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1.
Int J Biol Macromol ; 145: 668-681, 2020 Feb 15.
Artigo em Inglês | MEDLINE | ID: mdl-31883887

RESUMO

Marsypianthes chamaedrys (Lamiaceae) is a medicinal plant popularly used against envenomation by snakebite. Pharmacological studies have shown that extracts of M. chamaedrys have antiophidic, anti-inflammatory and anticoagulant properties, supporting the ethnopharmacological use. In this study, an aqueous extract of aerial parts of M. chamaedrys showed anticoagulant activity in the activated partial thromboplastin time assay (0.54 IU/mg). The bioassay-guided fractionation using ethanol precipitation and gel filtration chromatography on Sephadex G-50 and Sephadex G-25 resulted in a water-soluble fraction with increased anticoagulant activity (Fraction F2-A; 2.94 IU/mg). A positive correlation was found between the amount of uronic acids and the anticoagulant potential of the active samples. Chemical and spectroscopic analyses indicated that F2-A contained homogalacturonan, type I rhamnogalacturonan, type II arabinogalactan and α-glucan. UV and FT-IR spectra indicated the possible presence of ferulic acid. Pectic polysaccharides and type II arabinogalactans may be contributing to the anticoagulant activity of the aqueous extract of M. chamaedrys in the APTT assay.


Assuntos
Anticoagulantes/farmacologia , Lamiaceae/química , Extratos Vegetais/farmacologia , Polissacarídeos/química , Anticoagulantes/química , Coagulação Sanguínea/efeitos dos fármacos , Testes de Coagulação Sanguínea , Cromatografia Líquida de Alta Pressão , Humanos , Extração Líquido-Líquido , Espectroscopia de Ressonância Magnética , Compostos Fitoquímicos/análise , Compostos Fitoquímicos/química , Extratos Vegetais/química , Plantas Medicinais/química , Espectroscopia de Infravermelho com Transformada de Fourier
2.
J Leukoc Biol ; 83(4): 1038-48, 2008 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-18198209

RESUMO

Lymphopoiesis and myelopoiesis continuously generate mature cells from hematopoietic cell progenitors during the lifetime of the organism. The identification of new endogenous or exogenous substances that can act specifically on the differentiation of distinct cell lineages is of relevance and has potential therapeutical use. Kalanchoe brasiliensis (Kb) is a medicinal plant from the Crassulaceae family, used in folk medicine to treat inflammatory and infectious diseases. Here, we show that short-term treatment of naïve mice with Kb led to a strong and selective inhibition of lymphopoiesis, affecting B and T cell lineages without reduction of the myeloid lineage development. Similar effects were observed after treatment with the highly purified compound kalanchosine dimalate (KMC), obtained from Kb. Numbers of mature lymphocytes in secondary lymphoid organs were preserved in Kb(KMC)-treated mice. The effect of Kb(KMC) was not a result of secondary augmentation of plasma levels of endogenous corticoids; neither involves TNF-alpha, type-I IFN, or TLR2/TLR4 ligands, which have all been described as selective inhibitors of lymphopoiesis. Flow cytometry analysis of the phenotypes of T and B cell precursors indicate a blockade of maturation on IL-7-dependent, proliferative stages. In vitro, Kb(KMC) inhibited the IL-7-dependent proliferation of pre-B cells and does not induce massive apoptosis of B and T cell precursors. These results suggest that Kb(KMC) is selectively blocking lymphopoiesis through a mechanism that does not involve the previously characterized substances, possibly acting on the IL-7 signaling pathway, opening new perspectives for a potential therapeutic use of Kb-derived drugs.


Assuntos
Interleucina-7/antagonistas & inibidores , Linfopoese/fisiologia , Malatos/farmacologia , Animais , Anti-Inflamatórios/farmacologia , Divisão Celular/efeitos dos fármacos , Interleucina-7/farmacologia , Kalanchoe , Linfopoese/efeitos dos fármacos , Masculino , Camundongos , Camundongos Endogâmicos C57BL , Camundongos Knockout , Modelos Animais , Extratos Vegetais , Receptores Tipo I de Fatores de Necrose Tumoral/deficiência , Receptores Tipo I de Fatores de Necrose Tumoral/genética , Receptor 2 Toll-Like/deficiência , Receptor 2 Toll-Like/genética
3.
Int Immunopharmacol ; 8(6): 828-35, 2008 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-18442786

RESUMO

Kalanchoe brasiliensis (Kb) is a medicinal plant from the Crassulaceae family, used in folk medicine to treat inflammatory and infectious diseases. Here we show that short-term treatment of mice with a highly purified compound named kalanchosine dimalate (KMC), obtained from Kb, led to a strong and selective inhibition of B cell development in the bone marrow, without affecting the myeloid lineage development. Numbers of mature B lymphocytes in bone marrow or peripheral lymphoid organs were preserved in KMC treated mice. The inhibitory effect of KMC was acute and rapidly reverted with the interruption of the treatment. In vitro, KMC, inhibited the interleukin-7 dependent proliferation of B cell precursors and do not induce cell death. Also in vitro, the maturation of B cell precursors was not affected by KMC. KMC does not inhibit the proliferative response to IL-3 or IL-2. These results suggest that KMC is selectively affecting B cell lymphopoiesis, possibly acting on the IL-7 signaling pathway, opening new perspectives for a potential therapeutic usage of Kb derived drugs.


