RESUMO
ETHNOPHARMACOLOGICAL RELEVANCE: Sesquiterpene lactones are organic compounds derived mainly from plants that exhibit anti-inflammatory and antitumor activities being one of the key mechanism of action of NF-kB pathway and synthesis of cytokines such as IL-1 and TNF- α. AIM OF THE STUDY: The overall objective of the present study was to evaluate the anti-inflammatory action of a sesquiterpene lactone diacethylpiptocarphol (DPC) from Vernonia scorpioides (Lam.) Pers. and parthenolide (PTH) in Balb-c mice with DSS-induced colitis. MATERIALS AND METHODS: The anti-inflammatory effects of Intraperitonial administration of DPC (5â¯mg/kg/day) were evaluated in Balb/c mice with DSS-induced colitis, and further the body weight measurement, TNF-α and TGF-ß level was determined. RESULTS: After intraperitoneal treatment for one week, DSS-induced colitis was significantly reduced in mice treated with either of both sesquiterpenes lactones, as witnessed by reduced cellular infiltration, tissue damage, TNF-α production, and enhanced production of TGF-ß. CONCLUSIONS: Sesquiterpene lactone DPC, isolated from Vernonia scorpioides showed anti-inflammatory activity, in this experimental model of colitis the sesquiterpene lactones DPC and PTH exhibit equal anti-inflammatory activity.
Assuntos
Anti-Inflamatórios/uso terapêutico , Colite/tratamento farmacológico , Lactonas/uso terapêutico , Sesquiterpenos/uso terapêutico , Vernonia , Animais , Colite/sangue , Colite/induzido quimicamente , Colite/patologia , Colo/efeitos dos fármacos , Colo/patologia , Sulfato de Dextrana , Flores , Injeções Intraperitoneais , Masculino , Camundongos Endogâmicos BALB C , Folhas de Planta , Fator de Crescimento Transformador beta/sangue , Fator de Necrose Tumoral alfa/sangueRESUMO
Leaves of the pantropical genus Bauhinia (Fabaceae) are known popularly as cow's foot, due to their unique characteristic bilobed aspect. The species Bauhinia forficata (Brazilian Orchid-tree) is widely used in folk medicine as an antidiabetic. The present work investigates the hypoglycemic activity of the dried extracts of Bauhinia forficata leaves in vivo, as well as the influence of the drying and granulation processes on this activity. The fluid extract was dried to generate oven-dried (ODE), spray-dried (SDE) and wet granulation (WGE) extracts, with the aid of colloidal silicon dioxide and/or cellulose:lactose mixture. The dried extracts were characterized by spectrophotometric, chromatographic and photo microscopy image analysis. 200 mg/kg body wt., p.o. of each dried product were administered orally to male Wistar rats over 7 days old, for biomonitoring of the hypoglycemic activity profile. The effect of the extracts was studied in STZ-induced diabetic rats. After 7 days of treatment, fasting glucose was determined, and the livers were removed, dried on tissue paper, weighed, and stored at -20 degrees C to estimate hepatic glycogen. Our results show that spray-drying or oven-drying processes applied to B. forficata extracts did not significantly alter its flavonoid profile or its hypoglycemic activity. Indeed, the dried extracts of B. forficata act differently from glibenclamide. Despite the lower active content in WGE, because of the higher concentration of adjuvants, the use of the granulation process improved the manufacturing properties of the ODE, making this material more appropriate for use in tablets or capsules.
