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Braz. J. Pharm. Sci. (Online) ; 54(3): e17382, 2018. tab, graf
Artigo em Inglês | LILACS | ID: biblio-974400


Effective management of schizophrenia, acute mania, mixed episodes associated with bipolar disorders, and depression can be managed with aripiprazole moiety. In the present research work an attempt was made to minimize the dose related side effects thus improving the quality life of the patients. A novel biopolymer was isolated from the fruits of Trachyspermum ammi. Ten optimized nanosized aripiprazole loaded formulations were prepared in 1-5% concentration of biopolymer (FA1-FA5) and sodium CMC (FM1-FM5) by solvent casting technique. The formulated flexy films were evaluated for thickness, folding endurance, weight uniformity, surface pH, mucoadhesivity, In-vitro drug release studies, In-vivo pharmacodynamic study and stability studies. The isolated biopolymer showed inbuilt fimability and mucoadhesivity and consists of carbonyl, hydroxyl and thiocarbonyl functional groups. All formulations showed folding endurance from 153 to 170, mucoadhesion time in the range of 24-48hrs., and in-vitro drug release was performed using dynamic Franz Diffusion cell and analyzed using BIT-SOFTWARE. The experimental animals showed improved activity score on actophotometer. The formulated nanosized aripiprazole loaded bio-flexy films showed pharmacotherapeutic response. Conclusion can be drawn that optimized formulation showed effective Pharmacodynamic activity and can be used as for improving therapeutic efficacy of aripiprazole through this platform.

Esquizofrenia/diagnóstico , Aripiprazol/efeitos adversos , Mucosa Bucal , Palato Mole , Biopolímeros/agonistas , Técnicas In Vitro/instrumentação , Carum/efeitos adversos
Braz. J. Pharm. Sci. (Online) ; 53(4): e00076, 2017. tab, graf
Artigo em Inglês | LILACS | ID: biblio-889414


ABSTRACT Considering the reported activity of carvone in the literature, this study aimed to evaluate the antimicrobial, cytotoxic and chemopreventive activities of (+)- and (-)-carvone, (+)- and (-)- hydroxydihydrocarvone and α,ß-epoxycarvone. (+)-Hydroxydihydrocarvone (HC+), (-)-hydroxydihydrocarvone (HC-) and α,ß-epoxycarvone (EP) were obtained by synthesis using (+)-carvone (C+) or (-)-carvone (C-) as precursors. The antifungal activity (MIC and MFC) were evaluated against Candida parapsilosis, C. tropicalis, C. krusei and C. albicans and the antibacterial activity (MIC and MBC) against Escherichia coli and Staphylococcus aureus. The cytotoxicity assays were performed with human cancer cell lines HepG-2 and SiHa and the normal strain MRC-5 through sulphorrodamine B assay. Chemoprevention was evaluated through quinone reductase assay. Our results showed no cytotoxicity on tumor and normal cell lines and no induction of the quinone reductase enzyme. C- and HC- presented activity against E. coli. All compounds presented weak antifungal activity against C. tropicalis and C. parapsilosis. EP and C+ showed moderate activity against C. krusei. Results suggest the potential use of carvones and its derivatives as antifungal agents against Candida yeasts. The absence of cytotoxicity in cell lines indicates safety in the use of these compounds

Óleos Voláteis/análise , Quimioprevenção , Carum/classificação , Anti-Infecciosos/análise , Quimioprevenção , Antifúngicos
Braz. j. microbiol ; 45(2): 523-531, Apr.-June 2014. tab
Artigo em Inglês | LILACS | ID: lil-723118


Emergence of drug-resistant strains has demanded for alternative means of combating fungal infections. Oils of Carum copticum and Thymus vulgaris have long been used in ethnomedicine for ailments of various fungal infections. Since their activity has not been reported in particular against drug-resistant fungi, this study was aimed to evaluate the effects of oils of C. copticum and T. vulgaris on the growth and virulence of drug-resistant strains of Aspergillus spp. and Trichophyton rubrum. The gas chromatography-mass spectrometry analysis revealed thymol constituting 44.71% and 22.82% of T. vulgaris and C. copticum, respectively. Inhibition of mycelial growth by essential oils was recorded in the order of thymol > T. vulgaris > C. copticum against the tested strains. RBC lysis assay showed no tested oils to be toxic even up to concentration two folds higher than their respective MFCs. Thymol exhibited highest synergy in combination with fluconazole against Aspergillus fumigatus MTCC2550 (FICI value 0.187) and T. rubrum IOA9 (0.156) as determined by checkerboard method. Thymol and T. vulgaris essential oil were equally effective against both the macro and arthroconidia growth (MIC 72 µg/mL). A > 80% reduction in elastase activity was recorded for A. fumigatus MTCC2550 by C. copticum, T. vulgaris oils and thymol. The effectiveness of these oils against arthroconidia and synergistic interaction of thymol and T. vulgaris with fluconazole can be exploited to potentiate the antifungal effects of fluconazole against drug-resistant strains of T. rubrum and Aspergillus spp.

