JPS6281324A - Adipose tissue decomposing agent - Google Patents

Abstract

PURPOSE:To provide the titled decomposing agent containing a solvent-extract of Piper angustifolium and/or Boldea fragrans as an active component and useful as an agent for suppressing or preventing obesity and an agent for ameliorating constitutional obesity and hyperlipemia. CONSTITUTION:The leaf, stalk, bud, etc., (especially leaf) of Piper angustifolium (common name: matico, a plant of Piperaceae family) and/or Boldea fragrans (common name: boldo, a plant of Piperaceae family) is extracted with an organic solvent such as alcohol, ether, etc., or an inorganic solvent such as water to obtain an extracted component. The objective adipose tissue decomposing agent can be produced by using the extracted component as an active component. It can be used in the form of tablet or capsule for oral administration, syrup for oral administration, composition for injection or tea-bag. Dose: several tenth - several gram daily, especially 1.0-2.0g daily. Preferably, the agent is continuously administered for a long period at a low rate of application.

Description

DETAILED DESCRIPTION OF THE INVENTION Field of Industrial Application The present invention relates to an adipose tissue decomposing agent useful for suppressing or preventing obesity, and further as an improving agent for obesity and hyperlipidemia.

BACKGROUND OF THE INVENTION Preventing obesity or improving obesity has become a major concern for women and middle-aged and elderly men from the viewpoint of beauty and health.

Previously, DI! Oolong tea is said to be preferable for suppressing or preventing fullness or improving obesity. In addition, in order to suppress excessive calorie intake, 1 meal 1
People are also trying to limit their intake of snacks and drinks.

Problems to be Solved by the Invention Among the conventional obesity prevention methods mentioned above, drinking oolong tea indirectly leads to the suppression or prevention of obesity in terms of not ingesting sweetness, but it does not have its own effects. Its active anti-obesity effect is not measurable, and for people who are accustomed to stimulating drinks such as coffee and cola, it is not easy to completely cut out these drinks and switch to oolong tea only.

In addition, limiting the intake of meals, snacks, drinks, etc. can be said to be the most reliable way to prevent obesity, but such intake restrictions cause significant pain and should not be carried out for a long period of time. It is often difficult to do so.

In view of this situation, the present invention was achieved as a result of extensive research into the medicinal effects of various plants, particularly plants from South America.

Means for Solving the Problems The adipose tissue decomposition agent of the present invention is based on Piper angustifolium (PIPERANGUSTIFOLIUM) or/and Pordia Fistifolium (BOLDEA).
The active ingredient is a solvent extract of FRAGRANS.

If this extract is administered in any dosage form, free fatty acids can be effectively mobilized from adipose tissue, and obesity can be suppressed or prevented, and obesity and hyperlipidemia can be improved.

The present invention will be explained in detail below.

In the present invention, as raw materials, Piper 77ri7, Tea Oj) rum (PIPERANGUSTIFOLI), whose production area, medicinal properties, etc. are detailed in (1) and (2) below, are used as raw materials.
UM) or/and Pordia Fragrance (BO
LDEA FRAGRANS) is used. Although these are known to have various medicinal effects, their anti-obesity effect is unknown.

(1) Matikopiper angustifolium (PIPERANG)
The plant, which has the scientific name ``USTIFOLIUM'', is commonly called MATIGO, and belongs to the family Pepperaceae. Hereinafter, it will be simply referred to as "Matico."

Matico is mainly produced in South America.

It is usually used as a hemostatic agent. A decoction of matiko is said to be effective against diseases of the chest and larynx, pneumonia, and the larynx, and is also effective against bloody stools, dysentery, diarrhea, and an astringent stomach. In addition, taking a bath with matiko decoction is said to be effective against women's blood flow, irregular menstruation, sores in the uterus, and menstrual pain, and is also good for menstrual cramps.

(2) BOLDEA FRAGR
The plant with the scientific name ANS is commonly known as BOL.
DO) and belongs to the Osiroibanaceae family.