Assuntos
Linfócitos B/efeitos dos fármacos , Linfócitos B/imunologia , Interleucina-2/metabolismo , Interleucina-3/metabolismo , Interleucina-7/metabolismo , Linfopoese/efeitos dos fármacos , Malatos/farmacologia , Animais , Linfócitos B/fisiologia , Medula Óssea/efeitos dos fármacos , Medula Óssea/imunologia , Diferenciação Celular/efeitos dos fármacos , Linhagem da Célula , Proliferação de Células/efeitos dos fármacos , Células Cultivadas , Interleucina-2/imunologia , Interleucina-3/imunologia , Interleucina-7/imunologia , Kalanchoe , Linfopoese/imunologia , Malatos/isolamento & purificação , Masculino , Camundongos , Camundongos Endogâmicos C57BL
4.
Phytochemistry ; 67(18): 2071-7, 2006 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-16930642

RESUMO

The importance of flavonoids for the antileishmanial activity of Kalanchoe pinnata was previously demonstrated by the isolation of quercitrin, a potent antileishmanial flavonoid. In the present study, the aqueous leaf extract from the medicinal plant K. pinnata (Crassulaceae) afforded a kaempferol di-glycoside, named kapinnatoside, identified as kaempferol 3-O-alpha-L-arabinopyranosyl (1-->2) alpha-L-rhamnopyranoside (1). In addition, two unusual flavonol and flavone glycosides already reported, quercetin 3-O-alpha-L-arabinopyranosyl (1-->2) alpha-L-rhamnopyranoside (2) and 4',5-dihydroxy-3',8-dimethoxyflavone 7-O-beta-D-glucopyranoside (3), have been isolated. Their structures were determined via analyses of mono and bi-dimensional (1)H and (13)C NMR spectroscopic experiments and HR-MALDI mass spectra. Because of its restricted occurrence and its abundance in K. pinnata, flavonoid (2) may be a chemical marker for this plant species of high therapeutic potential. The three flavonoids were tested separately against Leishmania amazonenis amastigotes in comparison with quercitrin, quercetin and afzelin. The quercetin aglycone - type structure, as well as a rhamnosyl unit linked at C-3, seem to be important for antileishmanial activity.


Assuntos
Antiprotozoários/farmacologia , Flavonoides/química , Flavonoides/farmacologia , Kalanchoe/química , Leishmania/efeitos dos fármacos , Animais , Antiprotozoários/isolamento & purificação , Manosídeos/química , Manosídeos/farmacologia , Estrutura Molecular , Testes de Sensibilidade Parasitária , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Folhas de Planta/química , Proantocianidinas/química , Proantocianidinas/farmacologia , Quercetina/análogos & derivados , Quercetina/química , Quercetina/farmacologia
5.
J Ethnopharmacol ; 96(3): 563-8, 2005 Jan 15.
Artigo em Inglês | MEDLINE | ID: mdl-15619579

RESUMO

In the search for bioactive compounds, bioautography and ethanol precipitation of macromolecules (proteins, polysaccharides, etc.) of plant aqueous extracts were associated in an antifungal screening. Thus, the supernatants, precipitates (obtained by ethanol precipitation) and aqueous extracts were investigated of medicinal and fruit bearing plants used against skin diseases by the Brazilian population. The agar diffusion and broth dilution methods were used to assess the activity against three fungi: Candida albicans, Trichophyton rubrum and Cryptococcus neoformans. The results, evaluated by the diameter of the inhibition zone of fungal growth, indicate that six plant species, among the 16 investigated, showed significant antifungal activity. The minimal inhibitory concentration (MIC) was determined on plant extracts that showed high efficacy against the tested microorganisms. The most susceptible yeast was Trichophyton rubrum and the best antifungal activity was shown by Xanthosoma sagittifolium supernatant. The bioautography was performed only for the aqueous extracts and supernatants of those plants that showed antifungal activity against Candida albicans and Cryptococcus neoformans, using n-butanol/acetic acid/water (BAW) 8:1:1 to develop silica gel TLC plates. Clear inhibition zones were observed for aqueous extracts of Schinus molle (R(f) 0.89) and Schinus terebinthifolius (R(f) 0.80) against Candida albicans, as for supernatant of Anacardium occidentale (R(f) 0.31) against Cryptococcus neoformans. The separation of macromolecules from metabolites, as in the case of Anacardium occidentale, Solanum sp. and Xanthosoma sagittifolium, enhances antifungal activity. In other cases, the antifungal activity is destroyed, as observed for Momordica charantia, Schinus molle and Schinus terebinthifolius.


