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Expert Opinion on Investigational Drugs Volume 18, 2009 - Issue 3
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Reviews

Caprospinol: moving from a neuroactive steroid to a neurotropic drug

Laurent Lecanu McGill University Health Centre, The Research Institute of the McGill University Health Centre, 6100 Royalmount Avenue, Montreal, Quebec, H4P 2R2, Canada +1 514 283 6239; +1 514 283 6282; [email protected]
,
Laurent Tillement McGill University Health Centre, The Research Institute of the McGill University Health Centre, 6100 Royalmount Avenue, Montreal, Quebec, H4P 2R2, Canada +1 514 283 6239; +1 514 283 6282; [email protected]
,
Georges Rammouz McGill University Health Centre, The Research Institute of the McGill University Health Centre, 6100 Royalmount Avenue, Montreal, Quebec, H4P 2R2, Canada +1 514 283 6239; +1 514 283 6282; [email protected]
,
Jean Paul Tillement Académie Nationale de Médecine, 16 Rue Bonaparte, Paris, 75272, France
,
Janet Greeson Samaritan Pharmaceuticals, 101 Convention Center Drive, Las Vegas, 89109, USA
&
Vassilios Papadopoulos McGill University Health Centre, The Research Institute of the McGill University Health Centre, 6100 Royalmount Avenue, Montreal, Quebec, H4P 2R2, Canada +1 514 283 6239; +1 514 283 6282; [email protected]
Pages 265-276 | Published online: 09 May 2009

Bibliography

  • Birks J. Cholinesterase inhibitors for Alzheimer's disease. Cochrane Database Syst Rev 2006;25;(1):CD005593
  • Johannsen P, Salmon E, Hampel H, et al. Assessing therapeutic efficacy in a progressive disease: a study of donepezil in Alzheimer's disease. CNS Drugs 2006;20:311-25
  • Orgogozo JM, Small GW, Hammond G, et al. Effects of galantamine in patients with mild Alzheimer's disease. Curr Med Res Opin 2004;20:1815-20
  • Small GW, Kaufer D, Mendiondo MS, et al. Cognitive performance in Alzheimer's disease patients receiving rivastigmine for up to 5 years. Int J Clin Pract 2005;59:473-7
  • Bullock R, Touchon J, Bergman H, et al. Rivastigmine and donepezil treatment in moderate to moderately-severe Alzheimer's disease over a 2-year period. Curr Med Res Opin 2005;21:1317-27
  • Winblad B, Wimo A, Engedal K, et al. 3-year study of donepezil therapy in Alzheimer's disease: effects of early and continuous therapy. Dement Geriatr Cogn Disord 2006;21:353-63
  • Birks J, Harvey RJ. Donepezil for dementia due to Alzheimer's disease. Cochrane Database Syst Rev 2006;25;(1):CD001190
  • Courtney C, Farrell D, Gray R, et al. Long-term donepezil treatment in 565 patients with Alzheimer's disease (AD2000): randomised double-blind trial. Lancet 2004;363:2105-15
  • Schneider LS. AD2000: donepezil in Alzheimer's disease. Lancet 2004;363:2100-1
  • Kaduszkiewicz H, Zimmermann T, Beck-Bornholdt HP, et al. Cholinesterase inhibitors for patients with Alzheimer's disease: systematic review of randomised clinical trials. BMJ 2005;331:321-7
  • Kaduszkiewicz H, van den Bussche H, Zimmermann T. The evidence is not convincing. Int Psychogeriatr 2008;6:1-20
  • Areosa SA, Sherriff F, McShane R. Memantine for dementia. Cochrane Database Syst Rev 2005;18;(2):CD003154
  • McShane R, Areosa SA, Minakaran N. Memantine for dementia. Cochrane Database Syst Rev 2006;19;(2):CD003154
