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1.
World J Gastroenterol ; 23(24): 4369-4380, 2017 Jun 28.
Artigo em Inglês | MEDLINE | ID: mdl-28706419

RESUMO

AIM: To investigate the effects of Ground Cherry (Physalis angulata L.) standardized supercritical CO2 extract in trinitrobenzenesulphonic acid (TNBS) model of rat intestinal inflammation. METHODS: The animals were divided into groups that received vehicle or P. angulata extract (PACO2) orally at the doses 25, 50 and 100 mg/kg daily by 5 d before TNBS damage. Protective effects of PACO2 were assessed by macroscopic analysis, biochemical determinations of the levels of myeloperoxidase (MPO), alkaline phosphatase (ALP), glutathione and cytokines (such as INF-γ, IL-1ß, IL-6, IL-10 and TNF-α), gene expression evaluation (including Hsp70, heparanase, NF-κB, mitogen-activated protein kinases (Mapk) 1, 3, 6 and 9, and the mucins genes Muc 1, 2, 3 and 4) and histopathological studies using optical, and electronic (transmission and scanning) microscopy. RESULTS: PACO2 extract promoted a significant reduction in MPO and ALP activities, reducing oxidative stress and neutrophil infiltration. These effects were accompanied by significant reduction of colonic levels of IFN-γ and IL-6 and down-regulation of heparanase, Hsp70, Mapk3, Mapk9, Muc1 and Muc2 genes expression when compared with TNBS-control animals. In addition, protective effects were also evidenced by reduced neutrophil infiltration, recovery of cell architecture and replacement of mucin by histopathological and ultrastructural analysis. CONCLUSION: Physalis angulata supercritical CO2 extract is an intestinal anti-inflammatory product that modulates oxidative stress, immune response and expression of inflammatory mediators, with potentially utility for treating inflammatory bowel disease.


Assuntos
Anti-Inflamatórios/uso terapêutico , Colite/tratamento farmacológico , Physalis/química , Extratos Vegetais/uso terapêutico , Administração Oral , Fosfatase Alcalina/metabolismo , Animais , Dióxido de Carbono/química , Cromatografia com Fluido Supercrítico , Colite/induzido quimicamente , Colite/patologia , Colo/enzimologia , Colo/patologia , Colo/ultraestrutura , Citocinas/metabolismo , Modelos Animais de Doenças , Regulação para Baixo , Mucosa Intestinal/enzimologia , Mucosa Intestinal/patologia , Mucosa Intestinal/ultraestrutura , Masculino , Microscopia Eletrônica de Transmissão e Varredura , Proteínas Quinases Ativadas por Mitógeno/metabolismo , Infiltração de Neutrófilos/efeitos dos fármacos , Peroxidase/metabolismo , Ratos , Ratos Wistar , Ácido Trinitrobenzenossulfônico/toxicidade
2.
Artigo em Inglês | MEDLINE | ID: mdl-25883669

RESUMO

The use of topical retinoids to treat skin disorders and ageing can induce local reactions, while oral retinoids are potent teratogens and produce several unwanted effects. This way, efforts to explore complementary care resources should be supported. Based on this, we evaluate the antiageing effects of a supercritical CO2 extract from Bidens pilosa L. (BPE-CO2A) containing a standardized multicomponent mixture of phytol, linolenic, palmitic, linoleic, and oleic acids. BPE-CO2A was assessed for its effects on human dermal fibroblasts (TGF-ß1 and FGF levels using ELISA; collagen, elastin, and glycosaminoglycan by colorimetric assays, and mRNA expression of RXR, RAR, and EGFr by qRT-PCR) and human skin fragments (RAR, RXR, collagen, elastin, and glycosaminoglycan by immunohistochemical analysis). Levels of extracellular matrix elements, TGF-ß1 and FGF, and EGFr gene expression were significantly increased by BPE-CO2A. The modulation of RXR and RAR was positively demonstrated after the treatment with BPE-CO2A or phytol, a component of BPE-CO2A. The effects produced by BPE-CO2A were similar to or better than those produced by retinol and retinoic acid. The ability to stimulate extracellular matrix elements, increase growth factors, and modulate retinoid and rexinoid receptors provides a basis for the development of preparation containing BPE-CO2A as an antiageing/skin-repair agent.

3.
J Pharm Pharmacol ; 67(4): 597-604, 2015 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-25556766

RESUMO

OBJECTIVES: Zeyheria montana is a medicinal plant used in Brazilian folk medicine for treating skin affections, ulcers, inflammation and diarrhoea, and as an antisyphilitic and antiblenorrhagic agent, but little is known about its mechanisms of action. Herein, a bio-guided assay was carried out to further evaluate its antioxidant and immunomodulatory effects, and the possible benefits on experimental intestinal inflammation. METHODS: Extracts, partitions, fractions and isolated compounds were tested for inhibition of lipid peroxidation. Isolated compounds were tested in vitro for its antioxidant and immunomodulatory action prior to in-vivo evaluation in trinitrobenzenesulfonic acid-induced rat colitis. KEY FINDINGS: Two major compounds were identified in the leaf dichloromethane extract: 3'-hydroxy-5,7,4'-trimethoxyflavone and 6-hydroxy-5,7-dimethoxyflavone, which exhibited an antioxidant activity. The compounds protected the colonic glutathione levels in more than 90% despite the absence of protection against the gross macroscopic colonic damage. In addition, the compounds inhibited IL-1ß secretion by macrophages in 91.5% and 72.7% respectively, whereas both reduced IL-6 secretion in about 44.5%. CONCLUSIONS: The major active compounds from Z. montana leaves exerted antioxidant and immunomodulatory effects, endorsing the use of Z. montana in folk medicine as an anti-inflammatory agent. However, further investigation is still needed regarding medicinal plants and the identification of candidate compounds for the treatment of the inflammatory bowel diseases.


