RESUMO
ETHNOPHARMACOLOGICAL RELEVANCE: Cochlospermum regium is well-known as "Algodãozinho do cerrado" in folk Brazilian medicine, and is used to fight infections, inflammation and skin disorders. AIM OF THE STUDY: To identify the phytochemical constituents and the effects of the ethanolic extract of C. regium leaves (EECR) on inflammation and pain, and the effects of C. regium gel (GEECR) on wound healing. MATERIALS AND METHODS: Animals were treated with EECR (30-300 mg/kg) or GEECR (1.25 and 2.5%) and studies were conducted using carrageenan-induced pleurisy and paw edema tests, formalin-induced pain model, and excision wound model. RESULTS: In total, 25 compounds, including quercitrin, methyl gallate, and 1,2,3,4,6-pentagalloylhexose, with highest detectability were identified. The treatments reduced leukocyte migration, nitric oxide production, protein extravasation, edema, mechanical hyperalgesia, pain in both phases (neurogenic and inflammatory), cold hypersensitivity, and improved wound closure and tissue regeneration. CONCLUSIONS: The present findings established the anti-inflammatory, anti-nociceptive, and wound healing potential of the leaves of C. regium, confirming the potential therapeutic effect of this plant.
Assuntos
Bixaceae , Extratos Vegetais , Animais , Bixaceae/química , Extratos Vegetais/farmacologia , Extratos Vegetais/uso terapêutico , Extratos Vegetais/análise , Folhas de Planta/química , Etanol/química , Inflamação/tratamento farmacológico , Dor/tratamento farmacológico , Edema/induzido quimicamente , Edema/tratamento farmacológico , Carragenina , Analgésicos/efeitos adversosRESUMO
Coriolopsis rigida was isolated as an endophytic fungus from the medicinal plant Cochlospermum regium, and their production of secondary metabolites has not yet been investigated. Thus, the endophyte was cultivated on rice solid media to evaluate its ability to produce bioactive compounds and then the chloroform extract was obtained. Two phenolic compounds, tyrosol (1) and a new natural product p-hydroxyphenylacetamide (2), were isolated from the extract. The structures of the compounds were elucidated mainly by NMR. The extract showed potent antioxidant activity with an efficient concentration (EC50) value of 0.33 mg mL-1. Additionally, demonstrated allelopathic activity inhibited the seedling growth of Lactuca sativa L. and Raphanus sativus L. by 63% and 55%, respectively.
Assuntos
Plantas Medicinais , Polyporaceae , Fungos , Extratos Vegetais/farmacologiaRESUMO
Endophytic fungi are biodiverse and alternative source of bioactive compounds, due their different abilities of genetic expression and alteration of biosynthetic pathway when submitted to different culture conditions. The metabolic profile of three different crude extracts (A, B and C), obtained from the endophytic fungus Asordaria conoidea, were evaluated by HPLC and 1H NMR. Antioxidant and allelochemical activity were also evaluated. OSMAC diversified the metabolic production, mainly in the solid culture, where the tyrosol, 4-hydroxybenzaldehyde, 2-phenylacetamide and vanillic acid were isolated. The structures of the compounds were elucidated mainly by NMR. Extracts had antioxidant potential, however, only Extract C showed allelochemical activity, as inhibition of 65.5% in growth. This study confirms the efficiency of the OSMAC platform in producing extracts of different properties and compounds. Herein the A. conoidea was isolated for the first time as an endophytic microorganism.