  • Huey ED, Dustin IH, Overman GP, et al. Development of subtle psychotic symptoms with memantine: a case report. J Clin Psychiatry 2005;66:658-9
  • Aisen PS. Tarenflurbil: a shot on goal. Lancet Neurol 2008;7:468-9
  • Romanovskaia MG. Effect of cyproheptadine and dimebon on bacterial infection in animals receiving chlorazicin or aminazin. Farmakol Toksikol 1971;34:698-701
  • Doody RS, Gavrilova SI, Sano M, et al. Effect of dimebon on cognition, activities of daily living, behaviour, and global function in patients with mild-to-moderate Alzheimer's disease: a randomised, double-blind, placebo-controlled study. Lancet 2008;372:207-15
  • Siemers ER, Quinn JF, Kaye J, et al. Effects of a gamma-secretase inhibitor in a randomized study of patients with Alzheimer disease. Neurology 2006;66:602-4
  • Rocchi A, Pellegrini S, Siciliano G, et al. Causative and susceptibility genes for Alzheimer's disease: a review. Brain Res Bull 2003;61:1-24
  • Youdim MB, Buccafusco JJ. Multi-functional drugs for various CNS targets in the treatment of neurodegenerative disorders. Trends Pharmacol Sci 2005;26:27-35
  • Hall PF. Role of cytochrome P-450 in the biosynthesis of steroid hormones. Vitam Horm 1985;42:315-68
  • Yao ZX, Brown RC, Teper G, et al. 22R-Hydroxycholesterol protects neuronal cells from beta-amyloid-induced cytotoxicity by binding to beta-amyloid peptide. J Neurochem 2002;83:1110-19
  • Lecanu L, Yao W, Teper GL, et al. Identification of naturally occurring spirostenols preventing beta-amyloid-induced neurotoxicity. Steroids 2004;69:1-6
  • Modler AJ, Gast K, Lutsch G, et al. Assembly of amyloid protofibrils via critical oligomers–a novel pathway of amyloid formation. J Mol Biol 2003;325:135-48
  • Catalano SM, Dodson EC, Henze DA, et al. The role of amyloid-beta derived diffusible ligands (ADDLs) in Alzheimer's disease. Curr Top Med Chem 2006;6:597-608
  • Klein WL. Abeta toxicity in Alzheimer's disease: globular oligomers (ADDLs) as new vaccine and drug targets. Neurochem Int 2002;41:345-52
  • Dahlgren KN, Manelli AM, Stine WB Jr, et al. Oligomeric and fibrillar species of amyloid-beta peptides differentially affect neuronal viability. J Biol Chem 2002;277:32046-53
  • Lambert MP, Barlow AK, Chromy BA, et al. Diffusible, nonfibrillar ligands derived from Abeta1-42 are potent central nervous system neurotoxins. Proc Natl Acad Sci USA 1998;95:6448-53
  • Lecanu L, Papadopoulos V. Cutting-edge patents in Alzheimer's disease drug discovery: anticipation of potential future treatments. Recent Patents CNS Drug Discov 2007;2:113-23
  • Teper GL, Lecanu L, Greeson J, et al. Methodology for multi-site ligand-protein docking identification developed for the optimization of spirostenol inhibition of beta-amyloid-induced neurotoxicity. Chem Biodivers 2005;2:1571-9
  • Lecanu L, Sidahmed EL, Greeson J, Papadopoulos V. Caprospinol improves brain histopathology and recovers memory function in a rat model of Alzheimer's disease. Proceedings of the 8th International Conference AD/PD; 14 – 18 March, 2007, Salzburg, Austria
  • Gouras GK, Tsai J, Naslund J, et al. Intraneuronal Abeta42 accumulation in human brain. Am J Pathol 2000;156:15-20
  • Gyure KA, Durham R, Stewart WF, et al. Intraneuronal a-beta-amyloid precedes development of amyloid plaques in Down syndrome. Arch Pathol Lab Med 2001;125:489-92
