Background: For more than 60 years, the lack of new anti-tuberculosis drugs and the increase of resistant Mycobacterium tuberculosis lineages exhibit a therapeutic challenge, demanding new options for the treatment of resistant tuberculosis. Objective: Herein, we determined the (i) activities of (-)-camphene and derivatives and (ii) combinatory effect with pyrazinamide (PZA) against Mycobacterium tuberculosis in acidic pH and (iii) cytotoxicity in VERO cells. Methods: The activity of (-)-camphene and 15 derivatives were determined in M. tuberculosis H37Rv in culture medium at pH 6.0 by Resazurin Microtiter Assay Plate (REMA). The combinatory study of three (-)-camphene derivatives with PZA was carried out in seven multidrug-resistant (MDR) clinical isolates by REMA and Checkerboard, respectively. The assay of 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium (MTT) bromide in VERO cells was used to determine the derivatives cytotoxicity. Results: Four (-)-Camphene derivatives, (4), (5a) (5d) and (5h), showed reduction in MIC value at pH 6.0 compared to MIC detected at pH 6.8 in M. tuberculosis H37Rv and multidrug resistant clinical isolates. Three (-)-camphene derivatives, (4), (5d) and (5h), showed synergistic effect (FICI ≤ 0.5) combined with PZA and were more selective for M. tuberculosis than VERO cell (selective index from 7.7 to 84.2). Conclusion: Three (-)-camphene derivatives have shown to be promising anti-TB molecule scaffold due to the low MIC values in acidic pH against MDR M. tuberculosis clinical isolates, synergism with PZA and low cytotoxicity.
Background: There is critical need for new therapeutic options for treatment of diseases caused by mycobacteria. Materials & methods: Gallesia integrifolia essential oils (EOs) and crude extracts (CEs) were tested for their anti- Mycobacterium tuberculosis and anti-nontuberculous mycobacteria activity. Results: Minimum inhibitory concentration (MIC) of EOs ranged from 15.63 to 62.5 μg/ml against M. tuberculosis and 62.5 to >250 μg/ml against nontuberculous mycobacteria. CEs showed low activity. All EO tested demonstrated synergism with antituberculosis drugs. The cytotoxicity of EOs and CEs, in different cell lines, showed selectivity index from 2.2 to 9.8 and >0.056 to 2.0, respectively. Conclusion: G. integrifolia EOs are a candidate for the development of new therapeutic options in the treatment of tuberculosis and other mycobacterial diseases.
A diabetes gestacional é uma doença desenvolvida durante a gestação, que afeta e acarreta problemas tanto para a mãe quanto para o feto. Seu principal meio de diagnóstico é por meio do teste oral de tolerância à glicose, sendo realizado entre a 24.a e a 28.a semana da gestação. Podendo se manter mesmo após a gestação, seu diagnóstico precoce e início de tratamento se fazem muito importantes para minimizar os impactos na mãe e no feto. Este trabalho trata-se de uma revisão bibliográfica com o objetivo de conceituar e ressaltar a importância do diagnóstico da diabetes gestacional.
O Diabetes mellitus é uma doença de grande prevalência mundial. Ela pertence a um grupo de distúrbios metabólicos que resultam em níveis elevados de glicose no sangue, causada pela falta ou má absorção de insulina. A dosagem de hemoglobina glicada é um dos exames mais utilizados para o acompanhamento de pacientes diabéticos e a partir do seu resultado é possível avaliar os níveis glicêmicos no organismo pelos últimos três meses. É indicado ao paciente diabético manter a taxa de HbA1C abaixo dos 7%, reduzindo drasticamente as chances de desenvolvimento de complicações provenientes desta patologia, evidenciando assim, a importância no controle do Diabetes mellitus.
Background: The development of drugs is essential to eradicate tuberculosis. Materials & methods: Sixteen 3,5-dinitrobenzoylhydrazone (2–17) derivatives and their synthetic precursors 3,5-dinitrobenzoylhydrazide (1) and methyl ester (18) were screened for their anti- Mycobacterium tuberculosis ( Mtb) potential. Results: Twelve compounds had minimum inhibitory concentration (MIC) ranging from 0.24 to 7.8 μg/ml against the Mtb strain. The activity was maintained in multidrug-resistant Mtb clinical isolates. Only compound (17) showed activity against nontuberculous mycobacteria. The compounds exhibited a limited spectrum of activity, with an MIC >500 μg/ml against Gram-positive and -negative bacteria. Compounds (2), (5) and (11) showed a synergistic effect with rifampicin. An excellent selectivity index value was found, with values reaching 583.33. Conclusion: 3,5-dinitrobenzoylhydrazone derivatives could be considered as a scaffold for the development of antituberculosis drugs.
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