Assuntos
Feromônios , Sordariales , Antioxidantes/farmacologia , Fungos , Compostos OrgânicosRESUMO
O domínio Cerrado apresenta inúmeras espécies vegetais que produzem naturalmente óleos essenciais que são incluídos em uma das várias classes de metabólitos secundários. Objetivou-se caracterizar a constituição química e avaliar as atividades antioxidante e antifúngica do óleo essencial das flores de Cochlospermum regium. As flores de C. regium foram coletadas em área de Cerrado, em Rio Verde/GO, Brasil. Para extração do óleo essencial,foram utilizadas 100 g de flores, e em seguida, foram submetidas à hidrodestilação em aparelho tipo Clevenger, e o rendimento de óleo essencial, determinado em porcentagem. Em seguida, o óleo essencial foi analisado quanto à composição por cromatografia gasosa com espectrometria de massas acoplada CG-EM, e determinado quanto ao potencial antioxidante na redução do DPPH e como antifúngico por difusão em ágar sobre o isolado de Sclerotinia sclerotiorum. O rendimento médio de óleo essencial foi igual a 0,10%. Foram identificados 32 compostos, destacando-se os majoritários cariofileno E 9,76%, γ-muuroleno 16,69% e biciclogermacreno 39,82%. A atividade antioxidante apresentou 100% de redução do radical DPPH, para as concentrações entre 50 a 2 mg mL-1, e reduções de 85,77 a 13,18% (EC50) para as concentrações 1 a 0,031 mg mL-1de óleo essencial. Conclui-se que o óleo essencial de C. regium apresentou baixo rendimento, no entanto, contém muitos compostos sesquiterpenos hidrocarbonados e oxigenados, apresentando-se como excepcional agente antioxidante e antifúngico natural no combate a Sclerotinia sclerotiorum. Sendo assim, o óleo essencial das flores de C. regium se apresenta como um forte candidato para novas pesquisas que poderão ser aplicadas nas áreas da saúde, agrícola e alimentícia.(AU)
The Cerrado domain has numerous plant species that naturally produce essential oils, that are include in one of several classes of secondary metabolites. The objective of this study was to characterize the chemical composition and to evaluate the antioxidant and antifungal activities of the essential oil from Cochlospermum regium flowers. The flowers from C. regium were collected in an area of Cerrado, in Rio Verde/GO, Brazil. To extract the essential oil, 100 g of flowers were used, and then they were subjected to hydrodistillation in Clevenger-type apparatus, and the essential oil yield, determined in percentage. Then, the essential oil was analyzed for composition by gas chromatography with coupled mass spectrometry GC-MS, and determined as to the antioxidant potential in reducing DPPH and, as antifungal by agar diffusion in the isolate from Sclerotinia sclerotiorum. The essential oil was analyzed by gas chromatograph associated with mass spectrometry CG-MS and its antioxidant potential was evaluated by the free radical sequestration technique DPPH. The average yield of essential oil was 0.10%. 32 compounds were identified, in especially majority caryophyllene E 9.76%, γ-muurolene 16.69% and bicyclogermacrene 39.82%. The antioxidant activity showed 100% reduction in the DPPH radical, for concentrations between 50 to 2 mg mL-1, and reductions of 85.77 to 13.18% (IC50) for concentrations 1 to 0.031 mg mL-1of the essential oil. It is concluded that the essential oil from C. regium showed low yield, however, it contains many hydrocarbon and oxygenated sesquiterpenes compounds, presenting itself as an exceptional natural antioxidant and...(AU)
Assuntos
Bixaceae , Antioxidantes , Antifúngicos , Óleos Voláteis/químicaRESUMO
