Própolis vermelha e ação antifúngica: potencialidades e desafios / Red própolis and antifungal activity: potentialities and challenges / Propóleo rojo y acción antifúngica: potencialidades y desafíos

Introdução: a própolis é uma composição resinosa produzida por abelhas e utilizada em suas colmeias contra microrganismos. Existem diversos tipos desse composto, sendo o de coloração vermelha o último espécime relatado na literatura. Assim, dentre suas aplicabilidades, a atividade antifúngica da própolis vermelha tem sido explorada com vistas a ampliar sua ação terapêutica. Objetivo: explorar estudos acerca da ação antifúngica da própolis vermelha, identificando suas potencialidades e desafios. Metodologia: foi realizada uma revisão integrativa nas bases de dados bibliográficos MEDLINE (via PubMed), SciELO e Google Acadêmico, complementada por uma diligência nas bases de ensaios clínicos ReBEC e Clinical Trials. Em seguida todos os estudos selecionados foram explorados para obtenção do cenário atual sobre o tema. Resultados: foram incluídos 08 estudos, sendo 01 deles um ensaio clínico. Os estudos comprovam a ação antifúngica da própolis vermelha, principalmente contra Candida spp. e Paracoccidioides brasiliensis, e evidenciam a maior potência fungicida deste composto em detrimento de outros tipos de própolis. Conclusão: a ação antifúngica da própolis vermelha mostra-se uma potencialidade em diversos estudos. Entretanto, o volume de pesquisas científicas relativas a esse tema é insuficiente e a complexidade desse composto configura-se como um desafio à sua aplicabilidade.

Introduction: propolis is a resinous composition produced by compounds and used in their hives against microorganisms. There are several types of this compound, the red one is the last specimen reported in the literature. Thus, among its applicability, the antifungal activity of red propolis has been explored as a path to expand its therapeutic action. Objective: to explore studies about the antifungal action of red propolis, identifying its potentialities and challenges. Methodology: Na integrative review was carried out in the bibliographic databases MEDLINE (via PubMed), SciELO and Google Scholar, complemented by a diligence in ReBEC and Clinical Trials databases. Then, all selected studies were explorers to obtain the current scenario on the subject. Results: 08 studies were included, which 01 of them was a clinical trial. Studies prove the antifungal action of red propolis, mainly against Candida spp. and Paracoccidioides brasiliensis, and show the greater fungicidal power of this compound compared to other types of propolis. Conclusion: the antifungal action of red propolis shows potential in several studies. However, the volume of scientific research on this theme is insufficient and the complexity of this compound represents a challenge to its applicability.

Introducción: el propóleo es una composición resinosa producida por las abejas y utilizada en sus colmenas contra los microorganismos. Existen varios tipos de este compuesto, siendo el rojo el último ejemplar reportado en la literatura. Así, entre sus posibilidades de aplicación, se ha explorado la actividad antifúngica del propóleo rojo con vistas a ampliar su acción terapéutica. Objetivo: explorar estudios sobre la acción antifúngica del propóleo rojo, identificando sus potencialidades y desafíos. Metodología: Se realizó una revisión en las bases de datos bibliográficas MEDLINE (vía PubMed), SciELO y Google Scholar, complementada con una diligencia en las bases de datos de ensayos clínicos ReBEC y Clinical Trials. Luego se exploraron todos los estudios seleccionados para obtener el escenario actual sobre el tema. Resultados: Se incluyeron 08 estudios, 01 de los cuales fue un ensayo clínico. Los estudios demuestran la acción antifúngica del propóleo rojo, principalmente contra Candida spp. y Paracoccidioides brasiliensis, y muestran el mayor poder fungicida de este compuesto en detrimento de otros tipos de propóleos. Conclusión: la acción antifúngica del propóleo rojo muestra potencial en varios estudios. Sin embargo, el volumen de investigación científica sobre este tema es insuficiente y la complejidad de este compuesto representa un desafío para su aplicabilidad.

