RESUMO
OBJECTIVE: To investigate the effects of Araucaria sp. brown propolis (ABP) against trinitrobenzenesulfonic acid (TNBS)-induced colitis in rats. METHODS: Animals received vehicle (1% DMSO, 1 ml/kg) or hydroalcoholic extract of ABP (hydroalcoholic extract of Araucaria sp. brown propolis (HEABP), 30, 100, and 300 mg/kg) orally, or dexamethasone (25 mg/kg, s.c.) for 5 days. On day 4, the animals received intracolonic TNBS (150 mg/kg), on day 6 they were euthanized. The weight of the animals, the macroscopic and microscopic colonic damage, reduced glutathione (GSH) and malondialdehyde (MDA) levels, and the activity of glutathione S-transferase (GST), catalase (CAT), superoxide dismutase (SOD), and myeloperoxidase (MPO) were measured in colon homogenate. The action of HEABP and two isolated compounds in neutrophil migration was recorded. KEY FINDINGS: HEABP (100 and 300 mg/kg), but not dexamethasone, decreased colonic lesion, and increased colonic mucin staining. In parallel, HEABP decreased MDA and restored GSH levels and the activity of SOD, CAT, and GST in the colon. A dose-dependent inhibition of MPO activity was observed (LogIC50 = 1.9). Moreover, HEBPA and the junicedric and abietic acids inhibited the neutrophil chemotaxis in vitro and HEBPA reduced neutrophil migration in vivo. CONCLUSION: HEABP may be promising in the therapies for inflammatory bowel diseases, reducing oxidative and inflammatory damage, especially mediated by neutrophils.
Assuntos
Colite Ulcerativa , Malondialdeído , Estresse Oxidativo , Extratos Vegetais , Própole , Ratos Wistar , Ácido Trinitrobenzenossulfônico , Animais , Colite Ulcerativa/tratamento farmacológico , Colite Ulcerativa/induzido quimicamente , Colite Ulcerativa/patologia , Colite Ulcerativa/metabolismo , Própole/farmacologia , Masculino , Estresse Oxidativo/efeitos dos fármacos , Ratos , Extratos Vegetais/farmacologia , Malondialdeído/metabolismo , Colo/efeitos dos fármacos , Colo/patologia , Colo/metabolismo , Peroxidase/metabolismo , Glutationa/metabolismo , Superóxido Dismutase/metabolismo , Anti-Inflamatórios/farmacologia , Anti-Inflamatórios/isolamento & purificação , Modelos Animais de Doenças , Dexametasona/farmacologia , Traqueófitas/química , Catalase/metabolismo , Relação Dose-Resposta a Droga , Antioxidantes/farmacologia , Glutationa Transferase/metabolismoRESUMO
There is evidence that propolis exhibits anti-inflammatory, anticancer, and antioxidant properties. We assessed the potential beneficial effects of Brazilian propolis on liver injury in nonalcoholic fatty liver disease (NAFLD). Our findings demonstrate that Brazilian propolis suppresses inflammation and fibrosis in the liver of mice with NAFLD by inhibiting the expression of genes involved in endoplasmic reticulum (ER) stress. Additionally, Brazilian propolis also suppressed the expression of ER stress-related genes in HepG2 cells treated with an excess of free fatty acids, leading to cell apoptosis. A deeper analysis revealed that kaempferol, one of the components present in Brazilian propolis, induces cell proliferation through the mitogen-activated protein kinase (MAPK)/extracellular signal-regulated kinase (ERK) pathway and protects against oxidative stress. In conclusion, Brazilian propolis exhibits hepatoprotective properties against oxidative stress by inhibiting ER stress in NAFLD-induced model mice.