O domínio Cerrado apresenta inúmeras espécies vegetais que produzem naturalmente óleos essenciais que são incluídos em uma das várias classes de metabólitos secundários. Objetivou-se caracterizar a constituição química e avaliar as atividades antioxidante e antifúngica do óleo essencial das flores de Cochlospermum regium. As flores de C. regium foram coletadas em área de Cerrado, em Rio Verde/GO, Brasil. Para extração do óleo essencial,foram utilizadas 100 g de flores, e em seguida, foram submetidas à hidrodestilação em aparelho tipo Clevenger, e o rendimento de óleo essencial, determinado em porcentagem. Em seguida, o óleo essencial foi analisado quanto à composição por cromatografia gasosa com espectrometria de massas acoplada CG-EM, e determinado quanto ao potencial antioxidante na redução do DPPH e como antifúngico por difusão em ágar sobre o isolado de Sclerotinia sclerotiorum. O rendimento médio de óleo essencial foi igual a 0,10%. Foram identificados 32 compostos, destacando-se os majoritários cariofileno E 9,76%, γ-muuroleno 16,69% e biciclogermacreno 39,82%. A atividade antioxidante apresentou 100% de redução do radical DPPH, para as concentrações entre 50 a 2 mg mL-1, e reduções de 85,77 a 13,18% (EC50) para as concentrações 1 a 0,031 mg mL-1de óleo essencial. Conclui-se que o óleo essencial de C. regium apresentou baixo rendimento, no entanto, contém muitos compostos sesquiterpenos hidrocarbonados e oxigenados, apresentando-se como excepcional agente antioxidante e antifúngico natural no combate a Sclerotinia sclerotiorum. Sendo assim, o óleo essencial das flores de C. regium se apresenta como um forte candidato para novas pesquisas que poderão ser aplicadas nas áreas da saúde, agrícola e alimentícia.
The Cerrado domain has numerous plant species that naturally produce essential oils, that are include in one of several classes of secondary metabolites. The objective of this study was to characterize the chemical composition and to evaluate the antioxidant and antifungal activities of the essential oil from Cochlospermum regium flowers. The flowers from C. regium were collected in an area of Cerrado, in Rio Verde/GO, Brazil. To extract the essential oil, 100 g of flowers were used, and then they were subjected to hydrodistillation in Clevenger-type apparatus, and the essential oil yield, determined in percentage. Then, the essential oil was analyzed for composition by gas chromatography with coupled mass spectrometry GC-MS, and determined as to the antioxidant potential in reducing DPPH and, as antifungal by agar diffusion in the isolate from Sclerotinia sclerotiorum. The essential oil was analyzed by gas chromatograph associated with mass spectrometry CG-MS and its antioxidant potential was evaluated by the free radical sequestration technique DPPH. The average yield of essential oil was 0.10%. 32 compounds were identified, in especially majority caryophyllene E 9.76%, γ-muurolene 16.69% and bicyclogermacrene 39.82%. The antioxidant activity showed 100% reduction in the DPPH radical, for concentrations between 50 to 2 mg mL-1, and reductions of 85.77 to 13.18% (IC50) for concentrations 1 to 0.031 mg mL-1of the essential oil. It is concluded that the essential oil from C. regium showed low yield, however, it contains many hydrocarbon and oxygenated sesquiterpenes compounds, presenting itself as an exceptional natural antioxidant and...
Assuntos
Antifúngicos , Antioxidantes , Bixaceae , Óleos Voláteis/químicaRESUMO
O objetivo do trabalho foi avaliar os óleos essenciais de Cochlospermum regium e suas atividades antioxidante e antifúngica frente à Sclerotinia sclerotiorum e Colletotrichum gloeosporioides. Foram coletados raízes e folhas em indivíduos de C. regiumem uma área de Cerrado, o material foi processado, pesado e a extração dos óleos se deram pelo método de hidrodestilação em Clevenger. Os óleos tiveram seu rendimento avaliado, bem como as atividades antioxidante e antifúngica frente à S. sclerotiorum e C. gloeosporioides. Os rendimentos foram de 0,168 e 0,301% para folhas e raízes; a atividade antioxidante apresentou 100% de redução do radical DPPH foi de 100% nas concentrações entre 50 a 30 μL mL-1e a inibição micelial de 14,2 e 60,1% na concentração de 100 μL mL-1para S. sclerotiorum e de 84,4 e 81,3% para C. gloeosporioides para os óleos das raízes e folhas, respectivamente.