Assuntos
Anti-Inflamatórios/uso terapêutico , Antioxidantes/uso terapêutico , Bignoniaceae/química , Colite/tratamento farmacológico , Doenças Inflamatórias Intestinais/patologia , Intestinos/efeitos dos fármacos , Fitoterapia , Animais , Anti-Inflamatórios/farmacologia , Antioxidantes/farmacologia , Brasil , Colite/induzido quimicamente , Colite/metabolismo , Flavonoides/análise , Flavonoides/farmacologia , Flavonoides/uso terapêutico , Fatores Imunológicos/farmacologia , Fatores Imunológicos/uso terapêutico , Inflamação/induzido quimicamente , Inflamação/tratamento farmacológico , Doenças Inflamatórias Intestinais/tratamento farmacológico , Intestinos/patologia , Peroxidação de Lipídeos/efeitos dos fármacos , Masculino , Camundongos Endogâmicos BALB C , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Extratos Vegetais/uso terapêutico , Folhas de Planta , Ácido Trinitrobenzenossulfônico
4.
Phytomedicine ; 21(3): 240-6, 2014 Feb 15.
Artigo em Inglês | MEDLINE | ID: mdl-24176844

RESUMO

BACKGROUND: Coumarins, also known as benzopyrones, are plant-derived products with several pharmacological properties, including antioxidant and anti-inflammatory activities. Based on the wide distribution of coumarin derivatives in plant-based foods and beverages in the human diet, our objective was to evaluate both the antioxidant and intestinal anti-inflammatory activities of six coumarin derivatives of plant origin (scopoletin, scoparone, fraxetin, 4-methyl-umbeliferone, esculin and daphnetin) to verify if potential intestinal anti-inflammatory activity was related to antioxidant properties. METHODS: Intestinal inflammation was induced by intracolonic instillation of TNBS in rats. The animals were treated with coumarins by oral route. The animals were killed 48 h after colitis induction. The colonic segments were obtained after laparotomy and macroscopic and biochemical parameters (determination of glutathione level and myeloperoxidase and alkaline phosphatase activities) were evaluated. The antioxidant properties of these coumarins were examined by lipid peroxidation and DPPH assays. RESULTS: Treatment with esculin, scoparone and daphnetin produced the best protective effects. All coumarin derivatives showed antioxidant activity in the DPPH assay, while daphnetin and fraxetin also showed antioxidant activity by inhibiting lipid peroxidation. Coumarins, except 4-methyl-umbeliferone, also showed antioxidant activity through the counteraction of glutathione levels or through the inhibition of myeloperoxidase activity. DISCUSSION: The intestinal anti-inflammatory activity of coumarin derivatives were related to their antioxidant properties, suggesting that consumption of coumarins and/or foods rich in coumarin derivatives, particularly daphnetin, esculin and scoparone, could prevent intestinal inflammatory disease.


Assuntos
Anti-Inflamatórios/farmacologia , Antioxidantes/farmacologia , Colite/metabolismo , Colo/efeitos dos fármacos , Cumarínicos/farmacologia , Fitoterapia , Extratos Vegetais/farmacologia , Fosfatase Alcalina/metabolismo , Animais , Anti-Inflamatórios/uso terapêutico , Antioxidantes/uso terapêutico , Compostos de Bifenilo/metabolismo , Colite/etiologia , Colite/prevenção & controle , Colo/metabolismo , Cumarínicos/uso terapêutico , Esculina/farmacologia , Esculina/uso terapêutico , Glutationa/metabolismo , Inflamação/etiologia , Inflamação/metabolismo , Inflamação/prevenção & controle , Doenças Inflamatórias Intestinais/metabolismo , Doenças Inflamatórias Intestinais/prevenção & controle , Peroxidação de Lipídeos/efeitos dos fármacos , Masculino , Estresse Oxidativo/efeitos dos fármacos , Peroxidase/metabolismo , Picratos/metabolismo , Extratos Vegetais/uso terapêutico , Ratos , Ratos Wistar , Umbeliferonas/farmacologia , Umbeliferonas/uso terapêutico
5.
J Ethnopharmacol ; 151(1): 380-5, 2014.
Artigo em Inglês | MEDLINE | ID: mdl-24211392

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Stem bark and fruit pulp of Hymenaea stigonocarpa Mart ex. Hayne (Fabaceae) has been popularly used to treat inflammation and gastrointestinal diseases including ulcers, diarrhea and gastric pain. The aim of this study was to investigate the intestinal anti-inflammatory activity of a methanol extract derived from the stem bark and diet with fruit pulp of Hymenaea stigonocarpa in the TNBS model of intestinal inflammation in rats. MATERIAL AND METHODS: The intestinal anti-inflammatory activity of stem bark extract (100, 200 and 400mg/kg) and fruit pulp (10% and 5% in diet) was measured against the intestinal inflammatory process induced by TNBS (trinitrobenzesulphonic acid) in rats. The protective effects were evaluated as follows: evaluation of intestinal damage (damage score, extension of lesion, colon weight/length ratio), incidence of diarrhea and adherence to adjacent organs, colon glutathione (GSH) and malondialdehyde (MDA) contents, myeloperoxidase (MPO) and alkaline phosphatase (AP) activities. In addition, in vitro studies on lipid peroxidation in rat brain membranes and phytochemical profile were performed with both stem bark and fruit pulp. RESULTS: Treatment with 100, 200 and 400mg/kg of stem bark extract and 10% fruit pulp flour showed protective effects in the TNBS-induced colon damage, which was related to inhibition of MPO and AP activities, reduction in colon MDA content, and counteraction of GSH depletion induced by inflammatory process. A concentration-dependent inhibitory effect on the lipid peroxidation in rat brain membranes for stem bark and fruit pulp was determined, with an IC50 value of 5.25 ± 0.23 µg/mL and 27.33 ± 0.09 µg/mL, respectively. Similar phytochemical composition was observed in fruit and stem bark, including mainly flavonoids, condensed tannins and terpenes. CONCLUSIONS: Stem bark extract and fruit pulp flour of Hymenaea stigonocarpa prevented TNBS-induced colonic damage in rats and this protective effect were associated to an improvement of intestinal oxidative stress. The observed anti-inflammatory and antioxidant effects may be associated to the presence of flavonoids and tannins in the stem bark and fruit pulp of Hymenaea stigonocarpa.


