Model Analytical Development for Physical, Chemical, and Biological Characterization of Momordica charantia Vegetable Drug.

Momordica charantia is a species cultivated throughout the world and widely used in folk medicine, and its medicinal benefits are well documented, especially its pharmacological properties, including antimicrobial activities. Analytical methods have been used to aid in the characterization of compounds derived from plant drug extracts and their products. This paper developed a methodological model to evaluate the integrity of the vegetable drug M. charantia in different particle sizes, using different analytical methods. M. charantia was collected in the semiarid region of Paraíba, Brazil. The herbal medicine raw material derived from the leaves and fruits in different particle sizes was analyzed using thermoanalytical techniques as thermogravimetry (TG) and differential thermal analysis (DTA), pyrolysis coupled to gas chromatography/mass spectrometry (PYR-GC/MS), and nuclear magnetic resonance ((1)H NMR), in addition to the determination of antimicrobial activity. The different particle surface area among the samples was differentiated by the techniques. DTA and TG were used for assessing thermal and kinetic parameters and PYR-GC/MS was used for degradation products chromatographic identification through the pyrograms. The infusions obtained from the fruit and leaves of Momordica charantia presented antimicrobial activity.

Antifungal activity of topical microemulsion containing a thiophene derivative.

Fungal infections have become a major problem of worldwide concern. Yeasts belonging to the Candida genus and the pathogenic fungus Cryptococcus neoformans are responsible for different clinical manifestations, especially in immunocompromised patients. Antifungal therapies are currently based on a few chemotherapeutic agents that have problems related to effectiveness and resistance profiles. Microemulsions are isotropic, thermodynamically stable transparent systems of oil, water and surfactant that can improve the solubilization of lipophilic drugs. Taking into account the need for more effective and less toxic drugs along with the potential of thiophene derivatives as inhibitors of pathogenic fungi growth, this study aimed to evaluate the antifungal activity of a thiophene derivative (5CN05) embedded in a microemulsion (ME). The minimum inhibitory concentration (MIC) was determined using the microdilution method using amphotericin B as a control. The formulations tested (ME- blank and ME-5CN05) showed physico-chemical properties that would allow their use by the topical route. 5CN05 as such exhibited moderate or weak antifungal activity against Candida species (MIC = 270-540 µg . mL(-1)) and good activity against C. neoformans (MIC = 17 µg . mL(-1)). Candida species were susceptible to ME-5CN05 (70-140 µg . mL(-1)), but C. neoformans was much more, presenting a MIC value of 2.2 µg . mL(-1). The results of this work proved promising for the pharmaceutical industry, because they suggest an alternative therapy against C. neoformans.

Desenvolvimento e validação de metodologias analíticas para quantificação de um derivado tiofênico em sistemas microemulsionados / Development and validation of analytical methodologies for measurement of a tiophene derivative in microemulsion systems

O presente trabalho teve por objetivo validar métodos por espectrofotometria UV-Vis e por CLAE para a análise quantitativa de um derivado do tiofeno, o 2-[(3,4-dicloro-benzilideno)-amino]-5,6-diidro-4H-ciclopen-ta[b]tiofeno-3-carbonitrila (5CN05) e aplicá-los no doseamento da molécula contida em microemulsões, Os métodos propostos foram validados conforme a Resolução 899/2003 da Agência Nacional de Vigilância Sanitária (ANVISA), O comprimento de onda de máxima absorção do fármaco 5CN05 foi detectado em λ max= 387nm, O método espectrofotométrico validado mostrou-se seletivo, apresentando linearidade na faixa de 3 a 16 µg.mL-1, coeficiente de correlação (r) igual a 0,9998 e limites de detecção e quantificação de 0,12 µg.mL-1 e 0,41 µg.mL-1, respectivamente, Para o método CLAE, observou-se linearidade na faixa de 0,1 a 3,0 µg.mL-1, r = 0,99915, limites de detecção e quantificação de 0,07 µg.mL-1 e 0,10 µg.mL-1 respectivamente, Para ambos os métodos, os parâmetros precisão, exatidão e robustez mostraram-se adequados para o uso pretendido, As metodologias propostas podem ser seguramente aplicadas para quantificação do 5CN05 em produtos farmacêuticos como microemulsões...

This study aims to validate methods of Uv-Vis) and HPLC for quantitative determination of a thiophene derivative, 2 - [(3,4-dichloro -benzylidene)-amino] -5,6-dihydro-4H-cyclopentyl-ta [b] thiophene-3- carbonitrile referred in this study as 5CN05, and apply them to quantify the 5CN05 in microemulsions. The proposed methods were validated according to the Resolution RE 899/2003 of the National Health Surveillance Agency (ANVISA). The 5CN05 was detected by UV-Vis at λ max= 387nm. The validated UVVis UVVis method proved to be selective, showing linearity in the range of 3-16 µg.mL-1, correlation coefficient (r) of 0.9998 and limits of detection and quantification of 0.12 µg.mL-1 and 0.41 µg.mL-1 respectively. For the CLAE method the linearity was observed in the range 0.1 to 3.0 µg.mL-1, r = 0.99915, limits of detection and quantification of 0.07 µg.mL-1 and 0.10 µg.mL-1 respectively. For both UV-Vis and CLAE methods, the precision parameters, accuracy and robustness were adequate for the intended use. The proposed methodologies can be safely applied to quantify the 5CN05 in pharmaceutical microemulsions products...