The objective of this work was to evaluate the essential oils of Cochlospermum regium and its antioxidant and antifungal activities against Sclerotinia sclerotiorum and Colletotrichum gloeosporioides. Roots and leaves were collected in individuals of C. regiumin a Cerrado area, the material was processed, weighed and extraction of the oils were by the hydroventilation method in Clevenger. The oils had their evaluated yield, as well as the antioxidant and antifungal activities against S. sclerotiorum and C. gloeosporioides. Yields were 0.168 and 0.301% for leaves and roots; the antioxidant activity showed 100% reduction of the DPPH radical was 100% in the concentrations between 50 and 30 μL mL-1and the mycelial inhibition of 14.2 and 60.1% in the concentration of 100 μL mL-1for S. sclerotiorum and 84.4 and 81.3% for C. gloeosporioides for root and leaf oils, respectively.
Assuntos
Antifúngicos/administração & dosagem , Antifúngicos/uso terapêutico , Ascomicetos , Bixaceae/química , Colletotrichum , Óleos VoláteisRESUMO
O objetivo do trabalho foi avaliar os óleos essenciais de Cochlospermum regium e suas atividades antioxidante e antifúngica frente à Sclerotinia sclerotiorum e Colletotrichum gloeosporioides. Foram coletados raízes e folhas em indivíduos de C. regiumem uma área de Cerrado, o material foi processado, pesado e a extração dos óleos se deram pelo método de hidrodestilação em Clevenger. Os óleos tiveram seu rendimento avaliado, bem como as atividades antioxidante e antifúngica frente à S. sclerotiorum e C. gloeosporioides. Os rendimentos foram de 0,168 e 0,301% para folhas e raízes; a atividade antioxidante apresentou 100% de redução do radical DPPH foi de 100% nas concentrações entre 50 a 30 μL mL-1e a inibição micelial de 14,2 e 60,1% na concentração de 100 μL mL-1para S. sclerotiorum e de 84,4 e 81,3% para C. gloeosporioides para os óleos das raízes e folhas, respectivamente.(AU)
The objective of this work was to evaluate the essential oils of Cochlospermum regium and its antioxidant and antifungal activities against Sclerotinia sclerotiorum and Colletotrichum gloeosporioides. Roots and leaves were collected in individuals of C. regiumin a Cerrado area, the material was processed, weighed and extraction of the oils were by the hydroventilation method in Clevenger. The oils had their evaluated yield, as well as the antioxidant and antifungal activities against S. sclerotiorum and C. gloeosporioides. Yields were 0.168 and 0.301% for leaves and roots; the antioxidant activity showed 100% reduction of the DPPH radical was 100% in the concentrations between 50 and 30 μL mL-1and the mycelial inhibition of 14.2 and 60.1% in the concentration of 100 μL mL-1for S. sclerotiorum and 84.4 and 81.3% for C. gloeosporioides for root and leaf oils, respectively.(AU)
Assuntos
Óleos Voláteis , Bixaceae/química , Ascomicetos , Colletotrichum , Antifúngicos/administração & dosagem , Antifúngicos/uso terapêuticoRESUMO
The main physiological consequence of diabetes mellitus is chronic hyperglycemia. This condition is related to the formation of free radicals including advanced glycation end products (AGES) and to an increase in inflammatory processes. Cochlospermum regium (Schrank) Pilg., part of the Bixaceae family, is a cerrado plant known for its anti-inflammatory effects. The objectives of this study were to analyze the constituent compounds of C. regium roots and to evaluate the antioxidant, antiglycation, antidiabetic, and anticholinergic effects of its hydromethanolic extract through in vitro and in vivo experimental models. The presence of phenols, flavonoids, condensed tannins, and flavonols was analyzed by liquid chromatography - photodiode array (LC/PDA) analysis. Whereas antioxidant activity was investigated via