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1.
Zhongguo Zhong Yao Za Zhi ; 45(2): 367-373, 2020 Jan.
Artigo em Chinês | MEDLINE | ID: mdl-32237320

RESUMO

To identify and verify the active ingredients from Astragalus membranaceus on hypertensive cardiac remodeling based on network pharmacology and heart RNA-sequencing data. The monomers of A. membranaceus and their intervention target database were established by using network pharmacology. The genes associated to cardiac remodeling were then screened by analyzing cardiac RNA-sequencing data. An overlap between genes related to cardiac remodeling and targets of ingredients form A. membranaceus was collected to obtain monomers with protective effect on hypertensive cardiac remodeling. Angiotensin Ⅱ(AngⅡ)-induced mouse cardiac remodeling model was used to validate the protective effect of active ingredients from A. membranaceus on hypertensive cardiac remodeling. Finally, a total of 81 monomers and 1 197 targets were enrolled in our database. Mouse RNA-sequencing data showed that 983 genes were significantly up-regulated and 465 genes were down-regulation in myocardial tissues of the cardiac remodeling mice as compared with blank group mice, respectively. Ninety-two genes were found via overlapping between genes related to cardiac remodeling and targets, involving 59 monomers from A. membranaceus. Further research found that vanillic acid(VA) could intervene 27 genes associated with hypertensive cardiac remodeling, ranking top 1. Meanwhile, VA could significantly inhibit AngⅡ-induced increase in ratio of heart weight to body weight and heart weight to tibial length, ANP and BNP mRNA levels in myocardial tissues, myocardial tissue damage, cardiac fibrosis level and cardiac hypertrophy level in vivo. Those results showed that network pharmacology screen-based VA has protective effect on AngⅡ-induced cardiac remodeling.


Assuntos
Astragalus propinquus/química , Hipertensão/genética , Ácido Vanílico/farmacologia , Remodelação Ventricular/efeitos dos fármacos , Angiotensina II , Animais , Coração , Camundongos , Substâncias Protetoras/farmacologia , Remodelação Ventricular/genética
2.
Plant Physiol Biochem ; 150: 109-120, 2020 May.
Artigo em Inglês | MEDLINE | ID: mdl-32135476

RESUMO

We investigated vanillic acid-induced salt tolerance in tomato by exploring the plant defense systems. Ten-d-old tomato (Solanum lycopersicum L. cv. Pusa Ruby) seedlings were treated with salt (NaCl; 150 mM) and vanillic acid (VA; 40 and 50 µM) separately and in combination with salt. Salinity restricted seedlings growth, biomass accumulation, chlorophyll and carotenoid contents. Salt-induced osmotic stress was indicated by lower leaf relative water content (RWC) and elevated proline (Pro) content, where higher Na+/K+ ratio indicated the ionic toxicity. Tomato seedlings went through oxidative damage due to acute reactive oxygen species (ROS) production and lipoxygenase (LOX) activity and confirmed by higher lipid peroxidation and membrane damage under salinity. Conversely, exogenous VA reduced osmotic and ionic toxicity in stressed-seedlings by enhancing the RWC and Pro level, and lowering Na+/K+ ratio, respectively. Exogenous VA up-regulated the components of antioxidant defense system in salt-treated seedlings resulted in the reduction of ROS production, LOX activity and membrane damage in stressed-seedlings. Additionally, VA application caused the reduction of toxic methylglyoxal accumulation under salt stress through the enhancement of glyoxalase system. Thus, VA-induced alleviation of osmotic, ionic and oxidative stresses leading to improve plant growth and chlorophyll synthesis in stressed-seedlings. So, VA significantly improves salinity tolerance and plant growth performance by involving the actions of plant antioxidant defense and glyoxalase systems.


Assuntos
Lycopersicon esculentum , Tolerância ao Sal , Ácido Vanílico , Lycopersicon esculentum/efeitos dos fármacos , Lycopersicon esculentum/enzimologia , Oxirredutases/metabolismo , Tolerância ao Sal/efeitos dos fármacos , Plântula/efeitos dos fármacos , Estresse Fisiológico/efeitos dos fármacos , Ácido Vanílico/farmacologia
3.
J Appl Microbiol ; 128(2): 387-400, 2020 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-31573730

RESUMO

AIMS: To study the individual and combined contribution of catechin, protocatechuic and vanillic acids to inhibit the adhesion of uropathogenic Escherichia coli (UPEC) on the surface of silicone catheters. METHODS AND RESULTS: The adhesion of UPEC to silicone catheters during the exposure to nonlethal concentrations of phenolic compounds was measured, as well as changes in motility, presence of fimbriae, extra-cellular polymeric substances, surface charge, hydrophobicity and membrane fluidity. The phenolic combination reduced 26-51% of motility, 1 log CFU per cm2 of adhered bacteria and 20-40% the carbohydrate and protein content in the biofilm matrix. Curli fimbriae, surface charge and cell hydrophobicity were affected to a greater extent by the phenolic combination. In the mixture, vanillic acid was the most effective for reducing bacterial adhesion, extra-polymeric substance production, motility, curli fimbriae and biofilm structure. Notwithstanding, protocatechuic acid caused major changes in the bacterial cell surface properties, whereas catechin affected the cell membrane functionality. CONCLUSION: Catechin, protocatechuic and vanillic acids have different bacterial cell targets, explaining the synergistic effect of their combination against uropathogenic E. coli. SIGNIFICANCE AND IMPACT OF STUDY: This study shows the contribution of catechin, protocatechuic and vanillic acids in producing a synergistic mixture against the adhesion of uropathogenic E. coli on silicone catheters. The action of catechin, vanillic and protocatechuic acids included specific contributions of each compound against the E. coli membrane's integrity, motility, surface properties and production of extracellular polymeric substances. Therefore, the studied mixture of phenolic compounds could be used as an antibiotic alternative to reduce urinary tract infections associated with silicone catheters.


