Tetradenia riparia (Lamiaceae) is native to Central Africa popularly known as myrrh, used in folk medicine to treat various diseases like malaria, gastroenteritis, and tropical skin disease. This research was to evaluate the antioxidant and antibacterial activities of the crude extract (CE) and fractions (FR) of the T. riparia by classical chromatography. The CE of T. riparia leaves was submitted to column chromatographic fractionation to obtain four fractions of the interest, which were identified by nuclear magnetic resonance and gas chromatograph coupled to mass spectrum: FR-I (abieta-7,9(11)-dien-13-β-ol), FR-II (Ibozol), FR-III (8 (14), 15-sandaracopimaradiene-2α, 18-diol and 8 (14), 15-sandaracopimaradiene-7α, 18-diol), and FR-IV (Astragalin, Boronolide and Luteolin). Total phenol content of CE and FR were measured, and antioxidant action by methods of DPPH (2,2-diphenyl-1-picrylhydrazyl), β-carotene/linoleic acid system, and ferric reducing/antioxidant power (FRAP) and the antibacterial activity was evaluated by the broth microdilution method with the determination of the minimum inhibitory concentration (MIC). The FR-IV presented antioxidant potential with 181.67 μg gallic acid/mg, IC of 0.61 μg/mL by DPPH method, 55.61% oxidation protection by β-carotene/linoleic acid system and 4.59 µM ferrous sulfate/mg of sample by FRAP, and the FR-I showed higher antibacterial potential on the strain Staphylococcus aureus with MIC 0.98 μg/mL, Enterococcus faecalis and Bacillus cereus with MIC 31.2 μg/mL. Thus, the fractionation of CE was extremely important to detect fractions with potential activities, and investigations are necessary regarding the mechanism of action and action in vivo.
Este trabalho relata uma experiência didática para estudantes do ensino médio, na qual foi abordado um tema de crescente interesse: a ciência forense. As atividades foram aplicadas a uma turma do 3º ano do período noturno de uma escola da rede pública localizada na cidade de Toledo (PR), na qual participaram aproximadamente 20 estudantes. Por intermédio de aulas expositivas e experimentais, que culminaram com uma simulação de um fato, denominada cena do crime, foi possível observar a motivação e participação dos alunos envolvidos. O uso da experimentação associada à ciência forense mostrou-se uma importante ferramenta didática para ser utilizada como facilitadora no processo de ensino-aprendizagem, bem como para a inserção dos conteúdos na disciplina de química no ensino médio. ensino de química, química forense, análises cena do crime
Abstract:In the present work, we report the synthesis and in vitro anticancer and antimicrobial activity evaluation of a new series of 1-substituted-β-carboline derivatives bearing a 4-benzylidene-4H-oxazol-5-one unity at C-3. The compound 2-[1-(4-methoxyphenyl)-9H-β-carbolin-3-yl]-4-(benzylidene)-4H-oxazol-5-one (11) was the most active derivative, exhibiting a potent cytotoxic activity against glioma (U251), prostate (PC-3) and ovarian (OVCAR-03) cancer cell lines with IC 50 values of 0.48, 1.50 and 1.07 µM, respectively. An in silico study of the ADME properties of the novel synthesized β-carboline derivatives was also performed.
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