RESUMO
The inhibitory action of F. halophila extracts (acetone, chloroform, and methanol) against key enzymes linked to diabetes (α-amylase, α-glucosidase), cognitive functions (acetyl cholinesterase (AChE), butyryl cholinesterase (BChE)), and hyperpigmentation (tyrosinase) was assessed. The mutagenic/antimutagenic activities were assessed and the phytochemical profile established by HPLC-MS/MS. The acetone extract showed the highest phenolic (55.22 mg GAE/g extract) and flavonoid (34.52 mg RE/g extract) contents. The chloroform extract was a potent inhibitor of cholinesterases (4.86 and 6.13 mg GALAE/g extract, against AChE and BChE, respectively). Cinnamic acid derivatives (methyl cinnamate, ferulic acid, methoxycinnamic acid isomer) were identified in the chloroform extract. Methanol extract showed potent inhibitory action against tyrosinase (137.63 mg KAE/g extract) and glucosidase (43.02 mmol ACAE/g extract). The chloroform extract (32.07 mg EDTAE/g extract) showed potent metal chelating potential. The neuroprotective action of the chloroform extract might be attributed to the metal chelating action coupled by the cholinesterase inhibitory potential. F. halophila showed no mutagenic capacity. When combined with 2-aminoflouren and 2-aminoanthracene, the acetone and chloroform extracts revealed excellent antimutagenicity in the presence of metabolic activation enzymes for Salmonella typhimurium TA98 and TA100 strains. The observed inhibitory effects of F. halophila against the studied enzyme suggest that this plant could be a promising source of bioactive phytochemicals for the management of clinical conditions.
Assuntos
Ferula/química , Compostos Fitoquímicos/análise , Compostos Fitoquímicos/farmacologia , Antioxidantes/análise , Antioxidantes/farmacologia , Quelantes/análise , Quelantes/farmacologia , Inibidores da Colinesterase/análise , Inibidores da Colinesterase/farmacologia , Cromatografia Líquida de Alta Pressão , Inibidores de Glicosídeo Hidrolases/análise , Inibidores de Glicosídeo Hidrolases/farmacologia , Monofenol Mono-Oxigenase/antagonistas & inibidores , Mutagênicos/análise , Mutagênicos/farmacologia , Componentes Aéreos da Planta/química , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Espectrometria de Massas em Tandem , alfa-Amilases/antagonistas & inibidoresRESUMO
This study gathers information about the effects of different extracts (methanol and water) from rhizomes and aerial parts of Iris schachtii on selected enzymes (cholinesterases, alpha-amylase and alpha-glucosidase, tyrosinase and lipase) as well as of their antioxidant capacities and antimutagenic properties in relation with their phenolic composition. The chemical composition was assessed by determining total phenolic and flavonoid content as well as individual phenolic compounds by HPLC-DAD. Moreover, antioxidant abilities of the investigated extracts were tested by using different assays including free radical scavenging (DPPH and ABTS), reducing power (CUPRAC and FRAP), phosphomolybdenum and metal chelating, overall rhizomes being indicated as a superior source of antioxidant compounds. HPLC analysis revealed the abundance of some phenolics including apigenin (2584 µg/g extract) and luteolin (2510 µg/g extract) in aerial parts extracts while rhizomes were rich in apigenin (4734 µg/g extract) and kaempferol (4214 µg/g extract). The methanolic extracts exhibited a high anti-lipase activity while all extracts presented a relatively high inhibition on α-glucosidase. Furthermore, interactions between dominant compounds from extracts and selected enzymes were investigated by molecular modeling studies in order to explain at a molecular level the interactions between selected compounds and active sites of the enzyme/s.
