title: Estrogen receptor ligands affect mitochondrial activity in SH-SY5Y human neuroblastoma cells.
abstract: We have studied the pharmacological regulation of mitochondrial activity in a human neuroblastoma cell line. Cyclosporin A was found to directly alter mitochondrial membrane potential and to decrease mitochondrial permeability as measured using calcein. The estrogen receptor ligands tamoxifen, nafoxidine and clomiphene were identified as agents which affect mitochondrial membrane potential in a cyclosporin A-like manner. Also when mitochondrial permeability was measured using calcein, tamoxifen, nafoxidine and clomiphene were effective in inhibiting dye loss from mitochondria. Nafoxidine and cyclosporin A inhibit effects of mastoparan on SH-SY5Y mitochondria. These studies indicate that estrogen receptor ligands appear to affect mitochondria in a cyclosporin A-like manner in human neuroblastoma cells.
authors: Merck Sharp and Dohme Research Laboratories, Neuroscience Research Centre, Terlings Park, Eastwick Road, Harlow, Essex CM20 2QR, UK.
authors: Peter B
authors: PB
authors: Simpson
authors: Anthony J
authors: AJ
authors: Woollacott
authors: Zahid
authors: Z
authors: Moneer
authors: Vikki
authors: V
authors: Rand
authors: Guy R
authors: GR
authors: Seabrook
mesh_terms: D016572:Cyclosporine / Q000494:pharmacology; D004305:Dose-Response Relationship, Drug; D004791:Enzyme Inhibitors / Q000494:pharmacology; D006801:Humans; D007425:Intracellular Membranes / Q000187:drug effects / Q000378:metabolism; D008024:Ligands; D008564:Membrane Potentials / Q000187:drug effects / Q000502:physiology; D008928:Mitochondria / Q000187:drug effects / Q000378:metabolism* / Q000502:physiology; D009447:Neuroblastoma / Q000378:metabolism*; D010539:Permeability / Q000187:drug effects; D011960:Receptors, Estrogen / Q000037:antagonists & inhibitors / Q000378:metabolism* / Q000502:physiology; D020845:Selective Estrogen Receptor Modulators / Q000494:pharmacology*; D014407:Tumor Cells, Cultured
chemical_list: D004791:Enzyme Inhibitors; D008024:Ligands; D011960:Receptors, Estrogen; D020845:Selective Estrogen Receptor Modulators; D016572:Cyclosporine