Evaluación de la fibrogénesis hepática en pacientes con esteatohepatitis no alcohólica tratados con propóleos rojo oral cubano / Evaluation of hepatic fibrogenesis in patients with nonalcoholic steatohepatitis treated with cuban oral red propolis

Introducción: La enfermedad por depósito graso no alcohólica constituye una pandemia del mundo contemporáneo. Su espectro silente atraviesa estadios de cronicidad y puede llegar a la cirrosis hepática y sobre esta pudiera desarrollarse un hepatocarcinoma. No existen tratamientos y solo se puede actuar sobre los factores de riesgo. Objetivo: Evaluar el efecto citohepatoprotector y antifibrótico del propóleos rojo cubano oral en pacientes con esteatohepatitis no alcohólica. Métodos: Se realizó un estudio longitudinal prospectivo en pacientes seleccionados de las consultas de Gastroenterología, Endocrinología y Medicina Interna del Hospital Clínico Quirúrgico Hermanos Ameijeiras durante el periodo de abril 2017 a abril 2018. El universo de estudio fue de 120 pacientes con diagnóstico imagenológico de hígado graso. La muestra quedó conformada por 70 pacientes con diagnóstico de hígado graso, y que cumplieron criterios de inclusión y exclusión. Las pruebas estadísticas aplicadas fueron análisis de frecuencia y porcentaje para las variables demográficas. La prueba T para las muestras relacionadas evaluó el comportamiento enzimático al inicio y al final del tratamiento y los cambios elastográficos fueron analizados mediante test de Kappa y porcentaje. Resultados: Las variables bioquímicas estudiadas mostraron una disminución estadísticamente significativa al final del tratamiento. Los cambios elastográficos al final del estudio evidenciaron la efectividad del tratamiento, en el cual el 91,4 por ciento de los pacientes evolucionaron hacia el menor grado de fibrosis. Conclusiones: El propóleos rojo cubano demostró ser un apifármaco con acción citohepatoprotectora y antifibrótica de valor terapéutico(AU)

Introduction: Nonalcoholic fat deposition disease is a pandemic in the contemporary world. Its silent spectrum goes through stages of chronicity and it can reach liver cirrhosis and on this a hepatic carcinoma could develop. There are no treatments and medical handling can act on only risk factors. Objective: To evaluate cytohepatoprotective and antifibrotic effect of oral Cuban red propolis in patients with nonalcoholic steatohepatitis. Methods: A prospective longitudinal study was carried out in selected patients from the Gastroenterology, Endocrinology and Internal Medicine consultations at Hermanos Ameijeiras Clinical Surgical Hospital from April 2017 to April 2018. The study universe was 120 patients with imaging diagnosis of fatty liver. The sample consisted of 70 patients with fatty liver diagnosis, who met the inclusion and exclusion criteria. Frequency and percentage analysis for the demographic variables were the statistical tests applied. The T test for the related samples evaluated the enzymatic behavior at the beginning and at the end of the treatment and the elastography changes were analyzed using Kappa and percentage tests. Results: The biochemical variables studied showed statistically significant decrease at the end of the treatment, which evidenced the effectiveness of the treatment. 91.4 percent of the patients progressed to a lower degree of fibrosis. Conclusions: Cuban red propolis proved to be a therapeutic drug with cytohepathoprotective and antifibrotic action(AU)

Hepatoprotective and antineoplastic potencial of red propolis produced by the bees Apis mellifera in the semiarid of Rio Grande do Norte, Brazil / Potencial hepatoprotetor e antineoplásico da própolis vermelha produzida pela abelha Apis mellifera no semiárido do Rio Grande do Norte, Brasil