Assuntos
Gênero Iris/química , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Antimutagênicos/farmacologia , Antioxidantes/farmacologia , Domínio Catalítico , Cromatografia Líquida de Alta Pressão , Inibidores Enzimáticos/farmacologia , Enzimas/metabolismo , Flavonoides/análise , Sequestradores de Radicais Livres/farmacologia , Simulação de Acoplamento Molecular , Fenóis/análise , Componentes Aéreos da Planta/química , Rizoma/química , Espectrofotometria UltravioletaRESUMO
BACKGROUND: The Cotoneaster species are widely used as traditional purposes in different countries including Turkey. PURPOSE: The study was performed to evaluate the biological and chemical profile of two extracts (methanol (T-Me; F-Me) and water (T-W; F-W)) from two parts (twigs and fruits) of Cotoneaster integerrimus. MATERIALS AND METHODS: Antioxidant (free radical scavenging (DPPH), reducing power (CUPRAC and FRAP), phosphomolybdenum and metal chelating), enzyme inhibitory (cholinesterase, tyrosinase, α-amylase and α-glucosidase), antimicrobial (standard microorganisms and methicillin-resistant Staphylococcus aureus isolates (MRSA)) and mutagenic/antimutagenic effects (by Ames assay) were tested for biological profile. For chemical profile, total and individual phenolic components were detected for each extract. RESULTS: Generally, T-Me reflected the strongest biological effects with the highest level of phenolics (115. 15 mgGAEs/g extract). Also, twig extracts had more potent biological effects as compared to flower extracts. Eight-teen phenolics were identified in the extracts. (-)- epicatechin was the major constituent in all extracts and is mainly responsible for biological activities observed. Its amount present in F-W and T-W were 9.27 and 32.89mg/g extract, respectively. Also, molecular docking was used to understand enzyme-epicatechin interactions. CONCLUSION: From these results, this plant has a great potential as a health promoter for developing novel functional food ingredients and pharmaceutical preparations.
Assuntos
Anti-Infecciosos/farmacologia , Antioxidantes/farmacologia , Catequina/química , Catequina/farmacologia , Estresse Oxidativo/efeitos dos fármacos , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Anti-Infecciosos/química , Antioxidantes/química , Suplementos Nutricionais , Frutas/química , Humanos , Rosaceae/química , TurquiaRESUMO
CONTEXT: Celtis glabrata is used in Turkey for the treatment of various health disorders. OBJECTIVE: The acetone, chloroform, ethanol, and methanol extracts of C. glabrata leaf, fruit, and seed were investigated to evaluate their antimutagenic activities. MATERIAL AND METHODS: The antimutagenicity of these extracts was determined by Ames test against mutagens (4-nitro-O-phenylenediamine, 2-aminofluorene (2-AF), and sodium azide (SA)). The extracts were used at concentrations between 5 and 0.005 mg/plate. RESULTS: The ethanol extracts of leaves exhibited strong antimutagenicity (70%) against 2-AF with S9 at 5 mg/plate on TA98. But methanol (61%, 53%) and acetone (53%, 52%) also revealed strong inhibition rates at concentrations of ≥ 0.5 mg/plate. Among the extracts, the highest activity (96%) was obtained from acetone extract against SA without S9, followed by chloroform extract (91%) at a dose of 5 mg/plate on TA100 with S9. Ethanol (without S9) and chloroform (with S9) extracts showed strong antimutagenicity at all doses. Exception of chloroform and acetone (without S9), all fruit extracts (with/without S9) manifested strong antimutagenicity at doses of ≥ 0.5 mg/plate on TA98 strain. Ethanol extracts revealed 68% inhibition against 2-AF on TA98. Acetone and ethanol extracts manifested 84% and 82% inhibition against SA on TA100, respectively. All the extracts of seeds revealed strong inhibition against 2-AF at ≥ 0.5 mg/plate doses on TA98, but acetone extract showed excellent antimutagenicity (94%). Moreover, the chloroform (74, 73, 63, 54%), acetone (74, 72, 70, 65%) and methanol (74, 67, 63, 61%) extracts of seeds revealed strong antimutagenic activity on TA100 against SA with S9. DISCUSSION AND CONCLUSION: This plant may be natural source of antimutagenic agents.
