Effects of liquid extract from Plinia cauliflora fruits residues on Chinese hamsters biochemical parameters / Efeitos do extrato líquido de resíduos de frutos de Plinia cauliflora sobre os parâmetros bioquímicos de hamsters chineses

Plinia cauliflora (Mart.) Kausel, popularly known as jabuticaba, is rich in polyphenols. Phenolic compounds exhibit several biological properties, which reflect on biomarkers such as biochemical parameters. In the present study, we evaluated the plasmatic levels of glucose, total cholesterol, HDL-cholesterol, triglycerides, and uric acid of Chinese hamsters fed for 45 days with a regular diet or cholesterol-enriched diet supplemented with a liquid extract obtained from P. cauliflora fruits residues standardized in ellagic acid and total phenolic compounds. The results showed that the concentrated extract obtained from jabuticaba residues increased the glycemia of animals fed with a regular diet and reduced the plasmatic uric acid levels of animals fed with a cholesterol-enriched diet. Since hyperuricemia is considered to be a significant risk factor of metabolic disorders and the principal pathological basis of gout, the liquid extract from P. cauliflora fruits residues would be a promising candidate as a novel hypouricaemic agent for further investigation.

Plinia cauliflora (Mart.) Kausel, popularmente conhecida como jabuticaba, é rica em polifenois. Os compostos fenólicos apresentam diversas propriedades biológicas, que refletem em biomarcadores, como os parâmetros bioquímicos. No presente estudo, avaliamos os níveis plasmáticos de glicose, colesterol total, HDL-colesterol, triglicerídeos e ácido úrico em hamsters chineses alimentados por 45 dias com dieta regular ou dieta enriquecida com colesterol suplementada com extrato líquido obtido de resíduos de frutos de P. cauliflora padronizado em ácido elágico e compostos fenólicos totais. Os resultados mostraram que o extrato concentrado obtido dos resíduos de jabuticaba aumentou a glicemia dos animais alimentados com dieta regular e reduziu os níveis plasmáticos de ácido úrico dos animais alimentados com dieta rica em colesterol. Uma vez que a hiperuricemia é considerada um fator de risco significativo de distúrbios metabólicos e a principal base patológica da gota, o extrato líquido dos resíduos de frutas de P. cauliflora seria um candidato promissor como um novo agente hipouricêmico para investigação posterior.

Effects of liquid extract from Plinia cauliflora fruits residues on Chinese hamsters biochemical parameters

Abstract Plinia cauliflora (Mart.) Kausel, popularly known as jabuticaba, is rich in polyphenols. Phenolic compounds exhibit several biological properties, which reflect on biomarkers such as biochemical parameters. In the present study, we evaluated the plasmatic levels of glucose, total cholesterol, HDL-cholesterol, triglycerides, and uric acid of Chinese hamsters fed for 45 days with a regular diet or cholesterol-enriched diet supplemented with a liquid extract obtained from P. cauliflora fruits residues standardized in ellagic acid and total phenolic compounds. The results showed that the concentrated extract obtained from jabuticaba residues increased the glycemia of animals fed with a regular diet and reduced the plasmatic uric acid levels of animals fed with a cholesterol-enriched diet. Since hyperuricemia is considered to be a significant risk factor of metabolic disorders and the principal pathological basis of gout, the liquid extract from P. cauliflora fruits residues would be a promising candidate as a novel hypouricaemic agent for further investigation.

Resumo Plinia cauliflora (Mart.) Kausel, popularmente conhecida como jabuticaba, é rica em polifenois. Os compostos fenólicos apresentam diversas propriedades biológicas, que refletem em biomarcadores, como os parâmetros bioquímicos. No presente estudo, avaliamos os níveis plasmáticos de glicose, colesterol total, HDL-colesterol, triglicerídeos e ácido úrico em hamsters chineses alimentados por 45 dias com dieta regular ou dieta enriquecida com colesterol suplementada com extrato líquido obtido de resíduos de frutos de P. cauliflora padronizado em ácido elágico e compostos fenólicos totais. Os resultados mostraram que o extrato concentrado obtido dos resíduos de jabuticaba aumentou a glicemia dos animais alimentados com dieta regular e reduziu os níveis plasmáticos de ácido úrico dos animais alimentados com dieta rica em colesterol. Uma vez que a hiperuricemia é considerada um fator de risco significativo de distúrbios metabólicos e a principal base patológica da gota, o extrato líquido dos resíduos de frutas de P. cauliflora seria um candidato promissor como um novo agente hipouricêmico para investigação posterior.