The objective of this study was to evaluate the hepatoprotective effect of the honey bee Apis mellifera ethanolic extract of the red propolis, obtained in four municipalities of the Rio Grande do Norte semi-arid region, through an in vitro evaluation of the antineoplastic potential in human hepatic carcinoma (HepG2) and normal cell lines (L929), and from the comet assay in hepatic cell lines (ZF-L hepatocytes) to evaluate the genoprotective potential of the extract. The hepatoprotective effect was also evaluated in vivo by the induction of chronic experimental hepatic lesions in rodents (Rattus norvegicus Berkenhout, 1769), Wistar line, by intraperitoneal administration of thioacetamide (TAA) at the dose of 0.2g/kg. The animals were distributed in the following experimental groups: G1 (control), G2 (treated with 500mg/kg ethanolic extract of propolis), G3 (treated with 500mg/kg of ethanolic extract and TAA) and G4 (treated with TAA). All rats were submitted to serum biochemical, macroscopic, histological and stereological biochemical exams of the liver. It was verified the genoprotective effect of red propolis since the mean damages promoted to DNA in cells tested with the extract were significantly lower than the mean of the positive control damage (hydrogen peroxide). The red propolis extract did not present cytotoxic activity to the tumor cells of human liver cancer, as well as to normal ones. The absence of cytotoxicity in normal cells may indicate safety in the use of the propolis extract. The results of the serum biochemical evaluation showed that the serum levels of the aminotransferase enzymes (AST) did not differ significantly between G1, G2 and G3 when compared to each other. G4 showed significant increase in levels compared to the other groups, indicating that the administration of the extract did not cause liver toxicity, as well as exerted hepatoprotective effect against the hepatic damage induced by TAA. The G3 and G4 animals developed cirrhosis, but in G3 the livers were characterized by the presence of small regenerative nodules and level with the surface of the organ, whereas in G4 the livers showed large regenerative nodules. The livers of the G1 and G2 animals presented normal histological appearance, whereas the livers of the G3 animals showed regenerative nodules surrounded by thin septa of connective tissue, and in G4 the regenerative nodules were surrounded by thick septa fibrous connective tissue. The analysis of the hepatic tissues by means of stereology showed that there was no statistical difference between the percentage of hepatocytes, sinusoids, and collagens in G1 and G2. In G3 the percentage of hepatocytes, sinusoids, and collagen did not differ significantly from the other groups. It was concluded that the ethanolic extract of the red propolis exerted a hepatoprotective effect, because it promoted in vitro reduction of the damage to the DNA of liver cells, antineoplastic activity in human hepatocellular carcinoma cell line (HepG2) and did not exert cytotoxic effect in normal cells or was able to reduce liver enzyme activity and the severity of cirrhosis induced by TAA in vivo.(AU)

Este estudo objetivou avaliar o efeito hepatoprotetor do extrato etanólico da própolis vermelha da abelha Apis mellifera, obtido em quatro municípios do semiárido do Rio Grande do Norte, mediante avaliação in vitro do potencial antineoplásico em linhagens de células de carcinoma hepático humano (HepG2) e em linhagens de células normais (L929), além do ensaio cometa em linhagens de células hepáticas (hepatócitos ZF-L) para avaliar o potencial genoprotetor do extrato. O efeito hepatoprotetor também foi avaliado in vivo através da indução de lesões hepática experimental crônica em roedores da espécie Rattus norvegicus (Berkenhout, 1769), linhagem Wistar, pela administração intraperitoneal de tioacetamida (TAA) na dose de 0,2g/kg. Os animais foram distribuídos nos seguintes grupos experimentais: G1 (controle), G2 (tratados com 500mg/kg de extrato etanólico da própolis), G3 (tratados com 500mg/kg de extrato etanólico e TAA) e G4 (tratados com TAA). Todos os ratos foram submetidos aos exames bioquímico sérico, anatomopatológico macroscópico, histológico e esteriológico do fígado. Foi constatado o efeito genoprotetor da própolis vermelha uma vez que as médias dos danos promovidos ao DNA em células testadas com o extrato foram significativamente inferiores à média dos danos do controle positivo (peróxido de hidrogênio). O extrato da própolis vermelha não apresentou atividade citotóxica para células tumorais de câncer de fígado humano, bem como para normais. A ausência de citotoxicidade em células normais, tal como constatado, pode indicar segurança no uso do extrato da própolis. Os resultados da avaliação bioquímica sérica demonstraram que os níveis séricos das enzimas aminotransferase (AST) não diferiram significativamente entre G1, G2 e G3, quando comparadas entre si. No G4 houve aumento significativo dos níveis em relação aos demais grupos, indicando que a administração do extrato não causou toxicidade hepática, bem como exerceu efeito hepatoprotetor frente ao dano hepático induzido pela TAA. Os animais dos G3 e G4 desenvolveram cirrose, porém no G3 os fígados caracterizaram-se pela presença de pequenos nódulos regenerativos e nivelados com a superfície do órgão, enquanto que no G4 os fígados apresentaram grandes nódulos regenerativos. Os fígados dos animais G1 e G2 apresentaram aspecto histológico normal, enquanto que os fígados dos animais do G3 apresentaram nódulos regenerativos circundados por finos septos de tecido conjuntivo, e nos do G4 os nódulos regenerativos foram circundados por espessos septos de tecido conjuntivo fibroso. A análise dos tecidos hepáticos por meio de estereologia mostrou que não houve diferença estatística entre o percentual de hepatócitos, sinusoides e colágenos nos G1 e G2. No G3 o percentual de hepatócitos, sinusoides e colágeno não diferiu significativamente dos demais grupos. Concluiu-se que o extrato etanólico da própolis vermelha exerceu efeito genoprotetor, por promover in vitro redução do dano ao DNA de células hepáticas, atividade antineoplásica em linhagem celular de carcinoma hepatocelular humano (HepG2) e não exerceu efeito citotóxico em células normais ou efeito hepatoprotetor in vivo com diminuição da gravidade da cirrose induzida por TAA.(AU)