Assuntos
Bauhinia/química , Glicemia/metabolismo , Diabetes Mellitus Experimental/tratamento farmacológico , Hipoglicemiantes/uso terapêutico , Fitoterapia , Extratos Vegetais/uso terapêutico , Animais , Química Farmacêutica , Dessecação , Formas de Dosagem , Flavonoides/análise , Glibureto/farmacologia , Hipoglicemiantes/isolamento & purificação , Hipoglicemiantes/farmacologia , Masculino , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Folhas de Planta , Ratos , Ratos WistarRESUMO
Vernonia scorpioides has been widely used in Brazil to treat skin problems and chronic wounds, such as ulcers of the lower limbs and diabetic lesions. In the present study, we investigated the effect of a dichloromethane (DCM) fraction of V. scorpioides leaf extract on Ehrlich ascitic and solid tumor-bearing mice. The animals were treated once a day with the DCM fraction at a concentration of 5 mg/kg, administered ip during and after the development of the tumor. The lifespan, weight, number and type of leukocytes, number of tumor cells, volume of solid and ascitic tumors were measured. The development of the tumor with pre-treated tumor cells in vitro with the DCM fraction (5 mg/kg) was analyzed and the animals were sacrificed after 7 days. The DCM fraction (5 mg/kg) totally inhibited tumor development when in direct contact with tumor cells, and also ascitic tumor development with in vitro treatment or when administered ip, in loco (after 7 days). Animals treated with the DCM fraction increased their lifespan ca. 2 weeks and maintained their body weight for 30 days. When applied immediately after the inoculation of the tumor cells in vivo, it totally abolished tumor development, with tumor development only decreasing when treatment was started 3 days after the tumor challenge. These data suggest an antineoplastic activity of the fraction. Oral or ip administration of DCM fraction (5 mg/kg) for 7 days did not reduce the solid tumor volume. The cytotoxic activity described here differs from the conventional immune suppressing profile of standard chemotherapy because it increases neutrophil influx to the peritoneal cavity. These results show that, besides exhibiting a tumoricidal activity, the DCM fraction also exhibits inflammatory activity.
Assuntos
Antineoplásicos Fitogênicos/uso terapêutico , Carcinoma de Ehrlich/tratamento farmacológico , Cloreto de Metileno/uso terapêutico , Folhas de Planta/química , Vernonia/química , Animais , Antineoplásicos Fitogênicos/isolamento & purificação , Ensaios de Seleção de Medicamentos Antitumorais , Injeções Intraperitoneais , Masculino , Cloreto de Metileno/isolamento & purificação , Camundongos , Extratos Vegetais/uso terapêuticoRESUMO
Vernonia scorpioides has been widely used in Brazil to treat skin problems and chronic wounds, such as ulcers of the lower limbs and diabetic lesions. In the present study, we investigated the effect of a dichloromethane (DCM) fraction of V. scorpioides leaf extract on Ehrlich ascitic and solid tumor-bearing mice. The animals were treated once a day with the DCM fraction at a concentration of 5 mg/kg, administered ip during and after the development of the tumor. The lifespan, weight, number and type of leukocytes, number of tumor cells, volume of solid and ascitic tumors were measured. The development of the tumor with pre-treated tumor cells in vitro with the DCM fraction (5 mg/kg) was analyzed and the animals were sacrificed after 7 days. The DCM fraction (5 mg/kg) totally inhibited tumor development when in direct contact with tumor cells, and also ascitic tumor development with in vitro treatment or when administered ip, in loco (after 7 days). Animals treated with the DCM fraction increased their lifespan ca. 2 weeks and maintained their body weight for 30 days. When applied immediately after the inoculation of the tumor cells in vivo, it totally abolished tumor development, with tumor development only decreasing when treatment was started 3 days after the tumor challenge. These data suggest an antineoplastic activity of the fraction. Oral or ip administration of DCM fraction (5 mg/kg) for 7 days did not reduce the solid tumor volume. The cytotoxic activity described here differs from the conventional immune suppressing profile of standard chemotherapy because it increases neutrophil influx to the peritoneal cavity. These results show that, besides exhibiting a tumoricidal activity, the DCM fraction also exhibits inflammatory activity.
Assuntos
Animais , Masculino , Camundongos , Antineoplásicos Fitogênicos/farmacologia , Carcinoma de Ehrlich/tratamento farmacológico , Cloreto de Metileno/farmacologia , Folhas de Planta/química , Vernonia/química , Antineoplásicos Fitogênicos/isolamento & purificação , Ensaios de Seleção de Medicamentos Antitumorais , Injeções Intraperitoneais , Cloreto de Metileno/isolamento & purificação , Extratos Vegetais/farmacologiaRESUMO
Vernonia scorpioides is traditionally widely used in Brazil to treat skin problems, including healing of chronic wounds, such as ulcers of the lower limbs and diabetic wounds. This work investigated the healing process on excisional wounds in the skin of mice, treated daily with an ointment containing 20 percent of the ethanol extract of the leaves of Vernonia scorpioides, compared with the control. A skin wound area of about 4 mm was excised on anaesthetised mice, and after 3, 7 and 14 days of treatment, the lesions were surgically removed and histologically processed. Wound healing activity was determined by the percentage of necrosis area, mononuclear inflammatory cells, fibroblasts and blood vessels. In the acute phase of healing, treatment with piracá extract enlarged the lesions and intensified the necrosis area, compared with the control group. However, the treatment did not inhibit either the recruitment and stimulation of inflammatory cells or the repair process. The results obtained indicate a harmful action of the extract immediately after tissue excision, demonstrated by the increased area of necrotic tissue, clotting and exudates formed in the treated groups. However, the extract did not inhibit the formation of granulation tissue.
