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1.
Environ Sci Pollut Res Int ; 26(29): 30220-30228, 2019 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-31422537

RESUMO

The effects of patchouli essential oil (PEO) as an alternative to antibiotics on ruminal methanogenesis, feed degradability, and enzyme activities were evaluated. The basal substrate was incubated without additives (control, CTL) and with monensin (MON, 6 µM/g DM) or patchouli essential oil (PEO, 90 µg/g DM) for 24 h. In three different runs, the gas production (GP) was recorded at 2, 4, 8, 12, and 24 h of incubation using a semi-automatic system. The results revealed that MON had decreased (P < 0.05) the net GP and CH4 production and digestible and metabolizable energy relative to PEO supplementation. The in vitro truly degraded organic matter was not influenced by PEO application, while was reduced (P = 0.027) with MON. Both PEO and MON had similar reducing effect on the activity of carboxymethylcellulase (P = 0.030), in vitro truly degraded neutral detergent fiber (P = 0.010), NH3-N concentrations (P = 0.012), acetate proportion (C2, P = 0.046), C2 to C3 ratio (P = 0.023), and total protozoal count (P = 0.017). Both additives recorded similar elevating potential on the α-amylase activity (P = 0.012), propionate (C3) proportion (P = 0.011), and microbial protein (P = 0.034) compared with CTL. Effects of MON and PEO on ruminal feed degradability, microbial enzyme activities, and total protozoa counts may be responsible for modifying rumen fermentation ecology. Addition of PEO may act as a desirable alternative rumen modifier for MON in ruminant diets.


Assuntos
Digestão/efeitos dos fármacos , Metano/metabolismo , Óleos Voláteis/farmacologia , Pogostemon/química , Rúmen/metabolismo , alfa-Amilases/metabolismo , Ração Animal/análise , Animais , Suplementos Nutricionais , Metabolismo Energético/efeitos dos fármacos , Fermentação/efeitos dos fármacos , Metano/análise , Monensin/farmacologia , Óleos Voláteis/isolamento & purificação , Ovinos
2.
Int J Mol Sci ; 20(17)2019 Aug 21.
Artigo em Inglês | MEDLINE | ID: mdl-31438541

RESUMO

Oxidative stress has been implicated in the pathogenesis of many diseases including chronic liver diseases. Nrf2 is a master transcriptional factor regulating the induction of cellular antioxidant defense systems. Here, the Nrf2-activating effect of the crude methanol extract of dried leaves of Pogostemon cablin Bentham was demonstrated by measuring the antioxidant response element (ARE)-driven luciferase activity and pachypodol, 4',5-dihydroxy-3,3',7-trimethoxyflavone, was isolated by bioactivity-guided fractionation and further separation using chromatographic techniques. To our knowledge, this is the first study to evaluate the antioxidant and cytoprotective effects of pachypodol in HepG2 cells as well as the underlying molecular mechanisms. Indeed, pachypodol protected HepG2 cells from cell death caused by tert-butylhydroperoxide-induced oxidative stress and also attenuated ROS production. The ability of pachypodol to activate Nrf2/ARE pathway was further confirmed by observing Nrf2 expression in nuclear fraction, mRNA levels of Nrf2 target antioxidants, and cellular glutathione content in HepG2 cells. Extracellular signal-regulated kinase (ERK) is one of the important kinases involved in Nrf2 activation. Pachypodol increased ERK phosphorylation and ERK inhibition by PD98059 totally abrogated the increase in ARE luciferase activity, nuclear Nrf2 accumulation and mRNA levels of antioxidant enzymes by pachypodol. In conclusion, pachypodol isolated from P. cablin can protect hepatocytes from oxidative injury, possibly mediated by enhancing endogenous antioxidant defense system through ERK-dependent Nrf2 activation.


Assuntos
MAP Quinases Reguladas por Sinal Extracelular/metabolismo , Fator 2 Relacionado a NF-E2/metabolismo , Pogostemon/química , Quercetina/análogos & derivados , Antioxidantes/química , Antioxidantes/farmacologia , MAP Quinases Reguladas por Sinal Extracelular/antagonistas & inibidores , Flavonoides/farmacologia , Células Hep G2 , Hepatócitos/efeitos dos fármacos , Hepatócitos/metabolismo , Humanos , Estresse Oxidativo/efeitos dos fármacos , Fosforilação/efeitos dos fármacos , Quercetina/química , Quercetina/farmacologia
3.
Spectrochim Acta A Mol Biomol Spectrosc ; 218: 155-160, 2019 Jul 05.
Artigo em Inglês | MEDLINE | ID: mdl-30981029

RESUMO

Recently, demand for authentication technology is growing rapidly in an attempt to overcome counterfeiting of high-value agricultural products, such as patchouli oil. Fingerprinting methods based on spectroscopy are one such technology being used for authentication. However, the spectral datasets obtained are multivariate in nature; containing thousands of data points for a single sample, making data acquisition and processing time-consuming. Therefore, reduction and simplification in the number of variables used required is needed to provide a more rapid and applicable method. Color cameras, which can capture image in the visible region light, could be such an alternative spectral data acquisition approach. In this research, a simplified spectroscopy method was developed for origin authentication of patchouli oil. The system consists of front ultraviolet light induced (365 nm) fluorescence and a white LED-based backlighting imaging system that consecutively captures the fluorescence and transmittance characteristics of the oil in the visible region. From the captured images, features were extracted and analyzed using Principle Component Analysis (PCA) to identify important image features for discrimination of origin. From the samples measured, the samples clustered around three islands of origin in the PCA space. A classification model based on fluorescence and transmittance image features (color values) could discriminate origin classes with a total accuracy of 88.46%. A lower accuracy was found for the Java class due to low sample numbers. This result demonstrates that the proposed system has the potential to be a rapid authentication tool for determining the geographical origin of patchouli oils.