Photoprotective activity and increase of SPF in sunscreen formulation using lyophilized red propolis extracts from Alagoas

ABSTRACT The excessive sun exposure, coupled with lack of sun protection represents one of the biggest risks to the occurrence of skin cancer and photoaging. Recent strategies for photoprotection have included the incorporation of natural antioxidant and anti-inflammatory compounds, into sunscreens, and the oral administration of natural antioxidant extracts. In this work, we use Brazilian red propolis extract because its antioxidant and anti-inflammatory activities. The aim of this work was to evaluate the sun protection factor and antioxidant activity of different hydroalcoholic extracts of red propolis (70% and 75%) prepared from lyophilized red propolis at room and high temperatures. The sun protection factor in vitro was determined by a spectrophotometric method developed by Mansur. The hydroalcoholic extracts of red propolis incorporated with Filter UVA-UVB 5% Gel Permulem TR-1 presented absorption in the UVB region. Also, the in vitro capacity of the hydroalcoholic extracts of red propolis to increase photoprotective activity of Filter UVA-UVB 5% Gel was evaluated. The hydroalcoholic extracts of red propolis incorporated presented higher values of sun protection factor and showed synergism in the photoprotective activity of Filter UVA-UVB 5% Gel Permulem TR-1. The antioxidant activity and sun protection factor are correlated with total phenolics content of the extracts and the hydroalcoholic extract of red propolis 75% at room temperature was choosen. The formulation developed with Filter UVA-UVB 5% Gel Permulem TR-1 with this hydroalcoholic extract of red propolis showed safe to be applied on the skin according HET-CAM test. Suggests indication of hydroalcoholic extract of red propolis (75% - room temperature) associated to photoprotective formulations for use in photoprotective products.

Phenolic Composition and Leishmanicidal Activity of Red Propolis and Dalbergia ecastaphyllum (L.) Taub (Fabaceae) Extracts from Sergipe, Brazil

ABSTRACT Leishmaniasis is a parasitic disease caused by protozoa of the Leishmania genus. It may manifest in visceral and tegumentary forms, and pentavalent antimonials are the first choice drugs used for the treatment. Frequently these drugs show low efficiency and high toxicity to mammalian host. The present study describes the chemical profile and the in vitro leishmanicidal effects of red propolis and Dalbergia ecastaphyllum extracts from Sergipe, Brazil, in Leishmania chagasi and Leishmania amazonensis promastigotes. The phenolic composition of the extracts was evaluated by direct infusion electrospray ionization mass spectrometry (ESI-MS) fingerprinting. The leishmanicidal effect was evaluated by the Resazurin colorimetric method. Similar composition profiles have been found for D. ecastaphyllum and propolis samples. The isoflavones formononetin, biochanin A, daidzein and pinocembrin were identified in both extracts. Propolis extract showed leishmanicidal activity in both L. chagasi and L. amazonensis, with IC50 values of 21.54 and 9.73 µg/mL, respectively. The D. ecastaphyllum extract presented activity only in L. amazonensis, with IC50 of 53.42 µg/mL. These results suggest that red propolis extract from Sergipe has the leguminosae D. ecastaphyllum as botanical origin, and that it presents potential leishmanicidal activity, which may be associated with the presence of the phenolic compounds found in its composition.

Red propolis: Chemical composition and pharmacological activity

Propolis has been used worldwide for years in folk medicine and currently marketed by the pharmaceutical industry. In Brazil, propolis was classified into 13 groups based on their organoleptics and physicochemical characteristics. The 13th type named red propolis has been an important source of investigation since late 90s. Their property comes from the countless compounds, including terpenes, pterocarpans, prenylated benzophenones and especially the flavonoids. This last compound class has been indicated as the responsible for its potent pharmacological actions, highlighting the antimicrobial, anti-inflammatory, antioxidant, healing and antiproliferative activities. The red propolis can also be found in other countries, especially Cuba, which has similar features as the Brazilian. Therefore, with the compilation of 80 papers, this review aims to provide a key reference for researchers interested in natural products and discovery of new active compounds, such as from propolis.

