Your browser doesn't support javascript.
Mostrar: 20 | 50 | 100
Resultados 1 - 20 de 1.899
Filtrar
Filtros adicionais











Intervalo de ano
1.
Chem Biol Interact ; 308: 339-349, 2019 Aug 01.
Artigo em Inglês | MEDLINE | ID: mdl-31170387

RESUMO

Magnolol, the most abundant bioactive constituent of the Chinese herb Magnolia officinalis, has been found with multiple biological activities, including anti-oxidative, anti-inflammatory and enzyme-regulatory activities. In this study, the inhibitory effects and inhibition mechanism of magnolol on human carboxylesterases (hCEs), the key enzymes responsible for the hydrolytic metabolism of a variety of endogenous esters as well as ester-bearing drugs, have been well-investigated. The results demonstrate that magnolol strongly inhibits hCE1-mediated hydrolysis of various substrates, whereas the inhibition of hCE2 by magnolol is substrate-dependent, ranging from strong to moderate. Inhibition of intracellular hCE1 and hCE2 by magnolol was also investigated in living HepG2 cells, and the results showed that magnolol could strongly inhibit intracellular hCE1, while the inhibition of intracellular hCE2 was weak. Inhibition kinetic analyses and docking simulations revealed that magnolol inhibited both hCE1 and hCE2 in a mixed manner, which could be partially attributed to its binding at two distinct ligand-binding sites in each carboxylesterase, including the catalytic cavity and the regulatory domain. In addition, the potential risk of the metabolic interactions of magnolol via hCE1 inhibition was predicted on the basis of a series of available pharmacokinetic data and the inhibition constants. All these findings are very helpful in deciphering the metabolic interactions between magnolol and hCEs, and also very useful for avoiding deleterious interactions via inhibition of hCEs.


Assuntos
Compostos de Bifenilo/metabolismo , Hidrolases de Éster Carboxílico/metabolismo , Lignanas/metabolismo , Sítios de Ligação , Biocatálise , Compostos de Bifenilo/química , Hidrolases de Éster Carboxílico/antagonistas & inibidores , Domínio Catalítico , Medicamentos de Ervas Chinesas/química , Medicamentos de Ervas Chinesas/metabolismo , Células Hep G2 , Humanos , Hidrólise , Cinética , Lignanas/química , Simulação de Acoplamento Molecular
2.
Life Sci ; 230: 97-103, 2019 Aug 01.
Artigo em Inglês | MEDLINE | ID: mdl-31129139

RESUMO

AIM: Acetaminophen (APAP) overdose is the most frequent cause of drug-induced liver damage. Magnolia officinalis is a traditional hepatoprotective Chinese medicine and Honokiol (HO) is the major active constituent. The present study was to investigate the effect of HO on APAP-induced hepatotoxicity and related mechanisms. MAIN METHODS: Four groups of mice were subjected to treatment as vehicle, APAP, APAP + HO and APAP + HO + NRF2 inhibitor. The morphological and biochemical assessments were used to evaluate the hepatoprotective effects. The extent of APAP-protein adducts was determined through evaluate the hepatic content 3­(cystein­S­yl)acetaminophen (APAP-Cys), the hydrolysis products of APAP-protein adducts. The activities of CYP2E1, CYP1A2 and CYP3A4 were evaluated by cocktail incubation, and the protein expression levels of NRF2, GCLC, GCLM, GS and GST were evaluated by western blot analysis. KEY FINDINGS: Morphological and biochemical assessments clearly demonstrated that HO could alleviate APAP-induced liver damage. The hepatoprotective effect of HO was positively associated with the reduction of APAP-protein adducts. Further investigation suggested that HO induced inhibition of CYP 2E1 and CYP2A1 as well as upregulation of GSH co-contributed to the reduction of APAP-protein adducts. Furthermore, HO induced activations of NRF2 and its target enzymes, such as GCLC, GCLM and GST, gave rise to the upregulation of GSH. SIGNIFICANCE: Our results suggested that HO could alleviate APAP-induced liver damage through reducing the generation of APAP-protein adducts, which might be mediated by inhibiting the activity of CYP 2E1 and CYP2A1 as well as enhancing the generation of GSH via NRF2 pathway.


Assuntos
Acetaminofen/toxicidade , Compostos de Bifenilo/farmacologia , Doença Hepática Induzida por Substâncias e Drogas/tratamento farmacológico , Lignanas/farmacologia , Acetaminofen/efeitos adversos , Acetaminofen/farmacologia , Animais , Compostos de Bifenilo/metabolismo , Glutationa/metabolismo , Lignanas/metabolismo , Fígado/efeitos dos fármacos , Fígado/metabolismo , Masculino , Camundongos , Camundongos Endogâmicos BALB C , Fator 2 Relacionado a NF-E2/antagonistas & inibidores , Fator 2 Relacionado a NF-E2/metabolismo , Estresse Oxidativo/efeitos dos fármacos , Substâncias Protetoras/farmacologia , Transdução de Sinais/efeitos dos fármacos
3.
Emerg Microbes Infect ; 8(1): 707-716, 2019.
Artigo em Inglês | MEDLINE | ID: mdl-31119985

RESUMO

Staphylococcus aureus (S. aureus) is one of the most serious human pathogens. α-Hemolysin (Hla) secreted by S. aureus is a key toxin for various infections. We herein report that Honokiol, a natural plant polyphenol, inhibits the secretion and hemolytic activity of staphylococcal Hla with concomitant growth inhibition of S. aureus and protection of S. aureus-mediated cell injury within subinhibitory concentrations. In parallel, Honokiol attenuates the staphylococcal Hla-induced inflammatory response by inhibiting NLRP3 inflammasome activation in vitro and in vivo. Consequently, the biologically active forms of the inflammatory cytokines IL-1ß and IL-18 are reduced significantly in response to Honokiol in mice infected with S. aureus. Experimentally, we confirm that Honokiol binds to monomeric Hla with a modest affinity without impairing its oligomerization. Based on molecular docking analyses in silico, we make a theoretical discovery that Honokiol is located outside of the triangular region of monomeric Hla. The binding model restricts the function of the residues related to membrane channel formation, which leads to the functional disruption of the assembled membrane channel. This research creates a new paradigm for developing therapeutic agents against staphylococcal Hla-mediated infections.