Assuntos
Apoptose , Estresse do Retículo Endoplasmático , Fígado , Hepatopatia Gordurosa não Alcoólica , Estresse Oxidativo , Própole , Própole/farmacologia , Própole/uso terapêutico , Animais , Estresse do Retículo Endoplasmático/efeitos dos fármacos , Humanos , Hepatopatia Gordurosa não Alcoólica/tratamento farmacológico , Hepatopatia Gordurosa não Alcoólica/patologia , Hepatopatia Gordurosa não Alcoólica/metabolismo , Células Hep G2 , Estresse Oxidativo/efeitos dos fármacos , Masculino , Fígado/efeitos dos fármacos , Fígado/patologia , Fígado/metabolismo , Apoptose/efeitos dos fármacos , Camundongos , Quempferóis/farmacologia , Quempferóis/uso terapêutico , Brasil , Proliferação de Células/efeitos dos fármacos , Camundongos Endogâmicos C57BLRESUMO
Propolis is a rich source of known and largely explored bioactive compounds with many pharmacological properties. It is used in several commercialized products, such as propolis-enriched honey, candies, mouth and throat sprays, soaps, toothpaste, and skin creams. However, the great diversity of propolis products and different types make the standardization of realistic quality control procedures challenging. Moreover, the extraction of propolis bioactive compounds depends on the technique and the solvent used. In Brazil, the Ministry of Agriculture, Livestock, and Supply (MAPA) set standards to establish commercialized propolis extracts' identity and quality. In addition, according to legislation, propolis extracts must present the main classes of phenols at 200 and 400 nm on the UV spectrum. Still, it is not specified which analysis method should be used to guarantee feasible quality control of the commercialized samples. For this, we proposed a new fast UHPLC-PDA-MS/MS method for analysis and quantification of propolis phenolic compounds. Moreover, we hypothesize that there is no efficient monitoring regarding the quality of the propolis extracts sold in Brazilian stores. Therefore, the present study aimed to perform quality control of 17 Brazilian propolis extracts produced in the Southeast region (green or brown - the most representative samples). The dry extract content (% g/mL), oxidation index (seconds), total flavonoids, and phenolics (% m/m) of each sample were compared with legislation. We conclude that using the UHPLC-PDA method and the investigation that allowed the comparison with the current legislation efficiently practical problems in the commercialization of propolis extracts. However, of the 17 analyzed samples, 6 did not meet the desired the recognized standards, denoting a lack of supervision and efficient quality control, which highlights a dangerous situation regarding the commercialization of this critical product used in several industrial fields, mainly in the food and pharmaceutical sector.
Assuntos
Própole , Brasil , Cromatografia Líquida de Alta Pressão/métodos , Flavonoides/análise , Preparações Farmacêuticas , Fenóis/análise , Extratos Vegetais , Própole/farmacologia , Controle de Qualidade , Padrões de Referência , Sabões/análise , Solventes , Espectrometria de Massas em Tandem , Cremes Dentais/análiseRESUMO
Propolis is a resinous material rich in flavonoids and involved in several biological activities such as antimicrobial, fungicide, and antiparasitic functions. Conventionally, ethanolic solutions are used to obtain propolis phytochemicals, which restrict their use in some cultures. Given this, we developed an alcohol-free high-performance extractive approach to recover antibacterial and antioxidants phytochemicals from red propolis. Thus, aqueous-solutions of ionic liquids (IL) and eutectic solvents were used and then tested for their total flavonoids, antioxidant, and antimicrobial activities. The surface-responsive technique was applied regarding some variables, namely, the time of extraction, the number of extractions, and cavitation power (W), to optimize the process (in terms of higher yields of flavonoids and better antioxidant activity). After that, four extractions with the same biomass (repetitions) using 1-hexyl-3-methylimidazolium chloride [C6mim]Cl, under the operational conditions fixed at 3.3 min and 300 W, were able to recover 394.39 ± 36.30 mg RuE. g-1 of total flavonoids, with total antioxidant capacity evaluated up to 7595.77 ± 5.48 µmol TE. g-1 dried biomass, besides inhibiting the growth of Staphylococcus aureus and Salmonella enteritidis bacteria (inhibition halo of 23.0 ± 1.0 and 15.7 ± 2.1, respectively). Aiming at the development of new technologies, the antimicrobial effect also presented by [C6mim]Cl may be appealing, and future studies are required to understand possible synergistic actions with propolis phytochemicals. Thereby, we successfully applied a completely alcohol-free method to obtain antimicrobials phytochemicals and highly antioxidants from red propolis, representing an optimized process to replace the conventional extracts produced until now.
RESUMO
Brazilian propolis (AF-08) is a dietary supplement containing a variety of flavonoids. It is used worldwide as a folk medicine. Flavonoids and a diet of fruits and vegetables containing them have been shown to reduce the risk of cardiovascular diseases (CVDs). Most of CVDs are caused by arterial thrombus formation. A thrombus is formed by the interaction between adhesion and aggregation of platelets to damaged blood vessels and blood coagulation consisting of extrisic and intrinsic pathways. Platelet aggregation and blood coagulation are closely linked to thrombosis. Therefore, we evaluated the effectiveness of AF-08 or its component flavonoids against thrombosis by examining their inhibition of platelet aggregation and blood coagulation. Human platelet-rich plasma was incubated with serial dilutions of AF-08 for 10 min to assess its inhibitory effect on platelet aggregation caused by collagen. The inhibitory effect of AF-08 on blood coagulation was evaluated by the prothrombin time (PT) and activated partial thromboplastin time (APTT), which reflect the coagulation function of extrinsic and intrinsic pathways, respectively. AF-08 significantly inhibited collagen-induced platelet aggregation but not PT and APTT, indicating that AF-08 inhibited platelet aggregation but not blood coagulation. Among three flavonoids contained in AF-08, apigenin and chrysin obviously inhibited platelet aggregation but the inhibitory effect of kaempferol was less effective. The three flavonoids did not affect PT and APTT. The inhibitory activity of AF-08 on human platelet aggregation without affecting blood coagulation was suggested to be partially due to apigenin and chrysin. AF-08 may be effective in suppressing platelet-based arterial thrombus formation and reducing the risk of CVDs.