Assuntos
Antifúngicos/química , Antifúngicos/farmacologia , Etanol/química , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Plantas Medicinais/química , Animais , Brasil , Candida albicans/efeitos dos fármacos , Precipitação Química , Chlorocebus aethiops , Cromatografia em Camada Fina , Cryptococcus neoformans/efeitos dos fármacos , Avaliação Pré-Clínica de Medicamentos , Humanos , Testes de Sensibilidade Microbiana , Componentes Aéreos da Planta/química , Raízes de Plantas/química , Trichophyton/efeitos dos fármacos , Células Vero , Água/química
6.
J Ethnopharmacol ; 102(2): 217-20, 2005 Nov 14.
Artigo em Inglês | MEDLINE | ID: mdl-16054793

RESUMO

The fresh juice from leaves of Sedum dendroideum Moc & Sessé (Crassulaceae) is used in Brazilian traditional medicine for the treatment of gastric and inflammatory disorders. The present investigation was carried out to evaluate in vivo antinociceptive and anti-inflammatory activities of this plant material. The oral administration (0.1-1g/kg) of the lyophilized Sedum dendroideum juice (L J) caused a significant dose-related reduction of acetic acid-induced writhing response (ID(50)=631 mg/kg) and inhibited croton oil-induced ear oedema formation (66% inhibition at 1g/kg) in mice. In the formalin-induced nociception in mice, L J (1g/kg) only inhibited the second phase of nociception (46%). Phytochemical investigation revealed four known kaempferol glycosides, here, described at the first time for this species. These flavonoids probably explain the antinociceptive and anti-inflammatory effects of the fresh juice of Sedum dendroideum.


Assuntos
Analgésicos/farmacologia , Anti-Inflamatórios/farmacologia , Flavonoides/análise , Folhas de Planta/química , Sedum/química , Animais , Relação Dose-Resposta a Droga , Flavonoides/farmacologia , Masculino , Camundongos
7.
Int Immunopharmacol ; 2(7): 875-83, 2002 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-12188029

RESUMO

The immunomodulatory effect of juice obtained from leaves of Kalanchoe brasiliensis (Kb) on zymosan-induced inflammation was investigated. C57B110 mice received a subcutaneous injection of 150 microg zymosan in the footpad. After 7 days, there was an increase in footpad thickness from 176 +/- 4 to 236 +/- 9 x 10(-2) mm and in blood flow in the footpad area, monitored by 99mTc, from 98 +/- 4 to 694 +/- 59 counts per minute (cpm). Zymosan induced a severe infiltration of leukocytes into the articular tissues and a 13-fold increase in the adjacent popliteal lymph node (PLN) weight. Beginning 2 days after the injection, mice were treated daily for 5 days with different concentrations of lyophilised Kb juice dissolved in water. Treatment with 480 mg/kg/day reduced footpad thickness to 193 +/- 5 x 10(-2) mm, leukocyte infiltration and blood flow to 150 +/- 18 cpm in the footpad area. PLN weight in zymosan-injected mice decreased from 6.5 +/- 0.5 to 1.5 +/- 0.4 mg, similarly to the decrease after treatment with indomethacin (3 mg/kg/day). Flow cytometric analysis of lymph node cells showed an important reduction in B cell number in Kb-treated mice. Treatment over a period of 10 days was also effective at reducing zymosan-induced inflammation, even when started 7 days after injection. These data suggest anti-inflammatory and immunosuppressive effects of K. brasiliensis that may account for its popularity in folk medicine against rheumatic diseases.


Assuntos
Adjuvantes Imunológicos/uso terapêutico , Anti-Inflamatórios não Esteroides/uso terapêutico , Kalanchoe , Adjuvantes Imunológicos/isolamento & purificação , Adjuvantes Imunológicos/farmacologia , Animais , Anti-Inflamatórios não Esteroides/isolamento & purificação , Anti-Inflamatórios não Esteroides/farmacologia , Divisão Celular/efeitos dos fármacos , Divisão Celular/imunologia , Inflamação/induzido quimicamente , Inflamação/tratamento farmacológico , Inflamação/imunologia , Linfócitos/citologia , Linfócitos/efeitos dos fármacos , Masculino , Camundongos , Extratos Vegetais/isolamento & purificação , Extratos Vegetais/farmacologia , Extratos Vegetais/uso terapêutico , Baço/citologia , Baço/efeitos dos fármacos , Zimosan/toxicidade
8.
Photochem Photobiol ; 89(2): 391-9, 2013.
Artigo em Inglês | MEDLINE | ID: mdl-23057576