Assuntos
Toxinas Bacterianas/metabolismo , Compostos de Bifenilo/administração & dosagem , Proteínas Hemolisinas/metabolismo , Inflamassomos/antagonistas & inibidores , Lignanas/administração & dosagem , Receptores de Superfície Celular/antagonistas & inibidores , Infecções Estafilocócicas/tratamento farmacológico , Staphylococcus aureus/efeitos dos fármacos , Células A549 , Animais , Antibacterianos/administração & dosagem , Antibacterianos/farmacologia , Anti-Inflamatórios/administração & dosagem , Anti-Inflamatórios/metabolismo , Anti-Inflamatórios/farmacologia , Toxinas Bacterianas/toxicidade , Compostos de Bifenilo/metabolismo , Compostos de Bifenilo/farmacologia , Sobrevivência Celular/efeitos dos fármacos , Modelos Animais de Doenças , Proteínas Hemolisinas/toxicidade , Histocitoquímica , Humanos , Lignanas/metabolismo , Lignanas/farmacologia , Fígado/patologia , Camundongos Endogâmicos C57BL , Simulação de Acoplamento Molecular , Ligação Proteica , Infecções Estafilocócicas/patologia , Staphylococcus aureus/metabolismo , Resultado do Tratamento
4.
J Food Sci ; 84(6): 1340-1345, 2019 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-31112293

RESUMO

Barley sprouts and wheat sprouts have received much interest as functional foods in many countries. In this study, the effects of heat processing and extraction temperature on the bioactive components and antioxidative properties were examined in barley and wheat sprout teas. Both barley and wheat sprout teas were processed with two different methods (steaming or pan-roasting). Crude protein was increased, and moisture content was the lowest, in the roasted barley and wheat sprout teas. Total phenolics content and flavonoid contents were significantly higher in the roasted teas than in the steamed teas. Vitamin C content was the highest after an extraction temperature of 55 °C (24.05 mg/mL) in the roasted wheat sprout tea. Both roasted barley and wheat sprout teas exhibited the most antioxidative effects in vitro, demonstrated by 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical-scavenging and nitrite-scavenging activities. Therefore, the roasting method can be considered an appropriate technique for the production of barley and wheat sprout teas. PRACTICAL APPLICATION: Barley and wheat sprouts have received much attention in recent years as functional food materials in many countries and can be consumed as a form of tea. Heat processing methods such as steaming and roasting were applied and compared to increase the bioactive components and antioxidative activity in barley and wheat sprout teas. We found that roasting showed higher bioactive components and antioxidative activity than steaming in both barley and wheat sprout teas. In addition, wheat sprouts tea showed better bioactive components and antioxidative activity compared with the barley sprout tea.


Assuntos
Antioxidantes/farmacologia , Bebidas/análise , Hordeum/química , Temperatura Alta , Extratos Vegetais/farmacologia , Plântula/química , Triticum/química , Antioxidantes/análise , Ácido Ascórbico/análise , Ácido Ascórbico/farmacologia , Compostos de Bifenilo/metabolismo , Culinária , Flavonoides/análise , Flavonoides/farmacologia , Humanos , Fenóis/análise , Fenóis/farmacologia , Picratos/metabolismo , Extratos Vegetais/química , Chá
5.
J Food Sci ; 84(5): 990-1001, 2019 May.
Artigo em Inglês | MEDLINE | ID: mdl-30945309

RESUMO

Red chicory leaves are appreciated sensorially and their constituents contain bioactive properties. The objectives of this study were as follows: to use an experimental design to extract anthocyanins from red chicory in aqueous solution at pH 2.5; to determine the stability of the extracts in relation to temperature and pH; and to evaluate the antioxidant activity and in vitro cytotoxic effect of the lyophilized and purified extracts. The best extraction conditions for the bioactive compounds from red chicory were a temperature of 64.2 °C for 25 min; the anthocyanin content was 73.53 ± 0.13 mg per 100 g fresh weight basis sample. The EC50 (Half maximal effective concentration) value for the antioxidant activity assay in relation to DPPH (2,2-diphenyl-1-picrylhydrazyl) with optimized extract was 0.363, which corresponds to a concentration of 39.171 µmol/L of anthocyanins. The activation energy for the degradation reaction of the anthocyanins from the red chicory extract was 84.88 kJ/mol. The optimized extract, which was rich in anthocyanins, showed chemical and biological antioxidant activity (protection against erythrocyte hemolysis) and inhibited lipid peroxidation in vitro. The Cichorium intybus L. extracts interfered on the levels of reactive oxygen species generation and the crude extract did not present procarcinogenic effect. PRACTICAL APPLICATION: Red chicory is basically consumed as a part of traditional dishes worldwide. Here, we developed a process to extract and purify the anthocyanins from Cichorium intybus leaves and test the extracts in terms of the chemical composition, thermal stability, antioxidant activity, and antiproliferative effects. The anthocyanin-rich extract presented antioxidant activity in chemical and biological assays and low cytotoxicity and cytoprotective effects in relation to HepG2, HCT8, and Caco-2 cell lines. Additionally, the red chicory extract protected human erythrocytes against hemolysis. This extract may be used as a natural colorant/antioxidant in foods.