RESUMO
An infusion of Campomanesia xanthocarpa Berg. (Myrtaceae) leaves (Guabiroba) and the herb Cuphea carthagenensis (Jacq.) J.F. Macbr. (Lythraceae) (Sete-sangrias) is traditionally used in the South of Brazil to treat high levels of cholesterol and triglycerides. The effects of the aqueous extracts of these herbs were investigated in rats fed on a high calorie diet. Chronic treatment with the Guabiroba aqueous extract induced a significant reduction in weight gain in the rats, compared to the control group. Also, biochemical analysis showed that this treatment reduced the glycemia, while no effects on lipidic levels were observed. The biochemical analysis of the animals treated with Sete-sangrias aqueous extract showed no effect on glucose and triglyceride levels, while chronic treatment with the Sete-sangrias aqueous extract induced a significant reduction in plasma cholesterol in rats.
Assuntos
Cuphea , Hipolipemiantes/farmacologia , Myrtaceae , Fitoterapia , Extratos Vegetais/farmacologia , Animais , Glicemia/efeitos dos fármacos , Colesterol/sangue , Hipolipemiantes/administração & dosagem , Hipolipemiantes/uso terapêutico , Masculino , Obesidade/prevenção & controle , Extratos Vegetais/administração & dosagem , Extratos Vegetais/uso terapêutico , Folhas de Planta , Ratos , Ratos Wistar , Triglicerídeos/sangue , Redução de PesoRESUMO
The ethanolic leaves extract of Vernonia scorpioides was investigated for its wound healing activity in guinea pigs. Administered once a day for 30 days, 200 mg of a hydrogel containing 50% of extract did not accelerate the closure time, but improved regeneration and organization of the new tissue.
Assuntos
Células Sanguíneas/efeitos dos fármacos , Fitoterapia , Extratos Vegetais/farmacologia , Vernonia , Cicatrização/efeitos dos fármacos , Administração Cutânea , Animais , Esquema de Medicação , Feminino , Cobaias , Hidrogel de Polietilenoglicol-Dimetacrilato , Masculino , Extratos Vegetais/administração & dosagem , Extratos Vegetais/uso terapêutico , Folhas de PlantaRESUMO
Investigation of the leaves of Raulinoa echinata Cowan (Rutaceae) has led to the isolation of several furofuran (2,6-diaryl-3,7-dioxabicyclo[3.3.0]-octane) lignan derivatives, namely (+)-sesamin, (+)-eudesmin, (+)-methylpiperitol (= kobusin), (+)-piperitol-gamma,gamma-dimethylallylether and the corresponding epi compounds: (+)-asarinin, (+)-epieudesmin, (+)-methylxanthoxylol, (+)-methylpluviatilol, (+)-xanthoxylol-gamma,gamma-dimethylallylether and (+)-pluviatilol-gamma,gamma-dimethylallylether. This is the first report of the chromatographic separation of the epimers (+)-methylxanthoxylol/(+)-methylpluviatilol and (+)-xanthoxylol-gamma,gamma-dimethylallylether/(+)-pluviatilol-gamma,gamma- dimethylallylether and of their NMR nOe difference studies.
Assuntos
Furanos/química , Lignanas/química , Lignanas/isolamento & purificação , Espectroscopia de Ressonância Magnética/métodos , Fenóis/química , Plantas/química , Dioxóis/análise , Dioxóis/química , Furanos/isolamento & purificação , Lignanas/análise , Fenóis/isolamento & purificaçãoRESUMO
Phytochemical survey of stems and leaves of the South Brazilian endemic Raulinoa echinata Cowan, Rutaceae led to the isolation of five limonoid derivatives: the widespread limonin, limonexic acid, kihadalactone B, a methoxylated limonexic acid derivative and a degraded limonoid structurally related to fraxinellone. The two latter compounds have been isolated for the first time. These compounds displayed weak inhibitory activity when assayed in vitro against trypomastigote forms of Trypanosoma cruzi. In this paper, the isolation, structure elucidation and bioactivity of these compounds are reported.
