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1.
Antibiotics (Basel) ; 8(2)2019 May 04.
Artigo em Inglês | MEDLINE | ID: mdl-31060239

RESUMO

Microbial resistance to currently available antibiotics is a public health problem in the fight against infectious diseases. Most antibiotics are characterized by numerous side effects that may be harmful to normal body cells. To improve the efficacy of these antibiotics and to find an alternative way to minimize the adverse effects associated with most conventional antibiotics, piperine and piperlongumine were screened in combination with conventional rifampicin, tetracycline, and itraconazole to evaluate their synergistic, additive, or antagonistic interactions against Staphylococcus aureus, Pseudomonas aeruginosa, and Candida albicans. The fractional inhibitory concentration index was used to estimate the synergistic effects of various combination ratios of the piperamides and antibiotics against the bacterial and fungal strains. Both piperine and piperlongumine showed synergistic effects against S. aureus when combined at various ratios with rifampicin. Synergistic interaction was also observed with piperine in combination with tetracycline against S. aureus, while antagonistic interaction was recorded for piperlongumine and tetracycline against S. aureus. All the piperamide/antibacterial combinations tested against P. aeruginosa showed antagonistic effects, with the exception of piperine and rifampicin, which recorded synergistic interaction at a ratio of 9:1 rifampicin/piperine. No synergistic interaction was observed when the commercial compounds were combined with itraconazole and tested against C. albicans. The results showed that piperine and piperlongumine are capable of improving the effectiveness of rifampicin and tetracycline. Dosage combinations of these bioactive compounds with the antibiotics used may be a better option for the treatment of bacterial infections that aims to minimize the adverse effects associated with the use of these conventional antibacterial drugs.

2.
J Ethnopharmacol ; 229: 157-166, 2019 Jan 30.
Artigo em Inglês | MEDLINE | ID: mdl-30336302

RESUMO

ETHNOBOTANICAL RELEVANCE: Piper guineense occurs commonly in West Africa where it is used for fungal infections instead of the costly and not always accessible conventional antifungals. Fungal, yeast-based diseases are common in West-Africa especially among those living with HIV/AIDS, and thus this study was performed in Imo state, South-Eastern Nigeria, where P. guineense is predominantly used for the treatment of fungal diseases, such as skin rashes, oral thrush and vaginosis. AIM OF STUDY: The scarce number of previous studies on the documentation of the traditional uses of P. guineense extracts for the treatment of fungal infections in Nigeria prompted this survey. The investigation focused on how traditional healers recognize and diagnose fungal infections, how P. guineense is collected, on the various parts used for the treatments, methods of preparations, administrations and treatments. In addition, an in vitro antifungal screening of P. guineense fruit and leaf extracts of various polarities, and piperine and piperlongumine, representing the main constituents in these extracts, were performed. METHODS: A house to house ethnobotanical survey was conducted using questionnaires. Twenty traditional medical practitioners (TMP) and herb sellers from ten villages were interviewed. Four human pathogenic strains of yeast and Cryptococcus neoformans, a yeast-like basidiomycete causing meningitis in immunocompromised individuals, were used for the antifungal screening. RESULTS: The traditional medical practitioners (TMP) and herb sellers explained that the leaves and fruits are the most commonly used plant parts for the treatments. The oral intake of the extracts in locally produced bamboo alcohol (Kai-kai) is the most common method of administration. In accordance with these recorded traditional uses, we found that extracts of P. guineense were growth inhibitory against the fungal strains with MIC values ranging from 39 to 2500 µg/mL. The lowest MIC value of 39 µg/mL was recorded for a methanol fruit extract against Candida albicans, C. glabrata and C. tropicalis. In addition, ethanol and hexane fruit extracts were effective against the growth of C. albicans and C. glabrata, respectively, with a MIC of 78 µg/mL. Piperlongumine and piperine were active against C. albicans with MIC values of 39 and 78 µg/mL respectively. CONCLUSION: P. guineense fruit and leaf extracts, as well as their piperamide alkaloid constituents piperine and piperlongumine, have interesting antifungal properties and could have potential as new antifungal scaffolds. Our results warrant further in-depth investigations to isolate and characterize piperamide alkaloids and other compounds responsible for the antifungal activity in the extracts.


Assuntos
Antifúngicos/uso terapêutico , Micoses/tratamento farmacológico , Fitoterapia , Piper , Extratos Vegetais/uso terapêutico , Adulto , África Ocidental , Idoso , Antifúngicos/farmacologia , Candida/efeitos dos fármacos , Candida/crescimento & desenvolvimento , Cryptococcus neoformans/efeitos dos fármacos , Cryptococcus neoformans/crescimento & desenvolvimento , Etnobotânica , Feminino , Frutas , Conhecimentos, Atitudes e Prática em Saúde , Humanos , Masculino , Medicinas Tradicionais Africanas , Testes de Sensibilidade Microbiana , Pessoa de Meia-Idade , Micoses/diagnóstico , Extratos Vegetais/farmacologia , Folhas de Planta , Inquéritos e Questionários , Adulto Jovem
3.
Antibiotics (Basel) ; 7(4)2018 Nov 09.
Artigo em Inglês | MEDLINE | ID: mdl-30423994