Assuntos
Antocianinas/farmacologia , Antineoplásicos Fitogênicos/farmacologia , Antioxidantes/farmacologia , Chicória/química , Aditivos Alimentares/farmacologia , Extratos Vegetais/farmacologia , Antocianinas/isolamento & purificação , Antineoplásicos Fitogênicos/isolamento & purificação , Antioxidantes/isolamento & purificação , Compostos de Bifenilo/metabolismo , Células CACO-2 , Carcinogênese/efeitos dos fármacos , Eritrócitos/efeitos dos fármacos , Aditivos Alimentares/isolamento & purificação , Células Hep G2 , Humanos , Peroxidação de Lipídeos/efeitos dos fármacos , Picratos/metabolismo , Extratos Vegetais/química , Folhas de Planta/química
6.
Microb Pathog ; 130: 253-258, 2019 May.
Artigo em Inglês | MEDLINE | ID: mdl-30910722

RESUMO

The present experiment evaluated how coronatine (COR) elicitation affects chemical and biological properties of cumin (Cuminum cyminum L.) seed essential oil (CSEO). Following isolation of the EO, its chemical composition was analyzed by gas chromatography-mass spectrometry; also, its bioactivities in terms of antimicrobial/antifungal, cytotoxic (measured by MTT assay) and antioxidant effects (evaluated by DPPH, ß-carotene bleaching (BCB) and TBARS methods) were evaluated. COR-elicitation significantly increased CSEO yield and the level of its chemical components, especially cumin aldehyde which is the main component of CSEO. Results showed that COR-elicitation significantly reduced the minimum inhibitory concentration (MIC) and the minimum bactericidal concentration (MBC) of CSEO against 4 Gram-positive and 3 Gram-negative bacteria and 2 fungi. Moreover, elicitation markedly enhanced the antioxidant and in vitro cytotoxic activity of CSEO. Therefore, COR may be regarded as a useful biotic elicitor for improving EO chemical and biological properties.


Assuntos
Aminoácidos/metabolismo , Cuminum/efeitos dos fármacos , Indenos/metabolismo , Óleos Voláteis/química , Sementes/efeitos dos fármacos , Anti-Infecciosos/análise , Anti-Infecciosos/farmacologia , Antineoplásicos/análise , Antineoplásicos/farmacologia , Antioxidantes/análise , Antioxidantes/farmacologia , Compostos de Bifenilo/metabolismo , Sobrevivência Celular/efeitos dos fármacos , Cromatografia Gasosa-Espectrometria de Massas , Testes de Sensibilidade Microbiana , Óleos Voláteis/farmacologia , Picratos/metabolismo , beta Caroteno/metabolismo
7.
Eur J Pharmacol ; 849: 135-145, 2019 Apr 15.
Artigo em Inglês | MEDLINE | ID: mdl-30731086

RESUMO

Identification of pharmacologically potent antioxidant compounds for their use in preventive medicine is thrust area of current research. This study was undertaken with the aim of determining the protective role of syringic acid (SA) on isoproterenol (ISO) induced myocardial infarction (MI) in rats. SA was orally given to rats for 21 days at three different concentrations (12.5, 25 and 50 mg/kg). At 20th and 21st day, rats were subcutaneously injected with ISO and at the end of experimental period, rats were killed. ISO induced myocardial damage was averted by pre-co-treatment of SA, as decrease was found in serum level of marker enzymes (CKMB, LDH, AST, ALT), lipid peroxidation, protein carbonyl (PC) and proinflammatory cytokines (TNFα, IL 6). Furthermore, content of glutathione (GSH) and activities of antioxidant enzymes in heart tissue were significantly raised. Improvement in infarct size and erythrocyte (RBCs) morphology was also observed. The biochemical findings were supported by histopathological outcome and protective effect of SA was found to be dose dependent. The results of our study demonstrated that the cardioprotective potential of SA in rat model of ISO induced MI might be due to anti-lipid peroxidative and endogenous antioxidant system enhancement effects.


Assuntos
Cardiotoxicidade/etiologia , Cardiotoxicidade/prevenção & controle , Citoproteção/efeitos dos fármacos , Ácido Gálico/análogos & derivados , Isoproterenol/toxicidade , Adenosina Trifosfatases/metabolismo , Animais , Biomarcadores/sangue , Compostos de Bifenilo/metabolismo , Peso Corporal/efeitos dos fármacos , Cardiotoxicidade/metabolismo , Cardiotoxicidade/patologia , Eritrócitos/efeitos dos fármacos , Eritrócitos/patologia , Fibrose , Ácido Gálico/farmacologia , Glutationa/metabolismo , Coração/efeitos dos fármacos , Masculino , Miocárdio/metabolismo , Miocárdio/patologia , Óxido Nítrico/metabolismo , Tamanho do Órgão/efeitos dos fármacos , Estresse Oxidativo/efeitos dos fármacos , Picratos/metabolismo , Ratos , Ratos Wistar
8.
Life Sci ; 221: 204-211, 2019 Mar 15.
Artigo em Inglês | MEDLINE | ID: mdl-30708101

RESUMO

AIMS: Honokiol is a hydroxylated biphenyl natural product and displays potent antitumor activity against several cancers including prostate cancer, melanoma, leukemia, and colorectal cancer. The present study was to investigate the in vitro activity of honokiol against A549 and 95-D human lung cancer cells. MAIN METHODS: A549 and 95-D cells were used with honokiol treatment. Cell viability was determined by CCK-8 assay. The cell migration and apoptosis were evaluated by wound healing assay and TUNEL staining method respectively. The expressions of ER-related proteins were analyzed by western blot and the CHOP siRNA was used to downregulate the CHOP expression. KEY FINDINGS: The results demonstrated that treatment of A549 and 95-D cells with honokiol significantly reduced cell viability in a dose- and time-dependent manner. Furthermore, honokiol treatment decreased cell migration and enhanced cell apoptosis, which is accompanied by the upregulation of the expressions of ER stress-induced apoptotic signaling molecules such as GRP78, phosphorylated PERK, phosphorylated eIF2α, CHOP, Bcl-2, Bax, and cleaved Caspase 9. Honokiol treatment-induced increase of ER stress-related signaling molecules and apoptotic proteins in A549 and 95-D cells were reversed by CHOP siRNA. SIGNIFICANCE: Collectively, we conclude that ER stress may participate in the action of the anticancer activity of honokiol in A549 and 95-D cells and induction of ER stress-related apoptosis may represent a novel therapeutic intervention for human lung cancer.