Assuntos
Anti-Inflamatórios/uso terapêutico , Colite/tratamento farmacológico , Hymenaea/química , Inflamação/tratamento farmacológico , Plantas Medicinais , Animais , Anti-Inflamatórios/administração & dosagem , Anti-Inflamatórios/química , Colite/induzido quimicamente , Relação Dose-Resposta a Droga , Inflamação/induzido quimicamente , Masculino , Casca de Planta/química , Caules de Planta/química , Distribuição Aleatória , Ratos , Ratos Wistar , Ácido Trinitrobenzenossulfônico/toxicidade
6.
J Ethnopharmacol ; 150(3): 1016-23, 2013 Dec 12.
Artigo em Inglês | MEDLINE | ID: mdl-24157378

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: An ethnopharmacological survey indicated that the bark from Qualea parviflora Mart. (Vochysiaceae) could be used to treat gastrointestinal disorders, such as diarrhea and intestinal inflammation. The objective of this study was to evaluate the effects of a methanolic extract from the bark of Qualea parviflora (QP) in an experimental model of diarrhea and intestinal inflammation induced in rodents. MATERIAL AND METHODS: The antidiarrheal and antispasmodic effects of QP were investigated by measuring intestinal motility, diarrhea, and intestinal fluid accumulation in rodents after challenging with a cathartic agent. In addition, the effects of QP on the contractility of the isolated mice-ileum preparation were determined. Acute intestinal inflammation was induced in male Wistar rats by the rectal administration of trinitrobenzenesulfonic acid (TNBS) in 50% ethanol (0.25 mL). QP was administered orally (for 5 days) prior to the induction of inflammation. The colonic injury and extent of inflammation were assessed by macroscopic damage scores and lesion length. The enhanced colonic mucosal injury, inflammatory response, and oxidative stress were evaluated by myeloperoxidase (MPO) activity; the tumor necrosis factor alpha (TNF-α), interleukin 1ß (IL1-ß), and malondialdehyde (MDA) levels; and the glutathione (GSH) content. RESULTS: Oral treatment with QP (500 mg/kg) delayed the onset of diarrhea, reduced the amount of liquid stool, and decreased the severity of the diarrhea and the evacuation index in rodents challenged with castor oil (p<0.01). Additionally, QP (150-500 µg/mL) demonstrated effective antispasmodic activity against carbachol-induced contractions of mouse ileum in vitro. Oral treatment (25 and 50 mg/kg/day) with QP significantly reduced the intestinal inflammation induced by TNBS in rats (52% and 45%, respectively). Improvement of colonic mucosal injury by treatment with QP was demonstrated by a decrease in MDA levels and an increase in GSH content in colonic tissue. QP also prevented intestinal inflammation as evidenced by reduced cytokine levels (TNF-α and IL1-ß) and low MPO activity. CONCLUSIONS: The ethnopharmacological usefulness of the bark from Qualea parviflora against diarrhea containing blood and mucus was supported by the observed antidiarrheal, antispasmodic, and intestinal antiinflammatory properties of this medicinal plant.


Assuntos
Anti-Inflamatórios/uso terapêutico , Antidiarreicos/uso terapêutico , Colite/tratamento farmacológico , Diarreia/tratamento farmacológico , Parassimpatolíticos/uso terapêutico , Extratos Vegetais/uso terapêutico , Traqueófitas , Animais , Anti-Inflamatórios/farmacologia , Antidiarreicos/farmacologia , Óleo de Rícino , Colite/induzido quimicamente , Colite/metabolismo , Colite/patologia , Colo/efeitos dos fármacos , Colo/metabolismo , Colo/patologia , Motilidade Gastrointestinal/efeitos dos fármacos , Glutationa/metabolismo , Íleo/efeitos dos fármacos , Íleo/fisiologia , Interleucina-1beta/metabolismo , Masculino , Malondialdeído/metabolismo , Metanol/química , Camundongos , Contração Muscular/efeitos dos fármacos , Parassimpatolíticos/farmacologia , Peroxidase/metabolismo , Fitoterapia , Casca de Planta , Extratos Vegetais/farmacologia , Ratos , Ratos Wistar , Solventes/química , Ácido Trinitrobenzenossulfônico , Fator de Necrose Tumoral alfa/metabolismo
7.
BMC Complement Altern Med ; 12: 62, 2012 May 04.
Artigo em Inglês | MEDLINE | ID: mdl-22559191

