
Antraquinonas/farmacologia , Antioxidantes/farmacologia , Inibidores Enzimáticos/farmacologia , Liliaceae/química , Fenóis/farmacologia , Potentilla/química , Antraquinonas/química , Antraquinonas/isolamento & purificação , Antioxidantes/química , Antioxidantes/isolamento & purificação , Colinesterases/metabolismo , Cromatografia Líquida de Alta Pressão , Relação Dose-Resposta a Droga , Inibidores Enzimáticos/química , Inibidores Enzimáticos/isolamento & purificação , Humanos , Monofenol Mono-Oxigenase/antagonistas & inibidores , Monofenol Mono-Oxigenase/metabolismo , Fenóis/química , Fenóis/isolamento & purificação , Relação Estrutura-Atividade , Turquia , alfa-Amilases/antagonistas & inibidores , alfa-Amilases/metabolismo , alfa-Glucosidases/metabolismoRESUMO
We investigated the antioxidant and enzyme inhibitory activities and chemical composition of the hydro-distilled essential oil (0.35% yield) from aerial parts of Thymus spathulifolius. Antioxidant capacity of the oil was assessed by different methods including free radical scavenging (DPPH and ABTS), reducing power (FRAP and CUPRAC) and phosphomolybdenum assay. Inhibitory activities were analyzed against acetylcholinesterase (AChE), butyrylcholinesterase (BChE), α-amylase, α-glucosidase, and tyrosinase. Twenty-one constituents were identified representing 97.2% of the total oil with thymol (50.5%), borneol (16.7%) and carvacrol (7.7%) as the major components. The essential oil exhibited good antioxidant activity with IC50 values of 3.82 and 0.22 mg/mL determined by free radical scavenging DPPH and ABTS, respectively. EC50 values of FRAP and CUPRAC were found to be 0.12 and 0.34 mg/mL, respectively. The results of the present study support the uses of T. spathulifolius essential oil as a source of natural antioxidants and bioactivities for functional foods and phytomedicines.
Assuntos
Antioxidantes/farmacologia , Inibidores Enzimáticos/química , Inibidores Enzimáticos/farmacologia , Lamiaceae/química , Óleos Voláteis/química , Óleos Voláteis/farmacologia , Componentes Aéreos da Planta/química , Acetilcolinesterase/metabolismo , Antioxidantes/química , Butirilcolinesterase/metabolismo , Cloretos/química , Cobre/química , Relação Dose-Resposta a Droga , Compostos Férricos/química , Cromatografia Gasosa-Espectrometria de Massas , Humanos , Monofenol Mono-Oxigenase/antagonistas & inibidores , Monofenol Mono-Oxigenase/metabolismo , Oxirredução , Relação Estrutura-Atividade , alfa-Amilases/antagonistas & inibidores , alfa-Amilases/metabolismo , alfa-Glucosidases/metabolismoRESUMO
Mentha spicata is one of the most popular species in the genus, and it is of great interest as a gastrointestinal and sedative agent in the folk medicine system. In this study, different M. spicata extracts, obtained by the use of four solvents (hexane, chloroform, acetone and acetone/water) were chemically characterized using HPLC-ESI-MS n, which allowed for identification of 27 phenolic compounds. The extracts' antioxidant and enzyme inhibitory properties were investigated. In addition, neuroprotective effects were evaluated in hypothalamic HypoE22 cells, and the ability of the extracts to prevent the hydrogen peroxide-induced degradation of dopamine and serotonin was observed. The best antioxidant effect was achieved for all the extraction methods using acetone/water as a solvent. These extracts were the richest in acacetin, eriodictyol, hesperidin, sagerinic acid, naringenin, luteolin, chlorogenic acid, chrysoeriol and apigenin. The intrinsic antioxidant and enzyme inhibition properties of the acetone/water extract could also explain, albeit partially, its efficacy in preventing prostaglandin E2 overproduction and dopamine depletion (82.9% turnover reduction) in HypoE22 cells exposed to hydrogen peroxide. Thus, our observations can provide a scientific confirmation of the neuromodulatory and neuroprotective effects of M. spicata.