RESUMO

Antioxidant compounds protect plants against oxidative stress caused by environmental conditions. Different light qualities, such as UV-A radiation and blue light, have shown positive effects on the production of phenols in plants. Kalanchoe pinnata (Lamarck) Persoon (Crassulaceae) is used for treating wounds and inflammations. Some of these beneficial effects are attributed to the antioxidant activity of plant components. We investigated the effects of blue light and UV-A radiation supplementation on the total phenol content, antioxidant activity and chromatographic profile of aqueous extracts from leaves of K. pinnata. Monoclonal plants were grown under white light, white plus blue light and white plus UV-A radiation. Supplemental blue light improved the antioxidant activity and changed the phenolic profile of the extracts. Analysis by HPLC of supplemental blue-light plant extracts revealed a higher proportion of the major flavonoid quercetin 3-O-α-L-arabinopyranosyl (1→2) α-L-rhamnopyranoside, as well as the presence of a wide variety of other phenolic substances. These findings may explain the higher antioxidant activity observed for this extract. Blue light is proposed as a supplemental light source in the cultivation of K. pinnata, to improve its antioxidant activity.


Assuntos
Antioxidantes/metabolismo , Kalanchoe/efeitos da radiação , Fenóis/metabolismo , Folhas de Planta/efeitos da radiação , Quercetina/análogos & derivados , Kalanchoe/metabolismo , Luz , Oxirredução , Extratos Vegetais/química , Folhas de Planta/metabolismo , Quercetina/biossíntese
9.
Nat Prod Commun ; 7(2): 175-8, 2012 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-22474947

RESUMO

The chemical composition and immunosuppressive potential of the flowers from Kalanchoe pinnata (Crassulaceae) were investigated. We found that the aqueous flower extract was more active than the leaf extract in inhibiting murine T cell mitogenesis in vitro. Flavonoids isolated from the flower extract were identified and quantitated based on NMR and HPLC-DAD-MS analysis, respectively. Along with quercetin, four quercetin glycosyl conjugates were obtained, including quercetin 3-O-beta-D-glucuronopyranoside and quercetin 3-O-beta-D-glucopyranoside, which are described for the first time in K. pinnata. All flavonoids inhibited murine T cell mitogenesis and IL-2 and IL-4 production without cell toxicity. This is the first report on the pharmacological activity of flowers of a Kalanchoe species, which are not used for curative purposes. Our findings show that K. pinnata flowers are a rich source of T-suppressive flavonoids that may be therapeutically useful against inflammatory diseases.


Assuntos
Flavonoides/química , Flavonoides/farmacologia , Flores/química , Kalanchoe/química , Linfócitos T/efeitos dos fármacos , Animais , Polaridade Celular , Proliferação de Células/efeitos dos fármacos , Citocinas/genética , Citocinas/metabolismo , Regulação da Expressão Gênica/efeitos dos fármacos , Imunossupressores/química , Imunossupressores/farmacologia , Linfonodos/citologia , Macrófagos/efeitos dos fármacos , Macrófagos/metabolismo , Camundongos , Camundongos Endogâmicos BALB C
10.
Expert Opin Ther Pat ; 22(10): 1111-21, 2012 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-22971104

RESUMO

INTRODUCTION: Influenza viruses are common agents of flu outbreaks, epidemics, and pandemics that have occurred through the centuries. Prevention and control of flu are of great clinical importance, since they cause serious damage to health, with a consequent impact on quality of life and economy of a country. Resistance against the current drugs justifies the development of new anti-influenza molecules. Flavonoids exhibit significant activity against flu through their anti-inflammatory and antiviral properties. The profile of these molecules makes them particularly promising as therapeutic agents against flu. AREAS COVERED: This review focus on the activity of flavonoids on different influenza virus targets as well as their use in patented pharmaceutical formulations. Twenty-one patents of these compounds for prophylaxis and treatment of influenza infection are discussed. EXPERT OPINION: The H1N1 influenza pandemic in 2009 resulted in a significant increase in the number of patents claiming pharmaceutical formulations for prophylaxis and treatment of flu. The research advances on flavonoids showing anti-influenza activity and the efforts made by researchers and industries consolidate the interest on new alternatives for the therapy of an infectious disease that represents a serious public health problem throughout the world.