  • McGeer PL, Akiyama H, Kawamata T, et al. Immunohistochemical localization of beta-amyloid precursor protein sequences in Alzheimer and normal brain tissue by light and electron microscopy. J Neurosci Res 1992;31:428-42
  • Takahashi RH, Milner TA, Li F, et al. Intraneuronal Alzheimer abeta42 accumulates in multivesicular bodies and is associated with synaptic pathology. Am J Pathol 2002;161:1869-79
  • Bastianetto S, Yao ZX, Papadopoulos V, et al. Neuroprotective effects of green and black teas and their catechin gallate esters against beta-amyloid-induced toxicity. Eur J Neurosci 2006;23:55-64
  • Yang F, Lim GP, Begum AN, et al. Curcumin inhibits formation of amyloid beta oligomers and fibrils, binds plaques, and reduces amyloid in vivo. J Biol Chem 2005;280:5892-901
  • Kanowski S, Herrmann WM, Stephan K, et al. Proof of efficacy of the ginkgo biloba special extract EGb 761 in outpatients suffering from mild to moderate primary degenerative dementia of the Alzheimer type or multi-infarct dementia. Pharmacopsychiatry 1996;29:47-56
  • Maurer K, Ihl R, Dierks T, et al. Clinical efficacy of Ginkgo biloba special extract EGb 761 in dementia of the Alzheimer type. J Psychiatr Res 1997;31:645-55
  • Yao Z, Drieu K, Papadopoulos V. The Ginkgo biloba extract EGb 761 rescues the PC12 neuronal cells from beta-amyloid-induced cell death by inhibiting the formation of beta-amyloid-derived diffusible neurotoxic ligands. Brain Res 2001;889:181-90
  • DeKosky ST, Williamson JD, Fitzpatrick AL, et al. Ginkgo biloba for prevention of dementia: a randomized controlled trial. JAMA 2008;300:2253-62
  • Gervais F, Paquette J, Morissette C, et al. Targeting soluble abeta peptide with tramiprosate for the treatment of brain amyloidosis. Neurobiol Aging 2007;28:537-47
  • Kaneko I, Yamada N, Sakuraba Y, et al. Suppression of mitochondrial succinate dehydrogenase, a primary target of beta-amyloid, and its derivative racemized at Ser residue. J Neurochem 1995;65:2585-93
  • Casley CS, Canevari L, Land JM, et al. Beta-amyloid inhibits integrated mitochondrial respiration and key enzyme activities. J Neurochem 2002;80:91-100
  • Casley CS, Land JM, Sharpe MA, et al. Beta-amyloid fragment 25-35 causes mitochondrial dysfunction in primary cortical neurons. Neurobiol Dis 2002;10:258-67
  • Pereira C, Santos MS, Oliveira C. Involvement of oxidative stress on the impairment of energy metabolism induced by A beta peptides on PC12 cells: protection by antioxidants. Neurobiol Dis 1999;6:209-19
  • Canevari L, Clark JB, Bates TE. Beta-amyloid fragment 25-35 selectively decreases complex IV activity in isolated mitochondria. FEBS Lett 1999;457:131-4
  • Bachurin SO, Shevtsova EP, Kireeva EG, et al. Mitochondria as a target for neurotoxins and neuroprotective agents. Ann NY Acad Sci 2003;993:334-44
  • Moreira PI, Santos MS, Moreno A, et al. Amyloid beta-peptide promotes permeability transition pore in brain mitochondria. Biosci Rep 2001;21:789-800
  • Moreira PI, Santos MS, Moreno A, et al. Effect of amyloid beta-peptide on permeability transition pore: a comparative study. J Neurosci Res 2002;69:257-67
  • Chen L, Yang X, Jiao H, et al. Tea catechins protect against lead-induced ROS formation, mitochondrial dysfunction, and calcium dysregulation in PC12 cells. Chem Res Toxicol 2003;16:1155-61