Assuntos
Agregação Plaquetária , Própole , Coagulação Sanguínea , Plaquetas , Colágeno , Humanos , Própole/farmacologiaRESUMO
ABSTRACT Propolis (bee glue) a product of Apis mellifera L. is a resinous mixture containing chiefly beeswax and resin harvested by bees from plant leaves, buds and exudates. Extracts of a propolis sample from Salitre, a municipality of Ceará state (northeast Brazil) were obtained with solvents of increasing polarity (hexane, chloroform, ethyl acetate and methanol). A chemical profile was carried out by GC-EI-MS and HPLC-DAD-ESI-MS/MS. Lupenone, lupeol, octanoic acid tetracosyl ester and octanoic acid hexacosyl ester were identified by GC-EI-MS. Antioxidant activity was evaluated by the DPPH and β-carotene discoloring methods, and anti-HIV activity by the in vitro inhibition of HIV-1 reverse transcriptase. The ethyl acetate extract exhibited the highest antioxidant and anti-HIV activity and was fractioned by column chromatography using silica gel and seven different eluents. The active fractions were submitted to semi preparative HPLC and the following compounds were isolated: caffeic acid, p-coumaric acid, diprenylcinnamic acid, quercetin, naringenin, isorhamnetin, quercetin-3-O-diglucoside,4,2′,4′-trihydroxy-2-methoxychalcone, gossypetin-3,3′,4′,7-tetramethyl ether, myricetin-3,7,3′-trimethyl ether and 5-hydroxy-3,6,7,8,4′-pentamethoxyflavone. The ethyl acetate extract and its fractions F5-F7, as well as quercetin, isorhamnetin, myricetin-3,7,3′-trimethyl ether and p-coumaric acid exhibited high antioxidant activity on both DPPH and β-carotene antioxidant methods. Isorhamnetin exhibited moderate inhibitory effect against HIV-1 reverse transcriptase (56.99 ± 3.91%), followed by naringenin (44.22 ± 1.71%), quercetin (43.41 ± 4.56%) and diprenylcinnamic acid (41.59 ± 2.59%). These results agree with previous authors who reported anti-HIV activity of flavonoids.
RESUMO
The protective effects of Brazilian propolis on capillary regression induced by chronically neuromuscular inactivity were investigated in rat soleus muscle. Four groups of male Wistar rat were used in this study; control (CON), control plus Brazilian propolis supplementation (CON + PP), 2-week hindlimb unloading (HU), and 2-week hindlimb unloading plus Brazilian propolis supplementation (HU + PP). The rats in the CON + PP and HU + PP groups received two oral doses of 500 mg/kg Brazilian propolis daily (total daily dose 1000 mg/kg) for 2 weeks. Unloading resulted in a decrease in capillary number, luminal diameter, and capillary volume, and an increase in the expression of anti-angiogenic factors, such as p53 and TSP-1, within the soleus muscle. Brazilian propolis supplementation, however, prevented these changes in capillary structure due to unloading through the stimulation of pro-angiogenic factors and suppression of anti-angiogenic factors. These results suggest that Brazilian propolis is a potential non-drug therapeutic agent against capillary regression induced by chronic unloading.
Assuntos
Capilares/efeitos dos fármacos , Membro Posterior/efeitos dos fármacos , Músculo Esquelético/efeitos dos fármacos , Própole/farmacologia , Substâncias Protetoras/farmacologia , Indutores da Angiogênese/metabolismo , Animais , Brasil , Capilares/metabolismo , Suplementos Nutricionais , Elevação dos Membros Posteriores/métodos , Masculino , Músculo Esquelético/metabolismo , Ratos , Ratos WistarRESUMO
Previous studies have reported on the phytotherapeutic potential of propolis from southern Brazil (Urupema, Santa Catarina State), in particular, its efficacy in the treatment of bovine mastitis. The present study evaluates the effect of seasonal variation on the chemical composition of propolis from southern Brazil and its resultant antimicrobial and cytotoxic activities in the context of treating bovine mastitis. Antimicrobial activity against Staphylococcus aureus was assessed, along with the cytotoxicity and induction of apoptosis in MAC-T bovine mammary epithelial cells. With the exception of spring propolis, the flavonoid quercetin was the main compound present in all samples. The minimum inhibitory concentration (MIC) of propolis against S. aureus from mastitic milk was 140 µg/mL for samples collected during the spring, autumn, and winter seasons, but 280 µg/mL for samples collected in summer. For MAC-T cells, the spring propolis extract was more toxic with an IC50 of 120 µg/mL. However, for 120 µg/mL of spring propolis extract, only 0.77% of necrotic and 37% of apoptotic MAC-T cells were found, respectively. Nonetheless, the induction of cell death through apoptosis by propolis extract suggests less severe damage to bovine mammary glands. Moreover, only negligible seasonal variation was found in the chemical composition of propolis from southern Brazil, and no biological activities were determined to be harmful. Therefore, this propolis shows promise as an alternative to commercial antimicrobials in the control of bovine mastitis, offering support for organic milk production.(AU)