RESUMO
In the present study, the methanolic, hydro-methanolic, dichloromethane, hexane and aqueous extracts of Salvia ceratophylla L. (Family: Lamiaceae), a lemon-scented herb, were tested for total phenolic (TPC) and flavonoid content (TFC) and antioxidant activities were evaluated using a battery of assays (2,2-diphenyl-1-picrylhydrazyl (DPPH), 2,2-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS), ferric reducing antioxidant power (FRAP), cupric reducing antioxidant capacity, total antioxidant capacity (TAC) (phosphomolybdenum) and metal chelating). Enzyme inhibitory effects were investigated using acetyl- (AChE), butyryl-cholinesterase (BChE), tyrosinase, α-amylase and α-glucosidase as target enzymes. Regarding the cytotoxic abilities, HepG2, B164A5 and S17 cell lines were used. The phytochemical profile was conducted using liquid chromatography-mass spectrometry/mass spectrometry (LC-MS/MS). Our data showed that the methanolic aerial extracts possessed the highest phenolic (72.50 ± 0.63 mg gallic acid equivalent per g) and flavonoid (43.77 ± 1.09 mg rutin equivalent per g) contents. The hydro-methanolic aerial extract showed significant DPPH radical scavenging activity (193.40 ± 0.27 mg TE per g) and the highest reducing potential against CUPRAC (377.93 ± 2.38 mg TE per g). The best tyrosinase activity was observed with dichloromethane root extract (125.45 ± 1.41 mg kojic acid equivalent per g). Among the tested extracts, hexane root extract exerted the highest antimicrobial potential with a minimum inhibitory concentration value of 0.048 mg mL-1. Methanolic root extract showed the lowest cytotoxicity (28%) against HepG2 cells. Phytochemical analysis revealed the presence of important polyphenolic compounds including luteolin, gallic acid, rosmarinic acid, to name a few. This research can be used as one methodological starting point for further investigations on this lemon-scented herb.
RESUMO
The present study outlines the phenolic composition and pharmacological properties of different extracts of Digitalis cariensis Boiss. ex Jaub. & Spach root and aerial parts. The metabolic profiles of the studied extracts were characterized by UHPLC-MS. The in vitro antioxidant and enzyme (acetylcholinesterase (AChE), butyrylcholinesterase (BChE), tyrosinase, α-amylase, and α-glucosidase) inhibitory potential of the extracts were determined. Bioinformatics and docking investigations were also conducted to support the enzyme inhibition test and predict putative targets for potential pharmacological applications. Overall, the methanolic extract followed by the water extract of the D. cariensis root were found to be superior source of antioxidant compounds except for metal chelating ability, in which the water extract of the root (26.34 ± 1.54 mg EDTAE/g) and aerial parts (16.47 ± 0.88 mg EDTAE/g) have showed the highest activity. The tested extracts were potent against AChE (9.11 ± 0.27-9.79 ± 0.28 mg GEs/g extract), α-amylase (0.12 ± 0.01- 0.50 ± 0.01 mmol ACEs/g extract) and α-glucosidase (0.28 ± 0.01-17.29 ± 0.24 mmol ACEs/ g extract). Notable activity against tyrosinase was displayed by the methanolic extracts (Root-MeOH: 123.71 ± 2.70 and aerial parts - MeOH: 137.96 ± 1.07 mg KAE/g extract), while none of the extracts were potent against BChE. According to docking investigations, the observed anti-tyrosinase effect could be related, at least partially, to the presence of luteolin, rosmarinic acid and kaempferol in the extracts. Results amassed herein is the first report on the biological attributes of D. cariensis, which validate the pharmacological uses of this plant.