Assuntos
Antivirais/farmacologia , Flavonoides/farmacologia , Vírus da Influenza A Subtipo H1N1/efeitos dos fármacos , Influenza Humana/tratamento farmacológico , Influenza Humana/prevenção & controle , Animais , Antivirais/química , Descoberta de Drogas , Flavonoides/química , Humanos , Vírus da Influenza A Subtipo H1N1/patogenicidade , Influenza Humana/virologia , Estrutura Molecular , Patentes como Assunto , Relação Estrutura-Atividade
11.
Pesqui. vet. bras ; 37(8): 859-865, Aug. 2017. tab, graf
Artigo em Inglês | LILACS, VETINDEX | ID: biblio-895510

RESUMO

An aqueous leaf extract of the medicinal species Kalanchoe gastonis-bonnieri (here denominated KGB) has been found to be effective as an antimicrobial agent against canine oral cavity bacteria in in vitro assays. In this study, we investigated the effect of topic oral administration of KGB on the development of dental biofilm in Beagle dogs. The experiments were performed with an experimental group (0.2% of KGB extract), a negative control group (0.9% of saline solution) and a positive control group (0.12% chlorhexidine). Each treatment was sprayed into the oral cavity daily for 28 days. Thirty Beagle dogs with similar characteristics and kept under the same management and diet were used. The measurement of dental plaque and calculus was performed using a computerized analytical method. The phenolic profile of KGB extract was analyzed by HPLC-DAD. KGB extract at 0.2% showed efficacy in controlling the formation of plaque compared to the negative control group, and dental calculus in relation to the negative and positive control groups. A significant difference was observed among these three groups. Peaks attributed to flavonoids and phenolic acids were identified in the HPLC-DAD chromatogram of the KGB extract. The presence of these substances could be related to the activity observed. Our findings demonstrate that treatment with KGB is effective in controlling periodontal disease in dogs, providing new insights into the medicinal properties of this plant. KGB extract has a potential use as a supplemental agent in pharmaceutical products for the prevention of periodontal disease.(AU)


Um extrato aquoso de folhas da espécie medicinal Kalanchoe gastonis-bonnieri (aqui denominado como KGB) foi efetivo como um agente antimicrobiano contra as bactérias da cavidade oral de cães em testes in vitro. Neste estudo, investigou-se o efeito da administração oral tópica de KGB sobre o desenvolvimento do biofilme dental em cães da raça Beagle. Os experimentos foram realizados com um grupo experimental (0,2% de extrato de KGB), um grupo controle negativo (0,9% de solução salina) e um grupo controle positivo (0,12% de gluconato de clorexidina). Cada tratamento foi aplicado no interior da cavidade oral diariamente durante 28 dias. Foram utilizados trinta cães da raça Beagle com características semelhantes e mantidos sob o mesmo manejo e dieta. A medição da placa bacteriana e cálculo dentários foi realizada utilizando-se um método de análise computadorizada. O perfil fenólico do extrato de KGB foi analisado por HPLC-DAD. O extrato de KGB a 0,2% mostrou eficácia no controle da formação de placa bacteriana em comparação com o grupo controle negativo, e de cálculo dentário em relação aos grupos controle negativo e positivo. Uma diferença significativa foi observada entre esses três grupos. Picos atribuídos a flavonoides e ácidos fenólicos foram identificados no cromatograma de HPLC-DAD do extrato de KGB. A presença de tais substâncias pode estar relacionada com a atividade observada. Os resultados demonstram que o tratamento com KGB é eficaz no controle da doença periodontal em cães, fornecendo novas perspectivas sobre as propriedades medicinais desta planta. O extrato de KGB tem uma utilização potencial como um agente suplementar em produtos farmacêuticos para a prevenção da doença periodontal.(AU)


Assuntos
Animais , Cães , Flavonoides , Extratos Vegetais/uso terapêutico , Cálculos Dentários/prevenção & controle , Kalanchoe , Placa Dentária/prevenção & controle , Doenças Periodontais/terapia
12.
Nat Prod Commun ; 6(7): 961-4, 2011 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-21834233

RESUMO

From the aqueous extract (Pc) of Petroselinum crispum (Mill) flat leaves specimens were isolated and identified the flavonoids apigenin (1), apigenin-7-O-glucoside or cosmosiin (2), apigenin-7-O-apiosyl-(1 --> 2)-O-glucoside or apiin (3) and the coumarin 2",3"-dihydroxyfuranocoumarin or oxypeucedanin hydrate (4). The inhibitory activity toward clotting formation and platelet aggregation was assessed for Pc flavonoids (1) and (2), and the coumarin (4). Pc showed no inhibition on clotting activity when compared with the control. On the other hand, a strong antiplatelet aggregation activity was observed for Pc (IC50 = 1.81 mg/mL), apigenin (IC50 = 0.036 mg/mL) and cosmosiin (IC50 = 0.18 mg/mL). In all cases ADP was used as inductor of platelet aggregation. Our results showed that Pc, apigenin and cosmosiin interfere on haemostasis inhibiting platelet aggregation. To the best of our knowledge this is the first report for the cosmosiin antiplatelet aggregation in vitro activity.


