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Anticancer Res ; 35(11): 6001-7, 2015 Nov.
Article in English | MEDLINE | ID: mdl-26504023

ABSTRACT

AIM: To investigate the in vivo effects of 3-indolylmethanamines 31B and PS121912 in treating ovarian cancer and leukemia, respectively. MATERIALS AND METHODS: Terminal deoxynucleotidyl transferase dUTP nick-end labeling (TUNEL) and western blotting were applied to demonstrate the induction of apoptosis. Xenografted mice were investigated to show the antitumor effects of 3-indolylmethanamines. (13)C-Nuclear magnetic resource (NMR) and western blotting were used to demonstrate inhibition of glucose metabolism. RESULTS: 31B inhibited ovarian cancer cell proliferation and activated caspase-3, cleaved poly (ADP-ribose) polymerase 1 (PARP1), and phosphorylated mitogen-activated protein kinases (MAPK), JUN N-terminal kinase/stress-activated protein kinase (JNK/SAPK) and p38. 31B reduced ovarian cancer xenograft tumor growth and PS121912 inhibited the growth of HL-60-derived xenografts without any sign of toxicity. Compound 31B inhibited de novo glycolysis and lipogenesis mediated by the reduction of fatty acid synthase and lactate dehydrogenase-A expression. CONCLUSION: 3-Indolylmethanamines represent a new class of antitumor agents. We have shown for the first time the in vivo anticancer effects of 3-indolylmethanamines 31B and PS121912.


Subject(s)
Amines/chemistry , Aniline Compounds/pharmacology , Antineoplastic Agents/pharmacology , Apoptosis/drug effects , Hydrocarbons, Aromatic/pharmacology , Indoles/chemistry , Ovarian Neoplasms/drug therapy , Animals , Blotting, Western , Cell Proliferation/drug effects , Female , Flow Cytometry , Humans , Indoles/pharmacology , Magnetic Resonance Spectroscopy , Mice , Mice, Nude , Ovarian Neoplasms/metabolism , Ovarian Neoplasms/pathology , Tumor Cells, Cultured , Xenograft Model Antitumor Assays
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