Assuntos
Compostos de Bifenilo/farmacologia , Estresse do Retículo Endoplasmático/efeitos dos fármacos , Lignanas/farmacologia , Células A549 , Apoptose/efeitos dos fármacos , Compostos de Bifenilo/metabolismo , Linhagem Celular Tumoral , Movimento Celular/efeitos dos fármacos , Sobrevivência Celular/efeitos dos fármacos , Humanos , Lignanas/metabolismo , Neoplasias Pulmonares/tratamento farmacológico , Neoplasias Pulmonares/metabolismo , RNA Interferente Pequeno , Transdução de Sinais , Fator de Transcrição CHOP/genética , Fator de Transcrição CHOP/metabolismo
9.
Prep Biochem Biotechnol ; 49(1): 82-87, 2019.
Artigo em Inglês | MEDLINE | ID: mdl-30621495

RESUMO

We investigated the effect of Agrobacterium rhizogenes-mediated transformation on antioxidant activity of Artemisia vulgaris "hairy" roots. It appeared that transformation may increase flavonoid content as well as DPPH-scavenging activity and ability to reduce Fe3+ as compared to the non-transformed plants. Some "hairy" roots accumulated flavonoids up to 73.1 ± 10.6 mg RE/g DW (while the amount of flavonoids in the leaves of non-transformed plants was up to 49.4 ± 5.0 mg RE/g DW). DPPH-scavenging activity of some "hairy" root lines was 3-3.8 times higher than such one of the roots of the control plants. The Fe3+-reducing power of most transgenic root extracts exceeded such power of the extracts of the roots of the control plants. The decrease in SOD activity was found in the most "hairy" root lines compared to the control roots. The increase of flavonoid content correlated with the increase of ability of extracts to scavenge DPPH*- radical and Fe3+ - reducing power. No correlation between SOD activity of extracts and concentration of flavonoids was found (p ≥ 0.2).Thus, transformation has led to the alteration in flavonoid accumulation and antioxidant activity in A. vulgaris "hairy" roots. Transgenic roots with high-antioxidant properties can be selected after A. rhizogenes-mediated transformation.


Assuntos
Agrobacterium/fisiologia , Antioxidantes/química , Artemisia/química , Flavonoides/análise , Extratos Vegetais/farmacologia , Raízes de Plantas/química , Compostos de Bifenilo/metabolismo , Flavonoides/metabolismo , Oxirredução , Picratos/metabolismo , Extratos Vegetais/química , Raízes de Plantas/microbiologia , Reação em Cadeia da Polimerase , Transformação Genética/fisiologia
10.
BMC Complement Altern Med ; 19(1): 30, 2019 Jan 28.
Artigo em Inglês | MEDLINE | ID: mdl-30691451

RESUMO

BACKGROUND: Exposure of skin to urban air pollutants is closely related to skin aging and inflammatory responses such as wrinkles formation, pigmentation spot, atopic dermatitis, and acne. Thus, a great deal of interest has been focused on the development of natural resources that can provide a protective effect to skin from pollutants. METHODS: The antioxidative activity of Camellia japonica flower extract (CJFE) was evaluated by 1,2-diphenyl-2-picrylhydrazyl (DPPH) and 2,2'-azino-bis-3-ethylbenzthiazoline-6-sulphonic acid (ABTS) assay, and the inhibitory effect of CJFE by urban air pollutants-induced reactive oxygen species (ROS) production was determined in cultured normal human dermal fibroblasts (NHDFs). We additionally investigated the protective effects of CJFE against urban air pollutant using in vitro and ex vivo model. RESULTS: CJFE with high phenolic concentration showed antioxidative activity on scavenging capacity of 1,2-diphenyl-2-picrylhydrazyl (DPPH) radicals and 2,2'-azino-bis-3-ethylbenzthiazoline-6-sulphonic acid (ABTS) radical cation in a concentration dependent manner. CJFE inhibited urban air pollutants-induced ROS generation, matrixmetalloproteinase-1 (MMP-1) production and a xenobiotic response element (XRE)-luciferase activity indicating the aryl hydrocarbon receptor (AhR) transactivation. In addition, CJFE showed an excellent protective activity against pollutants-induced deteriorating effect in ex vivo model. CJFE reduced the level of pollutants-induced malondialdehyde (MDA), lipid peroxidation marker, inhibited MMP-1 expression and increased collagen synthesis. It also reduced the cell numbers with pyknotic nuclei (mainly occurring in apoptosis) and detachment of dermo-epidermal junction (DEJ) induced by pollutants. CONCLUSIONS: Apparently, it is proposed that CJFE can be used as a protective material against pollutant-induced skin damages.