Assuntos
Cumarínicos/isolamento & purificação , Flavonoides/isolamento & purificação , Petroselinum/química , Extratos Vegetais/química , Inibidores da Agregação Plaquetária/isolamento & purificação , Cumarínicos/química , Cumarínicos/farmacologia , Flavonoides/química , Flavonoides/farmacologia , Humanos , Concentração Inibidora 50 , Estrutura Molecular , Ressonância Magnética Nuclear Biomolecular , Rotação Ocular , Tempo de Tromboplastina Parcial , Extratos Vegetais/isolamento & purificação , Extratos Vegetais/farmacologia , Folhas de Planta/química , Inibidores da Agregação Plaquetária/química , Inibidores da Agregação Plaquetária/farmacologia , Tempo de Protrombina , Espectrometria de Massas por Ionização por Electrospray
13.
J Ethnopharmacol ; 133(1): 132-7, 2011 Jan 07.
Artigo em Inglês | MEDLINE | ID: mdl-20883762

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Leaves from Kalanchoe pinnata (Lamarck) Persoon (Crassulaceae) are popularly used for healing wounds. Its antileishmanial properties are established in experimental animals, and its active flavonoid components have been identified. AIM OF THE STUDY: In this study, we attempted to standardize the extract from K. pinnata leaves by evaluating the influence of season of harvest, sunlight exposure and method of extraction on antileishmanial flavonoids content. MATERIALS AND METHODS: HPLC-DAD-MS was used to identify and quantify the active antileishmanial flavonoids in different extracts. ANOVA test for analyses of variance followed by the Tukey test of multiple comparisons were used in the statistical analysis. The antileishmanial potential was assessed by the activation of nitric oxide production by murine macrophage using the Griess method. RESULTS: We demonstrated that active flavonoids were significantly more abundant when the leaves were collected in the summer, and that aqueous extraction at 50°C allowed the highest flavonoid extraction. The benefit of sunlight exposure was confirmed in plants cultivated under direct sunlight when compared with those that grown under shade. Under sunny conditions the yield of the most active antileishmanial favonoid quercitrin was increased by 7-fold. All aqueous extracts tested were capable to enhance the macrophage nitric oxide production. However, hot aqueous extract from leaves collected in summer exhibited the higher activity, in agreement with HPLC-DAD-MS analysis tendency. In addition, with the aim of reducing the individual chemical variations of the plant constituents and optimizing the production of the active extract, it was obtained in vitro monoclonal KP specimens that were easily adapted to field conditions and were able to produce antileishmanial flavonoids. CONCLUSION: Our study reports the better conditions of cultivation, harvest and extraction protocol for obtaining a K. pinnata extract exhibiting the highest antileishmanial activity. Additionally, we propose the flavonoids quercetin 3-O-α-L-arabinopyranosyl (1→2)-α-L-rhamnopyranoside and quercitrin, as satisfactory chemical markers for standardization purposes.


Assuntos
Antiprotozoários/química , Flavonoides/análise , Kalanchoe/química , Leishmaniose/tratamento farmacológico , Extratos Vegetais/química , Estações do Ano , Animais , Antiprotozoários/farmacologia , Flavonoides/farmacologia , Kalanchoe/crescimento & desenvolvimento , Macrófagos/efeitos dos fármacos , Camundongos , Óxido Nítrico/metabolismo , Fitoterapia , Extratos Vegetais/farmacologia , Folhas de Planta
14.
Planta Med ; 75(4): 307-11, 2009 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-19085683

RESUMO

Leishmaniasis is a parasitic disease that threatens 350 million people worldwide. In a search for new antileishmanial drugs, the in vitro activity of flavonoids from Kalanchoe pinnata (Crassulaceae) was previously demonstrated in infected cells. In order to demonstrate the safety and oral activity of K. pinnata, flavonoids were evaluated in vivo in a murine model of cutaneous leishmaniasis. Daily oral doses of quercetin 3-O-alpha-L-arabinopyranosyl (1-->2)-alpha-L-rhamnopyranoside, quercetin 3-O-alpha-L-rhamnopyranoside, and free quercetin (16 mg/kg body weight) all were able to control the lesion growth caused by Leishmania amazonensis and to significantly reduce parasite load. These flavonoids were as effective as the crude K. pinnata aqueous extract given at 320 mg/kg body weight. HPLC-DAD-MS analysis of the plasma of extract-treated mice suggested that quercetin and quercetin glucuronides are the main metabolites of K. pinnata quercetin glycosides. Our results indicate that K. pinnata quercetin glycosides are important active components of the aqueous extract and that they possess potent oral efficacy against cutaneous leishmaniasis.