  • Eckert A, Keil U, Scherping I, et al. Stabilization of mitochondrial membrane potential and improvement of neuronal energy metabolism by Ginkgo biloba extract EGb 761. Ann NY Acad Sci 2005;1056:474-85
  • Eckert A, Keil U, Kressmann S, et al. Effects of EGb 761 Ginkgo biloba extract on mitochondrial function and oxidative stress. Pharmacopsychiatry 2003;36(Suppl 1):S15-23
  • Morin C, Zini R, Albengres E, et al. Evidence for resveratrol-induced preservation of brain mitochondria functions after hypoxia-reoxygenation. Drugs Exp Clin Res 2003;29:227-33
  • Zini R, Morin C, Bertelli A, et al. Effects of resveratrol on the rat brain respiratory chain. Drugs Exp Clin Res 1999;25:87-97
  • Mancuso C, Bates TE, Butterfield DA, et al. Natural antioxidants in Alzheimer's disease. Expert Opin Investig Drugs 2007;16:1921-31
  • Tillement L, Lecanu L, Yao W, et al. The spirostenol (22R, 25R)-20alpha-spirost-5-en-3beta-yl hexanoate blocks mitochondrial uptake of Abeta in neuronal cells and prevents Abeta-induced impairment of mitochondrial function. Steroids 2006;71:725-35
  • Fernandez-Vizarra P, Fernandez AP, Castro-Blanco S, et al. Intra-and extracellular Abeta and PHF in clinically evaluated cases of Alzheimer's disease. Histol Histopathol 2004;19:823-44
  • Manczak M, Anekonda TS, Henson E, et al. Mitochondria are a direct site of A beta accumulation in Alzheimer's disease neurons: implications for free radical generation and oxidative damage in disease progression. Hum Mol Genet 2006;15:1437-49
  • Palmi M, Davey G, Tipton KF, et al. Taurine, taurine analogues, and mitochondrial function and dysfuntion. Adv Exp Med Biol 2006;583:469-79
  • El IA. Taurine increases mitochondrial buffering of calcium: role in neuroprotection. Amino Acids 2008;34:321-8
  • Lecanu L, Greeson J, Papadopoulos V. Beta-amyloid and oxidative stress jointly induce neuronal death, amyloid deposits, gliosis, and memory impairment in the rat brain. Pharmacology 2006;76:19-33
  • Hazra A, Pyszczynski N, DuBois DC, et al. Pharmacokinetics of methylprednisolone after intravenous and intramuscular administration in rats. Biopharm Drug Dispos 2007;28:263-73
  • Ichihashi T, Kinoshita H, Shimamura K, et al. Absorption and disposition of epithiosteroids in rats (1): route of administration and plasma levels of epitiostanol. Xenobiotica 1991;21:865-72
  • Rammouz G, Papadopoulos V, Lecanu L. The neuroprotective steroid caprospinol crosses the blood brain barrier; analysis by liquid chromatography and tandem mass spectrometry. Proceedings of the International Congress on Hormonal Steroids and Hormones & Cancer; 27 – 30 September, 2008, Quebec City, Canada
  • Albert A, Gledhill W. Improved synthese of aminoacridiens. Part IV. Substituted 5-aminoacridines. J Soc Chem Indus 1945;64:169-72
  • Speirs I. The use of tacrine and suxamethonium in anaesthesia for caesarean section. Br J Anaesth 1966;38:394-400
  • Benveniste D, Hemmingsen L, Juul P. Tacrine inhibition of serum cholinesterase and prolonged succinylcholine action. Acta Anaesthesiol Scand 1967;11:297-309
  • Summers WK, Viesselman JO, Marsh GM, et al. Use of THA in treatment of Alzheimer-like dementia: pilot study in twelve patients. Biol Psychiatry 1981;16:145-53
  • Chatellier G, Lacomblez L. Tacrine (tetrahydroaminoacridine; THA) and lecithin in senile dementia of the Alzheimer type: a multicentre trial. Groupe Francais d'Etude de la Tetrahydroaminoacridine. BMJ 1990;300:495-9