Process optimization of physicochemical properties of spray-dried Hydrocotyle umbellata L. extract

Abstract Hydrocotyle umbellata L., Araliaceae, is a species that is recommended in Ayurvedic medicine for its effects on the central nervous system, such as anxiolytic and memory-stimulant effects. Despite the medicinal potential of this species, its phytopharmaceutical and technological potential to produce standardized extracts has not been investigated. This study analyzes the influence of spray drying parameters on the contents of the chemical markers (total phenolic, total flavonoid, and hibalactone) and the functional properties of H. umbellata extract. The optimization of drying conditions was performed using a central composite design combined with response surface methodology and desirability function approach. The mathematical models fitted to experimental data indicated that all the evaluated drying parameters significantly influenced the chemical contents. The optimal conditions were: inlet temperature of 120 °C, feed flow rate of 4 mL min-1, and colloidal silicon dioxide:maltodextrin ratio of 16%:4%. Under these conditions, the powder samples had spherical particles and desirable physicochemical and functional properties, such as low water activity and moisture content, good product recovery, reconstitution, and flowability. Thus, spray drying might be a promising technique for processing standardized H. umbellata extracts.

Effects of liquid extract from Plinia cauliflora fruits residues on Chinese hamsters biochemical parameters.

Plinia cauliflora (Mart.) Kausel, popularly known as jabuticaba, is rich in polyphenols. Phenolic compounds exhibit several biological properties, which reflect on biomarkers such as biochemical parameters. In the present study, we evaluated the plasmatic levels of glucose, total cholesterol, HDL-cholesterol, triglycerides, and uric acid of Chinese hamsters fed for 45 days with a regular diet or cholesterol-enriched diet supplemented with a liquid extract obtained from P. cauliflora fruits residues standardized in ellagic acid and total phenolic compounds. The results showed that the concentrated extract obtained from jabuticaba residues increased the glycemia of animals fed with a regular diet and reduced the plasmatic uric acid levels of animals fed with a cholesterol-enriched diet. Since hyperuricemia is considered to be a significant risk factor of metabolic disorders and the principal pathological basis of gout, the liquid extract from P. cauliflora fruits residues would be a promising candidate as a novel hypouricaemic agent for further investigation.

Acute exposure to environmentally relevant concentrations of benzophenone-3 induced genotoxicity in Poecilia reticulata.

The organic UV filter benzophenone-3 (BP-3), widely used in the commercial formulations of sunscreens and personal care products, is considered an emerging pollutant and has been associated with several human and environmental health concerns. However, knowledge about their mode of action and ecotoxicity on aquatic biota is scarce. In this scenario, the objective of this work was to evaluate the genotoxic, mutagenic, and erythrotoxicity effects of BP-3 in the guppy Poecilia reticulata after acute exposure. Adult females of P. reticulata were exposed to three non-lethal and environmentally relevant concentrations of BP-3 (10, 100, and 1000 ng L-1) during 96 h of exposure, and the somatic parameter [Fulton condition factor (K)], genotoxicity (comet assay), mutagenicity [micronucleus (MN) and erythrocyte nuclear abnormalities (ENA) tests] and erythrotoxicity parameters (such as total cell area and nucleus-cytoplasmic ratio) were analyzed. Results showed that the general physiological condition (K value) of fish was not affected by acute exposure to BP-3. However, BP-3 induced DNA damage at 100 and 1000 ng L-1 and increased the frequency of total ENA at 1000 ng L-1, specially lobed nucleus, when compared to control group, indicating its genotoxic and mutagenic effects. Furthermore, the BP-3 did not induce significant changes in the total cell area and nucleus-cytoplasmic ratio. In summary, results showed that the BP-3 at environmentally relevant concentration was genotoxic to freshwater fish P. reticulata, confirming its environmental risk.