Estudos prévios tem demonstrado o potencial terapêutico da propolis do Sul do Brasil (Urupema, Santa Catarina), em particular no tratamento da mastite bovina. O presente estudo tem como objetivo avaliar o efeito da variação sazonal sobre a composição química da própolis de Urupema do Sul do Brasil e suas atividades antimicrobiana e citotóxica visando o tratamento da mastite bovina. A atividade antimicrobiana contra Staphylococcus aureus foi avaliada, juntamente com a citotoxicidade e indução de apoptose em células epiteliais mamárias bovina da linhagem MAC-T. Com exceção da própolis da primavera, o flavonóide quercetina foi o composto majoritário em todas as amostras. A concentração inibitória mínima (CIM) da propolis contra S. aureus de leite mastítico foi 140 µg/mL para as amostras de primavera, outono e inverno e 280 µg/mL para a amostra coletada no verão. Para as células MAC-T, o extrato de própolis da primavera foi o mais tóxico, sendo a IC50 120 µg/mL. Entretanto, com 120 µg/mL do extrato de própolis primaveril, somente 0,77% de células MAC-T necróticas e 37% apoptóticas foram encontradas. Portanto, a indução da morte celular por apoptose pelo extrato de própolis sugere danos possivelmente menos graves a glândula mamária bovina. Além disso, somente uma pequena variação sazonal foi encontrada para a composição química da propolis do Sul do Brasil, a qual não prejudicou suas atividades biológicas. Portanto, esta própolis mostra como uma alternativa promissora ao uso de antimicrobianos comerciais no controle da mastite bovina e uma opção para subsidiar a produção orgânica de leite.Palavras-chave: Células MAC-T. Mastite bovina. Propolis brasileira. Staphylococcus aureus.(AU)
Assuntos
Animais , Feminino , Bovinos , Staphylococcus aureus/patogenicidade , Mastite Bovina , Própole , Estações do AnoRESUMO
Previous studies have reported on the phytotherapeutic potential of propolis from southern Brazil (Urupema, Santa Catarina State), in particular, its efficacy in the treatment of bovine mastitis. The present study evaluates the effect of seasonal variation on the chemical composition of propolis from southern Brazil and its resultant antimicrobial and cytotoxic activities in the context of treating bovine mastitis. Antimicrobial activity against Staphylococcus aureus was assessed, along with the cytotoxicity and induction of apoptosis in MAC-T bovine mammary epithelial cells. With the exception of spring propolis, the flavonoid quercetin was the main compound present in all samples. The minimum inhibitory concentration (MIC) of propolis against S. aureus from mastitic milk was 140 g/mL for samples collected during the spring, autumn, and winter seasons, but 280 g/mL for samples collected in summer. For MAC-T cells, the spring propolis extract was more toxic with an IC50 of 120 g/mL. However, for 120 g/mL of spring propolis extract, only 0.77% of necrotic and 37% of apoptotic MAC-T cells were found, respectively. Nonetheless, the induction of cell deaththrough apoptosis by propolis extract suggests less severe damage to bovine mammary glands. Moreover, only negligible seasonal variation was found in the chemical composition of propolis from southern Brazil, and no biological
Estudos prévios tem demonstrado o potencial terapêutico da propolis do Sul do Brasil (Urupema, Santa Catarina), em particular no tratamento da mastite bovina. O presente estudo tem como objetivo avaliar o efeito da variação sazonal sobre a composição química da própolis de Urupema do Sul do Brasil e suas atividades antimicrobiana e citotóxica visando o tratamento da mastite bovina. A atividade antimicrobiana contra Staphylococcus aureus foi avaliada, juntamente com a citotoxicidade e indução de apoptose em células epiteliais mamárias bovina da linhagem MAC-T. Com exceção da própolis da primavera, o flavonóide quercetina foi o composto majoritário em todas as amostras. A concentração inibitória mínima (CIM) da propolis contra S. aureus de leite mastítico foi 140 g/mL para as amostras de primavera, outono e inverno e 280 g/mL para a amostra coletada no verão. Para as células MAC-T, o extrato de própolis da primavera foio mais tóxico, sendo a IC50 120 g/mL. Entretanto, com 120 g/mL do extrato de própolis primaveril, somente 0,77% de células MAC-T necróticas e 37% apoptóticas foram encontradas. Portanto, a indução da morte celular por apoptose pelo extrato de própolis sugere danos possivelmente menos graves a glândula mamária bovina. Além disso, somente uma pequena variação sazonal foi encontrada para a composição química da propolis do Sul do Brasil, a qual não prejudicou suas
RESUMO