Assuntos
Antiprotozoários/farmacologia , Flavonas/química , Flavonas/farmacologia , Kalanchoe/química , Leishmaniose Cutânea/tratamento farmacológico , Administração Oral , Animais , Antiprotozoários/química , Flavonas/administração & dosagem , Camundongos , Camundongos Endogâmicos BALB C , Estrutura Molecular , Quercetina/análogos & derivados , Quercetina/química , Quercetina/farmacologia
15.
J Ethnopharmacol ; 124(2): 228-32, 2009 Jul 15.
Artigo em Inglês | MEDLINE | ID: mdl-19397977

RESUMO

AIM OF THE STUDY: To identify the compounds responsible for the antinociceptive and anti-inflammatory effects previously described for Sedum dendroideum, through bioassay-guided fractionation procedures. MATERIALS AND METHODS: Antinociceptive activity was evaluated through mouse acetic acid-induced writhing model. The anti-inflammatory activity was assessed through croton oil-induced mouse ear oedema and carrageenan-induced peritonitis. RESULTS: The Sedum dendroideum juice afforded seven known flavonoids identified with basis on NMR data. The oral administration of the major kaempferol glycosides kaempferitrin [1] (17.29 micromol/kg), kaempferol 3-O-beta-glucopyranoside-7-O-alpha-rhamnopyranoside [2] (16.82 micromol/kg), kaempferol 3-O-neohesperidoside-7-O-alpha-rhamnopyranoside [3] (13.50 micromol/kg) or alpha-rhamnoisorobin [5] (23.13 micromol/kg) inhibited by 47.3%, 25.7%, 60.2% and 58.0%, respectively, the acetic acid-induced nociception (indomethacin: 27.95 micromol/kg, p.o.; 68.9%). Flavonoids 1, 2, 3 or 5, at the same doses, reduced by 39.5%, 46.5%, 35.6% and 33.3%, respectively, the croton oil-induced oedema (dexamethasone: 5.09 micromol/kg, s.c.; 83.7%) and impaired leukocyte migration by 42.9%, 46.3%, 50.4% and 49.6%, respectively (dexamethasone: 5.09 micromol/kg, s.c.; 66.1%). CONCLUSIONS: Our findings show that the major kaempferol glycosides may account for the renowned medicinal use of Sedum dendroideum against pain and inflammatory troubles.


Assuntos
Analgésicos/uso terapêutico , Anti-Inflamatórios/uso terapêutico , Quempferóis/uso terapêutico , Dor/tratamento farmacológico , Fitoterapia , Preparações de Plantas/uso terapêutico , Sedum/química , Ácido Acético , Analgésicos/isolamento & purificação , Analgésicos/farmacologia , Animais , Anti-Inflamatórios/farmacologia , Carragenina , Inibição de Migração Celular/efeitos dos fármacos , Óleo de Cróton , Edema/induzido quimicamente , Edema/tratamento farmacológico , Glicosídeos/farmacologia , Glicosídeos/uso terapêutico , Quempferóis/isolamento & purificação , Quempferóis/farmacologia , Leucócitos/efeitos dos fármacos , Masculino , Camundongos , Dor/induzido quimicamente , Peritonite/induzido quimicamente , Peritonite/tratamento farmacológico , Folhas de Planta , Preparações de Plantas/química , Preparações de Plantas/farmacologia
16.
Planta Med ; 72(1): 81-3, 2006 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-16450304

RESUMO

Quercitrin (quercetin 3- O-alpha- L-rhamnopyranoside), one of the constituents of the biologically active aqueous extract obtained from Kalanchoe pinnata, is demonstrated to be a potent antileishmanial compound (IC50 approximately 1 microg/mL) with a low toxicity profile. This is the first time that antileishmanial activity is demonstrated for a flavonoid glycoside.


Assuntos
Antiparasitários/farmacologia , Kalanchoe/química , Leishmania/efeitos dos fármacos , Quercetina/análogos & derivados , Animais , Camundongos , Extratos Vegetais/farmacologia , Folhas de Planta/química , Quercetina/farmacologia
17.
Rev. bras. farmacogn ; 20(3): 441-452, jun.-jul. 2010. ilus, graf, tab
Artigo em Português | LILACS | ID: lil-555928

RESUMO

As algas vermelhas do gênero Laurencia são conhecidas como uma riquíssima fonte de metabólitos secundários. As principais classes químicas já isoladas são terpenos - sesquiterpenos, diterpenos, triterpenos - e acetogeninas. Estudos apontam que estas substâncias apresentam importantes atividades biológicas, principalmente citotóxica e antibacteriana. Existem ainda alguns poucos trabalhos com informações sobre atividade antiparasitária, antiviral e antifúngica dos metabólitos de Laurencia. O forte perfil bioativo observado em alguns estudos sugere que alguns destes metabólitos podem ser futuramente utilizados como fármacos ou como protótipos de novos agentes antitumorais e antibacterianos. Muitos dos metabólitos de Laurencia ainda não foram avaliados sob o ponto de vista farmacológico, o que representa um grande potencial a ser explorado por diversos campos da farmacologia.