Assuntos
Antioxidantes , Digitalis , Antioxidantes/farmacologia , Monofenol Mono-Oxigenase , Fenóis/farmacologia , Extratos Vegetais/farmacologiaRESUMO
The pharmacological properties of Asphodelus species have been advocated previously. In this respect, the present study attempts to unravel the antioxidant and enzyme inhibitory activity of root extracts of two Asphodelus species, namely, A. albus and A. aestivus. Data gathered demonstrated that the dichloromethane (25.49, 51.30, 104.31, and 81.58 mg Trolox equivalents [TEs]/g, for 2,2-diphenyl-1-picrylhydrazyl [DPPH], 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) [ABTS], cupric ion reducing antioxidant capacity [CUPRAC], and ferric reducing antioxidant power[FRAP] assays respectively) and ethyl acetate (20.60, 41.86, 89.07, and 57.85 mg TEs/g, for DPPH, ABTS, CUPRAC, and FRAP assays respectively) extracts of A. albus roots showed highest radical scavenging and reducing potential. These findings were in accordance with total phenolic content observed which showed the highest phenolic content of A. albus dichloromethane (30.74 mg gallic acid equivalents [GAEs]/g) and ethyl acetate (23.41 mg GAEs/g) extracts. Interestingly, A. albus and A. aestivus root extracts were active inhibitors of tyrosinase and lipase, with values varying from 56.52 to 71.49 mg kojic acid equivalent/g and 34.88 to 86.32 mg orlistat equivalent/g, respectively. Flavonoids, anthraquinones, and phenolic acids were identified as main individual compounds in chemical profile analysis. This is the first report of the presence of aloin A, aloin B, and aloesin in species other than in Aloe. Scientific evidences gathered from this study claimed the biological activity of the studied Asphodelus species and provided rationale for further investigations which might lead to the development of novel pharmacophores to alleviate oxidative stress related complications, obesity, as well as, skin hyperpigmentation complications.
Assuntos
Antioxidantes , Extratos Vegetais , Antioxidantes/farmacologia , Flavonoides , Metabolômica , Fenóis , Extratos Vegetais/farmacologiaRESUMO
INTRODUCTION: Natural products derived from medicinal plants provide beneficial cancer chemotherapeutic drugs. Bioactive constituents from plants are explored for their anticancer properties. METHODS: Three known compounds (deacetylbaccatin III, tasumatrol B, and taxawallin J) were isolated from Taxus wallichiana. Compounds were screened against four cancer cell lines, such as eA498, HepG2, NCI-H226, and MDR 2780AD. Cytotoxic activity was evaluated using MTT assay against cancer cell lines. RESULTS: Tasumatrol B showed good cytotoxic activity conducted for the improvement of inhibiting potential of these compounds against the cancer drug target protein (EGFR tyrosine kinase enzyme). The docking study showed that all compounds have binding affinities and interaction profile with the receptor tyrosine kinase. DISCUSSION: The study suggests that these compounds could be used for the discovery of novel inhibitors against the target receptors for the treatment of cancer.
RESUMO
Tragopogon dubius and Tussilago farfara are consumed as vegetables and used in folk medicine to manage common diseases. Herein, the chemical compositions and biological activities of different leaf extracts (ethyl acetate, methanol, and water) of T. dubius and T. farfara were evaluated. The antibacterial, antifungal, and antioxidant abilities of the extracts were tested using different assays including free radical scavenging, reducing power, phosphomolybdenum, and metal chelating assays. Enzyme inhibitory potentials were evaluated against cholinesterases, tyrosinase, α-amylase and α-glucosidase. Complexes of bioactive compounds (chlorogenic and rosmarinic acid) were docked into the enzymatic cavity of α-glucosidase and subjected to molecular dynamic calculation, enzyme conformational stability, and flexibility analysis. T. dubius and T. farfara extracts showed remarkable antioxidant potentials. Ethyl acetate extracts of T. dubius and T. farfara were the most potent inhibitors of acetylcholinesterase and butyrylcholinesterase. T. dubius ethyl acetate extract and T. farfara methanolic extract showed noteworthy activity against α-glucosidase. High performance liquid chromatography analysis revealed the abundance of some phenolic compounds including chlorogenic and rosmarinic acids. Ethyl acetate extract of T. dubius showed notable antifungal activity against all strains. Docking studies showed best pose for chlorogenic acid was stabilized by a network of hydrogen bonds with residues Asp1157, Asp1279, whereas rosmarinic acid showed several hydrogen bonds with Asp1157, Asp1420, Asp1526, Lys1460 and Trp1369. This study further validates the use of T. dubius and T. farfara in traditional medicine, as well as act as a stimulus for further studies for future biomedicine development. Communicated by Ramaswamy H. Sarma.