RESUMO

Piper guineense is a food and medicinal plant commonly used to treat infectious diseases in West-African traditional medicine. In a bid to identify new antibacterial compounds due to bacterial resistance to antibiotics, twelve extracts of P. guineense fruits and leaves, obtained by sequential extraction, as well as the piperine and piperlongumine commercial compounds were evaluated for antibacterial activity against human pathogenic bacteria. HPLC-DAD and UHPLC/Q-TOF MS analysis were conducted to characterize and identify the compounds present in the extracts with promising antibacterial activity. The extracts, with the exception of the hot water decoctions and macerations, contained piperamide alkaloids as their main constituents. Piperine, dihydropiperine, piperylin, dihydropiperylin or piperlonguminine, dihydropiperlonguminine, wisanine, dihydrowisanine and derivatives of piperine and piperidine were identified in a hexane extract of the leaf. In addition, some new piperamide alkaloids were identified, such as a piperine and a piperidine alkaloid derivative and two unknown piperamide alkaloids. To the best of our knowledge, there are no piperamides reported in the literature with similar UVλ absorption maxima and masses. A piperamide alkaloid-rich hexane leaf extract recorded the lowest MIC of 19 µg/mL against Sarcina sp. and gave promising growth inhibitory effects against S. aureus and E. aerogenes as well, inhibiting the growth of both bacteria with a MIC of 78 µg/mL. Moreover, this is the first report of the antibacterial activity of P. guineense extracts against Sarcina sp. and E. aerogenes. Marked growth inhibition was also obtained for chloroform extracts of the leaves and fruits against P. aeruginosa with a MIC value of 78 µg/mL. Piperine and piperlongumine were active against E. aerogenes, S. aureus, E. coli, S. enterica, P. mirabilis and B. cereus with MIC values ranging from 39⁻1250 µg/mL. Notably, the water extracts, which were almost devoid of piperamide alkaloids, were not active against the bacterial strains. Our results demonstrate that P. guineense contains antibacterial alkaloids that could be relevant for the discovery of new natural antibiotics.

4.
Am J Pharm Educ ; 73(8): 151, 2009 Dec 17.
Artigo em Inglês | MEDLINE | ID: mdl-20221344

RESUMO

OBJECTIVE: To improve pharmacy education through integrating theory and practice, coherent constructively aligned course entities, and enhanced deep-level learning. DESIGN: The reform was conducted collaboratively with faculty and staff members, students, and stakeholders in pharmacy. The curriculum, syllabus, and teaching methods were assessed through evaluations and research, conducting core content analyses, and measuring the workload of pharmacy education courses. The new curriculum, launched in August 2005, consists of 6 strands, comprised of different courses which run through the entire program. ASSESSMENT: Three years after the introduction of the reformed curriculum, the results of the reform are being evaluated. Ongoing assessments of teaching and learning will reveal how the education at the faculty level has developed since the reform. These assessment procedures are an integral part of the faculty's quality assurance program. CONCLUSION: The integration of practical training and theoretical studies was improved with personal study plans introduced to enhance students' learning.


Assuntos
Currículo , Educação em Farmácia/organização & administração , Faculdades de Farmácia/organização & administração , Docentes/organização & administração , Finlândia , Humanos , Aprendizagem , Desenvolvimento de Programas , Avaliação de Programas e Projetos de Saúde , Estudantes de Farmácia , Ensino/organização & administração , Carga de Trabalho
5.
J Agric Food Chem ; 51(16): 4563-9, 2003 Jul 30.
Artigo em Inglês | MEDLINE | ID: mdl-14705878

RESUMO

Water-soluble extracts from the Mentha species M. aquatica L. and M. haplocalyx Briq., the hybrids M. x dalmatica L. and M. x verticillata L., the varieties M. arvensis var. japanensis [M. arvensis L. var. piperascens Holmes ex Christ] and M. spicata L. var. crispa Benth, and M. x piperita L. "Frantsila", M. "Morocco", and M. "Native Wilmet" cultivars were screened for potential antioxidative properties. These properties included iron(III) reduction, iron(II) chelation, 1,1-diphenyl-2-picrylhydrazyl radical scavenging, and the ability to inhibit iron(III)-ascorbate-catalyzed hydroxyl radical-mediated brain phospholipid peroxidation. Total phenol content and qualitative and quantitative compositional analyses of each extract were also made. The extracts demonstrated varying degrees of efficacy in each assay, with the M. x piperita "Frantsila" extract being better than the other extracts, except for ferrous iron chelation. With the exception of iron chelation, it appeared that the level of activity identified was strongly associated with the phenolic content.


Assuntos
Antioxidantes/farmacologia , Mentha/química , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Animais , Compostos de Bifenilo , Química Encefálica , Bovinos , Compostos Férricos/química , Compostos Ferrosos/química , Hibridização Genética , Radical Hidroxila/química , Quelantes de Ferro/química , Peroxidação de Lipídeos/efeitos dos fármacos , Picratos/química , Especificidade da Espécie , Água
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