Antinociceptive and anti-inflammatory effects of ethanol extract from Vernonia polyanthes leaves in Rodents.

The ethanol extract from Vernonia polyanthes leaves (EEVP) was investigated for antinociceptive and anti-inflammatory effects at the doses (p.o.) of 100, 200 and 400 mg/kg in animal models. The extract reduced the number of abdominal contortions by 16.75% and 31.44% at a dose of 200 and 400 mg/kg, respectively. The results obtained showed that EEVP exerted a significant antinociceptive effect in the two phases of formalin. The EEVP increased the reaction time on a hot plate at the doses of 100, 200 and 400 mg/kg after 90 min of treatment. The paw edema was reduced by EEVP at the doses of 100, 200 and 400 mg/kg after 4 h of application of carrageenan. Doses of 200 and 400 mg/kg, administered 4 h before the carrageenan injection, significantly reduced the exudate volume (29.25 and 45.74%, respectively) and leukocyte migration (18.19 and 27.95%, respectively). These results suggest that V. polyanthes can be an active source of substances with antinociceptive and anti-inflammatory activities.

Antinociceptive and anti-inflammatory activities of the ethanol extract of Annona muricata L. leaves in animal models.

Antinociceptive and anti-inflammatory activities of the ethanol extract from Annona muricata L. leaves were investigated in animal models. The extract delivered per oral route (p.o.) reduced the number of abdominal contortions by 14.42% (at a dose of 200 mg/kg) and 41.41% (400 mg/kg). Doses of 200 and 400 mg/kg (p.o) inhibited both phases of the time paw licking: first phase (23.67% and 45.02%) and the second phase (30.09% and 50.02%), respectively. The extract (p.o.) increased the reaction time on a hot plate at doses of 200 (30.77% and 37.04%) and 400 mg/kg (82.61% and 96.30%) after 60 and 90 minutes of treatment, respectively. The paw edema was reduced by the ethanol extract (p.o.) at doses of 200 (23.16% and 29.33%) and 400 mg/kg (29.50% and 37.33%) after 3 to 4 h of application of carrageenan, respectively. Doses of 200 and 400 mg/kg (p.o.), administered 4 h before the carrageenan injection, reduced the exudate volume (29.25 and 45.74%) and leukocyte migration (18.19 and 27.95%) significantly. These results suggest that A. muricata can be an active source of substances with antinociceptive and anti-inflammatory activities.

Pharmacological properties of the ethanol extract of Muehlenbeckia platyclada (F. Muell.) meisn. leaves.

Antinociceptive and anti-inflammatory activities of the Muehlenbeckia platyclada leaves' ethanol extract were investigated in animal models. The extract (p.o.) reduced the number of abdominal contortions induced by acetic acid by 21.57% (400 mg/kg). After intraplantar injection of formalin, a dose of 400 mg/kg (p.o.) inhibited the time spent paw licking in the first phase (26.43%), while the second phase was inhibited by 10.90 and 36.65% at the doses of 200 and 400 mg/kg, respectively. The extract (p.o.) increased the reaction time on a hot plate at a dose of 400 mg/kg (32.68 and 40.30%) after 60 and 90 minutes of treatment, respectively. The paw edema was reduced by extract (p.o.) at doses of 100 (15.46 and 16.67%), 200 (22.68 and 25.64%) and 400 mg/kg (29.50 and 37.33%) after 3 to 4 h of carrageenan application, respectively. Doses of 100, 200 and 400 mg/kg (p.o.), administered 4 h after the carrageenan injection, reduced the exudate volume (11.28, 21.54 and 45.13%), while leukocyte migration was reduced by 21.21 and 29.70% at the doses of 200 and 400 mg/kg, respectively. These results indicate that the ethanol extract from M. platyclada may constitute a potential target for the discovery of new molecules with antinociceptive and anti-inflammatory activities that can be explored for their therapeutic use.

Methyl Chavicol and Its Synthetic Analogue as Possible Antioxidant and Antilipase Agents Based on the In Vitro and In Silico Assays.