Previous studies have reported on the phytotherapeutic potential of propolis from southern Brazil (Urupema, Santa Catarina State), in particular, its efficacy in the treatment of bovine mastitis. The present study evaluates the effect of seasonal variation on the chemical composition of propolis from southern Brazil and its resultant antimicrobial and cytotoxic activities in the context of treating bovine mastitis. Antimicrobial activity against Staphylococcus aureus was assessed, along with the cytotoxicity and induction of apoptosis in MAC-T bovine mammary epithelial cells. With the exception of spring propolis, the flavonoid quercetin was the main compound present in all samples. The minimum inhibitory concentration (MIC) of propolis against S. aureus from mastitic milk was 140 g/mL for samples collected during the spring, autumn, and winter seasons, but 280 g/mL for samples collected in summer. For MAC-T cells, the spring propolis extract was more toxic with an IC50 of 120 g/mL. However, for 120 g/mL of spring propolis extract, only 0.77% of necrotic and 37% of apoptotic MAC-T cells were found, respectively. Nonetheless, the induction of cell deaththrough apoptosis by propolis extract suggests less severe damage to bovine mammary glands. Moreover, only negligible seasonal variation was found in the chemical composition of propolis from southern Brazil, and no biological
Estudos prévios tem demonstrado o potencial terapêutico da propolis do Sul do Brasil (Urupema, Santa Catarina), em particular no tratamento da mastite bovina. O presente estudo tem como objetivo avaliar o efeito da variação sazonal sobre a composição química da própolis de Urupema do Sul do Brasil e suas atividades antimicrobiana e citotóxica visando o tratamento da mastite bovina. A atividade antimicrobiana contra Staphylococcus aureus foi avaliada, juntamente com a citotoxicidade e indução de apoptose em células epiteliais mamárias bovina da linhagem MAC-T. Com exceção da própolis da primavera, o flavonóide quercetina foi o composto majoritário em todas as amostras. A concentração inibitória mínima (CIM) da propolis contra S. aureus de leite mastítico foi 140 g/mL para as amostras de primavera, outono e inverno e 280 g/mL para a amostra coletada no verão. Para as células MAC-T, o extrato de própolis da primavera foio mais tóxico, sendo a IC50 120 g/mL. Entretanto, com 120 g/mL do extrato de própolis primaveril, somente 0,77% de células MAC-T necróticas e 37% apoptóticas foram encontradas. Portanto, a indução da morte celular por apoptose pelo extrato de própolis sugere danos possivelmente menos graves a glândula mamária bovina. Além disso, somente uma pequena variação sazonal foi encontrada para a composição química da propolis do Sul do Brasil, a qual não prejudicou suas
RESUMO
Previous studies have reported on the phytotherapeutic potential of propolis from southern Brazil (Urupema, Santa Catarina State), in particular, its efficacy in the treatment of bovine mastitis. The present study evaluates the effect of seasonal variation on the chemical composition of propolis from southern Brazil and its resultant antimicrobial and cytotoxic activities in the context of treating bovine mastitis. Antimicrobial activity against Staphylococcus aureus was assessed, along with the cytotoxicity and induction of apoptosis in MAC-T bovine mammary epithelial cells. With the exception of spring propolis, the flavonoid quercetin was the main compound present in all samples. The minimum inhibitory concentration (MIC) of propolis against S. aureus from mastitic milk was 140 µg/mL for samples collected during the spring, autumn, and winter seasons, but 280 µg/mL for samples collected in summer. For MAC-T cells, the spring propolis extract was more toxic with an IC50 of 120 µg/mL. However, for 120 µg/mL of spring propolis extract, only 0.77% of necrotic and 37% of apoptotic MAC-T cells were found, respectively. Nonetheless, the induction of cell death through apoptosis by propolis extract suggests less severe damage to bovine mammary glands. Moreover, only negligible seasonal variation was found in the chemical composition of propolis from southern Brazil, and no biological activities were determined to be harmful. Therefore, this propolis shows promise as an alternative to commercial antimicrobials in the control of bovine mastitis, offering support for organic milk production.(AU)
Estudos prévios tem demonstrado o potencial terapêutico da propolis do Sul do Brasil (Urupema, Santa Catarina), em particular no tratamento da mastite bovina. O presente estudo tem como objetivo avaliar o efeito da variação sazonal sobre a composição química da própolis de Urupema do Sul do Brasil e suas atividades antimicrobiana e citotóxica visando o tratamento da mastite bovina. A atividade antimicrobiana contra Staphylococcus aureus foi avaliada, juntamente com a citotoxicidade e indução de apoptose em células epiteliais mamárias bovina da linhagem MAC-T. Com exceção da própolis da primavera, o flavonóide quercetina foi o composto majoritário em todas as amostras. A concentração inibitória mínima (CIM) da propolis contra S. aureus de leite mastítico foi 140 µg/mL para as amostras de primavera, outono e inverno e 280 µg/mL para a amostra coletada no verão. Para as