Assuntos
Antibacterianos/farmacologia , Aderência Bacteriana/efeitos dos fármacos , Biofilmes/efeitos dos fármacos , Catequina/farmacologia , Hidroxibenzoatos/farmacologia , Infecções Urinárias/microbiologia , Escherichia coli Uropatogênica/efeitos dos fármacos , Ácido Vanílico/farmacologia , Cateteres/microbiologia , Sinergismo Farmacológico , Infecções por Escherichia coli/microbiologia , Fímbrias Bacterianas/efeitos dos fármacos , Fímbrias Bacterianas/genética , Fímbrias Bacterianas/metabolismo , Humanos , Fenóis/farmacologia , Silicones/análise , Escherichia coli Uropatogênica/crescimento & desenvolvimento , Escherichia coli Uropatogênica/fisiologia
4.
Immunopharmacol Immunotoxicol ; 41(6): 591-598, 2019 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-31595796

RESUMO

Background: Hispidulin, nepetin, and vanillic acid are phenolic compounds potentially possessing immunosuppressive property, however, no information on their pharmacological effect and cytotoxicity has been investigated on human T lymphocytes.Materials and methods: Human peripheral blood mononuclear cells were stimulated with anti-CD3/28 coated beads and treated with individual compound at different concentrations (50-200 µM). Inhibition of early cell activation and induction of apoptosis were analyzed by flow cytometric technique.Results: At 200 µM, frequencies of CD25 and CD69 in CD4+ and CD8+ T lymphocytes were markedly decreased by hispidulin and nepetin. When lowering to 100 and 50 µM, hispidulin had no effect on the expression of CD69 in CD4+ T cells, whereas nepetin selectively suppressed CD25 and CD69 expressions in CD8+ T cells at 100 µM and only inhibited CD69 in CD8+ T cells at 50 µM. For vanillic acid, no inhibitory effect was observed while cell activation was significantly increased for all treated concentrations. None of these compounds disturbed levels of total apoptotic cells in CD4+ and CD8+ populations.Conclusions: Hispidulin and nepetin, therefore, exhibit dose-dependent inhibitory activity of early T-cell activation without inducing cell death, considering feasible immunosuppressants for inflammation-related diseases. However, vanillic acid has no effect on immunosuppression but shows more potential on immunostimulation.HighlightsImmunosuppressive effects of hispidulin and nepetin on human T cells were studied.Dose-dependent activity for T-cell suppression was found in hispidulin and nepetin.Vanillic acid showed immunostimulating potential rather than immunosuppression.All compounds did not induce cell death.


Assuntos
Linfócitos T CD4-Positivos/imunologia , Linfócitos T CD8-Positivos/imunologia , Flavonas/farmacologia , Ativação Linfocitária/efeitos dos fármacos , Ácido Vanílico/farmacologia , Antígenos CD/imunologia , Humanos
5.
Oxid Med Cell Longev ; 2019: 3904905, 2019.
Artigo em Inglês | MEDLINE | ID: mdl-31379988

RESUMO

Coenzyme Q (CoQ), a redox-active lipid, is comprised of a quinone group and a polyisoprenoid tail. It is an electron carrier in the mitochondrial respiratory chain, a cofactor of other mitochondrial dehydrogenases, and an essential antioxidant. CoQ requires a large set of enzymes for its biosynthesis; mutations in genes encoding these proteins cause primary CoQ deficiency, a clinically and genetically heterogeneous group of diseases. Patients with CoQ deficiency often respond to oral CoQ10 supplementation. Treatment is however problematic because of the low bioavailability of CoQ10 and the poor tissue delivery. In recent years, bypass therapy using analogues of the precursor of the aromatic ring of CoQ has been proposed as a promising alternative. We have previously shown using a yeast model that vanillic acid (VA) can bypass mutations of COQ6, a monooxygenase required for the hydroxylation of the C5 carbon of the ring. In this work, we have generated a human cell line lacking functional COQ6 using CRISPR/Cas9 technology. We show that these cells cannot synthesize CoQ and display severe ATP deficiency. Treatment with VA can recover CoQ biosynthesis and ATP production. Moreover, these cells display increased ROS production, which is only partially corrected by exogenous CoQ, while VA restores ROS to normal levels. Furthermore, we show that these cells accumulate 3-decaprenyl-1,4-benzoquinone, suggesting that in mammals, the decarboxylation and C1 hydroxylation reactions occur before or independently of the C5 hydroxylation. Finally, we show that COQ6 isoform c (transcript NM_182480) does not encode an active enzyme. VA can be produced in the liver by the oxidation of vanillin, a nontoxic compound commonly used as a food additive, and crosses the blood-brain barrier. These characteristics make it a promising compound for the treatment of patients with CoQ deficiency due to COQ6 mutations.