Chemical and microbiological characterization of tinctures and microcapsules loaded with Brazilian red propolis extract / 药物分析学报

The aim of this study was to characterize tinctures and microcapsules loaded with an ethanol extract of red propolis through chemical, physicochemical and microbiological assays in order to establish quality control tools for nutraceutical preparations of red propolis. The markers (isoflavonoids, chalcones, pterocarpans, flavones, phenolic acids, terpenes and guttiferones) present in the tinctures A and B were identified and confirmed using LC/ESI/FTMS/Orbitrap. Four compositions (A, B, C and D) were prepared to contain B tincture of the red propolis with some pharmaceutical excipients and submitted to two drying processes, i. e. spray-drying and freeze-drying to obtain microcapsules loaded with the red propolis extract. The tinctures and microcapsules of the red propolis were submitted to the total flavonoid content and antioxidant activity tests. The antibacterial activity and minimum inhibitory concentration (MIC) were tested using Staphylococcus aureus ATCC 25293 and Pseudomonas aeruginosa ATCC 27853 strains. The tinctures and microcapsules presented high flavonoid quantities from 20.50 to 40.79 mg/100 mg of the microcapsules. The antioxidant activity and IC50 were determined for the tinctures A and B (IC50: 6.95 μg/mL and 7.48 μg/mL), the spray-dried microcapsules (IC50: 8.89–15.63 μg/mL) and the freeze-dried microcapsules (IC50: 11.83–23.36 μg/mL). The tinctures and microcapsules were proved to be bioactive against gram-positive and gram-negative bacteria with inhibition halos superior to 10 mm at concentration of 200 μg/mL and MIC values of 135.87–271.74 μg/mL using gram-positive strain and 271.74–543.48 μg/mL using gram-negative strain. The tinctures and microcapsules of the red propolis have a potential application for nutraceutical products.

Red propolis:Chemical composition and pharmacological activity

Propolis has been used worldwide for years in folk medicine and currently marketed by the pharmaceutical industry. In Brazil, propolis was classified into 13 groups based on their organoleptics and physicochemical characteristics. The 13th type named red prop-olis has been an important source of investigation since late 90s. Their property comes from the countless compounds, including terpenes, pterocarpans, prenylated benzophe-nones and especially the flavonoids. This last compound class has been indicated as the responsible for its potent pharmacological actions, highlighting the antimicrobial, anti-inflammatory, antioxidant, healing and antiproliferative activities. The red propolis can also be found in other countries, especially Cuba, which has similar features as the Brazilian. Therefore, with the compilation of 80 papers, this review aims to provide a key reference for researchers interested in natural products and discovery of new active compounds, such as from propolis.

Chemical and microbiological characterization of tinctures and microcapsules loaded with Brazilian red propolis extract / 药物分析学报

The aim of this study was to characterize tinctures and microcapsules loaded with an ethanol extract of red propolis through chemical, physicochemical and microbiological assays in order to establish quality control tools for nutraceutical preparations of red propolis. The markers (isoflavonoids, chalcones, pterocarpans, flavones, phenolic acids, terpenes and guttiferones) present in the tinctures A and B were identified and confirmed using LC/ESI/FTMS/Orbitrap. Four compositions (A, B, C and D) were prepared to contain B tincture of the red propolis with some pharmaceutical excipients and submitted to two drying processes, i. e. spray-drying and freeze-drying to obtain microcapsules loaded with the red propolis extract. The tinctures and microcapsules of the red propolis were submitted to the total flavonoid content and antioxidant activity tests. The antibacterial activity and minimum inhibitory concentration (MIC) were tested using Staphylococcus aureus ATCC 25293 and Pseudomonas aeruginosa ATCC 27853 strains. The tinctures and microcapsules presented high flavonoid quantities from 20.50 to 40.79 mg/100 mg of the microcapsules. The antioxidant activity and IC50 were determined for the tinctures A and B (IC50: 6.95 μg/mL and 7.48 μg/mL), the spray-dried microcapsules (IC50: 8.89–15.63 μg/mL) and the freeze-dried microcapsules (IC50: 11.83–23.36 μg/mL). The tinctures and microcapsules were proved to be bioactive against gram-positive and gram-negative bacteria with inhibition halos superior to 10 mm at concentration of 200 μg/mL and MIC values of 135.87–271.74 μg/mL using gram-positive strain and 271.74–543.48 μg/mL using gram-negative strain. The tinctures and microcapsules of the red propolis have a potential application for nutraceutical products.