células MAC-T, o extrato de própolis da primavera foi o mais tóxico, sendo a IC50 120 µg/mL. Entretanto, com 120 µg/mL do extrato de própolis primaveril, somente 0,77% de células MAC-T necróticas e 37% apoptóticas foram encontradas. Portanto, a indução da morte celular por apoptose pelo extrato de própolis sugere danos possivelmente menos graves a glândula mamária bovina. Além disso, somente uma pequena variação sazonal foi encontrada para a composição química da propolis do Sul do Brasil, a qual não prejudicou suas atividades biológicas. Portanto, esta própolis mostra como uma alternativa promissora ao uso de antimicrobianos comerciais no controle da mastite bovina e uma opção para subsidiar a produção orgânica de leite.Palavras-chave: Células MAC-T. Mastite bovina. Propolis brasileira. Staphylococcus aureus.(AU)
Assuntos
Animais , Feminino , Bovinos , Staphylococcus aureus/patogenicidade , Mastite Bovina , Própole , Estações do AnoRESUMO
A novel 2-phenoxychromone (1) and five known flavones (2-6) were isolated from northeastern Brazilian propolis in the state of Bahia. The chemical structures of these six compounds were determined by spectroscopic investigations and single-crystal X-ray analysis. The isolated compounds showed growth-inhibitory activities, in varying degrees, against human tumor cell lines. This is the first report on the discovery of a novel 2-phenoxychromone from propolis.
Assuntos
Antineoplásicos/farmacologia , Extratos Vegetais/farmacologia , Própole/química , Antineoplásicos/química , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Humanos , Extratos Vegetais/químicaRESUMO
Propolis is a resinous product produced by honey bees and is known to have antitumor functions. On the other hand, histone deacetylase (Hdac) inhibitors have recently attracted attention for their antitumor effects. In this study, we examined whether Brazilian green propolis has an Hdac inhibitory activity and its contribution on antitumor effects. By in vitro Hdac activity assay, Brazilian propolis extract (BPE) significantly inhibited the enzyme activity. Actually, BPE treatment increased the intracellular histone acetylation in Neuro2a cells. Regarding antitumor effect in Neuro2a cells, BPE treatment significantly decreased cell viability. An Hdac activator theophylline significantly attenuated the effect. Then, we analyzed whether the decreasing effect on cell number was caused by cell death or growth retardation. By live/dead cell staining, BPE treatment significantly increased the dead cell number. By cell cycle analysis, BPE treatment retarded cell cycle at the M-phase. Both of these cellular effects were suppressed by addition of theophylline. These data indicate that BPE induced both cell death and growth retardation via Hdac inhibitory activity. We demonstrated that Brazilian propolis bears regulatory functions on histone acetylation via Hdac inhibition, and the effect contributes antitumor functions. Our data suggest that intake of Brazilian propolis shows preventing effects against cancer.
RESUMO
The present study was conducted in order to evaluate the effect of Brazilian propolis (AF-08; 5, 10, 15, 30, 50, 100, and 200µg/mL) in protecting CHO-K1 cells against genotoxic and cytotoxic damage and clonogenic death induced by (60)Co gamma-radiation (1.0, 2.0, 4.0, and 6.0Gy). For this purpose, three interlinked endpoints were analyzed: induction of DNA damage by use of the micronucleus (MN) test (genotoxic damage), cell viability by means of the MTS assay, and differential staining (cytotoxic damage) and clonogenic death via the colony-formation test (cytotoxic damage). The MN test revealed that propolis alone (5-100µg/mL) was not genotoxic up to 100µg/mL and that 30µg/mL of propolis reduced the radiation-induced DNA damage (â¼56% reduction, p<0.05), exhibiting a radio-protective effect on irradiated CHO-K1 cells. On the other hand, analysis of cytotoxicity showed that a concentration of 50µg/mL presented a significant proliferative effect (p<0.001) when associated with radiation, decreasing the percentage of necrotic cells (p<0.01). No mediated cytotoxic effect was found, but the concentration of 200µg/mL was toxic when analyzed at 24 and 48h via the differential staining technique, but not at 72h after irradiation, analyzed with the MTS assay. Differential staining also showed that necrosis was the main death modality in irradiated cells and that apoptosis was induced only at the toxic concentration of propolis (200µg/mL). Concerning the clonogenic capacity, a concentration of 50µg/mL also exhibited a significant stimulating effect on cell proliferation (p<0.001), in agreement with the data from differential staining. Taken together, these data suggest that the use of propolis AF-08 for the prevention of the adverse effects of ionizing radiation is promising. Nevertheless, additional investigations are necessary for a better understanding of potential applications of propolis to improve human health.