Assuntos
Trifosfato de Adenosina/metabolismo , Ubiquinona/análogos & derivados , Ácido Vanílico/farmacologia , Sequência de Aminoácidos , Animais , Sistemas CRISPR-Cas/genética , Células HEK293 , Humanos , Mitocôndrias/metabolismo , Mutagênese Sítio-Dirigida , Isoformas de Proteínas/genética , Isoformas de Proteínas/metabolismo , Estrutura Terciária de Proteína , Espécies Reativas de Oxigênio/metabolismo , Alinhamento de Sequência , Ubiquinona/biossíntese , Ubiquinona/genética , Ubiquinona/metabolismo
6.
J Biochem Mol Toxicol ; 33(10): e22382, 2019 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-31468657

RESUMO

Vanillic acid (VA) is found in high concentrations in various plants and used as traditional medicine for various diseases. The aim of the existing study is to illustrate the protective effects of VA against benzo(a)pyrene (B(a)P)-induced lung cancer in Swiss albino mice. B(a)P (50 mg/kg b.wt.) was given orally to induce lung cancer in mice. The body weight, tumor incidence, carcinoembryonic antigen (CEA), neuron-specific enolase (NSE), and enzymatic/nonenzymatic antioxidants (superoxide dismutase, catalase, glutathione reductase, glutathione peroxidase, and glutathione) were estimated. Further histochemical investigation through hematoxylin and eosin staining was also carried out. B(a)P administered groups showed increased levels of serum pathological markers CEA, NSE along with reduced final body weight as well as decreased tissue enzymatic and nonenzymatic antioxidants activities, whereas VA treatment (200mg/kg/b.wt) along with B(a)P showed significantly reverted the above changes, which proves as prominent anticancer effects in experimentally induced lung cancer. Overall, these results suggest that VA has an efficient preventive action against B(a)P-induced lung cancer, and this is attributed to its free-radical scavenging antioxidant activities.


Assuntos
Benzo(a)pireno/toxicidade , Carcinógenos/toxicidade , Neoplasias Pulmonares/induzido quimicamente , Neoplasias Pulmonares/prevenção & controle , Ácido Vanílico/farmacologia , Animais , Antioxidantes/metabolismo , Antígeno Carcinoembrionário/metabolismo , Pulmão/efeitos dos fármacos , Pulmão/patologia , Neoplasias Pulmonares/enzimologia , Neoplasias Pulmonares/metabolismo , Masculino , Camundongos , Tamanho do Órgão/efeitos dos fármacos , Fosfopiruvato Hidratase/metabolismo
7.
J Biosci Bioeng ; 128(5): 622-629, 2019 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-31186185

RESUMO

In recent years, the number of patients with osteoporosis has increased as population grows older. Therefore, the chemoprevention of osteoporosis by better nutrition is important. White-rot fungi degrades milled wood lignin for growth and development. This degradation results in the formation of phenolic compounds such as syringic acid (SA) and vanillic acid (VA). In the artificial culture of edible mushrooms using a mushroom bed, the disposal of waste beds after mushroom cultivation is an important issue. The present study investigated the presence and amount of both SA and VA in the discarded waste beds after mushroom cultivation. The extracts from waste beds after cultivation of shiitake mushrooms, Lentinula edodes; buna shimeji, Hypsizygus marmoreus; maitake, Grifola frondosa; king trumpet mushrooms, Pleurotus eryngii; and butterscotch mushrooms, Pholiota microspora were analyzed using high performance liquid chromatography. Although the content of SA and VA was considerably different among the mushrooms, SA and VA were present in extracts obtained from all the waste beds. We also demonstrated that SA and VA exert their anti-osteoporotic effect independently of the estrogen receptor-mediated pathway using murine monocytic RAW264.7 cells, ovariectomized mice, and human breast cancer MCF-7 cells. Thus, these results suggest that the extracts are effective sources of SA and VA, which are effective in preventing osteoporosis.


Assuntos
Agaricales/química , Ácido Gálico/análogos & derivados , Osteoporose/tratamento farmacológico , Ácido Vanílico/farmacologia , Animais , Linhagem Celular , Ácido Gálico/química , Ácido Gálico/farmacologia , Humanos , Camundongos , Ácido Vanílico/química
8.
Eur J Pharmacol ; 859: 172481, 2019 Sep 15.
Artigo em Inglês | MEDLINE | ID: mdl-31228458

RESUMO

Osteoarthritis (OA) is a frequently seen arthropathy that features cartilage loss and destruction. Vanillic acid (VA), is a well-known flavonoid, which possesses various pharmacological activities. However, the effects of Vanillic acid on articular cartilage destruction and the pathogenesis of OA remain unknown. The present study observed that VA attenuated OA progression in vivo and vitro. VA inhibited the expression of inflammation responses, including cyclooxygenase-2 (COX-2), inducible nitric oxide synthase (iNOS), matrix metalloproteinases (MMPs) and aggrecanase -2(ADAMTS5). Moreover, the major markers of hypertrophic chondrocytes such as Collagen X, Runt related transcription factor 2 (Runx2) and Vascular endothelial growth factor (VEGFA) were also reduced by VA. In addition, the interleukin-1ß (IL-1ß) -stimulated collagen 2 and aggrecan destruction were suppressed by VA. Moreover, VA concentration -dependently inhibited IL-1ß induced production of High-mobility group box 1 (HMGB1), a classic damage-associated molecular pattern (DAMP) molecule with strong pro-inflammatory effects in OA. Meanwhile, we revealed that VA suppressed the IL-1ß induced activation of MAPK and PI3K/AKT/NF-κB pathways. In vivo, VA alleviated osteoarthritis progression in a rat OA model. Collectively, our results demonstrate that VA could potentially be a new candidate for OA therapy.