Assuntos
Flavonoides/química , Rosales/química , Triterpenos/química , Animais , Brasil , Flavonoides/isolamento & purificação , Flavonoides/farmacologia , Conformação Molecular , Estrutura Molecular , Rotação Ocular , Extratos Vegetais/química , Folhas de Planta/química , Caules de Planta/química , Triterpenos/isolamento & purificação , Triterpenos/farmacologia , Tripanossomicidas/química , Tripanossomicidas/isolamento & purificação , Tripanossomicidas/farmacologia , Trypanosoma cruzi/efeitos dos fármacosRESUMO
The hexane extract of the stems of Raulinoa echinata afforded the sesquiterpenes germacrene D (6), 1beta,6alpha-dihydroxy-4-(15)-eudesmene (4) and oplopanone (5); the triterpenes squalene, isomultiflorenol (7), isobauerenol (8) and friedelin (9); the protolimonoids melianone (2) and melianodiol (3); and the pyranocoumarin 3-(1'-1'-dimethylallyl)-lomatin (1), which has not been reported previously as a natural product; together with beta-sitosterol. The hexane extract and some of these compounds were assayed in vitro against trypomastigote forms of Trypanosoma cruzi. Brine shrimp lethality and antimicrobial activities of the crude extract and pure compounds were also evaluated.
Assuntos
Cumarínicos/química , Extratos Vegetais/química , Sesquiterpenos/química , Triterpenos/química , Tripanossomicidas/química , Trypanosoma cruzi/efeitos dos fármacos , Animais , Artemia , Bioensaio , Brasil , Cumarínicos/isolamento & purificação , Cumarínicos/farmacologia , Etnobotânica , Humanos , Extratos Vegetais/isolamento & purificação , Extratos Vegetais/farmacologia , Caules de Planta , Plantas Medicinais , Rosales/química , Sesquiterpenos/isolamento & purificação , Sesquiterpenos/farmacologia , Triterpenos/isolamento & purificação , Triterpenos/farmacologia , Tripanossomicidas/isolamento & purificação , Tripanossomicidas/farmacologia , Trypanosoma cruzi/parasitologiaRESUMO
We have isolated two phytoconstituents present in the B. forficata leaves, a medicinal plant employed in folk medicine specially for the treatment of diabetes. These compounds were isolated by column chromatography and identified as beta-sitosterol and kaempferol-3,7-dirhamnoside (kaempferitrin) by spectroscopical data and comparison with authentic samples. A comparative study with different parts of the plant indicated that the latter is present only in the leaves, suggesting that it might be useful for a suitable quality control of phytotherapeutics which contain this organ of B. forficata in its composition.
Assuntos
Fabaceae/química , Flavonoides/análise , Quempferóis , Plantas Medicinais/química , Sitosteroides/análise , Brasil , Diuréticos/análise , Diuréticos/química , Flavonoides/química , Hipolipemiantes/análise , Hipolipemiantes/química , Extratos Vegetais/química , Folhas de Planta/química , Sitosteroides/químicaRESUMO
In the present work we have investigated the analgesic activity of various extracts prepared from Aleurites moluccana leaves by using the writhing test in mice. The results showed that the hydroalcoholic extract and the hexane fraction exhibit potent antinociceptive action. We have also isolated and identified some chemical constituents from the hexane fraction. In addition, the nature of substances present in ethyl acetate and butanol fractions were evaluated by TLC. Such fractions revealed the presence of phenolic compounds. Chromatographic procedures carried out with hexane fraction revealed the presence of n-hentriacontane, α-amyrin, ß-amyrin, stigmasterol, ß-sitosterol and campesterol, which were identified by spectroscopic data and HRGC or HRGC/MS techniques. The compounds considerably inhibited acetic acid-induced abdominal constrictions, being more efficacious than aspirin and paracetamol. In addition, preliminary HPLC analysis indicated, using a UV detector, one main constituent in alcoholic extract.