Isoflavone formononetin from red propolis acts as a fungicide against Candida sp

Abstract A bioassay-guided fractionation of two samples of Brazilian red propolis (from Igarassu, PE, Brazil, hereinafter propolis 1 and 2) was conducted in order to determine the components responsible for its antimicrobial activity, especially against Candida spp. Samples of both the crude powdered resin and the crude ethanolic extract of propolis from both locations inhibited the growth of all 12 tested Candida strains, with a minimum inhibitory concentration of 256 µg/mL. The hexane, acetate and methanol fractions of propolis 1 also inhibited all strains with minimum inhibitory concentration values ranging from 128 to 512 µg/mL for the six bacteria tested and from 32 to 1024 µg/mL for the yeasts. Similarly, hexane and acetate fractions of propolis sample 2 inhibited all microorganisms tested, with minimum inhibitory concentration values of 512 µg/mL for bacteria and 32 µg/mL for yeasts. The extracts were analyzed by HPLC and their phenolic profile allowed us to identify and quantitate one phenolic acid and seven flavonoids in the crude ethanolic extract. Formononetin and pinocembrin were the major constituents amongst the identified compounds. Formononetin was detected in all extracts and fractions tested, except for the methanolic fraction of sample 2. The isolated isoflavone formononetin inhibited the growth of all the microorganisms tested, with a minimum inhibitory concentration of 200 µg/mL for the six bacteria strains tested and 25 µg/mL for the six yeasts. Formononetin also exhibited fungicidal activity against five of the six yeasts tested. Taken together our results demonstrate that the isoflavone formononetin is implicated in the reported antimicrobial activity of red propolis.

Efecto del tratamiento con extracto de propóleos rojo oral en la esteatohepatitis no alcohólica / Effect of treatment with oral red propolis extract on nonalcoholic teatohepatitis

Introducción: la esteatohepatitis no alcohólica es frecuente y puede evolucionar hacia la cirrosis. Sus opciones de tratamiento farmacológico son poco eficaces. Se conoce que los propóleos tienen acción antioxidante y antiinflamatoria y se han reportado efectos beneficiosos de los propóleos. Objetivo: identificar los cambios histológicos hepáticos en pacientes con esteatohepatitis tratados con extracto hidroalcohólico al 5 por ciento de propóleos rojo oral cubano durante un año. Métodos: se realizó un ensayo clínico aleatorizado, a doble ciegas, con grupo control, en 40 individuos de ambos sexos, entre 20 y 65 años, con índice de Kleiner entre 6 y 8, divididos en 2 grupos: propóleos y placebo. Las pruebas estadísticas aplicadas fueron chi-cuadrado y la prueba no paramétrica. Resultados: el Kleiner total en el grupo propóleos se redujo de 6 ± 0,65 a 3,15 ± 071 y en el grupo placebo de 6 ± 0,65 a 6,1 ± 0,97. En el grupo propóleos se redujeron la esteatosis, inflamación, balonamiento y fibrosis y los cambios en las enzimas hepáticas y las lipoproteínas plasmáticas fueron favorables. Conclusiones: el propóleos rojo puede ser una alternativa terapéutica para detener la progresión de la esteatohepatitis...

Introduction: nonalcoholic steatohepatitis is a common condition which may lead to cirrhosis. The existing drug therapy options are not very effective. It is a well known fact that propolis has an antioxidant and antiinflammatory effect. Reports on the benefits of propolis may be found in the literature. Objective: identify histological hepatic changes in patients with steatohepatitis treated with 5 percent hydroalcoholic oral extract of Cuban red propolis for a year. Methods: a double-blind randomized controlled clinical trial was conducted with 40 patients of both sexes aged 20-65 with 6-8 Kleiner index, who were divided in 2 groups: propolis and placebo. Statistical analysis was based on chi-square and nonparametric tests. Results: total Kleiner decreased from 6 ± 0.65 to 3.15 ± 071 in the propolis group and from 6±0.65 to 6.1±0.97 in the placebo group. In the propolis group there was also a decrease in steatosis, inflammation, ballooning and fibrosis. Changes in liver enzymes and plasmatic lipoproteins were favorable. Conclusions: red propolis may be a therapeutic alternative to stop the progress of esteatohepatitis...