Assuntos
Poluentes Atmosféricos/toxicidade , Camellia/química , Flores/química , Extratos Vegetais/farmacologia , Substâncias Protetoras/farmacologia , Benzotiazóis/metabolismo , Compostos de Bifenilo/metabolismo , Células Cultivadas , Fibroblastos/efeitos dos fármacos , Humanos , Oxirredução/efeitos dos fármacos , Picratos/metabolismo , Espécies Reativas de Oxigênio/metabolismo , Ácidos Sulfônicos/metabolismo
11.
Microb Pathog ; 128: 236-244, 2019 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-30611769

RESUMO

This work tested anti- Helicobacter pylori, free radicals scavenging and toxicity property as well as chemical constituents in the extract of chloroform (CE) and ethyl acetate (EAE) from the pedicel of Diospyros kaki L. (PDK-CE and PDK-EAE). There were 33 and 36 chemical constituents respectively in the extracts of PDK-CE and PDK-EAE, belonging to the fatty acids methyl ester, fatty acids, and stearic acids, as revealed by Gas Chromatography-Mass Spectrometry (GC-MS). The extracts did not exhibit any toxicity on NIH3T3 cells, but they significantly showed scavenging of NO, DPPH, and H2O2 free radicals. The extracts displayed in vitro anti-H. pylori activity. PDK-CE had the maximum inhibitory zone at a minimal inhibitory concentration (MIC) of 10 µg. ml-1 and the extract also triggered the cellular damage in the bacteria. PDK-CE extract had a high urease inhibitory activity (IC50 value of 8.5 µg). Further, in silico studies was performed by using 41 compounds against H. pylori urease (HPU) and H. pylori peptide deformylase (HPPD). The score value was the maximum (-19.58 kcal/mol) against HPU with 17-(5-ethyl-6-methylheptan-2-yl)-10,13-dimethyl-2,3,4,7,8,9,11,12,14,15,16,17-dodecahydro-1H-cyclopenta[a]phenanthren-3-ol, while the score value was the maximum (-14.51 kcal/mol) against HPPD with hexadecanoic acid. The results demonstrated the importance of the pedicel extracts in future pharmaceutical drug development against H. pylori infections.


Assuntos
Amidoidrolases/efeitos dos fármacos , Antibacterianos/farmacologia , Biologia Computacional/métodos , Diospyros/química , Helicobacter pylori/efeitos dos fármacos , Extratos Vegetais/farmacologia , Urease/efeitos dos fármacos , Animais , Antibacterianos/química , Compostos de Bifenilo/metabolismo , Morte Celular/efeitos dos fármacos , Embrião de Galinha , Membrana Corioalantoide/efeitos dos fármacos , Depuradores de Radicais Livres , Radicais Livres , Cromatografia Gasosa-Espectrometria de Massas/métodos , Infecções por Helicobacter/tratamento farmacológico , Helicobacter pylori/enzimologia , Peróxido de Hidrogênio/metabolismo , Concentração Inibidora 50 , Camundongos , Testes de Sensibilidade Microbiana , Simulação de Acoplamento Molecular , Células NIH 3T3/efeitos dos fármacos , Óxido Nítrico/metabolismo , Picratos/metabolismo , Extratos Vegetais/química
12.
Microb Pathog ; 127: 326-334, 2019 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-30553013

RESUMO

Reinwardtia indica (Lineceae) is a medicinal plant cultivated in the Himalayan region. It is effectively used in folk medicines for the treatment of various health complications. In the present study, the shade dried leaves and stem were extracted in three different solvents such as ethyl acetate, ethanol, and hydro-alcoholic. The antioxidant efficacy of these extracts was confirmed by using different in vitro assays: DPPH free radical scavenging, superoxide radical scavenging, lipid peroxidation, metal ion chelating capability and reducing power determination. Total phenol content was maximum in hydro alcoholic extract of leaf (540.37 mg per g of gallic acid equivalents) and stem (330.51 mg per g of gallic acid equivalents) while flavonoid content was maximum in ethanolic extract of leaf (305 mg per gram of rutin equivalents) and ethyl acetate extract of stem (170.6 mg per gram of rutin equivalents). The antioxidant activity of these extracts was positively correlated with their total phenol and flavonoid content. Among all tested extracts, ethanolic extract of leaf exhibit maximum zone of inhibition against all tested clinical isolates of bacterial (E. coli 11.00 ±â€¯1.73 mm, P. aeurogenosa 11.67 ±â€¯0.58 mm and S. aureus 10.33 ±â€¯1.53 mm) and fungal (C. albicans 11.33 ±â€¯1.10 mm) pathogens, while ethyl acetate extracts of the leaf and stem showed minimum inhibitory concentration against all tested microorganisms. Thus, R. indica extracts can be used as potent natural antioxidant having antifungal and antibacterial action.


Assuntos
Antibacterianos/farmacologia , Antioxidantes/farmacologia , Linaceae/química , Compostos Fitoquímicos/farmacologia , Extratos Vegetais/farmacologia , Antibacterianos/isolamento & purificação , Antioxidantes/isolamento & purificação , Compostos de Bifenilo/metabolismo , Escherichia coli/efeitos dos fármacos , Peroxidação de Lipídeos , Metais/metabolismo , Testes de Sensibilidade Microbiana , Oxirredução , Compostos Fitoquímicos/análise , Compostos Fitoquímicos/isolamento & purificação , Picratos/metabolismo , Extratos Vegetais/isolamento & purificação , Folhas de Planta/química , Caules de Planta/química , Pseudomonas aeruginosa/efeitos dos fármacos , Staphylococcus aureus/efeitos dos fármacos , Superóxidos/metabolismo
13.
Nutrients ; 10(12)2018 Dec 18.
Artigo em Inglês | MEDLINE | ID: mdl-30567311

RESUMO

Tagetes erecta L. has long been consumed for culinary and medicinal purposes in different countries. The aim of this study was to explore the potential benefits from two cultivars of T. erecta related to its polyphenolic profile as well as antioxidant and anti-aging properties. The phenolic composition was analyzed by LC-DAD-ESI/MSn. Folin-Ciocalteu, DPPH·, and FRAP assays were performed in order to evaluate reducing antiradical properties. The neuroprotective potential was evaluated using the enzymes acetylcholinesterase and monoamine oxidase. Caenorhabditis elegans was used as an in vivo model to assess extract toxicity, antioxidant activity, delayed aging, and reduced ß-amyloid toxicity. Both extracts showed similar phenolic profiles and bioactivities. The main polyphenols found were laricitin and its glycosides. No acute toxicity was detected for extracts in the C. elegans model. T. erecta flower extracts showed promising antioxidant and neuroprotective properties in the different tested models. Hence, these results may add some information supporting the possibilities of using these plants as functional foods and/or as nutraceutical ingredients.