  • Fitten LJ, Perryman KM, Gross PL, et al. Treatment of Alzheimer's disease with short- and long-term oral THA and lecithin: a double-blind study. Am J Psychiatry 1990;147:239-42
  • Gauthier S, Bouchard R, Lamontagne A, et al. Tetrahydroaminoacridine-lecithin combination treatment in patients with intermediate-stage Alzheimer's disease. Results of a Canadian double-blind, crossover, multicenter study. N Engl J Med 1990;322:1272-6
  • Farlow MR, Graham SM, Alva G. Memantine for the treatment of Alzheimer's disease: tolerability and safety data from clinical trials. Drug Saf 2008;31:577-85
  • Emre M, Mecocci P, Stender K. Pooled analyses on cognitive effects of memantine in patients with moderate to severe Alzheimer's disease. J Alzheimers Dis 2008;14:193-9
  • Atri A, Shaughnessy LW, Locascio JJ, et al. Long-term course and effectiveness of combination therapy in Alzheimer disease. Alzheimer Dis Assoc Disord 2008
  • Maj J, Sowinska H, Baran L, et al. Pharmacological effects of 1,3-dimethyl-5-aminoadamantane, a new adamantane derivative. Eur J Pharmacol 1974;26:9-14
  • Camanni F, Massara F, Fassio V, et al. Effect of five dopaminergic drugs on plasma growth hormone levels in acromegalic subjects. Neuroendocrinology 1975;19:227-40
  • Fischer PA, Jacobi P, Schneider E, et al. Effects of intravenous administration of memantine in parkinsonian patients (author's transl). Arzneimittelforschung 1977;27:1487-9
  • Gilman S, Koller M, Black RS, et al. Clinical effects of Abeta immunization (AN1792) in patients with AD in an interrupted trial. Neurology 2005;64:1553-62
  • Orgogozo JM, Gilman S, Dartigues JF, et al. Subacute meningoencephalitis in a subset of patients with AD after Abeta42 immunization. Neurology 2003;61:46-54
  • Quon D, Wang Y, Catalano R, et al. Formation of beta-amyloid protein deposits in brains of transgenic mice. Nature 1991;352:239-41
  • Wirak DO, Bayney R, Ramabhadran TV, et al. Deposits of amyloid beta protein in the central nervous system of transgenic mice. Science 1991;253:323-5
  • Duyckaerts C, Potier MC, Delatour B. Alzheimer disease models and human neuropathology: similarities and differences. Acta Neuropathol 2008;115:5-38
  • Schenk DB, Rydel RE, May P, et al. Therapeutic approaches related to amyloid-beta peptide and Alzheimer's disease. J Med Chem 1995;38:4141-54
  • Wolfe MS, Citron M, Diehl TS, et al. A substrate-based difluoro ketone selectively inhibits Alzheimer's gamma-secretase activity. J Med Chem 1998;41:6-9
  • Lukinova NI, Roussakova VV, Fortini ME. Genetic characterization of cytological region 77A-D harboring the presenilin gene of Drosophila melanogaster. Genetics 1999;153:1789-97
  • Struhl G, Greenwald I. Presenilin is required for activity and nuclear access of Notch in Drosophila. Nature 1999;398:522-5
  • De SB, Annaert W, Cupers P, et al. A presenilin-1-dependent gamma-secretase-like protease mediates release of Notch intracellular domain. Nature 1999;398:518-22
  • Wolfe MS, De Los AJ, Miller DD, et al. Are presenilins intramembrane-cleaving proteases? Implications for the molecular mechanism of Alzheimer's disease. Biochemistry 1999;38:11223-30
  • Hardy J, Israel A. Alzheimer's disease. In search of gamma-secretase. Nature 1999;398:466-7

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