Assuntos
Cartilagem/efeitos dos fármacos , Sistema de Sinalização das MAP Quinases/efeitos dos fármacos , NF-kappa B/metabolismo , Fosfatidilinositol 3-Quinases/metabolismo , Proteínas Proto-Oncogênicas c-akt/metabolismo , Ácido Vanílico/farmacologia , Animais , Cartilagem/metabolismo , Cartilagem/patologia , Sobrevivência Celular/efeitos dos fármacos , Condrócitos/efeitos dos fármacos , Condrócitos/patologia , Matriz Extracelular/efeitos dos fármacos , Matriz Extracelular/metabolismo , Hipertrofia/patologia , Interleucina-1beta/farmacologia , Osteoartrite/tratamento farmacológico , Osteoartrite/metabolismo , Osteoartrite/patologia , Ratos , Ratos Sprague-Dawley , Ácido Vanílico/uso terapêutico
9.
Biosci Biotechnol Biochem ; 83(7): 1205-1215, 2019 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-30999826

RESUMO

Panax ginseng C. A. Meyer has been widely used in skin care. Our previous study showed that the phenolic acids in ginseng root extract (GRE) impart inhibitory effects on melanogenesis. In this study, we found that as the most abundant component of phenolic acids in GRE, vanillic acid decreased tyrosinase activity and melanin levels with or without α-MSH stimulation and suppressed the expression of microphthalmia-associated transcription factor (MITF) and melanogenic enzymes in B16F10 cells. Furthermore, vanillic acid downregulated NOS activity, nitric oxide (NO) content, cGMP level, guanylate cyclase (GC) and protein kinase G (PKG) activity, and the phosphorylation of cAMP-response element-binding protein (CREB), whereas arbutin had no effect on the NO/PKG pathway. These findings indicate that vanillic acid in GRE suppressed melanogenesis by inhibiting the NO/PKG signaling pathways. This study provides a potential mechanism underlying the inhibitory effect of ginseng on melanogenesis.


Assuntos
Proteínas Quinases Dependentes de GMP Cíclico/antagonistas & inibidores , Melaninas/antagonistas & inibidores , Óxido Nítrico/antagonistas & inibidores , Panax/química , Extratos Vegetais/farmacologia , Raízes de Plantas/química , Transdução de Sinais/efeitos dos fármacos , Ácido Vanílico/farmacologia , Animais , Linhagem Celular Tumoral , Proteínas Quinases Dependentes de GMP Cíclico/metabolismo , Oxirredutases Intramoleculares/metabolismo , Melaninas/biossíntese , Melaninas/metabolismo , Glicoproteínas de Membrana/metabolismo , Camundongos , Fator de Transcrição Associado à Microftalmia/metabolismo , Monofenol Mono-Oxigenase/metabolismo , Óxido Nítrico/metabolismo , Óxido Nítrico Sintase/metabolismo , Oxirredutases/metabolismo , Regulação para Cima/efeitos dos fármacos , alfa-MSH/farmacologia
10.
Lett Appl Microbiol ; 68(4): 313-320, 2019 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-30790318

RESUMO

The aim of this study was the development of a novel and effective antibacterial formulation combining selected phytochemical compounds (quercetin, cuminaldehyde, indole-3-carbinol and vanillic acid) with ethylenediaminetetraacetic acid (EDTA), an aminopolycarboxylic acid. The antibacterial activity of the combinations was evaluated against Escherichia coli and Staphylococcus epidermidis in planktonic and sessile states as single and dual species. The compounds when applied individually demonstrated modest antibacterial activity. Nevertheless, synergy was observed when EDTA was combined with the selected phytochemicals, particularly with cuminaldehyde and indole-3-carbinol. These combinations were evaluated against single- and dual-species biofilms. An inactivation of 100% was obtained for almost all the biofilms, with E. coli biofilms showing the highest resistance. This study allowed the discovery of novel formulations of phytochemical compounds with antibacterial activity against E. coli and S. epidermidis single- and dual-species biofilms at concentrations close to the minimum bactericidal concentration. SIGNIFICANCE AND IMPACT OF THE STUDY: The synergistic combinations of EDTA and cuminaldehyde or indole-3-carbinol were effective against single- and dual-species E. coli and S. epidermidis planktonic cells and biofilms. The overall results highlight the role of phytochemical products as a green and sustainable source of antimicrobial potentiators to control bacteria in both planktonic and sessile states.