Assuntos
Dano ao DNA/efeitos dos fármacos , Raios gama/efeitos adversos , Micronúcleos com Defeito Cromossômico , Própole/farmacologia , Protetores contra Radiação/farmacologia , Animais , Brasil , Células CHO , Proliferação de Células/efeitos dos fármacos , Proliferação de Células/efeitos da radiação , Sobrevivência Celular/efeitos dos fármacos , Sobrevivência Celular/efeitos da radiação , Radioisótopos de Cobalto , Ensaio de Unidades Formadoras de Colônias , Cricetinae , Cricetulus , Relação Dose-Resposta a Droga , Micronúcleos com Defeito Cromossômico/efeitos dos fármacos , Micronúcleos com Defeito Cromossômico/efeitos da radiação , Própole/administração & dosagem , Protetores contra Radiação/administração & dosagemRESUMO
Propolis is a resin that bees collect from different plant sources and use in the defense of the bee community. The intricate composition of propolis varies depending on plant sources from different geographic regions and many types have been reported. Red coloured propolis found in several states in Brazil and in other countries has known antimicrobial and antioxidant activity. Different analytical methods have been applied to studies regarding the chemical composition and plant origins of red propolis. In this study samples of red propolis from different regions have been characterised using direct infusion electrospray ionisation mass spectrometry (ESI(-)-MS) fingerprinting. Data from the fingerprints was extracted and analysed by multivariate analysis to group the samples according to their composition and marker compounds. Despite similar colour, the red coloured propolis samples were divided into three groups due to contrasting chemical composition, confirming the need to properly characterise the chemical composition of propolis.
Assuntos
Própole/química , Animais , Biomarcadores/análise , Brasil , Cor , Espectrometria de Massas por Ionização por ElectrosprayRESUMO
Própolis é uma substância resinosa produzida por Apis mellifera, contendo principalmente resinas vegetais e cera das próprias abelhas. É usada na colmeia para diversas finalidades, como vedar aberturas, reparar as células e envolver invasores que foram mortos na colméia, além de contribuir para a quase constância da temperatura dentro da colmeia (28 - 30oC). A própolis é importante para as abelhas, pois é responsável pela manutenção de um ambiente quase estéril, agindo contra bactérias, fungos e até larvas invasoras. Em virtude do amplo espectro de atividades biológicas e farmacológicas associadas a esse produto, a própolis vem sendo extensivamente utilizada em medicina alternativa, bem como na indústria cosmética e alimentícia. Apesar dos numerosos estudos já realizados com própolis, os poucos que foram feitos visando ao uso em veterinária relacionavam-se a combate de endoparasitas. Muitas doenças de animais vêm acometendo o homem atualmente, tais como as transmitidas pelos carrapato vermelho do cão (Rhipicephalus sanguineus) e carrapato-estrela (Amblyomma cajennense). Problemas de saúde para o gado e queda da produtividade pecuária é causada pelo carrapato do boi (Rhipicephalus microplus). Além disso, é crescente o interesse de profissionais veterinários pelo uso de produtos naturais, sobretudo em relação aos animais domésticos. Vale lembrar que o uso indiscriminado de acaricidas levou à seleção de carrapatos resistentes, de modo que outras estratégias para o controle dessas pragas são de grande importância. Com isso, o intuito do presente projeto foi a determinação da atividade de extratos brutos de própolis brasileira e seus constituintes no controle de carrapatos específicos e generalistas. Foram preparados extratos clorofórmicos de amostras de própolis verde de Lavras (MG) e própolis preta de Picos (PI), anteriormente analisadas quimicamente. [...]
Propolis is a resinous substance produced by bees Apis mellifera, containing mainly plant exudates and bee waxes. It is used in the hive to close holes, repair cells and involve intruders that are killed inside the hive. Propolis is important to the bees, as it is responsible for the maintenance of the hive as a sterile environment, acting against bacteria, fungus and even invading larvae. Because of the wide range of biological and pharmacological activities of propolis, it has been extensivelly used in alternative medicine, as well as in cosmetic and food industries. However, few studies have been developed concerning the use of propolis to animal health. Nowadays, many animal diseases have affected humans, such as those transmited by ticks, the brown dog tick (Rhipicephalus sanguineus) and the star tick (Amblyomma cajennense). Cattle health problems and decrease of livestock productivity is caused by the cattle tick (Rhipicephalus microplus). In addition, the interest of veterinary professionals toward the use of natural products to animal health is increasing, mainly for the treatment of domestic animals. It is worth remembering that the indiscriminate use of acaricides leads to resistence selection. Thus, new strategies are of great importance for tick control. Hence, the aim of this project was to determine the activity of crude extracts of Brazilian propolis and their constituents for the control of specific and generalist ticks. Chloroform extracts were prepared from samples of green propolis from Lavras (state of Minas Gerais) and black propolis from Picos (state of Piauí), previously analyzed chemically. [...]