This study investigated the in vitro and in silico biological properties of the methyl chavicol (MC) and its analogue 2-[(4-methoxyphenyl)methyl]oxirane (MPMO), emphasizing the antioxidant and antilipase effects. MPMO was synthesized from MC that reacted with meta-chloroperbenzoic acid and, after separation and purification, was identified by 1H and 13C NMR and GC-MS. The antioxidant activity was investigated by DPPH, cooxidation ß-carotene/linoleic acid, and thiobarbituric acid assays. With the use of colorimetric determination, the antilipase effect on the pancreatic lipase was tested, while the molecular interaction profiles were evaluated by docking molecular study. MC (IC50 = 312.50 ± 2.28 µg/mL) and MPMO (IC50 = 8.29 ± 0.80 µg/mL) inhibited the DPPH free radical. The inhibition of lipid peroxidation (%) was 73.08 ± 4.79 and 36.16 ± 4.11 to MC and MPMO, respectively. The malonaldehyde content was significantly reduced in the presence of MC and MPMO. MC and MPMO inhibited the pancreatic lipase in 58.12 and 26.93%, respectively. MC and MPMO (-6.1 kcal·mol-1) produced a binding affinity value lower than did diundecylphosphatidylcholine (-5.6 kcal·mol-1). These findings show that MC and MPMO present antioxidant and antilipase activities, which may be promising molecular targets for the treatment of diseases associated with oxidative damage and lipid metabolism.

Antinociceptive and anti-inflammatory activities of the sesame oil and sesamin.

Sesame oil is widely consumed as nutritious food, cooking oil, and in pharmaceuticals and food. In this study, the antinociceptive and anti-inflammatory properties of the sesame oil and sesamin were investigated. The sesame oil and sesamin reduced the number of abdominal contortions at the doses 100, 200, or 400 mg/kg. The first and second phases of the time paw licking were inhibited by sesame oil and sesamin (100, 200, or 400 mg/kg). After 90 min of treatment, sesame oil and sesamin increased the reaction time on a hot plate (200 or 400 mg/kg). Considering the tail-immersion assay, the sesame oil and sesamin produced significant effect after 60 min at the doses of 100, 200, or 400 mg/kg. After 4 h of application of the carrageenan, the sesame oil and sesamin were effective against the paw edema. The exudate volume and leucocyte migration were also reduced by sesame oil and sesamin. These results suggest that sesamin is one of the active compounds found in sesame oil and justify the antinociceptive and anti-inflammatory properties of this product.

Development of mouthwash with Rosmarinus officinalis extract

Rosmarinus officinalis, which belongs to the Lamiaceae family, is a species of medicinal flora with therapeutic properties. In order to exploit the benefits of these properties, a mouthwash formulation was developed, with careful selection of raw materials to meet pharmacotechnical requirements. Extracts of the plant were incorporated into a mouthwash, which was shown to have inhibitory action in vitro against the micro-organisms commonly found in periodontics. Controls for assessing the quality of the drugs were carried out, quantifying phenols and flavonoids as chemical markers. Mouthwash solutions were formulated containing 0.1, 5 and 10% ethanol extract of R. officinalis; and 0.05, 5 and 10% of the hexane fraction of R. officinalis. In order to evaluate synergism, ethanol extract and hexane fraction were also added to formulations containing 0.05% sodium fluoride and 0.12% chlorhexidine digluconate. These formulations were assessed for inhibitory effect against the specific microorganisms involved in the process of bacterial plaque formation, S. mutans (ATCC25175) and C. albicans(ATCC 10231), frequently found in cases of oral infections. The agar diffusion method was used to evaluate the inhibitory activity of extracts and formulations. All mouthwash solutions displayed inhibitory activity having higher sensitivity to S. mutans for the 5% ethanol extract+0.05% sodium fluoride, and greater sensitivity to C. albicans for the 10% hexane fraction. Results were characterized by the appearance of a growth inhibition halo, justifying the utilization and association of extracts of R. officinalis.

