Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Reexamination Certificate
1999-09-15
2001-04-10
Weddington, Kevin E. (Department: 1614)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
C514S408000, C514S410000, C514S411000, C514S415000
Reexamination Certificate
active
06214831
ABSTRACT:
TECHNICAL FIELD
The present invention relates to a food, a drug and a feed which have lipid metabolism improving activity or anti-obesity activity.
BACKGROUND ART
The term lipid metabolism refers to the in vivo process of catabolism (decomposition) and anabolism (accumulation) of lipids, which are mainly triglycerides derived from food, and is intended to include, in the broad sense, reactions for transforming lipids into energy, biosynthesis of fatty acids, biosynthesis of acylglycerol, phospholipid metabolism, and cholesterol metabolism.
The term obesity means an excessive accumulation of fat in fat tissues of the parts of the body, and obesity is known to be closely related to hypertension, hyperlipidemia, diabetes, cerebral apoplexy, arteriosclerosis, myocardial infarction, etc.
Anti-obesity measures, or measures to treat or prevent obesity can be broadly classified into two groups; that is, i control of energy intake and promotion of energy consumption. Examples of the former are intake of substitutes for sugar and fat, intake of dietary fibers contained in foods such as konjak (devil's-tongue jelly), and intake of absorption-inhibiting substances or appetite-depressing substances such as
Gymnema sylvestre
(Japanese Published Unexamined Patent Application No. 343421/94). Examples of the latter are exercise, and intake of lipid metabolism improving agents such as capsaicin (Japanese Published Examined Patent Application No. 58303/92) and soybean peptides {Daizu Tanpakushitsu Eiyo Kenkyukai Kaishi [Nutritional Science of Soy Protein (Japan)], 13, 53-58 (1992)}. However, it is difficult to continue exercise, and there is a limitation to capsaicin intake because of its hot taste. Thus, a need exists for a development of an effective lipid metabolism improving agent.
At present, rich feed is administered to livestock, poultry and cultivated fish with the aim of promoting their growth. As a result, a lipid metabolism abnormality sometimes occurs in these livestock, poultry and cultivated fish. As for pets, an excessive intake of feed and lack of exercise sometimes cause the problem of obesity.
Evodiamine is a compound obtained from
Evodia rutaecaroa
of the family Rutaceae, which is a kind of crude drug [Journal of Pharmaceutical Sciences, 75, 612-613 (1986)].
Evodiamine is known to have various pharmacological activities, for example, activities as a chilly constitution improving agent (Japanese Published Unexamined Patent Application No. 305527/92), a brain function improving agent (Japanese Published Unexamined Patent Application No. 287724/88), an anti-inflammatory agent for external use (Japanese Published Unexamined Patent Application No. 312932/94) and a cardiotonic (Japanese Published Unexamined Patent Application No. 224622/85), vasorelaxation activity [European Journal of Pharmacology, ZU, 277-283 (1992)], and analgesic activity [Biol. Pharm. Bull., 20(3), 243-248 (1997)], as well as diuretic activity and sweating activity. However, there has been no report on lipid metabolism improving activity or anti-obesity activity thereof.
Rutaecarpine, dehydroevodiamine and hydroxyevodiamine are structurally analogous compounds which are obtained from
Evodia rutaecarpa
as well as evodiamine. The former two compounds have vasorelaxation activity like evodiamine [European Journal of Pharmacology, 27, 59-66 (1994), J. Cardiovasc. Pharmacol., 27(6), 845-853 (1996)]. Further, rutaecarpine has analgesic activity as well as evodiamine [Biol. Pharm. Bull., 20(3), 243-248 (1997)]. However, there has been no report on the above three compounds in respect of lipid metabolism improving activity or anti-obesity activity.