RESUMO

BACKGROUND: Inflammatory bowel disease (IBD) is a chronic inflammation of the intestinal epithelium that is driven by the intestinal immune system, oxidative stress and the loss of tolerance to the luminal microbiota. The use of dietary products containing ingredients such as fibres and carbohydrates and/or antioxidant compounds have been used as a therapeutic strategy for intestinal diseases because these products are considered effective in the modulation of the immune system and colonic microbiota. We investigated the beneficial effects of cattail rhizome flour (Typha angustifolia L.) in the trinitrobenzenesulphonic acid (TNBS) model of rat colitis. In addition, we investigated the effects of cattail rhizome flour on the intestinal anti-inflammatory activity of prednisolone, which is a reference drug that is used for treatment of human IBD. METHODS: The present study included the preparation of flour from rhizomes of cattail (Typha angustifolia L.); an evaluation of the qualitative phytochemical profile of cattail rhizomes; an evaluation of the efficacy of cattail rhizome flour in TNBS-induced rat colitis; an evaluation of the synergistic effects of cattail rhizome flour on the intestinal anti-inflammatory activity of prednisolone; and macroscopic, clinical, biochemical, histopathological and microbiological studies to assess the healing effects of cattail rhizome flour and its synergistic effects in TNBS-induced rat colitis. The data were analysed by ANOVA, Kruskal-Wallis and χ(2) tests. RESULTS: We tested several concentrations of cattail rhizome flour and found that dietary supplementation with 10% cattail rhizome flour showed the best effects at reducing the extension of the lesion, the colon weight ratio, adherences to adjacent organs and diarrhoea. These effects were related to inhibition of myeloperoxidase (MPO) and alkaline phosphatase (AP) activities and an attenuation of glutathione (GSH) depletion. The 10% cattail rhizome flour was as effective as prednisolone, and no synergistic effects were observed. Saponins, flavonoids and coumarins were detected in the rhizome flour. No changes were observed in the total number of lactic bacteria after dietary supplementation with cattail rhizome flour. CONCLUSIONS: Dietary supplementation with 10% cattail rhizome flour and its combination with prednisolone prevent TNBS-induced colonic damage in rats, but no synergistic effects were observed. The prevention of TNBS-induced colon damage was associated with an improvement in intestinal oxidative stress, which likely resulted from the antioxidant properties of the active compounds detected in the cattail rhizome. This protective effect was not related to an improvement in lactic bacteria counts.


Assuntos
Colite/dietoterapia , Colo/efeitos dos fármacos , Suplementos Nutricionais , Inflamação/prevenção & controle , Fitoterapia , Preparações de Plantas/uso terapêutico , Typhaceae/química , Fosfatase Alcalina/antagonistas & inibidores , Animais , Anti-Inflamatórios/farmacologia , Anti-Inflamatórios/uso terapêutico , Antioxidantes/metabolismo , Antioxidantes/farmacologia , Antioxidantes/uso terapêutico , Colite/metabolismo , Colite/patologia , Colo/metabolismo , Colo/patologia , Diarreia/tratamento farmacológico , Diarreia/etiologia , Fibras na Dieta/farmacologia , Fibras na Dieta/uso terapêutico , Modelos Animais de Doenças , Farinha , Glutationa/metabolismo , Inflamação/metabolismo , Inflamação/patologia , Mucosa Intestinal/efeitos dos fármacos , Mucosa Intestinal/metabolismo , Mucosa Intestinal/patologia , Masculino , Tamanho do Órgão , Peroxidase/antagonistas & inibidores , Preparações de Plantas/farmacologia , Prednisolona/farmacologia , Prednisolona/uso terapêutico , Ratos , Ratos Wistar , Rizoma , Ácido Trinitrobenzenossulfônico
8.
Artigo em Inglês | MEDLINE | ID: mdl-23346204

RESUMO

Background. This study was pathway of (-)-epicatechin (EC) in the prevention and treatment of intestine inflammation in acute and chronic rat models. Methods. Intestine inflammation was induced in rats using TNBS. The morphological, inflammatory, immunohistochemical, and immunoblotting characteristics of colon samples were examined. The effects of EC were evaluated in an acute model at doses of 5, 10, 25, and 50 mg/kg by gavage for 5 days. The chronic colitis model was induced 1st day, and treated for 21 days. For the colitis relapse model, the induction was repeated on 14th. Results. EC10 and EC50 effectively reduced the lesion size, as assessed macroscopically; and confirmed by microscopy for EC10. The glutathione levels were higher in EC10 group but decreased COX-2 expression and increased cell proliferation (PC) were observed, indicating an anti-inflammatory activity and a proliferation-stimulating effect. In the chronic colitis model, EC10 showed lower macroscopic and microscopic lesion scores and increase in glutathione levels. As in the acute model, a decrease in COX-2 expression and an increase in PC in EC10, the chronic model this increase maybe by the pathway EGF expression. Conclusion. These results confirm the activity of EC as an antioxidant that reduces of the lesion and that has the potential to stimulate tissue healing, indicating useful for preventing and treating intestine inflammation.

9.
J Ethnopharmacol ; 135(2): 463-8, 2011 May 17.
Artigo em Inglês | MEDLINE | ID: mdl-21453767

RESUMO

ETHNOPHARMACOLOGY RELEVANCE: Different plant species from Cordia genera are used in folk medicine as anti-inflammatory medication throughout the tropical and subtropical regions of the world. In Brazil, Cordia verbenacea is a medicinal plant known as "erva-baleeira". The alcoholic extracts, decoctions and infusions with leaves of C. verbenacea are used in Brazilian traditional medicine for treatment of cough, pneumonia, parasitic diseases and, especially, the inflammatory processes. Anti-inflammatory activity was already demonstrated; however, molecular mechanisms of action are not completely understood. Considering the importance of histamine in early events of inflammation and in allergic diseases, we evaluated the effect of ethanol extract of leaves of C. verbenacea on histamine release (in vitro and in vivo studies) from different types of mast cells induced by chemical agents using several species of rodents. MATERIALS AND METHODS: The extraction and quantification of histamine were performed by using an automatic fluorometric continuous flow system. RESULTS: The extract of C. verbenacea (30 µg/ml) reduced the in vitro secretion of histamine from rat mast cells induced by ionophore A23187, concanavalin A and compound 48/80, respectively, to 22.1 ± 2.2%, 24.3 ± 2.5% and 21.4 ± 2.1%. At the same concentration, the extract also inhibited the secretion of histamine from mast cells of guinea pig induced by ionophore A23187 to 33.3 ± 2.2%, and mast cells of hamster induced by ionophore A23187 and concanavalin A to 15.8 ± 2.5% and 10.8 ± 2.6%, respectively. The oral treatment with the extract (300 mg/kg) also inhibited the secretion of histamine induced by A23187 about to 36.3 ± 3.2% in rats. CONCLUSIONS: C. verbenacea inhibits the in vitro secretion of histamine from mast cells of different animal species, as well as the secretion of mast cells from animals treated with the extract, which gives not only the proven anti-inflammatory effect of the plant, but also anti-allergic effect, opening new possibilities for future anti-allergic herbal medicine.