Antifungal activity of topical microemulsion containing a thiophene derivative

Fungal infections have become a major problem of worldwide concern. Yeasts belonging to the Candida genus and the pathogenic fungus Cryptococcus neoformans are responsible for different clinical manifestations, especially in immunocompromised patients. Antifungal therapies are currently based on a few chemotherapeutic agents that have problems related to effectiveness and resistance profiles. Microemulsions are isotropic, thermodynamically stable transparent systems of oil, water and surfactant that can improve the solubilization of lipophilic drugs. Taking into account the need for more effective and less toxic drugs along with the potential of thiophene derivatives as inhibitors of pathogenic fungi growth, this study aimed to evaluate the antifungal activity of a thiophene derivative (5CN05) embedded in a microemulsion (ME). The minimum inhibitory concentration (MIC) was determined using the microdilution method using amphotericin B as a control. The formulations tested (ME- blank and ME-5CN05) showed physico-chemical properties that would allow their use by the topical route. 5CN05 as such exhibited moderate or weak antifungal activity against Candida species (MIC = 270-540 µg.mL-1) and good activity against C. neoformans (MIC = 17 µg.mL-1). Candida species were susceptible to ME-5CN05 (70-140 µg.mL-1), but C. neoformans was much more, presenting a MIC value of 2.2 µg.mL-1. The results of this work proved promising for the pharmaceutical industry, because they suggest an alternative therapy against C. neoformans.

Antifungal activity of topical microemulsion containing a thiophene derivative

Fungal infections have become a major problem of worldwide concern. Yeasts belonging to the Candida genus and the pathogenic fungus Cryptococcus neoformans are responsible for different clinical manifestations, especially in immunocompromised patients. Antifungal therapies are currently based on a few chemotherapeutic agents that have problems related to effectiveness and resistance profiles. Microemulsions are isotropic, thermodynamically stable transparent systems of oil, water and surfactant that can improve the solubilization of lipophilic drugs. Taking into account the need for more effective and less toxic drugs along with the potential of thiophene derivatives as inhibitors of pathogenic fungi growth, this study aimed to evaluate the antifungal activity of a thiophene derivative (5CN05) embedded in a microemulsion (ME). The minimum inhibitory concentration (MIC) was determined using the microdilution method using amphotericin B as a control. The formulations tested (ME- blank and ME-5CN05) showed physico-chemical properties that would allow their use by the topical route. 5CN05 as such exhibited moderate or weak antifungal activity against Candida species (MIC = 270-540 µg.mL-1) and good activity against C. neoformans (MIC = 17 µg.mL-1). Candida species were susceptible to ME-5CN05 (70-140 µg.mL-1), but C. neoformans was much more, presenting a MIC value of 2.2 µg.mL-1. The results of this work proved promising for the pharmaceutical industry, because they suggest an alternative therapy against C. neoformans.

Contaminação fúngica de plantas medicinais utilizadas em chás / Fungal contamination of medicinal plants used in teas

Este trabalho teve como objetivo avaliar a qualidade microbiológica quanto à presença de fungos filamentosos em ervas do tipo Peumus boldus Molina (Boldo), Pimpinella anisum L. (erva-doce) e Matricaria chamomilla L. (Camomila) comercializadas na cidade de Campina Grande (Paraíba). Nove amostras de cada planta foram analisadas, totalizando 27 amostras, obtidas aleatoriamente nas feiras livres e barracas informais da cidade. Cada 10 g de amostra foram suspensas em 90 mL de solução salina 0,89% estéril, obtendo-se o concentrado, a partir do qual foram realizadas diluições sucessivas. A seguir, uma alíquota de 0,1mL de cada diluição foi semeada em placas de Petri contendo Ágar Sabouraud Dextrose, as quais foram incubadas à temperatura ambiente por cinco a dez dias. Após este período foram contadas as colônias fúngicas presentes e realizados seus respectivos microcultivos para identificação através de microscópio óptico. Foram encontrados fungos toxigênicos como Aspergillus sp., Penicillium sp. e Fusarium sp., estando o primeiro presente em todas as amostras avaliadas. Também foram identificados os fungos Exophiala sp. E Fonsecaea sp., que possuem importância clínica, podendo causar micose. A forma como estas plantas são armazenadas para comercialização e a falta de fiscalização torna questionável a qualidade das plantas comercializadas para obtenção de chás, o que pode comprometer a saúde do consumidor ao utilizar esses produtos na forma de Chá.

The aim of this study was to assess the microbiological quality, with regard to the presence of filamentous fungi, of the tea herbs Peumus boldus Molina (boldo leaf), Pimpinella anisum L. (anise) and Matricaria chamomilla L. (wild chamomile) marketed in the city of Campina Grande (Paraiba State, Brazil). Nine samples of each plant, totaling 27 samples, were randomly collected in street markets and informal stalls in the city. In the laboratory, 10 g of each sample was ground and suspended in 90 mL of 0.89% sterile saline solution, affording the concentrate from which serial dilutions were obtained. Aliquots of 0.1 mL of each dilution were spread on plates of Sabouraud Dextrose Agar, which were then incubated at room temperature for five to ten days. After this period, the fungal colonies were counted, their morphology was analyzed and subcultures were made on slides for identification by optical microscope. Toxigenic fungi such as Aspergillus sp., Penicillium sp. and Fusarium sp. were found, the first being present in all plant samples. The fungi Exophiala sp. and Fonsecaea sp., which are clinically significant as they can cause mycoses, were also identified. The method of storing these plants before sale and the lack of inspection raise questions about the quality of the marketed herbs, suggesting that the health of the consumer who uses these products to make tea could be harmed.