Validation of a photostability indicating method for quantification of furanocoumarins from Brosimum gaudichaudii soft extract

ABSTRACT A validation study of a reverse-phase high-performance liquid chromatographic assay for the quantification of two furanocoumarins (psoralen and bergapten) in soft extract obtained from Brosimum gaudichaudii Trécul, Moraceae, roots was conducted. The developed method was sensitive, rapid, reproducible, easy and precise, and showed linearity (r > 0.99) in the range of 10-64 µg/ml for psoralen, and 9-56 µg/ml for bergapten. It also showed a good efficiency for the photodegradation analysis of psoralen and bergapten in the soft extract. The photostability results showed that the Higuchi model presented the best fitting to the obtained data. Both chemical markers showed stability over 2.6 days, suggesting potential applications of the extract in obtaining intermediate products from this plant material. Furanocoumarins take around 30 min to be activated by UV light, reaching the maximum biological potential. Thus, the results obtained to the Higuchi model, corresponding to 2.6 days of stability, shows feasibility with future applications of these chemical markers.

Acaricidal activity of ethanolic extracts of Stryphnodendron adstringens and Lafoensia pacari and oil resins from Copaifera sp. and Pterodon emarginatus against Sarcoptes scabiei var. suis / Atividade acaricida dos extratos etanólicos de Stryphnodendron adstringens Mart. e Lafoensia pacari A. St Hil., bem como das óleo-resinas de Copaifera sp. e Pterodon emarginatus Vogel, 1837 contra Sarcoptes scabiei var. suis

In vitro bioassay using Sarcoptes scabiei as a test microorganism is a viable method of study for diverse drugs with acaricidal properties. A great amount of assays proves the diverse and efficient biological activity of extracts and compounds from Brazilian savanna plants. This study had as main object, test and compare the acaricidal activity of four Brazilian Cerrado bioproducts: Stryphnodendron adstringens Mart., Copaifera sp., Lafoensia pacari A. St Hil. and Pterodon emarginatus Vogel, 1837. To perform this test S. scabiei mites were collected from crusts removed on ears of highly infected sows. The mites were selected and separated in Petri dishes with three different concentrations (25, 50 and 75%) of each bioproduct, to evaluate their potential acaricidal activity. The mortality of the mites was counted in each Petri dish every hour, during five hours. The statistical analyses demonstrated differences between the bioproducts tested. The oleoresin of Copaifera sp. and P. emarginatus presented the best results with 100% of mites mortality after treatment. The ethanolic extracts of S. adstringens and L. pacari demonstrated lower acaricidal activity when compared to the oleoresins, with little or no difference among the control groups tested. This bioassay demonstrated to be efficient, reliable, low cost and easy accomplishment. Oil resins from Copaifera sp. and P. emarginatus have in vitro acaricidal activity against adult females of S. scabiei var. suis.(AU)

O uso de Sarcoptes scabiei como microrganismo teste para bioensaio in vitro é um método de estudo viável para diversas drogas acaricidas. Muitos ensaios comprovam a diversidade e eficiência de atividade biocida de extratos e componentes presentes em plantas do cerrado brasileiro. Este trabalho objetivou testar e comparar a atividade acaricida de quatro bioprodutos do cerrado brasileiro: Stryphnodendron adstringens Mart., Lafoensia pacari A. St Hil., Copaifera sp. e Pterodon emarginatus Vogel, 1837. Para este estudo, ácaros S. scabiei foram colhidos em crostas removidas de orelhas de fêmeas suínas altamente infestadas. Os ácaros foram selecionados, separados e colocados em placas de Petri com três diferentes concentrações (25, 50 e 75%) de bioprodutos, para avaliar o potencial de atividade acaricida de cada um. Foi realizada a contagem da mortalidade dos ácaros em cada placa de Petri a cada hora, durante cinco horas. As análises estatísticas demonstraram diferenças entre os bioprodutos testados. As óleo-resinas de Copaifera sp. e P. emarginatus apresentaram os melhores resultados, com 100% de mortalidade dos ácaros após tratamento. Os extratos etanólicos de S. adstringens Mart. e L. pacari demonstraram menor atividade acaricida quando comparados as óleo-resinas, com pequena ou nenhuma diferença entre os resultados dos grupos controle. Este ensaio demonstrou ser uma ferramenta eficiente, confiável, de baixo custo e de fácil realização. As óleo-resinas Copaifera sp. e P. emarginatus possuem atividade acaricida in vitro sobre fêmeas adultas de S. scabiei var. suis.(AU)