Assuntos
Cordia/química , Mastócitos/metabolismo , Extratos Vegetais/farmacologia , Animais , Etanol/química , Cobaias , Liberação de Histamina/efeitos dos fármacos , Masculino , Extratos Vegetais/química , Ratos , Ratos Wistar
10.
Phytother Res ; 25(10): 1447-50, 2011 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-21351299

RESUMO

The present study isolated three major active flavonoids, two flavones named 4',5,7-trimethoxy-luteolin (1) and 6-hydroxy-5,7-dimethoxyflavone (2) and the flavanone 5-hydroxy-6,7-dimethoxyflavanone (3) from Zeyheria montana dichloromethane leaf extract. Isolation and purification were conducted with the application of column chromatography and structures were assigned by spectral analysis. All compounds were evaluated for cytotoxic activities against human tumor cell lines UACC-62 (melanoma), MCF-7 (breast), NCI-ADR/RES (breast expressing phenotype multiple drug resistance), 786-0 (renal), NCI-H460 (lung, non-small cells), PC-3 (prostate), OVCAR-3 (ovarian), HT-29 (colon) and K562 (leukemia) in vitro. All compounds were active in different degrees on several tumor cell lines and flavanone 3 showed cytotoxicity against almost all cell lines, particularly against human NCI-ADR/RES and K562 cell lines. In conclusion, three antiproliferative compounds were isolated for the first time from Zeyheria montana and its leaves were characterized as an important source of methoxylated flavones and flavanone as potential antitumor compounds.


Assuntos
Antineoplásicos Fitogênicos/uso terapêutico , Bignoniaceae/química , Flavanonas/uso terapêutico , Flavonas/uso terapêutico , Neoplasias/tratamento farmacológico , Fitoterapia , Extratos Vegetais/uso terapêutico , Antineoplásicos Fitogênicos/isolamento & purificação , Antineoplásicos Fitogênicos/farmacologia , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Flavanonas/isolamento & purificação , Flavanonas/farmacologia , Flavonas/isolamento & purificação , Flavonas/farmacologia , Flavonoides , Humanos , Estrutura Molecular , Neoplasias/patologia , Extratos Vegetais/isolamento & purificação , Extratos Vegetais/farmacologia , Folhas de Planta
11.
Artigo em Inglês | MEDLINE | ID: mdl-19592480

RESUMO

Baccharis dracunculifolia DC (Asteraceae) is a Brazilian medicinal plant popularly used for its antiulcer and anti-inflammatory properties. This plant is the main botanical source of Brazilian green propolis, a natural product incorporated into food and beverages to improve health. The present study aimed to investigate the chemical profile and intestinal anti-inflammatory activity of B. dracunculifolia extract on experimental ulcerative colitis induced by trinitrobenzenosulfonic acid (TNBS). Colonic damage was evaluated macroscopically and biochemically through its evaluation of glutathione content and its myeloperoxidase (MPO) and alkaline phosphatase activities. Additional in vitro experiments were performed in order to test the antioxidant activity by inhibition of induced lipid peroxidation in the rat brain membrane. Phytochemical analysis was performed by HPLC using authentic standards. The administration of plant extract (5 and 50 mg kg(-1)) significantly attenuated the colonic damage induced by TNBS as evidenced both macroscopically and biochemically. This beneficial effect can be associated with an improvement in the colonic oxidative status, since plant extract prevented glutathione depletion, inhibited lipid peroxidation and reduced MPO activity. Caffeic acid, p-coumaric acid, aromadendrin-4-O-methyl ether, 3-prenyl-p-coumaric acid, 3,5-diprenyl-p-coumaric acid and baccharin were detected in the plant extract.

12.
J Cosmet Dermatol ; 9(1): 35-43, 2010 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-20367671

RESUMO

BACKGROUND: Hydration and integrity of the stratum corneum (SC) is an important determinant of skin appearance, metabolism, mechanical properties, and barrier function. The presence of aquaglyceroporins and envelope proteins are crucial to provide greater corneocyte cohesion to keep water and other moisturizers in the skin. AIMS: In this study, we evaluated the ability of Piptadenia colubrina, a plant native of South American rain forests, in the expression of genes involved in skin capacitance and SC integrity. METHODS: The expression of genes for aquaporin-3 (AQP3), loricrin, involucrin (INV), and filaggrin (FLG) was measured by real-time PCR, using an in vitro model of human keratinocytes incubated with concentrations of 2.5, 5, 10, and 20 mg/mL of a hydroglycolic extract of P. colubrina (HEPC). The amount of AQP3 protein was also tested by immunohistochemistry in human skin explants. Clinical trials were conducted to evaluate the effects of a gel-cream containing HEPC on the glycerol index and skin capacitance. RESULTS: Hydroglycolic extract of P. colubrina increased both the expression and immunoreactivity of AQP3 in cultured keratinocytes and human skin explants. The gene induction to envelope proteins FLG and INV was also observed after cell incubation with HEPC. Skin capacitance was significantly improved in human volunteers under treatment with HEPC-containing cream. CONCLUSIONS: The extract of P. colubrina promotes cellular hydration and induces gene expression of envelope proteins providing greater corneocyte cohesion to keep water and other moisturizers in the skin and an appropriate epidermal adhesion. The in vitro findings were clinically confirmed and encourage the clinical use of this compound in skin care products.