DPPH, ABTS, ß-carotene/linoleic acid, and malondialdehyde colorimetric assays. Inhibition of AGEs was examined via a bovine serum albumin system whose glycosylating agent was glucose. Antidiabetic potential was examined in normoglycemic Wistar rats that received glucose overload, in alloxan-induced diabetic rats, and in rats that received a hyperglycemic diet. Disaccharidase inhibition was assessed using in vitro and in vivo methods, as was acetylcholinesterase (AChE) inhibition in brain structures. The hydromethanolic extract (CRHE) possessed a high concentration of phenolic compounds and showed antioxidant effects. The LC-DAD results revealed that CRHE contained a high concentration of phenolic acids and the majority was gallic acid. Treatment with CRHE caused significant inhibition of AGE formation. The oral glucose tolerance test (OGTT) in normoglycemic animals showed a reduction in blood glucose levels after treatment with 100 mg/kg CHRE, accompanied by an increase in hepatic glycogen content. There was also a significant reduction in the fasting glucose levels of alloxan-induced diabetic animals after 7 days of treatment with daily doses of 100 mg/kg. After 14 weeks of hyperglycemic diet, the last four or which were combined with 100 mg/kg CRHE treatment, there was a decrease in blood triglyceride levels. There was also a statistically significant decrease in the enzymatic activity of maltase, lactase and sucrase. The results demonstrate that oral administration of 30 and 100 mg/kg CRHE inhibited AChE activity in different brain structures. Thus, the extract of C. regium showed promising antioxidant, antiglycation, and antidiabetic effects that may be related to its high phenolic content.
Assuntos
Antioxidantes/farmacologia , Bixaceae/química , Inibidores da Colinesterase/farmacologia , Diabetes Mellitus Experimental/tratamento farmacológico , Hipoglicemiantes/farmacologia , Extratos Vegetais/farmacologia , Raízes de Plantas/química , Aloxano/farmacologia , Animais , Glicemia/efeitos dos fármacos , Diabetes Mellitus Experimental/induzido quimicamente , Diabetes Mellitus Experimental/metabolismo , Flavonoides/farmacologia , Teste de Tolerância a Glucose/métodos , Glicogênio/metabolismo , Hiperglicemia/tratamento farmacológico , Hiperglicemia/metabolismo , Masculino , Fenóis/química , Ratos , Ratos WistarRESUMO
ETHNOPHARMACOLOGICAL RELEVANCE: Cochlospermum regium (Bixaceae) is a native shrub of Brazil and its xylopodium (infusion/decoction) is being used for the treatment of gastritis, ulcers, arthritis, intestinal infections, gynaecological infections, skin diseases, among others. The aim of the present study was to evaluate the gastroprotective/antiulcer activity and the mechanism of action of hydroethanolic extract of C. regium xylopodium (HECr), using in vitro and in vivo models. Additionally, phytochemical constituents were identified by high-performance liquid chromatography (HPLC). MATERIALS AND METHODS: C. regium xylopodium was macerated with ethanol/water to obtain the HECr. The phytochemical characterisation was carried out by HPLC. The antiulcer efficacy of HECr (25, 100 and 400â¯mg/kg, p.o.) was evaluated using acute acidified ethanol (HCl/EtOH), piroxicam and water immersion-induced experimental ulcer models. Chronic gastric ulcer healing activity of HECr was evaluated through acetic acid (99.8%) - induced model. Histological analysis and myeloperoxidase (MPO), glutathione (GSH), catalase (CAT) activities were also evaluated in chronic ulcer induced gastric tissues. The plausible mode of action of the HECr was assessed by estimation of gastric wall mucus production and the role of gastric secretion in pylorus ligature. The animals were also pre-treated with various inhibitors which includes indomethacin (10â¯mg/kg, p.o.) a