Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Reexamination Certificate
2000-04-28
2002-03-19
Owens, Amelia (Department: 1625)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
C514S470000
Reexamination Certificate
active
06358998
ABSTRACT:
BACKGROUND OF THE INVENTION
1. Field of the Invention
The present invention relates to an agent for reducing body fat, comprising a dioxabicyclo[3.3.0]octane derivative as an active ingredient, and use of the same in the fields of food and drink products and feeds.
2. Background Art
In recent years, patients suffering from obesity have been increased also in Japan, and this is becoming a serious social problem. The Ministry of Health and Welfare has published, in November of last year, the outline of the results of the National Nutrition Survey in 1997, and has pointed out that, as compared with 10 years ago and 20 years ago, the proportion of obesity and overweight in men tends to increase, and one out of four men in twenties and one out of three men in thirties suffer from obesity or overweight. Possible factors in this include increased ingestion (hyperphagia), reduced excercise (lack of excercise), and a fluctuation in generation of body heat. Obesity causes accumulation of a large amount of body fat. This is causative of arteriosclerosis, hypertension, diabetes, and cardiac diseases, and, in some cases, leads to complications, such as angiopathy, neuropathy, and aphylaxis.
In a society these days in which health is a matter of interest, attention is drawn to the content of fat in foods, and meat having low saturated fatty acid content is preferred. Further, a great concern is shown for diet, fitness and the like for regulating body fat, particularly subcutaneous fat, visceral fat or the like, of humans.
Under these circumferences, there is a great social demand for body fat reducing agents which have excellent function and effect and are safe.
Dioxabicyclo[3.3.0]octane derivatives, particularly sesamin, are reported in an article entitled “Sesamin: A multifunctional Gift From Nature,” M. Sugano and K. Akimoto, “Journal of Chinese Nutrition Society,” 18, 1-11 (1993). This article describes, as possible advantages of sesamin, that sesamin interferes &dgr;-5-desaturase, an enzyme capable of unsaturating a reaction by which dihomo-&ggr;-linolenic acid is converted to arachidonic acid. This article further cites references discussing other possible effects of sesamin (activity to lower blood cholesterol, enhancement in detoxification of chemical materials and alcohols in the liver, protection against chemically induced breast cancer, and in vivo antioxiizing activity).
So far as the present inventors know, however, up to now, there have been no report such that dioxabicyclo[3.3.0]octane derivatives have activity to reduce body fat.
Accordingly, it is an object of the present invention to provide a novel agent for reducing body fat, which is highly stable and causes no significant side effect, and food and drink products and feeds containing the same.
SUMMARY OF THE INVENTION
The present inventors have repeated extensive and intensive studies using fat around kidney and fat around epididymis as an index of a reduction in body fat and, as a result, have found that dioxabicyclo[3.3.0]octane derivatives, which have been extracted or isolated from pepper seed, sesame meal, sesame oil or the like, or alternatively have been chemically synthesized, have activity to reduce body fat. This has led to the completion of the present invention.
Thus, the present invention provides an agent for reducing body fat, comprising a dioxabicyclo[3.3.0]octane derivative as an active ingredient, and a food or drink product and a feed having activity to reduce body fat, comprising said derivative.
DETAILED DESCRIPTION OF THE INVENTION
The dioxabicyclo[3.3.0]octane derivative to be used in the present invention is represented by formula (I):
wherein R
1
to R
6
each independently represent a hydrogen atom or an alkyl group having 1 to 3 carbon atoms, provided that R
1
and R
2
and/or R
4
and R
5
may combine together to form a methylene or ethylene group; and n, m, and 1 are each 0 or 1.
Specific examples of dioxabicyclo[3.3.0]octane derivatives include sesamin, sesaminol, episesamin, episesaminol, sesamolin, 2-(3,4-methylenedioxyphenyl)-6-(3-methoxy-4-hydroxyphenyl)-3,7-dioxabicyclo[3.3.0]-octane, 2,6-bis-(3-methoxy-4-hydroxyphenyl)-3,7-dioxabicyclo[3.3.0]octane, 2-(3,4-methylenedioxyphenyl)-6-(3-methoxy-4-hydroxyphenoxy)-3,7-dioxabicyclo[3.3.0]-octane, and other compounds. Among them, sesamin, episesamin, or a mixture of sesamin with episesamin is preferred.
These compounds may also be in the form of glycoside, and optically active substances are also embraced in the present invention.
According to the present invention, the dioxabicyclo[3.3.0]octane derivatives (hereinafter referred to as “derivative of the present invention”) may be used either solely or in a combination of two or more. The derivative of the present invention is not limited to a highly purified product, and may also be an extract composed mainly of one or a plurality of dioxabicyclo[3.3.0]octane derivatives described above (hereinafter referred to as the “extract composed mainly of the derivative of the present invention”). The extract composed mainly of the derivative of the present invention may be extracted from a naturally occurring product containing the derivative of the present invention by a conventional method. Naturally occurring products containing the derivative of the present invention include sesame oil, sesame meal, by-products obtained in the production process of sesame oil, sesame seed, acanthoponacis cortex, paulownia tree, bark of hakuka, long pepper, and asiasarum root. The content of the derivative of the present invention in the extract composed mainly of the derivative of the present invention is generally not less than 0.1% by weight, preferably not less than 1.0% by weight, more preferably not less than 5.0% by weight. In particular, desirably, the total content of sesamin and episesamin is not less than 0.05% by weight, preferably not less than 0.5% by weight, more preferably not less than 2.0% by weight.
When the derivative of the present invention is used as pharmaceutical preparations, the administration form may be any dosage form so far as oral administration can be conveniently carried out. The pharmaceutical preparations may be used either solely or in a combination of two or more, depending upon symptoms of patients.
These various preparations may be formulated by adding, to the basis, known adjuvants commonly used in the field of pharmaceutical preparations, such as fillers, binders, antiseptics, stabilizers, disintegrators, lubricants, and corrigents, depending upon purposes, according to a conventional method. If necessary, tonicity agents, stabilizers, antiseptics, and soothing agents may be added thereto.
External preparations, such as ointments and creams, may be formulated by a conventional method using as a base petrolatums, paraffins, fats and oils, lanolins, macrogols or the like. The dose may vary depending upon the purpose of administration and conditions of a subject, to which the preparation is to be administered, for example, sex, age, and weight. In general, however, in the case of oral administration to an adult, the dose may be properly regulated so that the total amount of the derivative of the present invention is 1 mg to 10 g, preferably 1 mg to 2 g, more preferably 1 mg to 200 mg, per day. On the other hand, in the case of parenteral administration, the dose may be properly regulated so that the total amount of the derivative of the present invention is 0.1 mg to 1 g, preferably 0.1 mg to 200 mg, more preferably 0.1 mg to 100 mg, per day.
The derivative of the present invention, when administered together with a conjugated linoleic acid, can enhance the effect of reducing body fat according to the present invention. When the derivative of the present invention is used in combination with the conjugated linoleic acid, the mixing ratio between the derivative of the present invention and the conjugated linoleic acid may be properly regulated in the range o
Iwata Toshio
Kasai Masaaki
Koba Kazunori
Okuyama Hitoshi
Sakono Masanobu
Foley & Lardner
Owens Amelia
Rinoru Oil Mills Co., LTD
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