Jabuticaba-Induced Endothelium-Independent Vasodilating Effect on Isolated Arteries / Efeito Vasodilatador Independente do Endotélio Induzido pela Jabuticaba (M. cauliflora) em Artérias Isoladas

Abstract Background: Despite the important biological effects of jabuticaba, its actions on the cardiovascular system have not been clarified. Objectives: To determine the effects of jabuticaba hydroalcoholic extract (JHE) on vascular smooth muscle (VSM) of isolated arteries. Methods: Endothelium-denuded aortic rings of rats were mounted in isolated organ bath to record isometric tension. The relaxant effect of JHE and the influence of K+ channels and Ca2+ intra- and extracellular sources on JHE-stimulated response were assessed. Results: Arteries pre-contracted with phenylephrine showed concentration-dependent relaxation (0.380 to 1.92 mg/mL). Treatment with K+ channel blockers (tetraethyl-ammonium, glibenclamide, 4-aminopyridine) hindered relaxation due to JHE. In addition, phenylephrine-stimulated contraction was hindered by previous treatment with JHE. Inhibition of sarcoplasmic reticulum Ca2+ ATPase did not change relaxation due to JHE. In addition, JHE inhibited the contraction caused by Ca2+ influx stimulated by phenylephrine and KCl (75 mM). Conclusion: JHE induces endothelium-independent vasodilation. Activation of K+ channels and inhibition of Ca2+ influx through the membrane are involved in the JHE relaxant effect.

Resumo Fundamentos: Embora a jabuticaba apresente importantes efeitos biológicos, suas ações sobre o sistema cardiovascular ainda não foram esclarecidas. Objetivos: Determinar os efeitos do extrato de jabuticaba (EHJ) sobre o músculo liso vascular (MLV) em artérias isoladas. Métodos: Aortas (sem endotélio) de ratos foram montadas em banho de órgãos isolados para registro de tensão isométrica. Foram verificados o efeito relaxante, a influência dos canais de K+ e das fontes de Ca2+ intra- e extracelular sob a resposta estimulada pelo EHJ. Resultados: Artérias pré-contraídas com fenilefrina apresentaram relaxamento concentração-dependente (0,380 a 1,92 mg/mL). O tratamento com bloqueadores de canais de K+ (tetraetilamônio, glibenclamida, 4-aminopiridina) prejudicaram o relaxamento pelo EHJ. A contração estimulada com fenilefrina também foi prejudicada pelo tratamento prévio com EHJ. A inibição da Ca2+ATPase do reticulo sarcoplasmático não alterou o relaxamento pelo EHJ. Além disso, o EHJ inibiu a contração causada pelo influxo de Ca2+ estimulado por fenilefrina e KCl (75 mM). Conclusão: O EHJ induz vasodilatação independente do endotélio. Ativação dos canais de K+ e inibição do influxo de Ca2+ através da membrana estão envolvidas no efeito relaxante do EHJ.

Jabuticaba-Induced Endothelium-Independent Vasodilating Effect on Isolated Arteries.

