RESUMO
Three new dihydroxanthones, muroxanthenones A-C (1-3), together with three known dihydroxanthones (4-6) were isolated from the fermentation products of an endophytic fungus Gliomastix murorum. Their structures were elucidated by spectroscopic methods, including extensive 1D and 2D NMR techniques. Compound 3 showed high cytotoxicities against NB4 and PC3 cell with IC(50) values of 2.2 and 2.8 µM. The other compounds also showed moderate cytotoxicities for some tested cell lines with IC(50) values between 4.1 and 9.5 µM.
Assuntos
Antineoplásicos/isolamento & purificação , Hypocreales/química , Xantonas/isolamento & purificação , Antineoplásicos/química , Antineoplásicos/farmacologia , Ensaios de Seleção de Medicamentos Antitumorais , Feminino , Fermentação , Humanos , Concentração Inibidora 50 , Estrutura Molecular , Ressonância Magnética Nuclear Biomolecular , Rizoma/química , Xantonas/química , Xantonas/farmacologiaRESUMO
Seven new unusual dibenzocyclooctadiene lignans, neglignans A-G (1-7), together with 16 known dibenzocyclooctadiene lignans, were isolated from the stems of Schisandra neglecta. Compounds 1 and 2 are the first dibenzocyclooctadiene lignans bearing a carboxyl group at C-4, and compounds 3 and 4 are the first 7,8-seco-dibenzocyclooctadiene lignans found from Nature. The new compounds (1-7) and several of the known compounds were evaluated for their anti-HIV activity and cytotoxicity. Compounds 2 and 6 showed anti-HIV-1 activities with therapeutic index values greater than 50, and compound 4 showed cytotoxicity against the NB4 and SHSY5Y cancer cell lines with IC50 values of 2.9 and 3.3 µM, respectively.
Assuntos
Fármacos Anti-HIV/isolamento & purificação , Fármacos Anti-HIV/farmacologia , Antineoplásicos Fitogênicos/isolamento & purificação , Antineoplásicos Fitogênicos/farmacologia , Ciclo-Octanos/isolamento & purificação , Ciclo-Octanos/farmacologia , Medicamentos de Ervas Chinesas/isolamento & purificação , Medicamentos de Ervas Chinesas/farmacologia , Lignanas/isolamento & purificação , Lignanas/farmacologia , Schisandra/química , Fármacos Anti-HIV/química , Antineoplásicos Fitogênicos/química , Ciclo-Octanos/química , Ensaios de Seleção de Medicamentos Antitumorais , Medicamentos de Ervas Chinesas/química , HIV-1/efeitos dos fármacos , Humanos , Concentração Inibidora 50 , Lignanas/química , Estrutura Molecular , Ressonância Magnética Nuclear Biomolecular , Caules de Planta/químicaRESUMO
Three new xanthones, 1,5-dihydroxy-3-hydroxyethyl-6-methoxycarbonylxanthone (1), 1-hydroxy-5- methoxy-3-hydroxyethyl-6-methoxycarbonylxanthone (2), and 1-hydroxy-3-hydroxyethyl- 8-ethoxycarbonylxanthone (3), along with seven known xanthones (4-10) were isolated from the fermentation products of an endophytic fungus Phomopsis sp.. Their structures were elucidated by spectroscopic methods including extensive 1D- and 2D-NMR techniques. Compounds 1-10 were also tested for their cytotoxicity against five human tumor cell lines (NB4, A549, SHSY5Y, PC3, and MCF7) by MTT method using paclitaxel as positive control. Compounds 1 and 3 showed cytotoxicity against A549 cell lines with IC50 values of 3.6 and 2.5 µM, respectively. In addition, 1 was cytotoxic to MCF7 cells with IC50 value of 2.7 µM.
Assuntos
Antineoplásicos/isolamento & purificação , Ascomicetos/química , Produtos Biológicos/química , Neoplasias/tratamento farmacológico , Xantonas/isolamento & purificação , Antineoplásicos/química , Antineoplásicos/farmacologia , Antineoplásicos/uso terapêutico , Produtos Biológicos/farmacologia , Produtos Biológicos/uso terapêutico , Linhagem Celular Tumoral , Endófitos/química , Fermentação , Humanos , Concentração Inibidora 50 , Células MCF-7 , Estrutura Molecular , Xantonas/química , Xantonas/farmacologia , Xantonas/uso terapêuticoRESUMO
AIM: To develop a prognostic gene set that can predict patient overall survival status based on the whole genome expression analysis. METHODS: Using Illumina HumanWG-6 BeadChip followed by semi-supervised analysis, we analyzed the expression of 47,296 transcripts in two batches of gastric cancer patients who underwent surgical resection. Thirty-nine samples in the first batch were used as the training set to discover candidate markers correlated to overall survival, and thirty-three samples in the second batch were used for validation. RESULTS: A panel of ten genes were identified as prognostic marker in the first batch samples and classified patients into a low- and a high-risk group with significantly different survival times (P = 0.000047). This prognostic marker was then verified in an independent validation sample batch (P = 0.0009). By comparing with the traditional Tumor-node-metastasis (TNM) staging system, this ten-gene prognostic marker showed consistent prognosis results. It was the only independent prognostic value by multivariate Cox regression analysis (P = 0.007). Interestingly, six of these ten genes are ribosomal proteins, suggesting a possible association between the deregulation of ribosome related gene expression and the poor prognosis. CONCLUSION: A ten-gene marker correlated with overall prognosis, including 6 ribosomal proteins, was identified and verified, which may complement the predictive value of TNM staging system.