Assuntos
Óleos Voláteis/análise , Imagem Óptica/métodos , Óleos Vegetais/análise , Pogostemon/química , Desenho de Equipamento , Geografia , Óleos Voláteis/classificação , Imagem Óptica/instrumentação , Óleos Vegetais/classificação , Pogostemon/classificação , Espectrometria de Fluorescência/instrumentação , Espectrometria de Fluorescência/métodos
4.
Chem Biodivers ; 16(5): e1900137, 2019 May.
Artigo em Inglês | MEDLINE | ID: mdl-30957408

RESUMO

A pair of new glycosidic epimers, cablinosides A (1a) and B (1b) were isolated from the leaves of Pogostemon cablin. The structures with absolute configurations of 1a and 1b were elucidated by extensive NMR investigation, and quantum chemical CD calculations. The epimer mixture 1 showed moderate α-glucosidase inhibitory activity and no significant cytotoxic activity against HepG2 cells.


Assuntos
Glicosídeos/química , Fenilacetatos/química , Pogostemon/química , Sobrevivência Celular/efeitos dos fármacos , Dicroísmo Circular , Glicosídeos/isolamento & purificação , Glicosídeos/farmacologia , Células Hep G2 , Humanos , Concentração Inibidora 50 , Espectroscopia de Ressonância Magnética , Conformação Molecular , Fenilacetatos/isolamento & purificação , Fenilacetatos/farmacologia , Folhas de Planta/química , Folhas de Planta/metabolismo , Pogostemon/metabolismo , Estereoisomerismo , alfa-Glucosidases/química , alfa-Glucosidases/metabolismo
5.
J Nat Prod ; 81(9): 1919-1927, 2018 09 28.
Artigo em Inglês | MEDLINE | ID: mdl-30188125

RESUMO

Seven novel guaiane sesquiterpenoids (1-7) and three known seco-guaianes were isolated from the volatile oil of Pogostemon cablin. Their structures including absolute configurations were determined by spectroscopic analyses, a modified Mosher's method, and X-ray diffraction and ECD data. The results indicated that the ECD Cotton effects arising from one or two nonconjugated olefinic chromophores could be applied to define the absolute configurations of guaiane sesquiterpenoids. Compounds 3 and 6 exhibited significant vasorelaxant activity against phenylephrine-induced and KCl-induced contractions of rat aorta rings [half-maximal effective concentration (EC50) of 3 against PHE-induced contraction, 5.4 µM; EC50 of 6 against PHE- and KCl-induced contractions, 1.6 and 24.2 µM, respectively]. They also showed antifungal activity against Candida albicans (minimum inhibitory concentrations, 500 and 300 µM, respectively). In addition, 2 and 7-9 displayed a neuroprotective effect against glutamate-induced injury in PC12 cells.


Assuntos
Óleos Voláteis/análise , Pogostemon/química , Sesquiterpenos de Guaiano/química , Animais , Antifúngicos/farmacologia , Masculino , Fármacos Neuroprotetores/farmacologia , Células PC12 , Ratos , Sesquiterpenos de Guaiano/isolamento & purificação , Sesquiterpenos de Guaiano/farmacologia , Vasodilatadores/farmacologia , Difração de Raios X
6.
Fitoterapia ; 130: 100-104, 2018 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-30145337

RESUMO

Pogostemins A-C (1-3), three new meroterpenoids with pyrone-sesquiterpenoid hybrid skeletons, were isolated from the aerial parts of Pogostemon auricularius. Their chemical structures were elucidated by 1D- and 2D-NMR and HRESIMS analyses. Compound 1 showed significant cytotoxicities against the human colon adenocarcinoma SW-480, epidermoid carcinoma KB, gastric cancer AGS, hepatoma cancer Hep-G2, and lung cancer LU-1 cell lines with IC50 values of 7.21, 8.49, 9.44, 11.75, and 12.76 µg/mL, respectively.


Assuntos
Antineoplásicos Fitogênicos/isolamento & purificação , Compostos Fitoquímicos/isolamento & purificação , Pogostemon/química , Terpenos/isolamento & purificação , Antineoplásicos Fitogênicos/farmacologia , Linhagem Celular Tumoral , Humanos , Estrutura Molecular , Compostos Fitoquímicos/farmacologia , Folhas de Planta/química , Plantas Medicinais/química , Terpenos/farmacologia , Vietnã
7.
Neotrop Entomol ; 47(6): 769-779, 2018 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-29995283

RESUMO

Leaf-cutting ants belonging to the genus Atta (Formicidae: Myrmicinae) are important pests in agricultural and forest environments. In the present study, we evaluated the formicidal activity of the essential oil of Pogostemon cablin and its nanoformulation on the leaf-cutting ants: Atta opaciceps (Borgmeier, 1939), Atta sexdens (Linnaeus, 1758), and Atta sexdens rubropilosa Forel, 1908. The nanoformulation was developed by magnetic stirring using polyoxyethylene (36%), pure ethanol (36%), essential oil of P. cablin (18%), and water (10%). Bioassays of acute toxicity by fumigation and behavioral bioassays in treated arenas, with and without choice, were performed. The essential oil of P. cablin and its nanoformulation demonstrated efficient insecticidal activity and irritability to ant species. The concentration required to kill 50% of workers varied from 1.06 to 2.10 µL L-1, with a mean time to death of less than or equal to 42 h. The essential oil of P. cablin and its nanoformulation reduced the displacement and velocity speed of the workers of A. opaciceps and A. sexdens rubropilosa in totally treated arenas. In the bioassays with choices, the three species of ants walked less and at a greater speed on the treated side of arena. This work demonstrates the potential of the essential oil of P. cablin and its nanoformulation to the generation of new formicidal products.