Assuntos
Antimutagênicos/farmacologia , Pareamento Incorreto de Bases/efeitos dos fármacos , Cannabaceae/química , Mutação da Fase de Leitura/efeitos dos fármacos , Extratos Vegetais/farmacologia , Salmonella typhimurium/efeitos dos fármacos , Antimutagênicos/intoxicação , Frutas/química , Mutagênicos/toxicidade , Extratos Vegetais/isolamento & purificação , Folhas de Planta/química , Salmonella typhimurium/genética , Sementes/químicaRESUMO
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.
Assuntos
Anti-Infecciosos/química , Antioxidantes/química , Inibidores Enzimáticos/química , Ganoderma/química , Fenóis/química , Extratos Vegetais/química , Doença de Alzheimer/enzimologia , Anti-Infecciosos/farmacologia , Antioxidantes/farmacologia , Bactérias/efeitos dos fármacos , Colinesterases/metabolismo , Cromatografia Líquida de Alta Pressão , Diabetes Mellitus/enzimologia , Inibidores Enzimáticos/farmacologia , Fungos/efeitos dos fármacos , Humanos , Monofenol Mono-Oxigenase/antagonistas & inibidores , Monofenol Mono-Oxigenase/metabolismo , Dermatopatias/enzimologia , alfa-Amilases/antagonistas & inibidores , alfa-Amilases/metabolismo , alfa-Glucosidases/metabolismoRESUMO
This study was focused on the analysis of the phenolic content, antioxidant, antibacterial, anti-cholinesterase, anti-tyrosinase, anti-amylase and anti-glucosidase activity of three solvent extracts from Cotoneaster nummularia. Moreover, water extract was tested in terms of mutagenic/anti-mutagenic effects. The antioxidant activities of these extracts were evaluated by DPPH, ABTS, O2, metal chelating, phosphomolybdenum, ß-carotene/linoleic acid, ferric and cupric reducing power assays. Enzyme inhibitory activities were also examined with colorimetric methods. Generally, methanol and water extracts exhibited excellent biological activities. These extracts were rich in phenolic and flavonoid content. Furthermore, Cotoneaster extracts indicated appreciable antibacterial properties against human pathogen strains. HPLC analysis showed that ferulic acid, chlorogenic acid, (-) - epicatechin and (+)-catechin were the major phenolics in extracts tested. These data offer that these extracts from C. nummularia may be considered as a potential source of biological agents for developing functional foods or drug formulations.
Assuntos
Extratos Vegetais/química , Rosaceae/química , Acetatos/química , Antibacterianos/química , Antibacterianos/isolamento & purificação , Antibacterianos/farmacologia , Antimutagênicos/química , Antimutagênicos/isolamento & purificação , Antimutagênicos/farmacologia , Antioxidantes/química , Antioxidantes/isolamento & purificação , Química Farmacêutica , Cromatografia Líquida de Alta Pressão , Inibidores Enzimáticos/química , Inibidores Enzimáticos/isolamento & purificação , Inibidores Enzimáticos/metabolismo , Enzimas/química , Enzimas/metabolismo , Flavonoides/análise , Flavonoides/química , Flavonoides/farmacologia , Alimento Funcional , Bactérias Gram-Negativas/efeitos dos fármacos , Bactérias Gram-Negativas/isolamento & purificação , Bactérias Gram-Positivas/efeitos dos fármacos , Bactérias Gram-Positivas/isolamento & purificação , Humanos , Metanol/química , Testes de Sensibilidade Microbiana , Testes de Mutagenicidade , Fenóis/análise , Fenóis/química , Fenóis/farmacologia , Extratos Vegetais/farmacologia , Ligação Proteica , Rosaceae/metabolismo , Salmonella typhimurium/efeitos dos fármacos , Salmonella typhimurium/genética , Água/químicaRESUMO
In this study, a hundred Klebsiella pneumoniae strains isolated from urinary tract infections were evaluated in terms of genotyping, susceptibility to certain antibiotics and detection of extended spectrum of beta lactamase (ESBL) production. The random amplified polymorphic DNA (RAPD-PCR) method was used to identify the genetic differentiation of K. pneumoniae isolates. A total of 26 different DNA bands ranging between 334 bp and 28033 bp were detected among the strains. It was found that 100 K. pneumoniae strains revealed 11 different RAPD profiles. Antibiotic susceptibility tests were conducted using a disc diffusion method against 16 antibiotics. Fifty-five different resistance profiles were determined among the strains. ESBL-productions of the strains were determined by the double disc synergy test (DDST) and ESBL E-test methods. ESBL production rates among the strains were found to be 55% by E-test method and 45% by DDST method. While ESBL-producing K. pneumoniae strains showed the greatest resistance to penicillin G (100%), followed by piperacillin (92.7%) and erythromycin (85.4%),the resistance rates of non ESBLproducing strains to those antibiotics were determined as 97.8%, 88.8% and 88.8%, respectively. Both groups of strains showed the highest sensitivity to meropenem. Based on the results obtained from the study, it was concluded that the detection of ESBL-producing strains by the E-test method was more sensitive than by the DDST method. Phenotypic and genotypic identification methods should be used together to detect ESBL presence. The RAPD-PCR method alone will not be adequate in the genotyping of the strains and alternative DNA-based methods should be used.