Antifúngicos/farmacologia , Aspergillus fumigatus/efeitos dos fármacos , Carum/química , Óleos Vegetais/farmacologia , Thymus (Planta)/química , Trichophyton/efeitos dos fármacos , Antifúngicos/isolamento & purificação , Antifúngicos/toxicidade , Aspergillus fumigatus/crescimento & desenvolvimento , Aspergillus fumigatus/fisiologia , Sinergismo Farmacológico , Eritrócitos/efeitos dos fármacos , Fluconazol/farmacologia , Cromatografia Gasosa-Espectrometria de Massas , Elastase Pancreática/antagonistas & inibidores , Óleos Vegetais/química , Óleos Vegetais/isolamento & purificação , Óleos Vegetais/toxicidade , Esporos Fúngicos/efeitos dos fármacos , Esporos Fúngicos/crescimento & desenvolvimento , Timol/análise , Trichophyton/fisiologia , Virulência/efeitos dos fármacos
Braz. j. microbiol ; 45(1): 89-96, 2014. ilus, tab
Artigo em Inglês | LILACS | ID: lil-709483


This study was conducted to evaluate the antibacterial effect of Carum copticum essential oil (Ajowan EO) against Listeria monocytogenes in fish model system. Ajowan EO chemical composition was determined by gas chromatography/mass spectral analysis and the highest concentration of Carum copticum essential oil without any significant changes on sensory properties of kutum fish (Rutilus frisii kutum) was assigned. Then the inhibitory effect of Ajowan EO at different concentrations in presence of salt and smoke component was tested on L. monocytogenes growth in fish peptone broth (FPB), kutum broth and cold smoked kutum broth at 4 ºC for 12 days. Ajowan EO completely decreased the number of L. monocytogenes in FPB after 12 days of storage, however, antimicrobial effect of EO significantly reduced in kutum and cold smoked kutum broth. Addition of 4% NaCl and smoke component improved the anti-listerial activity of Ajowan EO in all fish model broths.

Animais , Antibacterianos/farmacologia , Carum/química , Doenças dos Peixes/tratamento farmacológico , Doenças dos Peixes/microbiologia , Listeria monocytogenes/efeitos dos fármacos , Listeriose/veterinária , Óleos Voláteis/farmacologia , Antibacterianos/química , Antibacterianos/isolamento & purificação , Contagem de Colônia Microbiana , Meios de Cultura/química , Cyprinidae/microbiologia , Cromatografia Gasosa-Espectrometria de Massas , Listeriose/tratamento farmacológico , Listeriose/microbiologia , Viabilidade Microbiana/efeitos dos fármacos , Óleos Voláteis/química , Óleos Voláteis/isolamento & purificação , Cloreto de Sódio/metabolismo , Temperatura
Bol. latinoam. Caribe plantas med. aromát ; 9(6): 495-500, nov. 2010. tab
Artigo em Inglês | LILACS | ID: lil-644990


Natural essential oils are used extensively in fragrances, flavorants, and in the food and pharmaceutical industries. During hydrodistillation, a part of the essential oil becomes dissolved in the condensate and lost as this water is discarded. In this study, carvone and limonene content recovered from hydrodistillation waste water of caraway fruit were quantified using two methods for recovering dissolved aromatic molecules from condensate water: extraction through distillation and extraction by means of a solvent. This allows for the conservation of useful molecules which are typically discarded with the waste water produced during the distillation process. The objective of this study was to quantify the carvone and limonene content recoverable from waste water derived from the distillation of caraway essential oil. The well-known Clevenger method and a simpler, more practical technique employing cyclohexane as a solvent were employed to determine the recoverable content of aromatic molecules from the hydrosol. The chemical compositions of the respective recovered extracts were compared with those of the primary oils to analyze the efficacy of these methods. Recovered extract accounted for 10 to 40 percent of the total oil yield. The limonene and carvone molecules recovered using these methods were quantified through gas chromatography in order to characterize the composition of the secondary extract produced.

Los aceites esenciales naturales se utilizan ampliamente en las fragancias, saborizantes, y en la industria alimentaria y farmacéutica. Durante la hidrodestilación, una parte del aceite esencial se disuelve en el condensado y se pierde como agua de descarga. En este estudio, el contenido de carvona y limoneno recuperados del agua de desecho de la hidrodestilación de la fruta de alcaravea se cuantificaron utilizando dos métodos para recuperar las moléculas aromáticas disueltas en el agua condensada: extracción a través de la destilación y la extracción con un disolvente. Esto permite la conservación de las moléculas útiles que normalmente son desechadas con las aguas residuales producidas durante el proceso de destilación. El objetivo de este estudio fue cuantificar el contenido de carvona y limoneno recuperable de las aguas residuales procedente de la destilación del aceite esencial de alcaravea. El conocido método de Clevenger y una técnica sencilla y práctica que emplea ciclohexano como disolvente fueron utilizadas para determinar el contenido de moléculas aromáticas contenidas en el hidrosol. La composición química de los extractos recuperados fue comparada con los aceites primarios para analizar la eficacia de estos métodos. El extracto recuperado representa del 10 al 40 por ciento del contenido total de aceite esencial. Las moléculas de limoneno y carvona recuperadas mediante estos métodos se cuantificaron mediante cromatografía de gases con el fin de caracterizar la composición del extracto secundario.

Óleos Voláteis/isolamento & purificação , Óleos Voláteis/química , Carum , Cicloexanos/análise , Fracionamento Químico/métodos , Monoterpenos/análise , Cromatografia Gasosa , Destilação , Terpenos/análise