Assuntos
Formigas , Inseticidas , Óleos Voláteis , Pogostemon/química , Animais , Comportamento Animal , Testes de Toxicidade Aguda
8.
Protein Expr Purif ; 152: 13-22, 2018 12.
Artigo em Inglês | MEDLINE | ID: mdl-30017744

RESUMO

A proteomic approach was used to understand the molecular mechanisms underlying obstacles to the continuous cropping of Pogostemon cablin. We examined differences in protein abundance between control (CK) and continuously cropped (TR) P. cablin leaves at different time points (90, 150, and 210 days after culture). Comparative analysis by two-dimensional gel electrophoresis (2-DE) and mass spectrometry (MS) revealed 183 differentially expressed protein spots, of which 87 proteins or isoforms were identified using mass spectrometry. Among these differentially expressed proteins (DEPs), 50 proteins or isoforms showed increased abundance and 37 proteins or isoforms showed decreased abundance in the TR sample compared with the abundance in the CK sample. Bioinformatic tools were used to analyze the DEPs. These proteins were classified into 12 categories according to clusters of orthologous groups (COG) analysis, with the majority being involved in post-translational modification, protein turnover, and chaperones, followed by carbohydrate transport and metabolism, and finally, energy production and conversion. Protein-protein interactions revealed that 18 DEPs were involved in energy metabolism, 6 DEPs were involved in stress response, and 4 DEPs were involved in amino acid biosynthesis. Continuous cropping altered the expression of proteins related to energy metabolism, carbohydrate metabolism, and amino acid metabolism in P. cablin leaves. Among these processes, the most affected was energy metabolism, which may be pivotal for resistance to continuous cropping.


Assuntos
Regulação da Expressão Gênica de Plantas , Folhas de Planta/genética , Proteínas de Plantas/genética , Pogostemon/genética , Processamento de Proteína Pós-Traducional , Proteoma/genética , Transporte Biológico/genética , Metabolismo dos Carboidratos/genética , Biologia Computacional/métodos , Metabolismo Energético/genética , Ontologia Genética , Chaperonas Moleculares/classificação , Chaperonas Moleculares/genética , Chaperonas Moleculares/metabolismo , Anotação de Sequência Molecular , Folhas de Planta/química , Folhas de Planta/metabolismo , Proteínas de Plantas/classificação , Proteínas de Plantas/metabolismo , Pogostemon/química , Pogostemon/metabolismo , Mapeamento de Interação de Proteínas , Proteoma/classificação , Proteoma/metabolismo
9.
Lett Appl Microbiol ; 67(4): 400-410, 2018 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-30022505

RESUMO

The antifungal properties of 12 Eos, that is, Syzygium aromaticum, Pelargonium graveolens, Lavandula angustifolia, Cupresus sempervirens, Mentha piperita, Santolina chamaecyparissus, Citrus sinensis, Pogostemon patchouli, Thymus mastichina, Thymus vulgaris, Eucalyptus globulus and Rosmarinus officinalis, were screened. The influence of five doses of each EOs was tested against Botrytis cinerea, Sclerotinia sclerotiorum, Fusarium oxysporum, Phytophthora parasitica, Pythium aphanidermatum, Alternaria brassicae, Cladobotryum mycophilum and Trichoderma aggressivum f.sp. europaeum using disc-diffusion method. The mycelial growth inhibition and ED50 were calculated. The chemical analysis of the EOs was analysed using gas chromatography-mass spectroscopy. A total of 58 compounds were identified in the 12 EOs. All essential oils (EOs) analysed showed antifungal activity against the test pathogens in the range of 5·32-100%. The inhibitory effect of oils showed dose-dependent activity on the tested fungus. Based on the ED50 values, clove, rose geranium, peppermint and patchouli were the most effective. This study warrants further research into the practical use of EOs for the control of important myco- and phytopathogens in intensive horticulture. SIGNIFICANCE AND IMPACT OF THE STUDY: Due to the serious damage caused by fungal pathogens of vegetables and mushrooms, it is necessary to search for integrated strategies of disease control. This study provides relevant information about the effects of 12 essential oils (EOs) against eight pathogens of agricultural interest, included mycopathogens with emphasis on the possible future application of the EOs as alternative antifungal agents.


Assuntos
Antifúngicos/farmacologia , Ascomicetos/crescimento & desenvolvimento , Botrytis/crescimento & desenvolvimento , Fusarium/crescimento & desenvolvimento , Óleos Voláteis/farmacologia , Óleos Vegetais/farmacologia , Verduras/microbiologia , Agaricales , Ascomicetos/efeitos dos fármacos , Botrytis/efeitos dos fármacos , Citrus sinensis/química , Eucalyptus/química , Fusarium/efeitos dos fármacos , Lavandula/química , Testes de Sensibilidade Microbiana , Pelargonium/química , Pogostemon/química , Syzygium/química , Thymus (Planta)/química
10.
Microb Pathog ; 122: 162-173, 2018 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-29920307