selective inhibitor of cyclooxygenase, L-NAME (10â¯mg/kg, i.p.), an inhibitor of nitric oxide synthase, glibenclamide, a ATP-sensitive potassium channels (K+ATP) blocker (5â¯mg/kg, p.o.) or yohimbine (2â¯mg/kg, i.p.), an α2-adrenergic receptor antagonist. In vitro, Helicobacter pylori action was done by broth microdilution method. RESULTS: The HPLC analysis data revealed the presence of gallic acid, rutin, myricetin, morin and kaempferol. HECr promoted protective effect against acute ulcers induced by HCl/EtOH with inhibitions of 47.52% (pâ¯<â¯0.01) and 62.69% (pâ¯<â¯0.001) at 100 and 400â¯mg/kg, and in piroxicam by 34.11% (pâ¯<â¯0.05), 49.14% (pâ¯<â¯0.01) and 61.34% (pâ¯<â¯0.001), at 25, 100 or 400â¯mg/kg, respectively, and in water restraint stress by 78.26% inhibition, pâ¯<â¯0.001, at the dose of 400â¯mg/kg when compared to the vehicle control group respectively. In the chronic gastric ulcer model, HECr (25, 100 and 400â¯mg/kg p.o.) significantly (pâ¯<â¯0.001) decreased the injured area by 58.80%, 77.87% and 71.10% respectively. Histological examination indicated that oral treatment of HECr promoted healing of gastric lesions by regenerating gastric mucosa layer with less inflammatory cells. HECr augmented the GSH, CAT activities and reduced MPO level. The pre-treatment with HECr increased the gastric wall mucus production. It also significantly altered the gastric secretion parameters by causing the reduction in the gastric juice volume, elevated the pH level and reduced the total acidity at all doses tested when compared with the vehicle group. HECr at the most active dose (100â¯mg/kg) reversed completely the reduction of PGs, NO production, closure of K+ATP- channels and α2-adrenoreceptor blockage - induced damages. In microdilution assay, the HECr showed good anti-Helicobacter pylori effect with MICâ¯=â¯100⯵g/mL. CONCLUSION: The HECr presented preventive and curative effects in the experimental gastric ulcer models, besides good anti-Helicobacter pylori activity, which supports the traditional medicinal use of the xylopodium of this plant for gastrointestinal diseases. The underlying mechanisms of this antiulcerogenic/antiulcer action involve, at least, augmentation of mucus production, inhibition of gastric secretion, stimulation of PGs and NO synthesis. And that it involves activation of K+ATP channels and α-2-adrenergic receptors, in addition to an antioxidant activity, probably due to the presence of gallic acid and flavonoids in HECr.
Assuntos
Antiulcerosos/uso terapêutico , Bixaceae , Extratos Vegetais/uso terapêutico , Úlcera Gástrica/tratamento farmacológico , Ácido Acético , Animais , Anti-Inflamatórios não Esteroides , Antiulcerosos/farmacologia , Modelos Animais de Doenças , Etanol , Feminino , Mucosa Gástrica/efeitos dos fármacos , Mucosa Gástrica/metabolismo , Mucosa Gástrica/patologia , Helicobacter pylori/efeitos dos fármacos , Masculino , Camundongos , Fitoterapia , Piroxicam , Extratos Vegetais/farmacologia , Ratos Wistar , Úlcera Gástrica/induzido quimicamente , Úlcera Gástrica/metabolismo , Úlcera Gástrica/patologia , Estresse FisiológicoRESUMO
Essential oil from Cochlospermum regium (Schrank) Pilg. leaves (CR-EO) has been extracted by hydrodistillation; we analysed the CR-EO by gas chromatography coupled with mass spectrometry. We also conducted histochemical analysis on cross-sections of the central vein of young and adult leaves. A total of 32 compounds were qualitatively and quantitatively analysed, which represented 94.87% of the total CR-EO oil content. The CR-EO basically consisted of sesquiterpenes (96.87%); its main component was ß-copaen-4-α-ol (18.73%), followed by viridiflorol (12.67%). The histochemical analyses identified the main classes of compounds present in both young and adult leaves.