Assuntos
Envelhecimento/efeitos dos fármacos , Antioxidantes/farmacologia , Caenorhabditis elegans/efeitos dos fármacos , Fármacos Neuroprotetores/farmacologia , Fenóis/farmacologia , Polifenóis/farmacologia , Tagetes/química , Acetilcolinesterase/metabolismo , Peptídeos beta-Amiloides/metabolismo , Animais , Antioxidantes/análise , Compostos de Bifenilo/metabolismo , Caenorhabditis elegans/metabolismo , Flores/química , Alimento Funcional , Glicosídeos/análise , Glicosídeos/farmacologia , Modelos Animais , Monoaminoxidase/metabolismo , Fármacos Neuroprotetores/análise , Fenóis/análise , Picratos/metabolismo , Extratos Vegetais/farmacologia , Plantas Comestíveis , Polifenóis/análise , Especificidade da Espécie , Tagetes/classificação
14.
Molecules ; 23(12)2018 Dec 19.
Artigo em Inglês | MEDLINE | ID: mdl-30572648

RESUMO

The present study investigated the phenolic profiles and antioxidant properties of different fractions from Prinsepia utilis Royle fruits using molecular docking analysis to delineate their inhibition toward digestive enzymes. A total of 20 phenolics was identified and quantified. Rutin, quercetin-3-O-glucoside, and isorhamnetin-3-O-rutinoside were the major phenolic compounds in the total phenolic fraction and flavonoid-rich fraction. The anthocyanin-rich fraction mainly contained cyanidin-3-O-glucoside and cyanidin-3-O-rutinoside. All of the fractions exhibited strong radical scavenging activities and good inhibition on cellular reactive oxygen species (ROS) generation in H2O2-induced HepG2 cells, as evaluated by DPPH and 2,2'-azino-bis (3-ethylbenzothiazoline-6-sulphonic acid) (ABTS) assays. Moreover, the powerful inhibitory effects of those fractions against pancreatic lipase and α-glucosidase were observed. The major phenolic compounds that were found in the three fractions also showed good digestive enzyme inhibitory activities in a dose-dependent manner. Molecular docking analysis revealed the underlying inhibition mechanisms of those phenolic standards against digestive enzymes, and the theoretical analysis data were consistent with the experimental results.


Assuntos
Frutas/química , Fenóis/análise , Extratos Vegetais/química , Antioxidantes/química , Antioxidantes/farmacologia , Benzotiazóis , Compostos de Bifenilo/metabolismo , Ativação Enzimática/efeitos dos fármacos , Células Hep G2 , Humanos , Peróxido de Hidrogênio/farmacologia , Lipase/metabolismo , Simulação de Acoplamento Molecular , Picratos/metabolismo , Extratos Vegetais/farmacologia , Espécies Reativas de Oxigênio/metabolismo , Ácidos Sulfônicos , alfa-Glucosidases/metabolismo
15.
Molecules ; 24(1)2018 Dec 20.
Artigo em Inglês | MEDLINE | ID: mdl-30577525

RESUMO

Inflammation is a complex phenomenon that results as a healing response of organisms to different factors, exerting immune signaling, excessive free radical activity and tissue destruction. Lipoxygenases and their metabolites e.g., LTB4, are associated with allergy, cell differentiation and carcinogenesis. Lipoxygenase 12/15 has been characterized as a mucosal-specific inhibitor of IgA and a contributor to the development of allergic sensitization and airway inflammation. Development of drugs that interfere with the formation or effects of these metabolites would be important for the treatment of various diseases like asthma, psoriasis, ulcerative colitis, rheumatoid arthritis, atherosclerosis, cancer and blood vessel disorders. In this study we extended our previous research synthesizing a series of multi-target cinnamic acids from the corresponding aldehydes with suitable 4-OH/Br substituted phenyl acetic acid by Knoevenagel condensation. The final products 1i, 3i, 3ii, 4i, 6i, 6ii, and 7i were obtained in high yields (52⁻98%) Their structures were verified spectrometrically, while their experimentally lipophilicity was determined as RM values. The novel derivatives were evaluated for their antioxidant activity using DPPH, hydroxyl radical, superoxide anion and ABTS+•, anti-lipid peroxidation and soybean lipoxygenase inhibition assays. The compounds presented medium interaction with DPPH (30⁻48% at 100 µM). In contrast all the synthesized derivatives strongly scavenge OH radicals (72⁻100% at 100 µM), ABTS+• (24⁻83% at 100 µM) and presented remarkable inhibition (87⁻100% at 100 µM) in linoleic acid peroxidation (AAPH). The topological polar surface of the compounds seems to govern the superoxide anion scavenging activity. Molecular docking studies were carried out on cinnamic acid derivative 3i and found to be in accordance with experimental biological results. All acids presented interesting lipoxygenase inhibition (IC50 = 7.4⁻100 µM) with compound 3i being the most potent LOX inhibitor with IC50 = 7.4 µM combining antioxidant activities. The antioxidant results support the LOX inhibitory activities. The recorded in vitro results highlight compound 3i as a lead compound for the design of new potent lipoxygenase inhibitors for the treatment of asthma, psoriasis, ulcerative colitis, rheumatoid arthritis, atherosclerosis, cancer and blood vessel disorders.