BACKGROUND:: Despite the important biological effects of jabuticaba, its actions on the cardiovascular system have not been clarified. OBJECTIVES:: To determine the effects of jabuticaba hydroalcoholic extract (JHE) on vascular smooth muscle (VSM) of isolated arteries. METHODS:: Endothelium-denuded aortic rings of rats were mounted in isolated organ bath to record isometric tension. The relaxant effect of JHE and the influence of K+ channels and Ca2+ intra- and extracellular sources on JHE-stimulated response were assessed. RESULTS:: Arteries pre-contracted with phenylephrine showed concentration-dependent relaxation (0.380 to 1.92 mg/mL). Treatment with K+ channel blockers (tetraethyl-ammonium, glibenclamide, 4-aminopyridine) hindered relaxation due to JHE. In addition, phenylephrine-stimulated contraction was hindered by previous treatment with JHE. Inhibition of sarcoplasmic reticulum Ca2+ ATPase did not change relaxation due to JHE. In addition, JHE inhibited the contraction caused by Ca2+ influx stimulated by phenylephrine and KCl (75 mM). CONCLUSION:: JHE induces endothelium-independent vasodilation. Activation of K+ channels and inhibition of Ca2+ influx through the membrane are involved in the JHE relaxant effect. FUNDAMENTOS:: Embora a jabuticaba apresente importantes efeitos biológicos, suas ações sobre o sistema cardiovascular ainda não foram esclarecidas. OBJETIVOS:: Determinar os efeitos do extrato de jabuticaba (EHJ) sobre o músculo liso vascular (MLV) em artérias isoladas. MÉTODOS:: Aortas (sem endotélio) de ratos foram montadas em banho de órgãos isolados para registro de tensão isométrica. Foram verificados o efeito relaxante, a influência dos canais de K+ e das fontes de Ca2+ intra- e extracelular sob a resposta estimulada pelo EHJ. RESULTADOS:: Artérias pré-contraídas com fenilefrina apresentaram relaxamento concentração-dependente (0,380 a 1,92 mg/mL). O tratamento com bloqueadores de canais de K+ (tetraetilamônio, glibenclamida, 4-aminopiridina) prejudicaram o relaxamento pelo EHJ. A contração estimulada com fenilefrina também foi prejudicada pelo tratamento prévio com EHJ. A inibição da Ca2+ATPase do reticulo sarcoplasmático não alterou o relaxamento pelo EHJ. Além disso, o EHJ inibiu a contração causada pelo influxo de Ca2+ estimulado por fenilefrina e KCl (75 mM). CONCLUSÃO:: O EHJ induz vasodilatação independente do endotélio. Ativação dos canais de K+ e inibição do influxo de Ca2+ através da membrana estão envolvidas no efeito relaxante do EHJ.

An approach on phytoalexins: function, characterization and biosynthesis in plants of the family Poaceae / Uma abordagem sobre fitoalexinas: função, caracterização e biossíntese em plantas da família Poaceae

ABSTRACT: Phytoalexins are compounds that have been studied a few years ago, which present mainly antimicrobial activity. The plants of the family Poaceae are the most geographically widespread and stand out for their economic importance, once they are cereals used as staple food. This family stands out for having a variety of phytoalexins, which can be synthesized via the shikimic acid (the phenylpropanoids), or mevalonic acid, being considered terpenoid phytoalexins. The characterization of these compounds with antimicrobial activity is carried out using chromatographic techniques, and the high-performance liquid chromatography (HPLC) coupled with mass spectrometry are the most efficient methods in this process. This research aimed to present an approach of the function, characterization and biosynthesis of phytoalexins in plants of the family Poaceae.

RESUMO: As fitoalexinas são compostos que vêm sendo estudados há alguns anos, apresentando principalmente atividade antimicrobiana. As plantas da família Poaceae são as geograficamente mais difundidas e se destacam por sua importância econômica, uma vez que são os cereais que compõe a base da alimentação, em todos os continentes. Essa família se destaca por apresentar uma variedade de fitoalexinas, sendo que as mais importantes são sintetizadas a partir da via do ácido chiquímico. A caracterização desses compostos com atividade antimicrobiana é realizada por meio de técnicas cromatográficas, sendo que a cromatografia líquida de alta eficiência (HPLC) acoplada com espectrometria de massas é a técnica mais eficiente nesse processo. O trabalho apresenta como objetivo uma abordagem da função, caracterização, biossíntese e aplicações das fitoalexinas em plantas da família Poaceae.