Assuntos
Antibacterianos , Farmacorresistência Bacteriana , Klebsiella pneumoniae/efeitos dos fármacos , Infecções Urinárias/microbiologia , beta-Lactamases/metabolismo , Impressões Digitais de DNA , DNA Bacteriano/genética , Regulação Bacteriana da Expressão Gênica/fisiologia , Regulação Enzimológica da Expressão Gênica , Genótipo , Humanos , Infecções por Klebsiella/microbiologia , Klebsiella pneumoniae/genética , Técnica de Amplificação ao Acaso de DNA Polimórfico , beta-Lactamases/genéticaRESUMO
OBJECTIVE: Early detection of dyslipidemia and long-term prevention of atherosclerosis by controlling risk factors should begin in childhood. The purpose of this study was to evaluate the prevalence of dyslipidemia according to non-high density lipoprotein cholesterol (non-HDL-C) levels in children and also evaluate serum non-HDL-C levels according to age groups, gender difference and living areas. METHODS: Overall, 2896 children (1467 girls, 1429 boys) aged between 7-18 years, residing in urban and rural parts of Eskisehir, Turkey, were enrolled in this randomized cross-sectional study. Serum non-HDL-C, total cholesterol (TC) and triglyceride (TG) levels were assessed in all participants of the study. Statistical analysis was performed Student's independent-samples T test for comparison of lipid parameters and relations between lipid parameters and age, anthropometric measurements, body fat percentage were evaluated by Pearson correlation test. RESULTS: Serum non-HDL-C levels were significantly higher in girls (115.5+/-31.5mg/dl) than boys (106.7+/-30.2 mg/Dl) (p<0.001). For girls, serum non-HDL-C levels were higher in 7-10 year age group than in 11-14-year and 15-18-year age groups (p<0.01 and p<0.05, respectively). For boys serum non-HDL-C levels of 7-10 year age group were significantly higher than in 11-14-year and 15-18-year age groups (p<0.001 for both). Serum non-HDL-C, total cholesterol and triglyceride levels were higher in girls than in boys especially in the 7-10-year-old age group. Serum TC, LDL-C, and HDL-C levels were higher in urban area residents, while serum TG levels were higher in rural area residents (p<0.001). Serum non-HDL-C levels were similar in residents of different living areas (p>0.05). In both sexes, non-HDL-C levels positively correlated with age and lipid parameters except HDL-C levels and also negatively correlated with HDL-C levels. In boys, non-HDL-C levels also correlated with total body fat percentage, weight, height. The prevalence of dyslipidemia according to non-HDL-C levels was higher (13.2%) in girls than boys (8.9%) (p<0.001). The prevalence of elevated non-HDL-C levels was higher in urban area residents than in rural area residents (p<0.05). The dyslipidemia prevalence according to non-HDL-C levels was similar with dyslipidemia prevalence according to serum LDL-C levels. CONCLUSION: Our results are indicative of the prevalence of dyslipidemia in children is considerably common in our population. Serum non-HDL-C levels could be used as an appropriate tool for detecting dyslipidemia in childhood.