Assuntos
Biofilmes/crescimento & desenvolvimento , Ácido Edético/farmacologia , Escherichia coli/crescimento & desenvolvimento , Compostos Fitoquímicos/farmacologia , Staphylococcus epidermidis/crescimento & desenvolvimento , Antibacterianos/farmacologia , Benzaldeídos/farmacologia , Cimenos , Indóis/farmacologia , Testes de Sensibilidade Microbiana , Plâncton , Quercetina/farmacologia , Ácido Vanílico/farmacologia
11.
Biosci Biotechnol Biochem ; 83(3): 531-537, 2019 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-30422751

RESUMO

Asthma is a chronic allergic ailment affecting a considerably large population of the world. The aim of this study is to evaluate the ameliorative effects of vanillic acid against ovalbumin (OVA)-induced asthma in rat model. Asthma was induced in Sprague Dawley rats and vanillic acid was orally administered at 25 and 50 mg/kg body weight for 28 days. Rats challenged with OVA showed heavy signs of airway inflammation and remodeling similar to chronic asthma, evidenced by the increased differential cell counts and presence of inflammatory cytokines in the bronchoalveolar lavage fluid (BALF), along with elevated serum immunoglobulin levels, and the histological results. However, vanillic acid dose-dependently attenuated the manifestation of OVA-induced asthma (p < 0.05) through suppression of inflammatory mediators and modulation of immunoglobulin levels in rats. The asthma mitigating properties of vanillic acid might be due to suppression of oxidative stress and prevention of lung airway inflammation.


Assuntos
Asma/tratamento farmacológico , Pulmão/efeitos dos fármacos , Ovalbumina/imunologia , Ácido Vanílico/farmacologia , Animais , Antioxidantes/metabolismo , Asma/imunologia , Asma/metabolismo , Asma/patologia , Líquido da Lavagem Broncoalveolar/química , Modelos Animais de Doenças , Imunoglobulina E/sangue , Inflamação/tratamento farmacológico , Pulmão/imunologia , Pulmão/metabolismo , Pulmão/patologia , Masculino , Malondialdeído/metabolismo , Tamanho do Órgão/efeitos dos fármacos , Ratos , Ratos Sprague-Dawley , Ácido Vanílico/uso terapêutico
12.
Pharmacol Rep ; 71(1): 67-72, 2019 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-30471518

RESUMO

BACKGROUND: Transient receptor potential ankyrin-1 (TRPA1) channels expressed in the central terminal of dorsal root ganglion neurons in the spinal substantia gelatinosa (SG) play a role in modulating nociceptive transmission. Although plant-derived compounds exhibiting antinociception (such as eugenol, carvacrol and thymol) activate TRPA1 channels to enhance spontaneous excitatory transmission while hyperpolarizing membranes in SG neurons without TRPA1 activation, specific chemical moieties involved in synaptic modulation are unknown. METHODS: We examined the effects of other plant-derived compounds (guaiacol, vanillin, vanillic acid and p-cymene) on holding current and spontaneous excitatory transmission at -70 mV by applying the whole-cell patch-clamp technique to SG neurons in adult rat spinal cord slices. RESULTS: None of the compounds affected the frequency or amplitude of spontaneous excitatory postsynaptic current. Guaiacol and vanillic acid had no effect on holding currents, while vanillin and p-cymene produced an inward and outward current, respectively, in some neurons tested. Synaptic modulation was also observed within the same neuron as the activities of eugenol, carvacrol, thymol, and the chemically-related plant-derived compound zingerone occurred. CONCLUSION: A substituted group in eugenol and zingerone, but not in guaiacol, vanillin or vanillic acid, as well as an OH bound to the benzene ring of carvacrol and thymol, but not p-cymene, play a role in producing outward current and TRPA1 activation. Thus, the binding of such chemical moeties to the benzene ring of plant-derived compounds appears necessary to modulate nociceptive transmission in the SG. This information provides insight for the development of new analgesics based on plant-derived compounds.


Assuntos
Analgésicos/farmacologia , Extratos Vegetais/farmacologia , Substância Gelatinosa/efeitos dos fármacos , Canal de Cátion TRPA1/agonistas , Analgésicos/química , Animais , Benzaldeídos/química , Benzaldeídos/farmacologia , Cimenos , Potenciais Pós-Sinápticos Excitadores/efeitos dos fármacos , Guaiacol/química , Guaiacol/farmacologia , Técnicas In Vitro , Masculino , Estrutura Molecular , Monoterpenos/química , Monoterpenos/farmacologia , Extratos Vegetais/química , Ratos Sprague-Dawley , Relação Estrutura-Atividade , Substância Gelatinosa/metabolismo , Canal de Cátion TRPA1/metabolismo , Ácido Vanílico/química , Ácido Vanílico/farmacologia
13.
Mol Biol Rep ; 46(1): 997-1011, 2019 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-30569390

RESUMO

Neuroinflammation affects millions of people around the world as a result of injury or stress. Neuroinflammation represents almost all types of neurological diseases such as multiple sclerosis and Alzheimer's disease. Neurodegenerative diseases comprise demyelination and synaptic loss. The inflammatory response is further propagated by the activation of glial cells and modulation of constitutively expressed extracellular matrix proteins. The aim of the present study was to identify the anti-inflammatory effects of purified compounds gallic acid (GA, 1.0 µM) and vanillic acid (VA, 0.2 µM) on the lysolecithin (LPC, 0.003%)-induced model of inflammation. Hippocampal neurons were co-cultured with glial cells, and LPC was added to induce inflammation. Neurite outgrowth was measured by morphometry software. The level of myelination and demyelination was identified by immunostaining and sodium dodecyl sulfate polyacrylamide gel electrophoresis and western blotting techniques using different antibodies. Whole-cell patch clamp recordings were used to observe the sustained repetitive firing pattern. The data showed that GA and VA significantly increased the neurite outgrowth after 48 h in culture. Both compounds significantly reduced the expression of cyclooxygenase-2, NFκB, tenascin-C, chondroitin sulfate proteoglycans and glial fibrillary acidic protein in astrocytes in the LPC-induced model of inflammation. The level of myelin protein in neurites and oligodendrocyte cell bodies was significantly upregulated by GA and VA treatment. The reduction in sustained repetitive firing in the LPC-induced model of inflammation was reversed by both GA and VA treatment. This study supports the hypothesis that VA and GA have anti-inflammatory activities and could be regarded as potential treatments for neurodegenerative disease.