Hereinafter, it will be simply referred to as "Bold".

Bordo grows naturally in Chile, South America, and is also cultivated in Brazil, where it is famous as a medicinal plant.

Bordo leaf preparation has 11 beneficial effects and is effective for chronic hepatitis.
It is also known to have diuretic effects.

Obtaining the active ingredients from Matico, Bold, its leaves,
This is done by extracting stems, buds, etc. (especially leaves) using an appropriate organic or inorganic solvent.

Alcohol, ether, ester, ketone, etc. are used as the organic solvent, and water is usually used as the inorganic solvent, but extracts using hot water and/or alcohol are particularly preferred because they have a large adipose tissue decomposition effect.

(2) The above extract can be used in a conventional manner with any pharmaceutical carrier or excipient. Examples of dosage forms are listed below.

(1) Tablets or capsules for oral administration Binders (syrup, gum arabic, gelatin, sorbitol, tragacanth, polyvinylpyrrolidone, etc.), excipients (
lactose, sugar, cornstarch, calcium phosphate, sorbitol, glycine, etc.), lubricants (magnesium stearate, talc, polyethylene glycol, silica, etc.),
Conventional excipients such as disintegrants (potato starch, etc.), wetting agents (sodium lauryl sulfate, etc.) may also be contained. The tablets may also be coated by suitable methods.

(2) Oral liquid formulations may be aqueous or oily suspensions, solutions, syrups, elixirs, etc., or may be in dry form for reconstitution with water or a suitable vehicle before use.

This liquid formulation contains commonly used additives such as suspending agents (sorbitol syrup, methyl cellulose, quercose/sugar syrup, gelatin, hydroxyethyl cellulose, carboxymethyl cellulose, aluminum stearate gel, hydrogenated edible oils, etc.), emulsifying agents ( lecithin, sorbitan monooleate, gum arabic, etc.), non-aqueous vehicles (almond oil, fractionated coconut oil, oily esters, propylene glycol, ethyl alcohol
), preservatives (methyl p-hydroxybenzoate, propyl p-hydroxybenzoate, sorbic acid, etc.) may be contained.

(3) Injectable compositions may be in the form of suspensions, solutions, emulsions in oily or aqueous vehicles, and may contain formulation agents such as suspending agents, stabilizers, and dispersants. good.

The active ingredient may also be in powder form for reconstitution with a suitable vehicle, eg, sterile, pyrogen-free water, before use.

(4) Tea bag method The dried leaves of Matico or Bordo may be cut into small pieces and packed in a bag made of non-woven fabric, and then extracted with hot water before use.

Although the dosage is selected from a wide range, for example, 1
The net amount of extract per day is often a fraction of a gram to several grams, especially 1.0 to 2.0 g, and generally in small amounts over a long period of time (for example, from several weeks to several months, or even several years). It is preferred to continue administration.

The extracts of Erect Matico and Bordo have no acute toxicity and are highly safe as described below.

Extract the matico and bold parts with hot water,
After filtration, it was concentrated under reduced pressure and then freeze-dried. ICR male mice (24-26 g) fasted for 12 hours were given 2 g/kg of the above extracts of Matico and Bordo.
Acute toxicity tests were conducted on Matico and Bordo by administering one sip (the maximum dose that can be administered) and using survival and behavior within 24 hours as indicators, but 7 cases each died within 24 hours. Not a single case was observed. Furthermore, no noteworthy abnormal behavior was observed in the mouse behavior.

Effects Solvent extracts of Matico and Bordo have a clear adipose tissue decomposition promoting effect. Furthermore, since the effect is observed in the 70% ethanol aqueous extract and the hot water extract, it is thought that the active ingredient is mainly a water-soluble ingredient, and the hot water extract is thought to have a stronger effect. .

Example Next, the present invention will be further explained with reference to Examples.

The cross section of Matico manufactured by "Zu MQ Narairi" was extracted with a 70% aqueous ethanol solution and hot water, filtered, concentrated under reduced pressure, and then freeze-dried. This was extracted into a 70% ethanol extract and a water extract, which were used in experiments.