Assuntos
Aquaporina 3/metabolismo , Colubrina , Proteínas de Filamentos Intermediários/metabolismo , Proteínas de Membrana/metabolismo , Precursores de Proteínas/metabolismo , Pele/efeitos dos fármacos , Pele/metabolismo , Água/metabolismo , Administração Cutânea , Adulto , Aquaporina 3/genética , Emolientes/administração & dosagem , Emolientes/farmacologia , Feminino , Proteínas Filagrinas , Humanos , Técnicas In Vitro , Proteínas de Filamentos Intermediários/genética , Queratinócitos/efeitos dos fármacos , Queratinócitos/metabolismo , Proteínas de Membrana/genética , Pessoa de Meia-Idade , Fitoterapia , Extratos Vegetais/administração & dosagem , Extratos Vegetais/farmacologia , Reação em Cadeia da Polimerase , Precursores de Proteínas/genética , Absorção Cutânea/efeitos dos fármacos , Equilíbrio Hidroeletrolítico
13.
J Cosmet Dermatol ; 8(1): 56-62, 2009 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-19250168

RESUMO

BACKGROUND: Green Coffea arabica L. seed oil is being widely used in cosmetic formulations, although its effects on human skin cells are not clear and most observations are unpublished. AIMS: In this study, we evaluated the in vitro effects of green coffee (C. arabica L.) oil (GCO) on the synthesis of collagen, elastin, and glycosaminoglycans (GAG) and in the release of transforming growth factor-beta1 (TGF-beta1) and granulocyte-macrophage colony-stimulating factor (GM-CSF) by human skin fibroblasts. We also investigated the ability of GCO to increase aquaglycerolporins-3 (AQP-3) mRNA expression in cultured keratinocytes and human skin explants. METHODS: Human fibroblasts were incubated for 48 h with several GCO concentrations (3.12, 6.25, 12.5, 25.0 and 50.0 mg/mL). The levels of growth factors and extracellular matrix compounds in the culture supernatant were measured using commercial kits. To evaluate AQP-3 relative expression, using real-time reverse transcription polymerase chain reaction, keratinocytes were incubated for 3-6 h with the GCO optimal concentration of 25.0 mg/mL. Histological sections of human skin were also incubated with GCO (25.0 mg/mL) and immunostained by antiserum against AQP-3. RESULTS: Our results demonstrated that incubation with GCO produces a dose-dependent stimulation in the synthesis of collagen, elastin, and GAG, in addition to increasing the release of the growth factors TGF-beta1 and GM-CSF. GCO also induced the expression of AQP-3 mRNA, which reached levels up to 6.5-fold higher than those of the control cultures. CONCLUSION: The findings presented herein suggest that GCO might improve physiological balance in the skin, thus allowing the formation of new connective tissue, and preventing epidermis dryness by increasing AQP-3 levels. Taking into account the limitations of in vitro studies, it is encouraging in this context to consider CGO as an adjuvant to be used in dermocosmetic formulations. Clinical studies are in progress in our laboratory aiming to further investigate the protective effects of CGO in the skin.


Assuntos
Aquaporinas/metabolismo , Coffea , Matriz Extracelular/efeitos dos fármacos , Fibroblastos/efeitos dos fármacos , Óleos de Plantas/farmacologia , Preparações de Plantas/farmacologia , Análise de Variância , Aquaporinas/genética , Células Cultivadas , Matriz Extracelular/genética , Matriz Extracelular/metabolismo , Fibroblastos/citologia , Expressão Gênica , Fator Estimulador de Colônias de Granulócitos e Macrófagos/genética , Fator Estimulador de Colônias de Granulócitos e Macrófagos/metabolismo , Humanos , Imuno-Histoquímica , Probabilidade , RNA Mensageiro/análise , Reação em Cadeia da Polimerase Via Transcriptase Reversa , Sensibilidade e Especificidade , Pele/citologia , Fator de Crescimento Transformador beta1/genética , Fator de Crescimento Transformador beta1/metabolismo
14.
J Ethnopharmacol ; 121(3): 466-71, 2009 Jan 30.
Artigo em Inglês | MEDLINE | ID: mdl-19071206

RESUMO

AIM OF THE STUDY: Vochysia tucanorum is an important medicinal plant used in the Cerrado of Brazil against gastric disorders and this study reveals the pharmacological action of this traditional medicine use. MATERIALS AND METHODS: The methanolic extract (E-MeOH) and buthanolic fraction (Fr-Bu) obtained from V. tucanorum were challenged by different necrotizing agents in rodents. NO-synthase inhibitor (L-NAME) and SH blocker (NEM) were used to evaluate the participation of cytoprotective factors in E-MeOH and Fr-Bu gastroprotection. Antiulcerogenic action of V. tucanorum was evaluated in rats and mice at doses 250, 500 or 1000 mg/kg (E-MeOH) and 37.5, 75 or 150 mg/kg (Fr-Bu). RESULTS: Both E-MeOH and Fr-Bu present elevated gastroprotective action in all in vivo experimental models, without signs of acute toxicity. The mechanisms involved in the gastroprotective action of E-MeOH and Fr-Bu are related to the antioxidant activity and protection to gastric mucosa NO levels. Phytochemical investigations of Fr-Bu identified different pentacyclic triterpenoids such as betulinic acid, erythrodiol, epi-betulinic acid and mixtures of ursolic acid and oleanolic acid derivatives as the major constituents. The presence of such triterpenoids in Fr-Bu is probably related to the potent gastroprotective action of this medicinal plant species. CONCLUSION: Effectiveness in gastroprotection and the absence of acute toxicity indicate this species as a promising herbal drug that is in accordance with ethnopharmacological use against gastric disorders.


