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Id: lil-471845
Autor: Williams, L. A; Conrad, J; Vogler, B; Rõsner, H; Porter, R. B; Setzer, W; Barton, E. N; Levy, H. G; Mika, S; Klaiber, I; Nkurunziza, JP; Kraus, W.
Título: In vitro anti-proliferation/cytotoxic activity of epingaione and its derivatives on the human SH-SY5Y neuroblastoma and TE-671 sarcoma cells
Fonte: West Indian med. j;56(1):5-10, Jan. 2007.
Idioma: en.
Resumo: Epingaione (4-Methyl-1-(5-methyl-2, 3,4,5-tetrahydro-[2,3']bifuranyl-5-yl)-pentan-2-one) was isolated as one of the major lipophilic secondary metabolites from the leaves and stems of Bontia daphnoides L. The compound gave 79.24and 50.83anti-proliferation/cytotoxic activity on the human SH-SY5Y neuroblastoma and TE-671 sarcoma cells in vitro at 50 pg/mL, respectively. Epingaione was transformed into eleven derivatives under laboratory conditions using ethanol, some gave greater anti-proliferation/cytotoxic activity on the cancer cell lines tested. One of the derivatives (compound 2) with enhanced cytotoxic activity was elucidated as 5'-Ethoxy-5-methyl-5-(4-methyl-2-oxo-pentyl)-2,3,4,5-tetrahydro-5'H-[2,3']bifuranyl-2'-one. Both epingaione and compound 2 caused an accumulation of arrested or dead SH-SY5Y neuroblastoma in the m-phase of the cell cycle as revealed by the m-phase specific marker KE 67.
Descritores: Furanos/farmacologia
Myoporaceae
Neuroblastoma/tratamento farmacológico
Fitoterapia
Pentanonas/farmacologia
Sarcoma/tratamento farmacológico
-Linhagem Celular Tumoral
Sobrevivência Celular
Ensaios de Seleção de Medicamentos Antitumorais
Extratos Vegetais/química
Extratos Vegetais/farmacologia
Furanos/química
Folhas de Planta
Caules de Planta
Pentanonas/química
Proliferação Celular/efeitos dos fármacos
Limites: Seres Humanos
Responsável: BR1.1 - BIREME



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