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Title:
NEURITE ELONGATION AGENT, MEMORY-IMPROVING AGENT AND ANTI-ALZHEIMER AGENT COMPRISING 4'-DEMETHYLNOBILETIN OR 4'-DEMETHYLTANGERETIN AS ACTIVE INGREDIENT, AND PROCESS FOR PRODUCTION OF THE COMPOUND
Document Type and Number:
WIPO Patent Application WO/2010/140409
Kind Code:
A1
Abstract:
Disclosed is a pharmaceutical agent comprising demethyl polymethoxyflavonoid (that is a substance having an excellent physiologically active property) as an active ingredient, which can be produced by a process for which raw materials are readily available and which comprises simple steps and is highly safe for oral ingestion. Specifically disclosed are: a process for producing 4'-demethylnobiletin or 4'-demethyltangeretin, which is characterized by fermenting a skin of at least one fruit selected from citrus fruits belonging to section Acrumen in subgenus Metacitrus or section Aurantium in subgenus cephalocitrus both in genus Citrus or an extract of the skin with water utilizing at least one yeast plant selected from Aspergillus kawachii, Aspergillus awamori, Aspergillus oryzae, Aspergillus sojae, Aspergillus saitoi and Aspergillus usamii; and a neurite elongation enhancer, a memory-improving agent and an anti-alzheimer agent, each of which comprises the above-mentioned compound as an active ingredient.

Inventors:
KUSANO SHUICHI (JP)
TAMURA HIROSHI (JP)
Application Number:
PCT/JP2010/053958
Publication Date:
December 09, 2010
Filing Date:
March 10, 2010
Export Citation:
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Assignee:
FUJI SANGYO CO LTD (JP)
KUSANO SHUICHI (JP)
TAMURA HIROSHI (JP)
International Classes:
A61K31/352; A61K36/06; A61K36/75; A61P25/28; A61P35/00; A61P43/00; C07D311/30; C12P17/06; C12R1/66; C12R1/665; C12R1/69
Foreign References:
JP2003102430A2003-04-08
JP2002060340A2002-02-26
JP2002060340A2002-02-26
Other References:
BUISSON D. ET AL: "Biotransformation of polymethoxylated flavonoids: access to their 4'-O-demethylated metabolites", J. NAT. PROD., vol. 70, no. 6, 2007, pages 1035 - 1038, XP055086407, DOI: doi:10.1021/np070084q
LI S. ET AL: "Anti-inflammatory property of the urinary metabolites of nobiletin in mouse", BIOORG. MED. CHEM. LETT., vol. 17, no. 18, 2007, pages 5177 - 5181, XP022206848, DOI: doi:10.1016/j.bmcl.2007.06.096
FERNANDEZ M. ET AL: "Quantitative structure- activity relationship to predict differential inhibition of aldose reductase by flavonoid compounds", BIOORG. MED. CHEM., vol. 13, no. 9, 2005, pages 3269 - 3277, XP004841173, DOI: doi:10.1016/j.bmc.2005.02.038
See also references of EP 2438916A4
J PHARMACOL EXP THER., vol. 326, 2008, pages 739
KOGA N. ET AL., BIOL. PHARM. BULL., vol. 30, 2007, pages 2317
LI S. ET AL., BIOORG. MED. CHEM. LETT., vol. 17, 2007, pages 5177
TANAKA T., BULL. UNIV. OSAKA PREF., SER. B., vol. 21, 1969, pages 139 - 145
GU H. ET AL., NEUROSCI LETT., vol. 453, 2009, pages 204
Attorney, Agent or Firm:
YANO HIROYA (JP)
Hironari Yano (JP)
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