Assuntos
Animais , Acaricidas/análise , Controle de Ácaros e Carrapatos/métodos , Própole/administração & dosagem , Rhipicephalus/crescimento & desenvolvimento , Bioensaio/veterinária , Cromatografia Líquida/veterináriaRESUMO
Biological assays that have been performed on different types of Brazilian propolis have shown that type 6 propolis (G6) has a strong antimicrobial activity and a low flavonoid content. This study aimed to evaluate the correlation between the phenolic composition and the biological activities displayed by propolis G6 from the state of Bahia and green propolis, also known as type 12 (G12). The values of the flavonoids and the total phenolics in propolis G6 were different than those in propolis G12. Although the G12 variety presented greater antioxidant activity, propolis G6 proved to have greater antimicrobial and cytotoxic activities. The results showed that the phenolic compounds may not be the only compounds responsible for the biological activity. More detailed studies of the chemical composition and an assessment of the biological activity are required to establish the quality of propolis.
Ensaios biológicos realizados com diferentes tipos de própolis brasileira têm mostrado que a própolis do tipo 6 (G6) tem forte atividade antimicrobiana e menor teor de flavonóides. Este trabalho teve como objetivo avaliar a correlação entre a composição fenólica e atividades biológicas apresentadas pela própolis G6, do Estado da Bahia, e a própolis verde, do tipo 12 (G12). Os teores de flavonóides e fenólicos totais na própolis G6 foram diferentes dos teores da própolis G12. Apesar da G12 apresentar maior atividade antioxidante, a própolis G6 apresenta maior atividade antimicrobiana e citotóxica. Os resultados mostraram que os compostos fenólicos não são os únicos compostos responsáveis pela atividade biológica da própolis. Estudos mais específicos da composição química, em adição à avaliação das atividades biológicas, são requeridos para determinar a qualidade da própolis.
Assuntos
Própole/análise , Bioensaio/classificação , Compostos Fenólicos/análise , Própole/farmacocinética , Flavonoides/classificaçãoRESUMO
Propolis is one of the hive products that has been used extensively in folk medicine, due to its several biological and pharmacological properties. Besides, propolis-containing products have been intensely marketed by the pharmaceutical industry and health-food stores. This work was carried out in order to investigate whether propolis treatment could revert the metabolic alterations of streptozotocin-induced diabetic rats. Animals were kept in metabolic cages and diabetes was induced by a single dose of streptozotocin (35 mg/kg, IV). After a week, rats with glycemia higher than 230 mg/dL were divided into two groups and treated with ethanolic extract of propolis (10 and 90 mg/kg, PO) for seven days. Glycemia and free fatty acids were determined, as well as food and water intake, body weight and urine volume were registered weekly. Data showed no significant differences in the analyzed variables. Based on these results, one may conclude that propolis had no effects after diabetes establishment, in our conditions assays. Further assays with different concentrations of propolis and periods of administration should be carried out in order to evaluate its therapeutic potential in this disease.
RESUMO
Propolis is one of the hive products that has been used extensively in folk medicine, due to its several biological and pharmaeological properties. Besides, propolis-containing products have been intensely marketed by the pharmaceutical , industry and health-food stores. This work was carried out in order to investigate whether propolis treatment could revert the metabolic alterations of streptozotocin-induced diabetic rats. Animais were kept in metabolic cages and diabetes was induced by a single dose of streptozotocin (35 mg/kg, IV). After a week, rats with glicemia higher than 230 mg/dL were divided into two groups and treated with ethanolic extract of propolis (10 and 90 mg/kg, PO) for seven days. Glycemia and free fatty acids were determined, as well as food and water intake, body weight and, urine were registered weekly. Data showed no significant differences in the analyzed variables. Based on these results, one may conclude that propolis had no effects after diabetes establishment, in our conditions assays. Further assays with different concentrations of propolis and periods of administration should be carried out in order to evaluate its therapeutic potential in this disease
Assuntos
Animais , Masculino , Ratos , Diabetes Mellitus Experimental/induzido quimicamente , Própole/uso terapêutico , EstreptozocinaRESUMO
Propolis is a natural resinous substance collected by bees from vegetal sources and its therapeutic properties have been investigated. In this work, we evaluated the inhibitory activity of ethanolic extracts of propolis (EEP) from the Southeast and South of Brazil on coagulase-negative Staphylococcus (CNS) growth as well as the EEP in vitro synergism with antimicrobial drugs by using the diffusion method (E-test). The EEP chemical characteristics (dry weight, pH, flavonoid and phenolic compounds) were determined. Seven drugs were tested, and synergism was observed between three drugs and Southeast EEP, six drugs and South EEP, and one drug and ethanol control. Ethanolic extracts of propolis from the South of Brazil presented the greatest flavonoid content and synergism rate, while EEP from the Southeast presented the greatest anti-CNS activity and phenolic compound content. Results showed the correlation among anti-CNS activity, synergism rate and chemical characteristics of propolis.