The red alga of the genus Laurencia is known as an endless source of metabolites. The main substances produced are sesquiterpenes, diterpenes, triterpenes and acetogenins. Many studies reveal that these metabolites are active, especially cytotoxic and antibacterial. There are few other studies that describe the antiparasital, antifungal and antiviral actions of the metabolites produced by the alga of the genus Laurencia. The results observed in some studies suggest that these metabolites may be used in the future as drugs or lead compounds as antitumoral and/or antibacterial agents. Many metabolites have not been submitted to pharmacological studies which still represents an area to be explored.

18.
Planta Med ; 71(4): 362-3, 2005 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-15856415

RESUMO

The infusion of aerial parts (EI) of Eleusine indica Gaertn (Poaceae) is used in Brazil against airway inflammatory processes like influenza and pneumonia. Pre-treatment with 400 mg/kg of crude extract inhibited 98% of lung neutrophil recruitment in mice exposed to aerosols of lipopolysaccharide (LPS) from Gram-negative bacteria, in a dose-dependent manner. At 400 microg/kg, schaftoside (6-C-beta-glucopyranosyl-8-C-alpha-arabinopyranosylapigenin) and vitexin (8-C-beta-glucopyranosylapigenin), isolated from EI, inhibited 62% and 80% of lung neutrophil influx, respectively. These results may justify the popular use of E. indica against airway inflammatory processes.


Assuntos
Anti-Inflamatórios não Esteroides/farmacologia , Eleusine , Pneumopatias/tratamento farmacológico , Fitoterapia , Extratos Vegetais/farmacologia , Animais , Anti-Inflamatórios não Esteroides/administração & dosagem , Anti-Inflamatórios não Esteroides/uso terapêutico , Relação Dose-Resposta a Droga , Flavonas/administração & dosagem , Flavonas/farmacologia , Flavonas/uso terapêutico , Lipopolissacarídeos , Pneumopatias/induzido quimicamente , Masculino , Camundongos , Camundongos Endogâmicos BALB C , Componentes Aéreos da Planta , Extratos Vegetais/administração & dosagem , Extratos Vegetais/uso terapêutico
19.
Planta Med ; 69(4): 382-4, 2003 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-12709912

RESUMO

Blutaparon portulacoides (St. Hil.) Mears (= Philoxerus portulacoides St. Hil.) (Amaranthaceae) is a species occurring in the Brazilian coast in two botanical varieties. The chemical study of an ethanolic extract led to the isolation of spinacetin 3- O-robinobioside as well as an unique glycosylated pseudo-dimeric flavonoid identified as 8,8""-methylene bis(spinacetin 3- O-robinobioside) mainly by NMR analyses (1H, 1H- 1H COSY, 13C, HMQC, HMBC) and MALDI-TOF mass spectrometry.


Assuntos
Amaranthaceae , Flavonoides/química , Fitoterapia , Extratos Vegetais/química , Glicosilação , Humanos , Espectroscopia de Ressonância Magnética
20.
Rev. bras. farmacogn ; 18(supl): 785-797, Dec. 2008. ilus, mapas, tab
Artigo em Português | LILACS | ID: lil-509461

RESUMO

A asma é uma doença inflamatória crônica, que representa um problema de saúde pública com altos números de óbitos e elevado impacto socioeconômico. A patologia é caracterizada pela fase imediata, mediada pela resposta aguda de células inflamatórias, e a tardia, que é responsável pela resposta com envolvimento de células específicas do sistema imunológico. Atualmente, os principais tipos de fármacos utilizados no tratamento da asma são os broncodilatadores e agentes antiinflamatórios, que aliviam os sintomas de broncoespasmo e diminuem a inflamação das vias aéreas. Entretanto, terapias com esses medicamentos não são totalmente eficazes e provocam efeitos adversos. A escassez de fármacos seguros e o baixo acesso da população carente aos tratamentos utilizados estimulam a busca de novas substâncias potencialmente úteis no tratamento da asma. Produtos naturais de origem vegetal representam um grande potencial farmacológico contra asma, uma vez que podem fornecer moléculas diversas com mecanismos específicos para tratamento e controle da patologia. A busca por terapias mais eficientes e específicas para o processo asmático mostra que a procura nos produtos naturais é promissora e possui um papel importante para a descoberta de novas terapias contra a asma.


Asthma is a chronic inflammatory disease, which represents a huge public health problem in developed and developing countries, has high death rates and elevated socioeconomic implications. The pathology is characterized by two different phases: the initial stage, mediated by acute inflammatory cell response and the late phase, responsible for specific immune cells. Currently, the main drugs used for asthma treatment are bronchodilator and anti-inflammatory agents, which mechanisms focus the relief of symptoms and attenuation of airway inflammation. However, therapies with those drugs have side effects besides they are not totally effective. Poor accessibility in the development countries and scarcity of safety drugs lead the search for new drugs to asthma treatment. Herbal natural products have elevated pharmacological potential against asthma, once they provide several molecules with specific mechanisms for the pathology control and treatment. Thus, search in herbal natural products plays an important role to find out specific and effective mechanisms.

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