RESUMO

In the current study we have evaluated the antibiofilm and antivirulent properties of unexplored essential oils (EOs) obtained from Pogostemon heyneanus and Cinnamomum tamala against Methicillin Resistant Staphylococcus aureus (MRSA) strains. The EOs from both the aromatic plants was screened for their ability to prevent biofilm formation and to disrupt preformed biofilms. The efficacy of both the EOs to disrupt the preformed biofilms of various MRSA strains was determined by Confocal Laser Scanning Microscopy (CLSM) and Scanning Electron Microscopy (SEM).The EOs were further able to reduce the Extracellular polymeric substance (EPS) and slime synthesis the two factors of the biofilm assemblage. The EOs was also found to be effective in reducing virulence factors like staphyloxanthin and hemolysin. In silico docking studies were performed for the major components of essential oils and dehydroxysqualene synthase of MRSA which is responsible for the synthesis of staphyloxanthin. The results suggest that (E)-nerolidol showed better binding affinity towards the enzyme. Other compounds have similar binding strengths with the enzyme. Furthermore, the synergistic effect EOs along with the commercially available DNaseI and Marine Bacterial DNase (MBD) showed that the synergistic effect had enhanced biofilm disruption ability. The results show that EOs from P. heyneanus and C. tamala has potential antivirulent and biofilm inhibitory properties against clinical and drug resistant S. aureus strains. The present study highlights the importance of bioprospecting plant based natural products as an alternative for antibiotics owing to the emergence of multi-drug resistant strains.


Assuntos
Antibacterianos/farmacologia , Biofilmes/efeitos dos fármacos , Cinnamomum/química , Staphylococcus aureus Resistente à Meticilina/efeitos dos fármacos , Staphylococcus aureus Resistente à Meticilina/crescimento & desenvolvimento , Óleos Voláteis/farmacologia , Pogostemon/química , Antibacterianos/isolamento & purificação , Biopolímeros/metabolismo , Proteínas Hemolisinas/biossíntese , Staphylococcus aureus Resistente à Meticilina/metabolismo , Microscopia Confocal , Microscopia Eletrônica de Varredura , Óleos Voláteis/isolamento & purificação , Virulência/efeitos dos fármacos , Fatores de Virulência/biossíntese , Xantofilas/biossíntese
11.
Planta Med ; 84(12-13): 953-963, 2018 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-29689585

RESUMO

High-field NMR is an expensive and important quality control technique. In recent years, cheaper and simpler low-field NMR has become available as a new quality control technique. In this study, 60 MHz 1H-NMR was compared with GC-MS and refractometry for the detection of adulteration of essential oils, taking patchouli essential oil as a test case. Patchouli essential oil is frequently adulterated, even today. In total, 75 genuine patchouli essential oils, 10 commercial patchouli essential oils, 10 other essential oils, 17 adulterants, and 1 patchouli essential oil, spiked at 20% with those adulterants, were measured. Visual inspection of the NMR spectra allowed for easy detection of 14 adulterants, while gurjun and copaiba balsams proved difficult and one adulterant could not be detected. NMR spectra of 10 random essential oils differed not only strongly from patchouli essential oil but also from one another, suggesting that fingerprinting by low-field NMR is not limited to patchouli essential oil. Automated chemometric evaluation of NMR spectra was possible by similarity analysis (Mahalanobis distance) based on the integration from 0.1 - 8.1 ppm in 0.01 ppm increments. Good quality patchouli essential oils were recognised as well as 15 of 17 deliberate adulterations. Visual qualitative inspection by GC-MS allowed for the detection of all volatile adulterants. Nonvolatile adulterants, and all but one volatile adulterant, could be detected by semiquantitation. Different chemometric approaches showed satisfactory results. Similarity analyses were difficult with nonvolatile adulterants. Refractive index measurements could detect only 8 of 17 adulterants. Due to advantages such as simplicity, rapidity, reproducibility, and ability to detect nonvolatile adulterants, 60 MHz 1H-NMR is complimentary to GC-MS for quality control of essential oils.


Assuntos
Óleos Voláteis/normas , Óleos Vegetais/normas , Pogostemon/química , Contaminação de Medicamentos , Cromatografia Gasosa-Espectrometria de Massas , Espectroscopia de Ressonância Magnética , Óleos Voláteis/química , Óleos Vegetais/química , Controle de Qualidade , Refratometria , Reprodutibilidade dos Testes
12.
J Mycol Med ; 28(2): 332-339, 2018 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-29571979

RESUMO

The prevalence and fatality rates with biofilm-associated candidal infections have remained a challenge to the medical fraternity despite major advances in the field of antifungal therapy. Traditionally, essential oils (EOs) from the aromatic plants have been found to be excellent therapeutic agents to treat fungal ailments. The present study explores the antivirulent and antibiofilm effects of under explored leaf EOs of Indian patchouli EO extracted from Pogostemon heyneanus (PH), Indian cassia from Cinnamomum tamala (CT) and camphor EO from C. camphora (CC) against Candida species. The EOs were investigated for its efficacy to disrupt the young and preformed Candida spp. biofilms and to inhibit the yeast to hyphal transition, a hallmark virulent trait of C. albicans. The ability of these EOs to inhibit metabolically active cells was assessed through XTT assay. Of these three EOs, CT EO showed enhanced biofilm inhibition than others and hence it was further selected to study its biomass inhibition potential and exopolysaccharide layer disruption ability. The CT EO reduced the biomass of the preformed biofilms of all three Candida strains, which was supported by confocal microscopy. It also disrupted the exopolysaccharide layer of the Candida strains as shown by scanning electron microscopy. The present findings validate the effectiveness of EOs against the virulence of Candida spp. and emphasize the pharmaceutical potential of several native but yet unexplored wild aromatic plants in the prospect of therapeutic application.