Assuntos
Antiulcerosos/farmacologia , Antioxidantes/farmacologia , Magnoliopsida , Fitoterapia , Extratos Vegetais/farmacologia , Úlcera Gástrica/prevenção & controle , Animais , Antiulcerosos/efeitos adversos , Antiulcerosos/uso terapêutico , Antioxidantes/efeitos adversos , Antioxidantes/uso terapêutico , Brasil , Etilmaleimida/farmacologia , Mucosa Gástrica/efeitos dos fármacos , Peroxidação de Lipídeos/efeitos dos fármacos , Masculino , Camundongos , NG-Nitroarginina Metil Éster/farmacologia , Óxido Nítrico/metabolismo , Extratos Vegetais/efeitos adversos , Extratos Vegetais/uso terapêutico , Folhas de Planta , Ratos , Ratos Wistar , Úlcera Gástrica/induzido quimicamente , Triterpenos/efeitos adversos , Triterpenos/farmacologia , Triterpenos/uso terapêutico
15.
Photodermatol Photoimmunol Photomed ; 24(6): 308-13, 2008 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-19000188

RESUMO

BACKGROUND: Exposure to ultraviolet (UV) radiation induces generation of reactive oxygen species, production of proinflammatory cytokines and melanocyte-stimulating hormone (MSH) as well as increase in tyrosinase activity. The potential photoprotective effects of Coccoloba uvifera extract (CUE) were evaluated in UV-stimulated melanocytes. METHODS: Human epidermal melanocytes were used as an in vitro model to evaluate the effects of CUE on the production interleukin-1alpha (IL-1alpha), tumor necrosis factor alpha (TNF-alpha), and alpha-MSH under basal and UV-stimulated conditions. Antioxidant and anti-tyrosinase activities were also evaluated in membrane lipid peroxidation and mushroom tyrosinase assay, respectively. RESULTS: Coccoloba uvifera L. showed antioxidant and anti-tyrosinase activities and also inhibited the production of IL-1alpha, TNF-alpha and alpha-MSH in melanocytes subjected to UV radiation (P<0.01). Moreover, CUE inhibited the activity of tyrosine kinase in cell culture under basal and UV radiation conditions (P<0.001), corroborating the findings of the mushroom tyrosinase assay. CONCLUSION: This study supports the photoprotective potential of CUE.


Assuntos
Melanócitos/efeitos dos fármacos , Polygonaceae/química , Antioxidantes/farmacologia , Células Cultivadas , Inibidores Enzimáticos/farmacologia , Humanos , Hormônios Estimuladores de Melanócitos/metabolismo , Melanócitos/metabolismo , Monofenol Mono-Oxigenase/antagonistas & inibidores , Monofenol Mono-Oxigenase/metabolismo , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Proteínas Tirosina Quinases/metabolismo , Fator de Necrose Tumoral alfa/imunologia
16.
Ann Bot ; 102(5): 699-711, 2008 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-18765441

RESUMO

BACKGROUND AND AIMS: Bignoniaceae is a Neotropical family with >100 genera, only two of which, Jacaranda and Digomphia, have a developed staminode. Jacaranda oxyphylla, whose flowers possess a conspicuous glandular staminode, is a zoophilous cerrado species. Here, the composition of the secretion of the glandular trichome and the influence of the staminode on the pollination biology and reproductive success of J. oxyphylla were studied. METHODS: The floral morphology, pollen viability, stigma receptivity, nectar volume and nectar concentration were studied. Compatibility system experiments were performed and floral visitors were observed and identified. Experiments comparing the effect of staminode presence and absence on pollen removal and pollen deposition efficiency were conducted in open-pollinated flowers. Histochemistry, thin-layer chromatography (TLC) and gas chromatography coupled to flame ionization detection (GC-FID) analyses were performed to determine the main chemical components of the staminode's glandular trichome secretion. KEY RESULTS: Flower anthesis lasted 2 d and, despite the low frequency of flower visitation, pollination seemed to be effected mainly by medium-sized Eulaema nigrita and Bombus morio bees, by the small bee Exomalopsis fulvofasciata and occasionally by hummingbirds. Small bees belonging to the genera Ceratina, Augochlora and Trigona were frequent visitors, collecting pollen. Jacaranda oxyphylla is predominantly allogamous. Staminode removal resulted in fewer pollen grains deposited on stigmas but did not affect total pollen removal. The secretion of capitate glandular trichome occurs continually; the main chemical compounds detected histochemically were phenolic and terpenoid (essential oils and resins). Monoterpene cineole, pentacyclic triterpenes and steroids were identified by TLC and GC-FID. CONCLUSIONS: The staminode of J. oxyphyllla is multifunctional and its importance for female reproductive success was attributed mainly to the secretion produced by capitate glandular trichomes. This secretion is involved in complex chemical interactions with pollinating bees, including the solitary bees Euglossini. These bees are common pollinators of various species of Jacaranda.


Assuntos
Bignoniaceae/fisiologia , Pólen/fisiologia , Polinização/fisiologia , Animais , Bignoniaceae/anatomia & histologia , Bignoniaceae/citologia , Bignoniaceae/ultraestrutura , Brasil , Ecologia , Frutas/fisiologia , Insetos/fisiologia , Extratos Vegetais/metabolismo , Pólen/anatomia & histologia , Pólen/citologia , Pólen/ultraestrutura , Reprodução , Simbiose/fisiologia , Terpenos/metabolismo
17.
J Ethnopharmacol ; 119(1): 94-8, 2008 Sep 02.
Artigo em Inglês | MEDLINE | ID: mdl-18588967

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Cordia verbenacea is a medicinal plant popularly used in Brazil as anti-inflammatory, antiulcer and anti-rheumatic agent without detailed pharmacological and toxicological studies. AIM OF THE STUDY: The study was aimed to investigate the effects of Cordia verbenacea in antiulcer, analgesic and antioxidant assays, as well as to evaluate its toxic effects and phytochemical profile. MATERIAL AND METHODS: Antiulcer activity of plant extract was evaluated using ethanol/HCl, ethanol and piroxican-induced gastric lesions methods. The pH, volume and total acid of gastric juice were determined by pylorus-ligated assay. Analgesic activity was evaluated by writhing, tail-flick and hot-plate tests. Antioxidant activity was determined by in vitro lipoperoxidation assay. Acute toxicity and number of deaths were evaluated by Hippocratic screening. RESULTS: The ethanol leaf extract shows a potent antiulcer activity in the ethanol/HCl and absolute ethanol-induced gastric lesions. The IC(50) value of plant extract on the lipid peroxidation was 76.11mug/ml. Preliminary phytochemical tests were positive for flavonoids, steroids, saponins, fixed acids, alkaloids and phenols. In the analgesic models the extract did not present any activity. CONCLUSIONS: Cordial verbenaceae showed a potent antiulcer activity at the dose of 125mg/kg and this effect may be associated with an improvement in stomach antioxidant mechanisms.