Inhibition of Saccharomyces cerevisiae Pdr5p by a natural compound extracted from Brazilian Red Propolis

Multidrug resistance of cancer cells and pathogenic microorganisms leading to the treatment failure of some forms of cancer or life-threatening bacterial or fungal infections is often caused by the overexpression of multidrug efflux pumps belonging to the ATP-binding cassette transporters superfamily. The multidrug resistance of fungal cells often involves the overexpression of efflux pumps belonging to the pleiotropic drug resistance (PDR) family of ABC transporters. Possibly the best-studied fungal PDR transporter is the multidrug resistance transporter Pdr5p of Saccharomyces cerevisiae. Some research groups have been searching for new inhibitors of these efflux pumps in order to alleviate resistance. Natural products are a great source for the discovery of new compounds with biological activity. Propolis is a complex resinous material collected by honeybees from exudates and buds of certain plant sources and this material is thought to serve as a defense substance for bee hives. Propolis is widely used in traditional medicine and is reported to have a broad spectrum of pharmacological properties. Literature reported some biological functionalities of propolis, such as antibacterial, antiviral, fungicidal, anti-inflammatory and anti-carcinogenic activities. The chemical composition of propolis is qualitatively and quantitatively variable. Components isolated from methanolic extract of red Brazilian propolis (Alagoas, Northeast of Brazil) are isoflavonoids (including pterocarpans, isoflavans, isoflavones), flavanones and polyprenylated benzophenones. In this work we demonstrated the effects of five different isolated compounds on the ATPase activity of Pdr5p. Out of all five substances tested, only BRP-1 was able to completely abolish the enzymatic activity while others worked as positive modulators of the enzyme activity. BRP-1also inhibited the efflux of Rhodamine 6G from yeast cells overexpressing Pdr5p. Taken together, these results demonstrate that Brazilian propolis could be a source of promising compounds that can alleviate the MDR phenomenon, particularly in some fungi, where it could be used as an adjuvant for the treatment with azoles.

Variabilidade sazonal dos constituintes da própolis vermelha e bioatividade em Artermia salina / Seasonal variability of red propolis constituents and brine shrimp bioassay

A própolis é uma substância resinosa coletada pelas abelhas de diversas partes das plantas. Sua composição depende da época, vegetação e local de coleta. Apresenta diversas atividades biológicas como antimicrobiana, antioxidante, antitumoral, dentre outras. Foi realizado estudo da variabilidade sazonal, nos meses de fevereiro, junho e outubro de 2006, dos constituintes voláteis da própolis vermelha de Pernambuco através da extração por headspace dinâmico e identificação por cromatografia gasosa acoplada com espectrometria de massas (CG-EM). Foram identificados 34 constituintes voláteis, sendo monoterpenos e monoterpenóides, sesquiterpenos e sesquiterpenóides, fenilpropanóides, aldeídos, cetonas e η-alcanos. Os constituintes majoritários foram o trans-anetol, α-copaeno e o metil cis-isoeugenol. Também foi realizado o perfil fitoquímico por cromatografia em camada delgada (CCD), através da qual os constituintes fenólicos foram identificados como majoritários. Com o extrato bruto metanólico da própolis, realizou-se o ensaio de letalidade em Artemia salina, que demonstrou DL50 de 18,9 µg/mL, sugerindo uma possível atividade antitumoral.

Propolis is a resinous hive product collected by honeybees from plant sources. The composition of the propolis depends on the season, the vegetation, and the area of collection. It presents a diverse biological activities such as antimicrobial, antioxidant and antitumoral. The seasonal variability of the red propolis constituents from Pernambuco State were accomplished in the months of February, June and October of 2006. The volatile red propolis constituients were captured by the dynamic headspace technique and analyzed by GC-MS. In the analysis of the samples, 34 constituents were identified as the mono and sesquiterpens, phenylpropanoids, aldehydes, cetons and n-alcanes, presenting as majority constituents the trans-anethol, α-copaene and methyl cis-isoeugenol. The phytochemistry profile was performed by thin layer chromatography (TLC). Through this technique the majority constituents were identified as phenols. The Brine shrimp bioassay was used to evaluate of the red propolis methanolic extract, which demonstrated a DL50 of 18.9 µg/mL and an activity antitumoral was possibly suggested.