Assuntos
Antifúngicos/farmacologia , Biofilmes/efeitos dos fármacos , Candida/efeitos dos fármacos , Cinnamomum zeylanicum/química , Óleos Voláteis/farmacologia , Pogostemon/química , Candida/patogenicidade , Candida/ultraestrutura , Candida albicans/efeitos dos fármacos , Candidíase/microbiologia , Humanos , Hifas/efeitos dos fármacos , Hifas/ultraestrutura , Testes de Sensibilidade Microbiana , Microscopia Eletrônica de Varredura , Virulência
13.
World J Gastroenterol ; 24(6): 693-705, 2018 Feb 14.
Artigo em Inglês | MEDLINE | ID: mdl-29456408

RESUMO

AIM: To elucidate the mechanism of patchouli alcohol (PA) in treatment of rat models of diarrhea-predominant irritable bowel syndrome (IBS-D). METHODS: We studied the effects of PA on colonic spontaneous motility using its cumulative log concentration (3 × 10-7 mol/L to 1 × 10-4 mol/L). We then determined the responses of the proximal and distal colon segments of rats to the following stimuli: (1) carbachol (1 × 10-9 mol/L to 1 × 10-5 mol/L); (2) neurotransmitter antagonists including Nω-nitro-L-arginine methyl ester hydrochloride (10 µmol/L) and (1R*, 2S*)-4-[2-Iodo-6-(methylamino)-9H-purin-9-yl]-2-(phosphonooxy)bicyclo[3.1.0]hexane-1-methanol dihydrogen phosphate ester tetraammonium salt (1 µmol/L); (3) agonist α,ß-methyleneadenosine 5'-triphosphate trisodium salt (100 µmol/L); and (4) single KCl doses (120 mmol/L). The effects of blockers against antagonist responses were also assessed by pretreatment with PA (100 µmol/L) for 1 min. Electrical-field stimulation (40 V, 2-30 Hz, 0.5 ms pulse duration, and 10 s) was performed to observe nonadrenergic, noncholinergic neurotransmitter release in IBS-D rat colon. The ATP level of Kreb's solution was also determined. RESULTS: PA exerted a concentration-dependent inhibitory effect on the spontaneous contraction of the colonic longitudinal smooth muscle, and the half maximal effective concentration (EC50) was 41.9 µmol/L. In comparison with the KCl-treated IBS-D group, the contractile response (mg contractions) in the PA + KCl-treated IBS-D group (11.87 ± 3.34) was significantly decreased in the peak tension (P < 0.01). Compared with CCh-treated IBS-D rat colon, the cholinergic contractile response of IBS-D rat colonic smooth muscle (EC50 = 0.94 µmol/L) was significantly decreased by PA (EC50 = 37.43 µmol/L) (P < 0.05). Lack of nitrergic neurotransmitter release in stress-induced IBS-D rats showed contraction effects on colonic smooth muscle. Pretreatment with PA resulted in inhibitory effect on L-NAME-induced (10 µmol/L) contraction (P < 0.05). ATP might not be the main neurotransmitter involved in inhibitory effects of PA in the colonic relaxation of stress-induced IBS-D rats. CONCLUSION: PA application may serve as a new therapeutic approach for IBS-D.


Assuntos
Diarreia/tratamento farmacológico , Motilidade Gastrointestinal/efeitos dos fármacos , Síndrome do Intestino Irritável/tratamento farmacológico , Sesquiterpenos/farmacologia , Estresse Psicológico/complicações , Animais , Colo/efeitos dos fármacos , Colo/patologia , Colo/fisiopatologia , Diarreia/patologia , Diarreia/psicologia , Modelos Animais de Doenças , Relação Dose-Resposta a Droga , Humanos , Síndrome do Intestino Irritável/patologia , Síndrome do Intestino Irritável/psicologia , Masculino , Contração Muscular/efeitos dos fármacos , Músculo Liso/efeitos dos fármacos , Músculo Liso/fisiologia , Componentes Aéreos da Planta/química , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Pogostemon/química , Ratos , Ratos Sprague-Dawley , Sesquiterpenos/uso terapêutico , Resultado do Tratamento
14.
Phytomedicine ; 39: 111-118, 2018 Jan 15.
Artigo em Inglês | MEDLINE | ID: mdl-29433672

RESUMO

BACKGROUND: Non-steroidal anti-inflammatory drugs (NSAIDs) are most widely used as effective anti-inflammatory agents. However, their clinical application brings about inevasible gastrointestinal side effects. Pogostemon cablin is a traditional herbal medicine used for the treatment of gastrointestinal diseases in China. One of its representative components, the tricyclic triterpenoid ß-patchoulone (ß-PAE) has demonstrated great anti-inflammatory activity and gastroprotective effect against ethanol-induced gastric injury, but its protective effect against gastric ulcer induced by indomethacin is still unknown. PURPOSE: To assess the protective effect of ß-PAE against ulcer produced by indomethacin and reveal the underlying pharmacological mechanism. STUDY DESIGN: We used an indomethacin-induced gastric ulcer model of rats in vivo. METHODS: Gastroprotective activity of ß-PAE (10, 20, 40 mg/kg, i.g.) was estimated via indomethacin-induced gastric ulcer model in rats. Histopathological and histochemical assessment of ulcerated tissues were performed. Protein and mRNA expression were determined by Elisa, Western blotting and qRT-PCR. RESULTS: ß-PAE could inhibit ulcer formation. Histopathological and histochemical assessment macroscopically demonstrated that ß-PAE alleviates indomethacin-induced gastric ulceration in dose-dependent manner. After administration of ß-PAE, elevated tumor necrosis factor -α level was significantly decreased and the phosphorylation of JNK and IκB was markedly inhibited. ß-PAE suppressed the levels of E-selectin, P-selectin, intercellular adhesion molecule-1, vascular cell adhesion molecule and monocyte chemoattractant protein 1, as well as myeloperoxidase. Meanwhile, ß-PAE increased cyclooxygenase enzyme activities (COX-1 and COX-2) to enhance the production of prostaglandin E2. Proangiogenic protein, vascular endothelial growth factor and its receptor fms-like tyrosine kinase-1 mRNA expression were promoted while anti-angiogenic protein, endostatin-1 and its receptor ETAR mRNA expression were decreased. CONCLUSION: ß-PAE may provide gastroprotection in indomethacin-induced gastric ulcer in rats by reducing inflammatory response and improving angiogenesis.