Assuntos
Ácido Gálico/farmacologia , Inflamação/patologia , Bainha de Mielina/patologia , Degeneração Neural/patologia , Ácido Vanílico/farmacologia , Potenciais de Ação/efeitos dos fármacos , Animais , Doenças Desmielinizantes , Modelos Animais de Doenças , Proteínas da Matriz Extracelular/metabolismo , Proteína Glial Fibrilar Ácida/metabolismo , Lisofosfatidilcolinas/farmacologia , Camundongos Endogâmicos BALB C , Bainha de Mielina/efeitos dos fármacos , Crescimento Neuronal/efeitos dos fármacos
14.
Molecules ; 23(11)2018 Oct 30.
Artigo em Inglês | MEDLINE | ID: mdl-30380712

RESUMO

The objective of this study was to evaluate the effect of combining catechin, protocatechuic, and vanillic acids against planktonic growing, adhesion, and biofilm eradication of uropathogenic Escherichia coli (UPEC), as well as antioxidant agents. The minimum inhibitory concentrations (MIC) of protocatechuic, vanillic acids and catechin against the growth of planktonic bacteria were 12.98, 11.80, and 13.78 mM, respectively. Mixing 1.62 mM protocatechuic acid + 0.74 mM vanillic acid + 0.05 mM catechin resulted in a synergistic effect acting as an MIC. Similarly, the minimum concentrations of phenolic compounds to prevent UPEC adhesion and biofilm formation (MBIC) were 11.03 and 7.13 mM of protocatechuic and vanillic acids, respectively, whereas no MBIC of catechin was found. However, combinations of 1.62 mM protocatechuic acid + 0.74 mM vanillic acid + 0.05 mM catechin showed a synergistic effect acting as MBIC. On the other hand, the minimum concentrations to eradicate biofilms (MBEC) were 25.95 and 23.78 mM, respectively. The combination of 3.20 mM protocatechuic acid, 2.97 mM vanillic acid, and 1.72 mM catechin eradicated pre-formed biofilms. The antioxidant capacity of the combination of phenolics was higher than the expected theoretical values, indicating synergism by the DPPH•, ABTS, and FRAP assays. Effective concentrations of catechin, protocatechuic, and vanillic acids were reduced from 8 to 1378 times when combined. In contrast, the antibiotic nitrofurantoin was not effective in eradicating biofilms from silicone surfaces. In conclusion, the mixture of phenolic compounds was more effective in preventing cell adhesion and eradicating pre-formed biofilms of uropathogenic E. coli than single compounds and nitrofurantoin, and showed antioxidant synergy.


Assuntos
Antibacterianos/farmacologia , Catequina/farmacologia , Hidroxibenzoatos/farmacologia , Ácido Vanílico/farmacologia , Antibacterianos/química , Antioxidantes/química , Antioxidantes/farmacologia , Biofilmes/efeitos dos fármacos , Catequina/química , Humanos , Hidroxibenzoatos/química , Testes de Sensibilidade Microbiana , Plâncton/efeitos dos fármacos , Escherichia coli Uropatogênica/efeitos dos fármacos , Escherichia coli Uropatogênica/patogenicidade , Ácido Vanílico/química
15.
J Cancer Res Ther ; 14(6): 1285-1290, 2018.
Artigo em Inglês | MEDLINE | ID: mdl-30488845

RESUMO

Objectives: The aim of this study was to evaluate the chemopreventive potential of vanillic acid against 7,12-dimethylbenz(a)anthracene (DMBA)-induced hamster buccal pouch oral carcinogenesis. Materials and Methods: Determine the tumor incidence, tumor volume and burden, assessment of the status of Phase I and Phase II detoxification enzymes were measured in the liver and buccal mucosa of hamsters using specific colorimetric methods. Results: One hundred percent tumor formation was observed in DMBA alone treated hamsters. Phase I and Phase II detoxification enzymes status were significantly altered DMBA-induced oral carcinogenesis. Vanillic acid (200 mg/kg bw p.o) significantly restored the biochemical variables of liver and buccal mucosa in DMBA + vanillic acid treated hamsters to near normal range compared with DMBA alone treated hamsters. Conclusion: The present study thus shows chemopreventive potential of vanillic acid in DMBA-induced hamster buccal pouch carcinogenesis. Vanillic acid improves the phase I and phase II detoxification enzymes in DMBA treated hamsters.