Assuntos
Asteraceae/química , Tragopogon/química , Tussilago/química , Acetilcolinesterase/metabolismo , Antioxidantes/química , Butirilcolinesterase/metabolismo , Cinamatos/farmacologia , Depsídeos/farmacologia , Inibidores Enzimáticos/química , Inibidores Enzimáticos/farmacologia , Flavonoides/sangue , Flavonoides/farmacologia , Simulação de Acoplamento Molecular/métodos , Monofenol Mono-Oxigenase/metabolismo , Fenóis/química , Extratos Vegetais/química , Extratos Vegetais/farmacologia , alfa-Amilases/metabolismo , alfa-Glucosidases/metabolismo , Ácido RosmarínicoRESUMO
OBJECTIVES: This study investigates into the biological effects of solvent extracts (ethyl acetate, methanol, and water) of Scutellaria orientalis L. and Scutellaria salviifolia Benth. based on its enzyme inhibitory activity and antioxidant ability together with the screening of bioactive compounds. METHODS: Total and individual bioactive components were determined using spectrophotometric and HPLC-ESI-MS methods. Six antioxidant assays were conducted and enzyme inhibition was tested against key enzymes linked to the pathology of common chronic disorders. KEY FINDINGS: Results revealed that the aqueous extracts of both plants exerted better 2,2'-azino-bis(3-ethylbenzothiazoline)-6-sulfonic acid scavenging, reducing power, metal chelating, and α-glucosidase inhibitory activities. The methanol extracts showed highest tyrosinase inhibition and antioxidant activity in phosphomolybdenum assay while the less polar ethyl acetate extracts showed better acetylcholinesterase, butyrylcholinesterase, and α-amylase inhibition. Phytochemical evaluation by HPLC-ESI-MS revealed the presence of high amounts of flavones. CONCLUSIONS: Scutellaria orientalis and S. salviifolia are important sources of bioactive agents that warrants further studies.
Assuntos
Antioxidantes/farmacologia , Inibidores Enzimáticos/farmacologia , Extratos Vegetais/farmacologia , Scutellaria/química , Antioxidantes/isolamento & purificação , Cromatografia Líquida de Alta Pressão/métodos , Inibidores Enzimáticos/isolamento & purificação , Solventes/química , Especificidade da Espécie , Espectrometria de Massas por Ionização por Electrospray/métodos , Espectrofotometria/métodosRESUMO
Extracts (methanol, ethyl acetate, and water) from Dianthus calocephalus Boiss. prepared by different extraction techniques (maceration, Soxhlet, and ultrasonication) were studied for possible inhibitory action against key enzymes (α-amylase, α-glucosidase, acetyl cholinesterase, butyryl cholinesterase, and tyrosinase). Antioxidant potential was established using a battery of assays and phenolic compounds profiled by RP-HPLC. Binding pose of tyrosinase with rutin was studied by means of molecular docking. Methanol extracts showed the highest phenolic (39.35-40.25 mgGAE/g) content and rich in rutin (61.38-72.07â¯mg/g extract). Ethyl acetate extracts of D. calocephalus were potent inhibitors of acetyl (1.45-1.48 mgGALAE/g) and butyryl (2.44-2.74 mgGALAE/g) cholinesterases. Docking studies showed that rutin interacts with the side chains of the key amino acid residues and to the copper atom found at the active site of tyrosinase. Methanol extracts showed highest antioxidant capacity. D. calocephalus showed interesting biological properties that could be further studied to manage diabetes, neurodegenerative diseases, Alzheimer's disease, and hyperpigmentation.