Assuntos
Indometacina/efeitos adversos , Substâncias Protetoras/farmacologia , Sesquiterpenos/farmacologia , Úlcera Gástrica/induzido quimicamente , Úlcera Gástrica/tratamento farmacológico , Indutores da Angiogênese/farmacologia , Animais , Anti-Inflamatórios não Esteroides/efeitos adversos , Antiulcerosos/farmacologia , Dinoprostona/metabolismo , Medicamentos de Ervas Chinesas/farmacologia , Mucosa Gástrica/efeitos dos fármacos , Mucosa Gástrica/metabolismo , Mucosa Gástrica/patologia , Masculino , Pogostemon/química , Ratos Sprague-Dawley , Sesquiterpenos de Guaiano , Úlcera Gástrica/patologia , Fator de Necrose Tumoral alfa/metabolismo
15.
Chem Biol Interact ; 283: 30-37, 2018 Mar 01.
Artigo em Inglês | MEDLINE | ID: mdl-29339218

RESUMO

Patchoulene epoxide (PAO), a tricyclic sesquiterpene isolated from the long-stored patchouli oil, has been demonstrated the anti-inflammatory activity in vivo based on our previous study. However, the gastric protective effect of PAO still remains unknown. Therefore, in the present study, ethanol-induced gastric ulcer model was carried out to evaluate the anti-ulcerogenic activity of PAO and to elucidate the potential mechanisms that involves. According to our results, macroscopic examination revealed that PAO could significantly reduce ethanol-induced gastric ulcer areas as compared with the vehicle group, which was also supported by the histological evaluation result. As for its potential mechanism, the anti-inflammatory activity of PAO contributed to gastric protection through reversing the imbalance between pro- and anti-inflammatory cytokines and modulating the expressions of NF-κB pathway-related proteins including p-IκBα, IκBα, p-p65 and p65. Besides, PAO was able to enhance the expressions of antioxidant enzymes including glutathione (GSH), superoxide dismutase (SOD) and catalase (CAT), and down-regulate malonaldehyde (MDA), an indicator of lipid peroxidation. Furthermore, immunohistochemistry analysis exhibited potent anti-apoptosis effect of PAO, as evidence by down-regulating the protein expression of caspase-3, Fas and Fasl. Additionally, we also demonstrated that PAO could replenish PGE2 and NO mucosal defense. In conclusion, these findings suggested that PAO has gastric protective activity against ethanol and this might be related to its influence on inflammatory response, oxidative stress, apoptosis cascade and gastric mucosal defense.


Assuntos
Anti-Inflamatórios/farmacologia , Apoptose/efeitos dos fármacos , Estresse Oxidativo/efeitos dos fármacos , Sesquiterpenos/farmacologia , Úlcera Gástrica/prevenção & controle , Animais , Anti-Inflamatórios/química , Anti-Inflamatórios/uso terapêutico , Caspase 3/metabolismo , Catalase/metabolismo , Citocinas/análise , Citocinas/metabolismo , Regulação para Baixo/efeitos dos fármacos , Etanol/toxicidade , Inflamação/prevenção & controle , Peroxidação de Lipídeos/efeitos dos fármacos , Masculino , Óleos Vegetais/química , Pogostemon/química , Pogostemon/metabolismo , Ratos , Ratos Sprague-Dawley , Sesquiterpenos/química , Sesquiterpenos/uso terapêutico , Estômago/patologia , Úlcera Gástrica/induzido quimicamente , Úlcera Gástrica/patologia , Superóxido Dismutase/metabolismo
16.
J Ethnopharmacol ; 220: 188-196, 2018 Jun 28.
Artigo em Inglês | MEDLINE | ID: mdl-28965754