Dissolution test of herbal medicines containing Paullinia cupana: validation of methods for quantification and assessment of dissolution / Ensaio de dissolução de medicamentos fitoterápicos contendo Paullinia cupana: validação de métodos de quantificação e avaliação de dissolução

"Guaraná" (Paullinia cupana) is used as a physical activity enhancer and stimulator due to its methylxanthines and condensed tannins. The aim of this work was to evaluate the dissolution behavior of five herbal medicines in the form of capsules and tablets containing guaraná. Assay and dissolution methods were validated and results obtained allowed simultaneous marker quantification with precision, accuracy, selectivity and robustness. Findings showed that 100 percent of the herbal medicinal products analyzed did not provide satisfactory results concerning the presence of four markers, 60 percent had three markers (caffeine, catechin and epicatechin), while 40 percent had only caffeine at tested dosage forms. In addition, after 30 minutes, only capsule A showed at least 80 percent of the dissolved markers. In other capsules, marker dissolution did not exceed 60 percent whereas 60 percent of the samples had some characteristic pharmacotechnical problems. These results evidence the need for rigorous quality control to help ensure the therapeutic action of these drugs. To this end, dissolution studies are an essential tool for quality assurance of herbal medicines.

Guaraná (Paullinia cupana) é utilizado como revigorante e estimulante devido à presença de metilxantinas e taninos condensados. Este trabalho visou avaliar o comportamento de dissolução de cinco fitoterápicos, na forma de cápsulas e comprimidos, contendo guaraná. O método de quantificação e de dissolução foram validados e os resultados obtidos permitiram a quantificação dos marcadores simultaneamente, com precisão, exatidão, seletividade e robustez. Foi verificado que 100 por cento dos fitoterápicos analisados encontravam em desacordo quanto à presença dos quatro marcadores, sendo que 60 por cento apresentaram três marcadores (cafeína, catequina e epicatequina) e 40 por cento apresentaram somente a cafeína. Além disso, após o tempo de 30 minutos de ensaio foi possível observar que somente a cápsula A apresentou pelo menos 80 por cento dos marcadores dissolvidos. Nas demais cápsulas o comportamento de dissolução apresentado pelos marcadores não ultrapassou 60 por cento e, além disso, 60 por cento das amostras apresentaram alguns problemas farmacotécnicos característicos. Frente aos resultados obtidos torna-se evidente a necessidade de um rigoroso controle de qualidade que contribua para assegurar a ação terapêutica desses medicamentos e, nesse sentido, o estudo de dissolução constitui uma ferramenta essencial para a garantia de qualidade dos fitoterápicos.

Aspectos técnicos e legais do gerenciamento de resíduos químico-farmacêuticos / Technical and legal aspects on management of chemical and pharmaceutical residues

O risco ambiental decorrentes da geração de resíduos tem aumentado com o progresso tecnológico, bem como com o aumento populacional. Destacam-se, neste contexto, os riscos potenciais decorrentes da rotina de indústrias químico-farmacêuticas, bem como de laboratórios de ensino e pesquisa associados. Por esta razão, vários projetos visando à otimização do tratamento de resíduos industriais e/ou laboratoriais vêm sendo propostos. A presente revisão apresenta uma síntese das estratégias implantadas no sentido de minimizar ou solucionar problemas relacionados ao manejo dos resíduos, provenientes de indústrias, instituições de pesquisa e ensino, entre outros potenciais geradores de resíduos. Apresentam-se as diretrizes legais mais gritantes e alguns aspectos técnicos relacionados à segregação, acondicionamento, tratamento e descarte final destes resíduos.

The environmental risks from waste production has arisen with the technological progress, as well as with the world population increase. The risks from the industrial or academic routines in pharmaceutical or fine chemical plants and projects are remarkable. For this reason, many projects focusing on the optimization of waste treatment in these places have been proposed. This paper, reviews some of the main strategies introduced, in order to solve or decrease the problems, in the management of pharmaceutical-chemical wastes in industry, universities, among other potential kind of waste generators. The main regulatory and technical aspects, associated to segregation, packaging, treatment and final disposal of these wastes are presented.