Rosmarinus officinalis, pertencente à família Lamiaceae, é um exemplar da flora medicinal que possui propriedades terapêuticas. No intuito de usufruir destes benefícios, desenvolveu-se uma formulação de enxaguatório bucal com seleção criteriosa de matérias-primas que atendessem os requisitos farmacotécnicos. Incorporaram-se extratos dessa planta e verificou-se a capacidade inibitória in vitro frente a micro-organismos frequentemente encontrados em periodontias. Controles foram efetuados para a avaliação da qualidade dos fármacos, quantificando-se como marcadores químicos, os fenóis e os flavonóides. Formulações de enxaguatórios contendo 0,1, 5 e 10% de extrato etanólico de R. officinalis; e 0,05, 5 e 10% da fração hexânica de R. officinalis foram preparadas. Para avaliar o sinergismo, o extrato e a fração hexânica também foram adicionados às formulações que continham fluoreto de sódio 0,05% e diguclonato de clorexidina 0,12%. Nessas formulações avaliou-se a capacidade inibitória frente a micro-organismos específicos do processo de formação de placa bacteriana, S. mutans (ATCC 25175) e C. albicans (ATCC 10231), frequentemente encontrada em quadros de infecções orais. Foi empregado o método de difusão em ágar para a avaliação da atividade inibitória dos extratos e das formulações. Todos os enxaguatórios demonstraram atividade inibitória, verificando-se maior sensibilidade a S. mutans, quando se utilizou extrato etanólico 5% + fluoreto de sódio 0,05% e sensibilidade maior a C. albicans, quando se utilizou fração hexânica a 10%. Os resultados foram caracterizados pelo aparecimento de halo de inibição de crescimento, justificando a utilização e associação dos extratos de R. officinalis.

Avaliação da qualidade físico-química de cápsulas manipuladas de carbamazepina / Evaluation of physico-chemical quality of manipulated capsules of carbamazepine

O presente trabalho avaliou a qualidade de três formulações farmacêuticas, denominadas A, B e C, obtidas através de processo magistral. Foram realizados testes de identificação do fármaco, peso médio e perfil de dissolução das cápsulas contendo carbamazepina (200 mg), assim como determinação dos parâmetros cinéticos e da eficiência de dissolução (ED). Os testes de identificação confirmaram a autenticidade da carbamazepina e o peso médio da formulação B foi significativamente maior (p < 0,05) que os das formulações A e C. No entanto, a formulação A não atendeu aos critérios especificados, apresentando baixa ED. Os dados revelaram que a avaliação da qualidade dos medicamentos manipulados, como a carbamazepina, e o uso de excipientes adequados podem contribuir para uma resposta terapêutica desejada.

The present study evaluated the quality of three pharmaceutical formulations, named A, B and C, obtained from manipulated process. Drug identification, average weight, dissolution profile, kinetic parameters, and Dissolution Efficiency (DE) were determined from the carbamazepine capsules (200 mg). The obtained data proved the authenticity of carbamazepineand the average weight of the B formulation was significantly higher (p < 0.05) than those of A and C formulations. However, the A formulation not attended the specified criteria, presenting low DE value. The results showed that the quality evaluation of manipulated medicines such as carbamazepine, and the use of suitable excipients can contributed for a desired therapeutic response.

Uso etnomedicinal do chá de Morus nigra L. no tratamento dos sintomas do climatério de mulheres de Muriaé, Minas Gerais, Brasil / Ethnomedicinal use of tea from Morus nigra L. in the treatment of the climacteric symptoms in women from Muriaé, Minas Gerais, Brazil

Morus nigra L. (Moraceae), conhecida como amoreira, é usada popularmente, entre outros fins medicinais, para reposição hormonal. O objetivo do presente estudo foi avaliar o uso etnomedicinal do chá das folhas de M. nigra no tratamento dos sintomas do climatério. A pesquisa se baseou na aplicação de um questionário semiestruturado em mulheres residentes em Muriaé ? MG, que utilizavam chá de amoreira. A análise quantitativa foi determinada pela concordância de uso popular corrigida (CUPc). As características das mulheres entrevistadas foram: faixa etária entre 32 e 61 anos, cinco donas de casa, oito católicas, quatro com ensino fundamental incompleto e cinco haviam tido menopausa. Além de outros fins medicinais, nove das mulheres usavam o chá de amoreira para amenizar sintomas do climatério, resultando em uma CUPc de 90%. As amigas e os médicos foram as principais fontes de recomendação do uso do chá nas formas de infusão ou de decocção, com variação de dosagem e de aprazamento. Gases, aumento do apetite e diurese foram os efeitos adversos relatados, sendo que quatro das mulheres já tinham feito terapia hormonal para alívio dos sintomas do climatério. Os resultados confirmam a utilização do chá de M. nigra no tratamento de sintomas do climatério, apresentando um alto consenso de informação.