Assuntos
Antracenos/farmacologia , Anticarcinógenos/farmacologia , Carcinogênese/efeitos dos fármacos , Mucosa Bucal/efeitos dos fármacos , Neoplasias Bucais/induzido quimicamente , Neoplasias Bucais/tratamento farmacológico , Piperidinas/farmacologia , Ácido Vanílico/farmacologia , Animais , Antioxidantes/metabolismo , Carcinogênese/induzido quimicamente , Carcinogênese/metabolismo , Carcinógenos/farmacologia , Carcinoma de Células Escamosas/induzido quimicamente , Carcinoma de Células Escamosas/tratamento farmacológico , Carcinoma de Células Escamosas/metabolismo , Bochecha/patologia , Cricetinae , Peroxidação de Lipídeos/efeitos dos fármacos , Fígado/efeitos dos fármacos , Fígado/metabolismo , Masculino , Mesocricetus , Desentoxicação Metabólica Fase I/fisiologia , Desintoxicação Metabólica Fase II/fisiologia , Mucosa Bucal/metabolismo , Neoplasias Bucais/metabolismo
16.
Molecules ; 23(10)2018 Oct 08.
Artigo em Inglês | MEDLINE | ID: mdl-30297681

RESUMO

Colon cancer is the second most common cause of cancer deaths in the USA and Europe. Despite aggressive therapies, many tumors are resistant to current treatment protocols and epidemiological data suggest that diet is a major factor in the etiology of colon cancer. This study aimed to evaluate the antioxidant activity and the influence of 3,4-dihydroxyphenylacetic (3,4-DHPAA), p-coumaric (p-CoA), vanillic (VA) and ferulic (FA) acids on cell viability, cell cycle progression, and rate of apoptosis in human colon adenocarcinoma cells (HT-29). The results showed that all compounds tested reduce cell viability in human colon cancer cells. 3,4-DHPAA promoted the highest effect antiproliferative with an increase in the percentage of cells in G0/G1 phase, accompanied by a reduction of cells in G2/M phase. Cell cycle analysis of VA and FA showed a decrease in the proportion of cells in G0/G1 phase (10.0 µM and 100.0 µM). p-CoA and FA acids increased the percentage of apoptotic cells and non-apoptotic cells. 3,4-DHPAA seems to be the substance with the greatest potential for in vivo studies, opening thus a series of perspectives on the use of these compounds in the prevention and treatment of colon cancer.


Assuntos
Adenocarcinoma/tratamento farmacológico , Proliferação de Células/efeitos dos fármacos , Neoplasias do Colo/tratamento farmacológico , Hidroxibenzoatos/farmacologia , Ácido 3,4-Di-Hidroxifenilacético/farmacocinética , Ácido 3,4-Di-Hidroxifenilacético/farmacologia , Adenocarcinoma/patologia , Apoptose/efeitos dos fármacos , Divisão Celular/efeitos dos fármacos , Sobrevivência Celular/efeitos dos fármacos , Neoplasias do Colo/patologia , Simulação por Computador , Ácidos Cumáricos/farmacocinética , Ácidos Cumáricos/farmacologia , Células HT29 , Humanos , Hidroxibenzoatos/classificação , Hidroxibenzoatos/farmacocinética , Propionatos/farmacocinética , Propionatos/farmacologia , Ácido Vanílico/farmacocinética , Ácido Vanílico/farmacologia
17.
J Plant Physiol ; 231: 251-260, 2018 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-30321751

RESUMO

The treatment of the cotyledons of pepper plants with vanillyl nonanoate (VNT), a synthetic capsinoid similar to capsiate, protected systemically the plant against a root pathogen (the hemibiotrophic oomycete Phytophthora capsici) and an aerial pathogen (the necrotrophic fungus Botrytis cinerea). VNT treatment reduced both the symptoms and the colonization by these pathogens. VNT induced systemically two PR (Pathogenesis-related) genes and a gene involved in phytoalexin biosynthesis. VNT also induced systemically the reinforcement of cell walls with lignin both in the roots and the leaves. The increase in lignin was correlated with an increase in peroxidase gene expression and activity, pointing to the role of this enzyme in lignin polymerization. The results suggest that VNT induces systemic resistance at least in part by means of lignification.


Assuntos
Capsicum/efeitos dos fármacos , Resistência à Doença/efeitos dos fármacos , Ácidos Graxos/farmacologia , Lignina/metabolismo , Ácido Vanílico/análogos & derivados , Botrytis , Capsicum/metabolismo , Capsicum/microbiologia , Capsicum/fisiologia , Regulação da Expressão Gênica de Plantas/efeitos dos fármacos , Peroxidase/metabolismo , Phytophthora , Doenças das Plantas/microbiologia , Raízes de Plantas/microbiologia , Ácido Vanílico/farmacologia
18.
Life Sci ; 211: 126-132, 2018 Oct 15.
Artigo em Inglês | MEDLINE | ID: mdl-30195619