Assuntos
Analgésicos/administração & dosagem , Antiulcerosos/administração & dosagem , Cordia/química , Extratos Vegetais/administração & dosagem , Analgésicos/isolamento & purificação , Analgésicos/toxicidade , Animais , Antiulcerosos/isolamento & purificação , Antiulcerosos/toxicidade , Antioxidantes/administração & dosagem , Antioxidantes/isolamento & purificação , Antioxidantes/toxicidade , Brasil , Modelos Animais de Doenças , Relação Dose-Resposta a Droga , Feminino , Suco Gástrico/química , Suco Gástrico/efeitos dos fármacos , Concentração Inibidora 50 , Peroxidação de Lipídeos/efeitos dos fármacos , Masculino , Medicina Tradicional , Camundongos , Dor/tratamento farmacológico , Medição da Dor , Extratos Vegetais/toxicidade , Folhas de Planta , Úlcera Gástrica/tratamento farmacológico , Testes de Toxicidade Aguda
18.
J Ethnopharmacol ; 117(1): 170-4, 2008 Apr 17.
Artigo em Inglês | MEDLINE | ID: mdl-18304768

RESUMO

AIM OF THE STUDY: Cissus sicyoides L. is a medicinal plant popularly known in Brazil against various diseases and the research interest in this plant is justifiable because of its potential medicinal value in stomachache and gastric ulcer. MATERIALS AND METHODS: The methanolic extract obtained from the leaves of Cissus sicyoides (Cc) was evaluated for the ability to protect the gastric mucosa against injuries caused by necrotizing agents (0.3 M HCl/60% EtOH, absolute ethanol, piroxicam and pylorus ligature) in rodents. We also evaluated microcirculation, antioxidant action and participation of NO (nitric oxide) and sulfhydryls (SH) groups in the Cc gastroprotective action. RESULTS: Administration of Cc significantly reduced gastric lesions induced by different ulcerogenic agents in rodents. This extract administered by oral route significantly increased gastric volume without exerting antisecretory effect. The Cc effect involved an increase of the defense mechanism of the gastrointestinal mucosa such as NO and SH groups that prevent and attenuate the ulcer process. The Cc also has antioxidant property against oxidative stress but does not modify microcirculation response in gastric mucosa. CONCLUSIONS: These results confirmed the traditional use of Cissus sicyoides for the treatment of gastric ulcer.


Assuntos
Cissus , Mucosa Gástrica/efeitos dos fármacos , Óxido Nítrico/fisiologia , Extratos Vegetais/farmacologia , Compostos de Sulfidrila/fisiologia , Animais , Mucosa Gástrica/irrigação sanguínea , Masculino , Camundongos , Microcirculação , Fitoterapia , Ratos , Ratos Wistar , Úlcera Gástrica/tratamento farmacológico
19.
Braz. j. microbiol ; 38(4): 717-719, Oct.-Dec. 2007. tab
Artigo em Inglês | LILACS | ID: lil-473487

RESUMO

The present study aimed at evaluating the in vitro antimicrobial activity of methanolic extracts of some medicinal plants against Escherichia coli, Salmonella Typhimurium, Staphylococcus aureus and Enterococcus sp. The methanolic extract of Caryophyllus aromaticus presented the highest anti-S. aureus activity and was effective against all bacterial strains tested.


Avaliou-se a atividade antimicrobiana in vitro de extratos metanólicos de algumas plantas medicinais frente a Escherichia coli, Salmonella Typhimurium, Staphylococcus aureus e Enterococcus sp. O extrato metanólico de Caryophyllus aromaticus foi o mais eficaz para todas as bactérias testadas e apresentou a melhor atividade anti-S. aureus.

20.
Mem Inst Oswaldo Cruz ; 101(4): 387-90, 2006 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-16951808

RESUMO

Searches for substances with antimicrobial activity are frequent, and medicinal plants have been considered interesting by some researchers since they are frequently used in popular medicine as remedies for many infectious diseases. The aim of this study was to verify the synergism between 13 antimicrobial drugs and 8 plant extracts--"guaco" (Mikania glomerata), guava (Psidium guajava), clove (Syzygium aromaticum), garlic (Allium sativum), lemongrass (Cymbopogon citratus), ginger (Zingiber officinale), "carqueja" (Baccharis trimera), and mint (Mentha piperita)--against Staphylococcus aureus strains, and for this purpose, the disk method was the antimicrobial susceptibility test performed. Petri dishes were prepared with or without dilution of plant extracts at sub-inhibitory concentrations in Mueller-Hinton Agar (MHA), and the inhibitory zones were recorded in millimeters. In vitro anti-Staphylococcus aureus activities of the extracts were confirmed, and synergism was verified for all the extracts; clove, guava, and lemongrass presented the highest synergism rate with antimicrobial drugs, while ginger and garlic showed limited synergistic capacity.


Assuntos
Antibacterianos/farmacologia , Extratos Vegetais/farmacologia , Staphylococcus aureus/efeitos dos fármacos , Sinergismo Farmacológico , Humanos , Recém-Nascido , Testes de Sensibilidade Microbiana , Infecções Estafilocócicas/microbiologia
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