Morus nigra L. (Moraceae), known as mulberry, is used in folk medicine, including hormone replacement. The objective of this study was to evaluate the ethnomedicinal use of the tea of the leaves of M. nigra in the treatment of climacteric symptoms. The research was based on the application of a semi-structured questionnaire in women from city of Muriaé, Minas Gerais state, Brazil, which reported the use of the tea from mulberry. The quantitative analysis was based on the corrected popular use concordance (cPUC). The characteristics of the interviewed women were: aged 32 to 61 years, 5 housewives, 8 catholic, 4 with incomplete primary education, and 5 have had menopause. In addition to other medical purposes, 9 of the women used the mulberry tea to alleviate symptoms of menopause, resulting in a cPUC of 90%. The main recommendation of use was made by friends (6) and physicians (2), under infusion (7) or decoction (3) forms, with a range of dosing and administration. Gases, increased appetite and urine output were the adverse effects reported, and 4 of women had already used hormonal therapy to relieve the symptoms of menopause. The results confirm the use of tea from M. nigra in the treatment of climacteric symptoms, with high consensus information.

Propriedades biológicas das sementes de Joannesia princeps Vellozo / Biological properties of the Joannesia princeps Vellozo seeds

Este trabalho teve como objetivo avaliar as propriedades biológicas do extrato metanólico, obtido por Soxhlet, seguido de partição líquido/líquido (frações hexânica, diclorometânica, em acetato de etila, butanólica e residual) das sementes de Joannesia princeps. A atividade laxante foi avaliada pelo teste da motilidade intestinal em camundongos. O método de difusão em ágar utilizando Staphylococcus aureus ATCC 29737, Streptococcus mutans ATCC 25175, Escherichia coli ATCC 11229, Salmonella typhimurium ATCC 13111 e Pseudomonas aeruginosa ATCC 90271 e o bioensaio em Artemia salina foram utilizados para investigação da atividade antibacteriana e da toxidez, respectivamente. O extrato metanólico, as frações e a semente pulverizada aumentaram significativamente a motilidade intestinal. O extrato metanólico e a fração residual inibiram o crescimento de todas as amostras bacterianas de referência testadas, enquanto as frações hexânica e diclorometânica inibiram Staphylococcus aureus ATCC 29737, Salmonella typhimurium ATCC 13111 e Streptococcus mutans ATCC 25175. As frações em acetato de etila e butanólica foram ativas somente para S. aureus ATCC 29737. O extrato metanólico e as frações hexânica, diclorometânica e butanólica produziram CL50 de 56,28, 16,72, 14,82 e 67,29 ?g/mL, respectivamente. Os resultados mostraram que as sementes de J. princeps exibem atividades laxante e antibacteriana, sendo tóxicas para A. salina.

The aim of the present study was to evaluate the biological properties of the methanol extract, obtained by Soxhlet, followed by liquid/liquid partition with organic solvents (hexane, dichloromethane, ethyl acetate, butanol and residual fractions) of the Joannesia princeps seeds. Laxative activity was tested through the intestinal motility model in mice. The agar diffusion method using Staphylococcus aureus ATCC 29737, Streptococcus mutans ATCC 25175, Escherichia coli ATCC 11229, Salmonella typhimurium ATCC 13111 and Pseudomonas aeruginosa ATCC 90271and the Brine Shrimp Lethality bioassay were used to evaluate the antibacterial activity and the toxicity, respectively. The methanol extract, the fractions and the powder seeds increased the intestinal motility significantly. The methanol extract and residual fraction inhibited all reference strains tested, while the hexane, dichloromethane, ethyl acetate and butanol fractions inhibited only S. aureus ATCC 29737. The hexane and dichloromethane fractions were active against Salmonella typhimurium ATCC 13111 and Streptococcus mutans ATCC 25175. The methanol extract and hexane, dichloromethane and butanol fractions produced LC5056.28, 16.72, 14.82 and 67.29 ?g/mL, respectively. The results showed that J. princeps seeds present laxative and bacterial activities, being toxic to A. salina.