Assuntos
Cinamatos/farmacologia , Benzotiazóis/química , Benzotiazóis/metabolismo , Compostos de Bifenilo/química , Compostos de Bifenilo/metabolismo , Radical Hidroxila/química , Radical Hidroxila/metabolismo , Inflamação/metabolismo , Peroxidação de Lipídeos/efeitos dos fármacos , Lipoxigenase/metabolismo , Estresse Oxidativo/efeitos dos fármacos , Picratos/química , Picratos/metabolismo , Ácidos Sulfônicos/química , Ácidos Sulfônicos/metabolismo
16.
BMC Complement Altern Med ; 18(1): 240, 2018 Aug 22.
Artigo em Inglês | MEDLINE | ID: mdl-30134897

RESUMO

BACKGROUND: Here, we determined in vitro antioxidant activity, total phenols and flavonoids and evaluated antiproliferative activity of three medicinal plant extracts: Trigonella foenum-graecum (Fenugreek), Cassia acutifolia (Senna) and Rhazya stricta (Harmal). METHODS: The leaves of the three medicinal plants were extracted with 70% ethanol. Antioxidant activities of the extracts were determined by using DPPH (1,1-diphenyl-2-picrylhydrazyl) assay. Total flavonoid and phenolic contents were determined using colorimetric assays. MTT assay was used to estimate the antiproliferative activities of the extracts against human hepatoma (HepG2) cancer cell line. In addition, the effects of R. stricta extract on cell cycle, colony formation, and wound healing of HepG2 cells and tube formation of HUVEC cells were assessed. RESULTS: Percentage inhibition of DPPH scavenging activity were dose-dependent and ranged between (89.9% ± 0.51) and (28.6% ± 2.07). Phenolic contents ranged between (11.5 ± 0.013) and (9.7 ± 0.008) mg GAE/g while flavonoid content ranged between (20.8 ± 0.40) and (0.12 ± 0.0.01) mg QE/g. Antiproliferative results of the extracts were found to be consistent with their antioxidant activity. Among the extracts evaluated, that of R. stricta showed the best antioxidant, antiproliferative and antimetastatic activities at low concentration. It also inhibited the colony-formation capacity of HepG2 cells and exhibited antiangiogenic activity. Cell cycle analysis showed significant arrest of cells at G2/M phase 12 and 48 h after treatment and significant arrest at G1/S phase after 24 h of treatment. Consistent data were observed in western blot analysis of protein levels of Cdc2 and its cyclin partners. CONCLUSIONS: These findings introduce R. stricta as a potentially useful anti-metastatic agent and a novel potential anti-tumour agent for hepatocellular carcinoma (HCC) treatment.


Assuntos
Antineoplásicos , Antioxidantes , Fabaceae/química , Extratos Vegetais , Antineoplásicos/química , Antineoplásicos/farmacologia , Antioxidantes/química , Antioxidantes/farmacologia , Compostos de Bifenilo/metabolismo , Sobrevivência Celular/efeitos dos fármacos , Flavonoides/análise , Células Hep G2 , Células Endoteliais da Veia Umbilical Humana , Humanos , Medicina Tradicional , Fenóis/análise , Picratos/metabolismo , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Folhas de Planta/química , Plantas Medicinais/química
17.
Artigo em Inglês | MEDLINE | ID: mdl-30121456

RESUMO

Traditional Tibetan medicine (TTM) has been valuable for the identification of new therapeutic leads. Nevertheless, reports about the chemical constituents of TTM are meager owing to the lack of suitable purification techniques. In this study, an off-line two-dimensional reversed-phase/hydrophilic interaction liquid chromatography (2D RP/HILIC) technique guided by on-line HPLC-DPPH has been established for the isolation of pure antioxidants from the extract of Dracocephalum heterophyllum. According to the chromatographic recognition outcome of the HPLC-DPPH system, the first-dimensional (1D) separation on the Megress C18 preparative column yielded 6 antioxidative fractions (61.4% recovery) from the ethyl acetate fraction (6.1 g). In the second-dimensional (2D) separation, a HILIC XAmide preparative column was employed. In total, 8 antioxidants were isolated from D. heterophyllum with a purity of >95%, which indicated the efficiency of the developed method to prepare antioxidative compounds with high purity from plant extracts. In addition, this method was highly efficient for the preparation of structural analogues of the antioxidative polyphenols and could be applied for the purification of structural analogues from other resources.


Assuntos
Antioxidantes/isolamento & purificação , Cromatografia de Fase Reversa/métodos , Lamiaceae/química , Extratos Vegetais/química , Antioxidantes/análise , Antioxidantes/química , Antioxidantes/metabolismo , Compostos de Bifenilo/análise , Compostos de Bifenilo/metabolismo , Cromatografia Líquida de Alta Pressão/métodos , Interações Hidrofóbicas e Hidrofílicas , Picratos/análise , Picratos/metabolismo
18.
Int J Mol Sci ; 19(8)2018 Jul 27.
Artigo em Inglês | MEDLINE | ID: mdl-30060488

RESUMO

Chitosan oligosaccharide (COS), derived through hydrolysis of chitosan, has been proved to be an effective plant immunity elicitor, eco-friendly, and easily soluble in water, and influenced several secondary metabolites content to improve fruit qualities. COS are widely used in agriculture to improve the defense response in plants. The purpose of this study was to investigate the pre-harvest treatment effect of COS on the quality of strawberry (Fragaria × ananassa cv.qingxiang). COS was dissolved in distilled water at a concentration of 50 mg·L-1 and sprayed at four different growth stages of strawberry plants, namely seedling stage, before flowering, fruit coloring (the stage of fruit from white to red) and full bloom. Uniform size, shape, color, without any visible damage, and disease-free fruits were harvested for determining the quality. The results showed that the fruit firmness, viscosity, lignin, sugars, protein, total soluble solid, and titratable acidity content increased in COS-treated fruits compared to control. In addition, COS pre-harvest treatment had a positive effect on anthocyanin, total phenol, flavonoid, vitamin C content and DPPH(2,2-diphenyl-1-picrylhydrazyl) scavenging activity of strawberry. Moreover, COS also increased the cell wall composition and regulated gene expression of some important enzymes involved in ethylene compound biosynthesis and cell wall degradation. The finding of this study suggests that pre-harvest application of COS is very useful for improving quality and antioxidant capacity of strawberry.