Assuntos
Dianthus/química , Extratos Vegetais/análise , Extratos Vegetais/farmacologia , Rutina/análise , Acetatos/química , Acetilcolinesterase/efeitos dos fármacos , Antioxidantes/farmacologia , Butirilcolinesterase/efeitos dos fármacos , Domínio Catalítico , Inibidores da Colinesterase/análise , Inibidores da Colinesterase/farmacologia , Cromatografia Líquida de Alta Pressão/métodos , Cromatografia de Fase Reversa/métodos , Simulação por Computador , Metanol/química , Modelos Moleculares , Monofenol Mono-Oxigenase/metabolismo , Extratos Vegetais/metabolismo , Rutina/metabolismo , Rutina/farmacologia , Água/química , alfa-Amilases/antagonistas & inibidores , alfa-Glucosidases/efeitos dos fármacosRESUMO
Bidens tripartita L. is a traditional phyto-remedy used in several countries, yet there is still a paucity of data on its biological potential. We aimed to provide new insights on the pharmacological potential of extracts prepared from B. tripartita via highlighting its antioxidant, key enzymes inhibitory potency, and DNA protecting effects. Phytochemical profile was established using High-Performance Liquid Chromatography with Diode-Array Detection (HPLC-DAD) and bioactive compound(s) docked against target enzymes using in silico methods. Cytotoxicity against three cancer cell lines was assessed using the methylthiazolyldiphenyl-tetrazolium bromide (MTT) cell viability test. The main compounds were luteolin-7-glucoside (cynaroside), chlorogenic acid, and epicatechin in the extracts. The methanol extract exhibited the highest radical scavenging activity. Ethyl acetate extract showed strongest α-amylase inhibitory activity, while the best α-glucosidase inhibitory effect recorded for the methanol extract. Molecular docking showed that cynaroside strongly interact to α-glucosidase cavity by establishing six hydrogen bonds. B. tripartita extracts were found to protect supercoiled form of pUC19 plasmid (>70%) and also showed anti-proliferative properties. Results amassed in the present study add on to a growing body of literature on the multi-pharmacological potency of B. tripartita which can be applied to bio-products development geared towards management of common diseases.
Assuntos
Bidens/química , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Linhagem Celular , Sobrevivência Celular/efeitos dos fármacos , Cromatografia Líquida de Alta Pressão , Simulação por Computador , Simulação de Acoplamento Molecular , alfa-Glucosidases/química , alfa-Glucosidases/metabolismoRESUMO
Diospyros lotus L. possesses different therapeutic activities such as antioxidant, anti-proliferative, anti-microbial and sedative. However, no studies on the sedative-hypnotic activity of 7-methyljuglone are reported. In the present study, we have evaluated in vivo the anxiolytic-hypnotic like effects of 7-methyljuglone in mice with open field and phenobarbitone-induced sleeping time tests. We have also assessed in silico the involvement of GABAA, GABAB and 5HT1 neurotransmission in its mechanism of action. The intraperitoneal administration of 7-methyljuglone (2.5-10mg/kg) reduce significantly the number of crossed lines in mice open field test and concomitantly it shown a significant activity in term of onset of sleeping time and also in its duration. Moreover, 7-methyljuglone demonstrated in silico an interesting interaction with GABAA but not GABAB and 5HT1binding sites. All of these results, taken together, 7-methyljuglone may be an innovative candidate for designing new pharmaceutical and therapeutic applications.
Assuntos
Diospyros/química , Hipnóticos e Sedativos/farmacologia , Naftoquinonas/farmacologia , Extratos Vegetais/farmacologia , Animais , Antioxidantes/metabolismo , Masculino , Camundongos , Camundongos Endogâmicos BALB CRESUMO
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.
