RESUMO
The study of the chemical constituents of branches and twigs of Cratoxylum cochinchinense collected in Singapore led to the isolation and structural elucidation of four new xanthones, named cratoxanthone A (1), B (2), C (3), and D (4), together with six known xanthones (5-10) and one known dihydroanthracenone (11). Eight xanthones (including 1 and 2) and 11 were tested for their antiproliferative activity in three human carcinoma cell lines (lung adenocarcinoma A549, colorectal carcinoma Colo205, and epidermoid carcinoma KB) and a human acute lymphoblastic leukemia B cell line (NALM-6), and the mitochondrial membrane potential was determined in KB cells. New xanthones 1 and 2 attenuated NALM-6 cell proliferation with IC50 values of 17.78 and 8.27 µM, respectively. Furthermore, KB cells treated with these compounds had significantly decreased mitochondrial membrane potentials. Notably, the proliferation of A549 cells was specifically inhibited by 11, but not the xanthones.
Assuntos
Antineoplásicos Fitogênicos/farmacologia , Proliferação de Células/efeitos dos fármacos , Clusiaceae/química , Extratos Vegetais/farmacologia , Xantonas/farmacologia , Antineoplásicos Fitogênicos/isolamento & purificação , Linhagem Celular Tumoral , Humanos , Potencial da Membrana Mitocondrial/efeitos dos fármacos , Brotos de Planta/química , Singapura , Xantonas/isolamento & purificaçãoRESUMO
Study of the chemical constituents of the stems of Derris trifoliata Lour. (Leguminosae) collected in Singapore led to the isolation and identification of three known and two new rotenoid derivatives. The new derivatives, named derrisfolin A (1) and B (2), inhibited nitric oxide production in murine macrophage-like RAW 264.7 cells stimulated with interferon-gamma and lipopolysaccharide.
Assuntos
Derris/química , Óxido Nítrico/antagonistas & inibidores , Rotenona/análogos & derivados , Animais , Linhagem Celular , Camundongos , Estrutura MolecularRESUMO
A study of the chemical constituents of the stems of Derris trifoliata Lour. (Leguminosae) led to the isolation and identification of one new rotenoid, 6aalpha,12aalpha-12a-hydroxyelliptone ( 3), together with five other known rotenoids. In a search for novel cancer chemopreventive agents (anti-tumor promoters), we carried out a primary screening of five of the rotenoids isolated from the plant for their inhibitory effects on Epstein-Barr virus early antigen (EBV-EA) activation induced by 12- O-tetradecanoylphorbol 13-acetate (TPA) in Raji cells. The inhibitory activity of 3 was found to be equivalent to that of beta-carotene without any cytotoxicity. Deguelin ( 4) and alpha-toxicarol ( 5) exhibited a marked inhibitory effect on mouse skin tumor promotion in an in vivo two-stage carcinogenesis test. This investigation indicated that rotenoids might be valuable anti-tumor promoters.
Assuntos
Antineoplásicos Fitogênicos/farmacologia , Fabaceae/química , Papiloma/prevenção & controle , Fitoterapia , Extratos Vegetais/farmacologia , Rotenona/análogos & derivados , Neoplasias Cutâneas/prevenção & controle , Animais , Antígenos Virais/efeitos dos fármacos , Antígenos Virais/fisiologia , Antineoplásicos Fitogênicos/uso terapêutico , Benzopiranos/química , Benzopiranos/farmacologia , Benzopiranos/uso terapêutico , Linhagem Celular , Feminino , Herpesvirus Humano 4/fisiologia , Humanos , Camundongos , Camundongos Endogâmicos ICR , Papiloma/induzido quimicamente , Extratos Vegetais/química , Extratos Vegetais/uso terapêutico , Caules de Planta/química , Rotenona/farmacologia , Rotenona/uso terapêutico , Neoplasias Cutâneas/induzido quimicamente , Ativação Viral/efeitos dos fármacos , beta Caroteno/farmacologia , beta Caroteno/uso terapêuticoRESUMO
A study of the chemical constituents of the stems of Derris trifoliata Lour. (Leguminosae) led to the isolation and identification of one new rotenoid, 6aalpha,12aalpha-12a-hydroxyelliptone ( 3), together with five other known rotenoids. In a search for novel cancer chemopreventive agents (anti-tumor promoters), we carried out a primary screening of five of the rotenoids isolated from the plant for their inhibitory effects on Epstein-Barr virus early antigen (EBV-EA) activation induced by 12- O-tetradecanoylphorbol 13-acetate (TPA) in Raji cells. The inhibitory activity of 3 was found to be equivalent to that of beta-carotene without any cytotoxicity. Deguelin ( 4) and alpha-toxicarol ( 5) exhibited a marked inhibitory effect on mouse skin tumor promotion in an in vivo two-stage carcinogenesis test. This investigation indicated that rotenoids might be valuable anti-tumor promoters.