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: The aerial parts of Pogostemon cablin (Blanco) Benth. for the treatment of cardiodynia have been documented in Mingyi Bielu of late Han Dynasty, in addition to that the Ca2+ antagonized activities of P. cablin and its critically pharmacological ingredient patchouli alcohol (PA) were reported previously. AIM OF THE STUDY: To investigate the relaxant effects of PA on rat isolated thoracic aortas and further explore its potential mechanisms of actions. MATERIALS AND METHODS: The aortas with endothelium and without endothelium were prepared and suspended in the organ bath for isometric tension recordings. The responses to accumulative concentrations of PA in endothelium-intact (E + ) aortas with basal tension and in different treated aortas pre-contracted with potassium chloride (KCl) or phenylephrine (PHE) were observed; the effects of L-NAME and indomethacin in aortas with intact endothelium, and of L-NAME, propranolol, tetraethtylamine (TEA), 4-aminopyridine (4-AP), barium chloride (BaCl2), glyburide in aortas with endothelial denudation on PA-produced vasorelaxation were assessed; the influences of PA on extracellular Ca2+ influx and intracellular Ca2+ release were measured in Ca2+-free medium. Finally, the abilities of PA to inhibit KCl- and PHE-induced contractions were compared to that of verapamil in E- aortas. RESULTS: PA produced vasorelaxant effects in KCl- and PHE-precontracted E + aortas in a concentration-dependent manner, which had no statistically different from that in KCl- and PHE-precontracted E- aortas. PA (10 µM) significantly reduced KCl-induced contractions while PHE-induced contractions were significantly reduced by 100 µM of PA instead of 10 µM and 30 µM in aortas with endothelium. Pre-incubation of E + aortas with L-NAME as well as indomethacin and of E- aortas with L-NAME, propranolol, TEA, 4-AP, BaCl2 and glyburide had no obvious effects on vasorelaxation of PA. In endothelium-removed aortas around Ca2+-free solution, PA remarkably lowered the contractions stimulated with Ca2+ and PHE, and application of ruthenium red and heparin further enhanced the abilities of PA to reduce PHE-caused contractions. In aortas without endothelium, 100 µM of PA markedly attenuated KCl-induced contractions but not affect PHE-induced contractions. Verapamil at the equal dose markedly attenuated KCl- and PHE-induced contractions, and the inhibitory effects on KCl-induced contractions were more forceful than that on PHE-induced contractions. In combined usage, the inhibitory effects on the contractions elicited by KCl were evidently weaker than that of verapamil alone and indifferently stronger than that of PA alone, and the inhibitory effects on the contractions elicited by PHE were evidently weaker than that of single verapamil but stronger than that of single PA. CONCLUSION: PA may act as a Ca2+ antagonist to exert an intensively vasorelaxant effects through endothelium-independent pathway, and its mechanisms underlying the vasoactivities seem to be associated with the blockade of extracellular Ca2+ influx through VDCCs and ROCCs in vascular smooth muscle cells (VSMCs) membrane and intracellular Ca2+ releases through IP3R- and RYR-mediated Ca2+ channels in sarcolemma.


Assuntos
Bloqueadores dos Canais de Cálcio/farmacologia , Pogostemon/química , Sesquiterpenos/farmacologia , Vasodilatação/efeitos dos fármacos , Animais , Aorta Torácica/efeitos dos fármacos , Aorta Torácica/metabolismo , Cálcio/metabolismo , Bloqueadores dos Canais de Cálcio/isolamento & purificação , Canais de Cálcio/efeitos dos fármacos , Canais de Cálcio/metabolismo , Endotélio Vascular/efeitos dos fármacos , Endotélio Vascular/metabolismo , Masculino , Miócitos de Músculo Liso/efeitos dos fármacos , Miócitos de Músculo Liso/metabolismo , Componentes Aéreos da Planta , Ratos , Ratos Sprague-Dawley
17.
Artif Cells Nanomed Biotechnol ; 46(6): 1171-1179, 2018 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-28859534

RESUMO

Mosquitoes pose a threat to humans and animals, causing millions of deaths every year. Vector control by effective eco-friendly pesticides of natural origin is a serious issue that requires urgent attention. The employment of green-reducing extracts for nanoparticles biosynthesis in a rapid and single-step process represents a promising strategy. In this study, silver nanoparticles (AgNPs) were biofabricated using an essential oil of Aquilaria sinensis (AsEO) and Pogostemonis Herba essential oil of Pogostemon cablin (PcEO) in one step and cost-effective manner. UV-vis spectrophotometry, Fourier transform infrared spectroscopy, scanning electron microscopy, transmission electron microscopy, X-ray diffraction analysis and energy-dispersive X-ray spectroscopy were used to confirm the AgNPs formation and their biophysical characterization. The larvicidal and pupicidal toxicity of AsEO, PcEO and biosynthesized AgNPs were evaluated against larvae and pupae of the dengue and Zika virus vector Aedes albopictus. Compared to the tested essential oils, the biofabricated AgNPs showed the highest toxicity against larvae and pupae of Ae.albopictus. In particular, the LC50 values of AsEO ranged from 44.23 (I) to 166 (pupae), LC50 values of PcEO ranged from 32.49 (I) to 90.05(IV), LC50 values of AsEO-AgNPs from 0.81 (I) to 1.12 (IV) and LC50 values of PcEO-AgPNs from 0.85 (I) to 1.19 (IV). Furthermore, histological analysis of the midgut cells of the control and treated larvae exhibited that the epithelial cells and brush border were highly affected by the fabricated AgNPs compared to the essential oils (AsEO and PcEO). Overall, the A. sinensis and P. cablin essential oils fabricated AgNPs have a potential of application as a biopesticide for mosquito control through safer and cost-effective approach.


Assuntos
Aedes/efeitos dos fármacos , Nanopartículas Metálicas/química , Nanopartículas Metálicas/toxicidade , Óleos Voláteis , Pogostemon/química , Prata , Thymelaeaceae/química , Animais , Dengue/transmissão , Trato Gastrointestinal/efeitos dos fármacos , Inseticidas , Larva/efeitos dos fármacos , Nanopartículas Metálicas/ultraestrutura , Controle de Mosquitos , Mosquitos Vetores/efeitos dos fármacos , Óleos Voláteis/química , Óleos Voláteis/farmacologia , Prata/química , Prata/farmacologia , Infecção por Zika virus/transmissão
18.
J Physiol Sci ; 68(3): 281-291, 2018 May.
Artigo em Inglês | MEDLINE | ID: mdl-28365907

RESUMO

Patchouli oil, an essential aroma oil extracted from patchouli leaf during short-term exposure with five and ten drops either inhibited (at 1 or 2 h) or stimulated (at 4 h) the platelet MAO-A activity depending on the dosages of the aroma oil mainly due to inhibition or stimulation of its K m. The long-term 15 consecutive days exposure (with two or five drops) of patchouli oil, on the other hand, maximally stimulated the platelet MAO-A activity with five drops patchouli oil for 1 h exposure, but further continuation of its exposure with same doses (two or five drops) for 30 consecutive days significantly stimulated (with two drops) and inhibited (with five drops) the platelet MAO-A activity due to stimulation and inhibition respectively of its corresponding both K m and V max. These results thus suggest that this aroma oil exposure may modulate the blood platelet serotonergic regulation depending on the dose, duration, and conditions of exposure.