Evodia rutaecarpa,
which is a plant belonging to the genus Evodia, is not only used as a stomachic, a diuretic and an analgesic, but also is known to have activities as a hair-nourishing food (Japanese Published Unexamined Patent Application No. 1619/86), cosmetics containing extract of
Evodia rutaecarpa
(Japanese Published Unexamined Patent Application No. 122414/84), an alcohol absorption-inhibiting agent (Japanese Published Unexamined Patent Application No. 264534/91), and a therapeutic agent for periodontal disease (Japanese Published Unexamined Patent Application No. 148426/87). However, there has been no report on lipid metabolism improving activity or anti-obesity activity thereof.
Fagara rhetza,
which is an Indonesian traditional medicinal herb belonging to the genus Fagara, is known to have an effect on malaria, diarrhea and vomiting [Chem. Pharm. Bull., 40(9), 2325-2330 (1992)]. However, no report has been made on lipid metabolism improving activity or anti-obesity activity thereof.
Zanthoxylum rhetsa
and
Zanthoxylum budrunga,
which are plants belonging to the genus Zanthoxylum, have been reported to have cytotoxicity [J. Nat. Prod., 42(6), 697 (1979)]. However, no report has been made on lipid metabolism improving activity or anti-obesity activity thereof.
Araliopsis tabouensis
and
Araliopsis sovauxii,
which are plants belonging to the genus Araliopsis, are known to have an effect on gonorrhea [Planta medica, 29, 310-317 (1976)]. However, no report has been made on lipid metabolism improving activity or anti-obesity activity thereof.
DISCLOSURE OF THE INVENTION
The present invention relates to a food having lipid metabolism improving activity or anti-obesity activity which comprises, as an active ingredient, a compound selected from the group consisting of compounds represented by formula (I):
wherein
represents
(wherein R
1
represents hydrogen or hydroxy, and R
2
represents hydrogen or lower alkyl; or R
1
and R
2
are combined together to form a bond) or
(wherein R
3
represents lower alkyl); n represents 0 when
is
and represents 1 when
is
and X
−
represents an anion, and salts thereof (hereinafter collectively referred to as evodiamine compounds).
The present invention also relates to a lipid metabolism improving agent or an anti-obesity agent which comprises an evodiamine compound as an active ingredient; a method for lipid metabolism improvement or anti-obesity which comprises administering an effective amount of an evodiamine compound; the use of an evodiamine compound for the preparation of a pharmaceutical composition which is useful for lipid metabolism improvement or anti-obesity; the use of an evodiamine compound for lipid metabolism improvement or anti-obesity; and a composition for lipid metabolism improvement or anti-obesity which comprises, in pharmaceutically acceptable dosage form, an effective amount of an evodiamine compound in association with a pharmaceutically acceptable carrier.
Further, the present invention relates to a feed having lipid metabolism improving activity or anti-obesity activity which comprises an evodiamine compound as an active ingredient.
Furthermore, the present invention relates to a feed additive having lipid metabolism improving activity or anti-obesity activity which comprises an evodiamine compound as an active ingredient; a method for lipid metabolism improvement or anti-obesity of an animal which comprises administering an effective amount of an evodiamine compound; the use of an evodiamine compound for the preparation of a feed additive which is useful for lipid metabolism improvement or anti-obesity; the use of an evodiamine compound for lipid metabolism improvement or anti-obesity of an animal; and a composition for lipid metabolism improvement or anti-obesity of an animal which comprises, in pharmaceutically acceptable dosage form, an effective amount of an evodiamine compound in association with a pharmaceutically acceptable carrier.
In the definitions of the groups in formula (I), the lower alkyl represented by R
2
and R
3
, means a straight-chain or branched alkyl group having 1-6 carbon atoms, such as methyl, ethyl, propyl, isopropyl, butyl, sec-butyl, tert-butyl, pentyl, neopentyl and hexyl. Preferred is methyl.
Examples of the anions are hydrogen ion, halogen ions, ani
Kobayashi Yoshinori
Nakano Yumiko
Yokoo Yoshiharu
Fitzpatrick ,Cella, Harper & Scinto
Kyowa Hakko Kogyo Co. Ltd.
Weddington Kevin E.
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