Assuntos
Quitosana/farmacologia , Produtos Agrícolas/efeitos dos fármacos , Fragaria/efeitos dos fármacos , Fragaria/metabolismo , Oligossacarídeos/farmacologia , Antocianinas/metabolismo , Ácido Ascórbico/metabolismo , Compostos de Bifenilo/metabolismo , Parede Celular/química , Parede Celular/enzimologia , Parede Celular/metabolismo , Quitosana/química , Produtos Agrícolas/química , Produtos Agrícolas/metabolismo , Flavonoides/metabolismo , Flores/química , Flores/metabolismo , Qualidade dos Alimentos , Fragaria/química , Regulação da Expressão Gênica de Plantas/efeitos dos fármacos , Oligossacarídeos/química , Picratos/metabolismo , Plântula/química , Plântula/metabolismo , Água/química
19.
Pestic Biochem Physiol ; 149: 123-136, 2018 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-30033008

RESUMO

Drought stress is one of the most important environmental factors that limit plant growth. Canola is an important agricultural crop grown primarily for its edible oil. In this study, penconazole (PEN), a triazole growth regulator, and calcium (Ca2+), a secondary messenger, were used to analyses their role in decease sensitivity and induce tolerance to drought stress in canola. Plants were treated by various PEG concentrations (0, 5, 10, and 15%) without or with PEN (15 mg l-1) and Ca2+ (15 mM). According to the obtained results in two cultivars of canola (RGS003 and Sarigol), improvement of growth by PEN and Ca2+observed at low concentration of drought (5%). Betterment of growth by PEN can be explained by induction in DPPH (1, 1-diphenyl-2- picrylhydrazyl), chlorophyll and P content and reduction in Electrolyte leakage in cultivar RGS003. Growth recovery by PEN is concomitant by increase in DPPH, succinate dehydrogenase, chlorophyll, carotenoid and K+ content in cultivar Sarigol. Ca2+ treatment by induction in Relative water content, DPPH, chlorophyll, carotenoid, indole-3-acetic acid content and the content of Ca2+ and K+ causes increase in growth in cultivar Sarigol. Overall, application of PEN and Ca2+ improved the performance in canola under drought stress. These results provide novel insights about the physiological and molecular roles of PEN and Ca2+ in canola plant tolerance against drought stress.


Assuntos
Adaptação Fisiológica/efeitos dos fármacos , Brassica rapa/efeitos dos fármacos , Cálcio/farmacologia , Secas , Reguladores de Crescimento de Planta/farmacologia , Triazóis/farmacologia , Compostos de Bifenilo/metabolismo , Brassica rapa/genética , Brassica rapa/metabolismo , Brassica rapa/fisiologia , Calmodulina/genética , Carotenoides/metabolismo , Clorofila/metabolismo , Regulação da Expressão Gênica de Plantas/efeitos dos fármacos , Genes de Plantas , Ácidos Indolacéticos/metabolismo , Peroxidases/metabolismo , Fósforo/metabolismo , Picratos/metabolismo , Potássio/metabolismo , Proteínas Quinases/genética , Reação em Cadeia da Polimerase Via Transcriptase Reversa , Succinato Desidrogenase/metabolismo
20.
Meat Sci ; 145: 9-15, 2018 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-29859422

RESUMO

In this study, clove essential oil (CL) or eugenol (EU) containing cellulose acetate (CA) or acrylic component/hydrophobically modified starch (AC/S) coatings on corona treated oriented polypropylene film (OPP) were designed and investigated for their possible applications as antioxidant packaging materials for fresh meat. The antioxidant properties of the coatings were investigated by Vapour Phase-DPPH (2,2-diphenyl-1-picrylhydrazyl) assay. The CA coatings containing CL or EU showed 43-92% and 43-94% inhibition against DPPH free radicals through the vapour phase, respectively, whereas AC/S/CL and AC/S/EU coatings resulted in DPPH inhibition of 21-65% and 25-84%, respectively. AC/S/EU and CA/EU coatings on OPP containing from 0.32 ±â€¯0.03 to 6.40 ±â€¯0.14 g/m2 of EU were used to prepare packaging for fresh beef (Longissimus thoracis). After 14 days, the lipid oxidation in beef steaks kept in control and antioxidant packages was 3.33 and 1.00-1.22 mg of malondialdehyde per kilogram of meat, respectively. Moreover, red colour of beef in antioxidant packages was retained.


Assuntos
Antioxidantes , Eugenol , Embalagem de Alimentos/métodos , Conservação de Alimentos/métodos , Óleos Voláteis , Carne Vermelha/análise , Syzygium/química , Animais , Antioxidantes/farmacologia , Compostos de Bifenilo/metabolismo , Bovinos , Celulose/análogos & derivados , Cor , Eugenol/farmacologia , Conservantes de Alimentos/farmacologia , Humanos , Peroxidação de Lipídeos , Malondialdeído/metabolismo , Músculo Esquelético/metabolismo , Picratos/metabolismo , Polipropilenos , Amido , Substâncias Reativas com Ácido Tiobarbitúrico
SELEÇÃO DE REFERÊNCIAS
DETALHE DA PESQUISA