Assuntos
Plaquetas/efeitos dos fármacos , Monoaminoxidase/metabolismo , Óleos Voláteis/administração & dosagem , Pogostemon/química , Animais , Masculino , Mamíferos , Extratos Vegetais/administração & dosagem , Folhas de Planta/química , Ratos , Ratos Wistar
19.
Rapid Commun Mass Spectrom ; 32(3): 221-229, 2018 Feb 15.
Artigo em Inglês | MEDLINE | ID: mdl-29178526

RESUMO

RATIONALE: The direct detection of nonpolar and low-polarity solvent extracts of herbal medicine is difficult by conventional electrospray ionization mass spectrometry (ESI-MS). This problem can be solved by solvent-assisted electrospray ionization mass spectrometry (SAESI-MS). With the help of assisted solvents (ESI-friendly solvents) at the tip of the spray needle, compounds (especially the low-polarity compounds) in nonpolar and low-polarity solvent extracts can be ionized directly. METHODS: Herbal medicines were ultrasonically extracted with nonpolar or low-polarity solvents, such as petroleum ether. Thereafter, the extracts were analyzed by conventional ESI-MS, atmospheric pressure chemical ionization mass spectrometry (APCI-MS) and SAESI-MS. The mass spectra obtained from these three methods were compared and analyzed. RESULTS: Unstable ion signals, and even no ion signals, were observed when the nonpolar and low-polarity solvent extracts were detected directly by conventional ESI-MS. Better specificity, higher sensitivity or cleaner spectra were acquired from SAESI-MS by comparing with the performance of conventional ESI-MS. The ion signals generated by SAESI-MS and APCI-MS were observed in clearly different m/z ranges. A variety of potential compounds were detected in the petroleum ether extracts of Pogostemon cablin and Ligusticum chuanxiong. The relative abundances and signal intensities of the same ion signals from the stems, leaves and decoction pieces of Pogostemon cablin were significantly different by SAESI-MS. CONCLUSIONS: As a convenient and efficient method, SAESI-MS can be used to directly detect compounds (especially the low-polarity compounds) in nonpolar or low-polarity solvent extracts of herbal medicines, providing abundant chemical information for pharmacological studies. SAESI-MS allows the simultaneous qualitative analysis of multiple compounds in the same complex samples and is thus particularly suitable for the preliminary screening of compounds in complex samples. SAESI-MS can be used to differentiate the different parts of herbal medicines.


Assuntos
Extratos Vegetais/análise , Extratos Vegetais/química , Solventes/química , Espectrometria de Massas por Ionização por Electrospray/métodos , Alcanos/química , Ligusticum/química , Folhas de Planta/química , Caules de Planta/química , Pogostemon/química
20.
Mol Med Rep ; 16(4): 4511-4520, 2017 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-28791344

RESUMO

Various plant-derived compounds exhibit immunosuppressive activity in pre­clinical investigations, suggesting that they may serve as natural alternatives for the prevention of inflammatory disorders and autoimmune diseases. The aim of the current study was to explore the immunosuppressive potential of pogostone (PO) derived from Pogostemon cablin (Blanco) Benth. Carboxyfluorescein diacetate succinimidyl ester­labeled cell tracking demonstrated that PO (20­80 µM) inhibited Concanavalin A (ConA)­stimulated lymphocyte proliferation, which was mediated by G0/G1 phase arrest and accompanied by significant decreases in the expression of CD69 (early­stage activation marker) and CD25 (mid­stage activation marker) in T cells, as indicated by flow cytometry analysis. Furthermore, the proliferation blocking ability of PO (5­80 µM) was not associated with cytotoxicity in normal lymphocytes or apoptosis in ConA­stimulated lymphocytes. The inflammatory cytokine profile determination using a cytometric beads assay revealed that PO inhibited release of anti­inflammatory interleukin (IL)­10 and pro­inflammatory IL­6 from the stimulated lymphocytes. Furthermore, PO (10, 20 or 40 mg/kg) ameliorated the T­cell mediated delayed type hypersensitivity response in Balb/c mice by reducing leukocyte infiltration and tissue edema, providing a further validation of the direct immunosuppressive activity of PO. Together, the present data suggest that PO would suppress T cell response via a direct non­cytotoxic inactivation at the early stage, accompanied by regulation of the inflammatory cytokine profile, which highlights clinical implications for treatment of immune-based disorders.


Assuntos
Imunossupressores/farmacologia , Óleos Voláteis/farmacologia , Extratos Vegetais/farmacologia , Pogostemon/química , Linfócitos T/efeitos dos fármacos , Linfócitos T/fisiologia , Animais , Apoptose/efeitos dos fármacos , Ciclo Celular/efeitos dos fármacos , Sobrevivência Celular/efeitos dos fármacos , Citocinas/metabolismo , Citotoxicidade Imunológica/efeitos dos fármacos , Imunofenotipagem , Imunossupressores/química , Mediadores da Inflamação/metabolismo , Ativação Linfocitária/efeitos dos fármacos , Ativação Linfocitária/imunologia , Masculino , Camundongos , Óleos Voláteis/química , Extratos Vegetais/química
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