RESUMO

Ischemic stroke is one of the leading causes of neurological deterioration and mortality worldwide. Neuroprotective strategies are being investigated to minimize cognitive deficits after ischemic events. Here we investigated the neuroprotective potential of vanillic acid (VA) in an animal model of transient bilateral common carotid artery occlusion and reperfusion (BCCAO/R). Adult male Wistar rats (250-300 g) were randomly divided in 4 groups and submitted to either cerebral hypoperfusion-reperfusion or a sham surgery after two-weeks of pretreatment with VA and/or normal saline. To induce the animal model of hypoperfusion, bilateral common carotid arteries were occluded (2VO model) for 30 min, followed by 72 h of reperfusion. Subsequently, their cognitive performance was evaluated in a Morris water maze (MWM) test, and also hippocampi were removed for ELISA assays and TUNEL staining test. The results showed that 2VO significantly reduced the spatial memory performance in MWM. As well as, BCCAO/R increased the level of IL-6, TNF-α and TUNEL positive cells, and also decreased the contents of IL-10 in the hippocampus of vehicle- pretreated groups as compared to the sham-operated groups. Furthermore, 14 consecutive days pretreatment with VA significantly restored the spatial memory, decreased the levels of IL-6, TNF-α and TUNEL positive cells and also increased the IL-10 levels in the hippocampi of the BCCAO/R rats. VA alone did not show any change neither in the status of various cytokines nor behavioral and TUNEL staining tests over sham values. Our data confirm that VA could potentially serve as a novel, promising, and accessible neuroprotective agent against cerebrovascular insufficiency states and vascular dementia.


Assuntos
Transtornos Cerebrovasculares/complicações , Modelos Animais de Doenças , Hipocampo/efeitos dos fármacos , Inflamação/prevenção & controle , Transtornos da Memória/prevenção & controle , Fármacos Neuroprotetores/farmacologia , Ácido Vanílico/farmacologia , Animais , Hipocampo/imunologia , Hipocampo/patologia , Inflamação/etiologia , Inflamação/patologia , Masculino , Transtornos da Memória/etiologia , Transtornos da Memória/patologia , Estresse Oxidativo/efeitos dos fármacos , Ratos , Ratos Wistar , Reperfusão
19.
Pak J Pharm Sci ; 31(5): 1951-1957, 2018 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-30150194

RESUMO

In order to investigate the anti-inflammatory activity of flavonoids, phenolic acids, and alkaloids from the flowers of Trollius chinensis, some representative compounds, namely, orientin, 2"-O-ß-L-galactopyranosylorientin, vitexin, quercetin, isoquercetin, luteolin, veratric acid, proglobeflowery acid, trollioside, and trolline were selected to study their inhibitory effects against LPS-induced NO, IL-6, and TNF-ß release in RAW264.7 cells. At the higher concentration, both phenolic acids and flavonoids inhibited the production of NO, whereas only phenolic acids showed this effect at the lower concentration. Although trolline had stronger cytotoxicity, it exhibited a potential effect of decreasing NO production induced by LPS in the non-toxic concentration range. In addition, all tested compounds decreased the production of IL-6 and TNF-a by almost 50% at both the higher and lower concentrations. It is concluded that the anti-inflammatory activity of the phenolic acids is stronger than that of the flavonoids.


Assuntos
Anti-Inflamatórios/farmacologia , Sobrevivência Celular/efeitos dos fármacos , Flores , Extratos Vegetais/farmacologia , Ranunculaceae , Ácido Vanílico/análogos & derivados , Alcaloides/isolamento & purificação , Alcaloides/farmacologia , Animais , Anti-Inflamatórios/isolamento & purificação , Apigenina/isolamento & purificação , Apigenina/farmacologia , Sobrevivência Celular/fisiologia , Relação Dose-Resposta a Droga , Flavonoides/isolamento & purificação , Flavonoides/farmacologia , Glucosídeos/isolamento & purificação , Glucosídeos/farmacologia , Camundongos , Extratos Vegetais/isolamento & purificação , Células RAW 264.7 , Ácido Vanílico/isolamento & purificação , Ácido Vanílico/farmacologia
20.
Food Funct ; 9(8): 4366-4375, 2018 Aug 15.
Artigo em Inglês | MEDLINE | ID: mdl-30043820

RESUMO

Anthocyanins have a positive effect on resistant obesity; however they cannot usually be absorbed directly but, instead, are metabolized by gut microbiota. This study will examine the effects and the mechanism of vanillic acid on the prevention of obesity induced by diet, which is one of the anthocyanin metabolites. We fed C57BL/6J mice vanillic acid supplements in a high fat and high fructose diet for 16 weeks. Body weight, fat pat weight, and food and water intake were monitored. Glucose homeostasis was assessed with a glucose or insulin tolerance test. The sizes of adipose cells and lipid droplets were analyzed by histology staining, while the expression of genes and proteins was analyzed by quantitative real-time PCR, western blot and tissue-blot immunoassay. The results demonstrated that vanillic acid contributed to the reduction of body weight gain, improved glucose tolerance and insulin resistance, and maintained body temperature. Furthermore, vanillic acid was found to promote thermogenesis and mitochondrial synthesis of brown adipose tissue and inguinal white adipose tissue. This study demonstrated that vanillic acid could prevent obesity by activating BAT thermogenesis and the promotion of inguinal WAT browning.


Assuntos
Tecido Adiposo Marrom/efeitos dos fármacos , Tecido Adiposo Branco/efeitos dos fármacos , Obesidade/tratamento farmacológico , Termogênese/efeitos dos fármacos , Ácido Vanílico/farmacologia , Tecido Adiposo Marrom/metabolismo , Tecido Adiposo Branco/metabolismo , Animais , Peso Corporal/efeitos dos fármacos , Metabolismo Energético/efeitos dos fármacos , Humanos , Masculino , Camundongos , Camundongos Endogâmicos C57BL , Obesidade/metabolismo , Obesidade/fisiopatologia
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