Assuntos
Achillea/química , Anti-Infecciosos/farmacologia , Antioxidantes/farmacologia , Inibidores Enzimáticos/farmacologia , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Achillea/classificação , Amilases/antagonistas & inibidores , Amilases/química , Anti-Infecciosos/química , Anti-Infecciosos/isolamento & purificação , Antioxidantes/química , Antioxidantes/isolamento & purificação , Inibidores Enzimáticos/química , Inibidores Enzimáticos/isolamento & purificação , Alimento Funcional/análise , Monofenol Mono-Oxigenase/antagonistas & inibidores , Monofenol Mono-Oxigenase/química , Extratos Vegetais/isolamento & purificaçãoRESUMO
Members of the genus Lathyrus are used as food and as traditional medicines. In order to find new sources of biologically-active compounds, chemical and biological profiles of two Lathyrus species (L. czeczottianus and L. nissolia) were investigated. Chemical profiles were evaluated by HPLC-ESI-MSn, as well as by their total phenolic and flavonoid contents. In addition, antioxidant, enzyme inhibitory, and cytotoxic effects were also investigated. Antioxidant properties were tested by using different assays (DPPH, ABTS, CUPRAC, FRAP, phosphomolybdenum, and metal chelation). Cholinesterases (AChE and BChE), tyrosinase, α-amylase, and α-glucosidase were used to evaluate enzyme inhibitory effects. Moreover, vitexin (apigenin-8-C-glucoside) and 5-O-caffeoylquinic acid were further subjected to molecular docking experiments to provide insights about their interactions at molecular level with the tested enzymes. In vitro cytotoxic effects were examined against human embryonic kidney cells (HEK293) by using iCELLigence real time cell analysis system. Generally, L. czeczottianus exhibited stronger antioxidant properties than L. nissolia. However, L. nissolia had remarkable enzyme inhibitory effects against cholinesterase, amylase and glucosidase. HPLC-ESI-MSn analysis revealed that flavonoids were major components in these extracts. On the basis of these results, Lathyrus extracts were rich in biologically active components; thus, these species could be utilized to design new phytopharmaceutical and nutraceutical formulations.
RESUMO
In this work, the biological and chemical fingerprints of three extracts (ethyl acetate, methanol, and water) from two Potentilla species (Potentilla reptans and P. speciosa) were investigated. Antioxidant, enzyme inhibitory, and cytotoxic activities were performed for the biological fingerprint. For the chemical characterization, total bioactive components, and individual phenolic components were determined using photometric and HPLC methods, respectively. The main identified phenolic compounds in these extracts were rutin and catechin. Methanol and water extracts contained the highest total phenolic and flavonoid content. The results of antioxidant assays showed that methanol and water extracts displayed higher antioxidant activity compared to the ethyl acetate extract. Generally, methanol and water extracts exhibited higher biological activities correlated with higher levels the bioactive components. For P. speciosa, the methanol extract exhibited the highest enzyme inhibitory activity (except BChE inhibitory activity). P. reptans exhibited also high antiproliferative activity against MCF-7 cells whilst P. speciosa had weak to moderate activity against both of A549 and MCF-7 cell lines. The results suggest that Potentilla species could be potential candidates for developing new phyto-pharmaceuticals and functional ingredients.
RESUMO
This work reports the antioxidant, antimicrobial, and inhibitory effects of methanol and water extracts from Ganoderma applanatum (GAM: methanol extract and GAW: water extract) and G. resinaceum (GRM: methanol extract and GRW: water extract) against cholinesterase, tyrosinase, α-amylase and α-glucosidase. The total phenolics, flavonoids contents, and HPLC profile of phenolic components present in the extracts, were also determined. Antioxidant activities were investigated by using different assays, including DPPH, ABTS, FRAP, CUPRAC, phosphomolybdenum and metal chelating assays. Antimicrobial activity of the tested Ganoderma extracts was also studied by the broth microdilution method. Generally, the highest antioxidant (59.24 mg TEs per g extract for DPPH, 41.32 mg TEs per g extract for ABTS, 41.35 mg TEs per g extract for CUPRAC, 49.68 mg TEs per g extract for FRAP, 130.57 mg AAEs per g extract for phosphomolybdenum and 26.92 mg EDTAEs per g extract) and enzyme inhibitory effects (1.47 mg GALAEs per g extract for AChE, 1.51 mg GALAEs per g extract for BChE, 13.40 mg KAEs per g extract for tyrosinase, 1.13 mmol ACEs per g extract for α-amylase and 2.20 mmol ACEs per g extract for α-glucosidase) were observed in GRM, which had the highest concentrations of phenolics (37.32 mg GAEs g(-1) extract). Again, Ganoderma extracts possess weak antibacterial and antifungal activities. Apigenin and protocatechuic acid were determined as the main components in GRM (1761 µg per g extract) and GAM (165 µg per g extract), respectively. The results suggest that the Ganoderma species may be considered as a candidate for preparing new food supplements and can represent a good model for the development of new drug formulations.