Atividade antibacteriana frente ao Streptococcus mutans e estabilidade de produtos naturais contendo extrato de Mikania glomerata Sprengel / Antibacterial activity against Streptococcus mutans and stability of the natural products containing extract from Mikania glomerata Sprengel

Mikania glomerata Sprengel (Asteraceae), conhecida como guaco, é usada popularmente como broncodilatador, antiasmático e expectorante, cujos efeitos são atribuídos à presença de cumarinas. O presente estudo avaliou o efeito de extratos e formulações (soluções antissépticase xaropes) contendo guaco, com ou sem própolis, sobre o crescimento de S. mutans e a estabilidade das soluções anti-sépticas. A atividade antibacteriana dos extratos e formulações sobre S. mutans ATCC 25175 foi realizada pelo método de difusão em ágar e, posteriormente, através da aplicação desse mesmo procedimento, determinou-se a estabilidade das soluções anti-sépticas submetidas à temperatura ambiente e sob refrigeração (8ºC - 10ºC), mensalmente, por um período de três meses. Os extratos de guaco e de própolis e as soluções anti-sépticas inibiram o crescimento de S. mutans. No primeiro mês, com exceção da soluçãoanti-séptica com guaco 5%, todas as demais inibiram o crescimento do microrganismo testado. No segundo mês, somente as soluções anti-sépticas contendo própolis produziram inibição bacteriana. Após três meses de armazenamento, as soluções contendo própolis, em temperatura ambiente, foram ativas e estáveis. Os resultados mostram que formulações contendo guaco, com ou sem própolis, foram ativas sobre S. mutans, mas podem perder a estabilidade em decorrência da temperatura. No entanto, estes achados demonstram que os produtos naturais podem ser uma alternativa importante no combate à formação da cárie e placa dentária.

Mikania glomerata Sprengel (Asteraceae), known as guaco, is commonly used as bronchodilator, antiasthmatic, and expectorant, and the effects observed are attributed to coumarin. The aim of the present study was to evaluate the effect of the extracts and formulations (antiseptic solutions and syrup) containing guaco, with or without propolis, against Streptococcus mutans, and the stability of the antiseptic solutions. The antibacterial activity of the extracts and the formulations against S. mutans ATCC 25175 was assessed by agar diffusion, with the same procedure being used to determine the stability of the antiseptic solutions under room temperature and refrigeration (8º - 10ºC) during a period of three months. The extracts containing guaco and propolis and the antiseptic solutions inhibited the growth of S. mutans. After the first month, except for the antiseptic solution with guaco 5%, all of them inhibited the microorganism tested. In the second month, only the antiseptic solution containing propolis produced the bacterial inhibition. In the last month, under room temperature, the solutions with propolis were active and stable. The results showed that the formulations containing guaco, with or without propolis, were active against S. mutans, but could lose stability depending on temperature. However, this report emonstrated that natural products could be an important alternative against oral infections, including tooth decay and dental plaque.

Aspectos da qualidade da tetraciclina em preparações farmacêuticas sólidas: correlação entre os métodos de dosagem por cromatografia líquida de alta eficiência e turbidimétrico / Aspects of the quality of tetracycline in solid pharmaceutical formulations: correlation between HPLC and microbiological methods

As tetraciclinas são encontradas no mercado sob várias formas farmacêuticas, sendo provenientes de diversos laboratórios farmacêuticos. Com o objetivo de avaliar a qualidade destes medicamentos, foram realizados os ensaios de dissolução in vitro e determinação quantitativa. Um total de 38 amostras de cápsulas de cloridrato de tetraciclina, fosfato de tetraciclina e cloridrato de oxitetraciclina e drágea de cloridrato de doxiciclina, englobando 12 fabricantes, foram analisadas. A dissolução do princípio ativo foi determinada para todas as amostras, conforme o método recomendado pela USP XXIII. Das amostras, duas foram reprovadas e outras quatro foram aprovadas após o reteste. A variação dos valores individuais obtidos no ensaio de dissolução para cada amostra, foi significativa, apresentando coeficiente de variação de até 14,2 por cento...