Avaliação biológica de Foeniculum vulgare (Mill. ) (Umbelliferae/Apiaceae) / Biological evaluation of Foeniculum vulgare (Mill. ) (Umbelliferae/Apiaceae)

Foeniculum vulgare Mill. é espécie herbácea da família Umbelliferae, nativa da região do Mediterrâneo e da Ásia Menor, amplamente distribuída em todo o território brasileiro. É conhecida popularmente como funcho ou erva-doce e usada na medicina como analgésico, digestivo, carminativo, diurético, expectorante, lactígeno, anti-inflamatório, e antiespasmódico. O extrato bruto etanólico para a verificação das atividades biológicas foi preparado a partir de sementes compradas no comércio. Para a realização do perfil fitoquímico foi utilizada a cromatografia em camada delgada analítica; a atividade antimicrobiana foi determinada pelo teste de difusão em disco de papel e da concentração inibitória mínima (CIM); a atividade antinociceptiva foi realizada pelo método de contorções abdominais em cobaias. Os micro-organismos testados foram isolados clínicos multirresistentes obtidos do Setor de Bacteriologia do Hospital das Clínicas de Pernambuco. O estudo fitoquímico identificou a maioria dos compostos secundários presentes na fração metanólica das sementes, sendo eles: triterpenos, glicosídeos de flavanóides, terpenos menores (monoterpenóides, sesquiterpenóide e diterpenóides), e açúcares redutores. Os resultados obtidos mostraram que o extrato etanólico apresentou maior atividade frente à Micrococcus spp. (CIM=250µg/mL). Os resultados da avaliação da atividade antinociceptiva demonstraram que apenas a dosagem de 298 mg/Kg quando comparado com o padrão indometacina conseguiu uma redução significativa no número de contorções abdominais dos animais. Estudos posteriores deverão ser realizados para a identificação e isolamento de alguns compostos secundários, bem como a realização de outros protocolos de analgesia.

Foeniculum vulgare Mill. (Umbelliferae) is a herbaceous plant of the family Umbelliferae, native to the Mediterranean and Asia Minor region and widely distributed all over the Brazilian territory. It is commonly known as fennel or "erva-doce" and has been used in medicine as analgesic, digestive, carminative, diuretic, expectorant, lactigenous, anti-inflammatory, and antispasmodic agent. Crude ethanolic extract for the verification of biological activities was prepared from seeds bought in the market. For the phytochemical profile, analytical thin-layer chromatography was used; the antimicrobial activity was determined by the paper disc diffusion test and minimum inhibitory concentration (MIC); the antinociceptive activity was verified by the method of abdominal writhings in the animals. The tested microorganisms were multiresistant clinical isolates obtained from the Bacteriology Sector of the Clinical Hospital of Pernambuco. The phytochemical study identified the majority of secondary compounds present in the methanolic fraction of seeds, as follows: triterpenes, flavanoid glycosides, smaller terpenes (monoterpenoids, sesquiterpenoids and diterpenoids) and reducing sugars. The obtained results showed that the ethanolic extract had greater activity against Micrococcus spp. (MIC=250µg/mL). Results of the evaluation of the antinociceptive activity demonstrated that only the dosage of 298 mg/Kg, compared to the indomethacin pattern, led to a significant reduction in the number of abdominal writhings in the animals. Further studies will be carried out for the identification and isolation of some secondary compounds, as well as other analgesic protocols.

Synthesis and antitumour activity of the Primin (2-methoxy-6-n-pentyl-1,4-benzoquinone) and analogues.

Cancer is a serious worldwide health threat, killing almost seven million people per year. Quinones are an important class of antitumour agents that are activated by tumour hypoxia. Primin (2-methoxy-6-n-pentyl-1,4-benzo-quinone), a naturally-occurring product obtained from Primula obconica (Primulaceae) has shown antimicrobial and antitumour properties. The synthesis of the Primin to obtain 3-, 5- or 6-alkyl substituted derivatives has been previously attempted seeking antitumour activity. The intermediate reaction products, 2-methoxy-hydroquinone-di-(2'-tetrahydro-pyranyl) ether and 2-methoxy-6-n-pentyl-hydroquinone-di-(2'-tetrahydropyranyl) ether were obtained and evaluated against sarcoma 180 (S-180) and Ehrlich carcinoma, as well as toxicity tests were performed. The antitumour activity tests showed that these intermediate compounds were able to inhibit S-180 sarcoma and Ehrlich carcinoma growth in mice. These results indicated that the tetrahydropyranyl protect group conserved the antitumour activity in comparison with quinone group, however, it exhibited a less toxic effect, with no characteristic of quinones. These results can suggest that compound 2-methoxy-6-n-pentyl-hydroquinone-di-(2'-tetrahydropyranyl) ether may act as a prodrug with some advantages in comparison with the Primin.