Similarly, the ridges of Bord were extracted with a 70% aqueous ethanol solution and hot water, filtered, concentrated under reduced pressure, and then freeze-dried. This was extracted into a 70% ethanol extract and a water extract, which were used in experiments.

In addition, as a control example, cedron (CHDROM) (scientific name: LIPPIA Cl), a medicinal plant from South America
TRl0DO-RA, SIMA CEDRON)
, CIANCAPIEDRA
(Scientific name: PHYLLANTT) IIJS NIRt
lRI), MOLLE (scientific name: D
AVANA DEPENDENS), Oolong tea from China, and Japanese tea are similarly 70%
Extraction was performed with an aqueous ethanol solution or hot water and used in the experiment.

The yield of the specimen by extraction was as follows.

EtOH means ethanol.

Warm” Matiko? 0% Et01 (aqueous extract 9.4z Bordo 7θ% EtOH aqueous extract 18.1! Cedron 70% EtOH aqueous extract 12.3%
Chankabi Etra 70%E tOH aqueous extract 6.4z% -C,
z 70% EtOH aqueous extract 13.8% Matico hot water extract 17.3 X Bordo hot water extract 24.8 X Cedron hot water extract 21.72 Oolong tea hot water extract
19.4% Japanese tea (sencha) hot water extract
25.0% A
iol.

Chera, 239.375 (1984)), the effect on free adipocytes was investigated.

That is, male Wistar rats (
After cutting 8 g of parathyroid adipose tissue (body weight 150-200 g) into small pieces, Taleb-Slinger (K r
Add to 20 ml of phosphate buffer (KRP buffer, pH 7,4), incubate at 37°C for 50 minutes, filter through nylon mesh, remove
Centrifugation was performed for 30 seconds using rpa+, and the remaining fat cell layer was aspirated. After washing the adipocyte layer twice with KRPIi buffer in the same manner, KRP buffer was added to make the total volume 201. K containing 5% bovine serum albumin in 0.25+wl of this suspension
Add 0.5 ml of RP buffer and 0.11 l of KRP buffer as a test solution or control solvent, incubate at 37°C for 2 hours, and release fatty acids using Doll's method (V, P,
Dole, J., Cl1n.

Invest, 35.150 (195B)).

The results are shown in Table 1.

Table 1 Note 10 Food stamps are controls, wooden stamps are examples.

#marked is a control example.

2. The unit for the concentration column is 1 gg/ml.

3.No means the number of exams.

4. The unit in the M fatty acid column is Eq/g.

From Table 1, when 100 g/ml or 200 gg/ml of the test substance is applied to free fatty acids, 70
% ethanol aqueous extract, isothermal aqueous extract.

and a 70% aqueous ethanol extract of Bordo.

It can be seen that the isothermal water extract significantly mobilizes free fatty acids from free adipocytes. Among the control samples, oolong tea and Japanese tea hot water extracts were found to significantly mobilize free fatty acids from free fat cells, but the effect was much smaller than that of Matico and Bordo. Recognize.

“ ■1 Thin 11'I] No adrenaline
Epinephrine was added to the method described in (A) at a final concentration of 0.5 g/ml, and the released fatty acids were measured.

The results are shown in Table 2.

Table 2 Note 1. ☆ marks are controls, wooden marks are examples, and # marks are control examples.

2. The unit for the concentration column is gg/II.

3.No means the number of exams.

4. The middle value in the column for M-separated fatty acids is JLEQ/g.

The following can be understood from Table 2.

That is, when 0.5 g g/ml of adrenaline is applied to free fat cells, free fatty acids are released.

When Matico's 70% ethanol aqueous extract, isothermal water extract, and Bordo's 70% ethanol aqueous extract, isothermal water extract are applied to this, there is a tendency for the release of free fatty acids by adrenaline to increase. .

However, when a 70% ethanol aqueous solution extract of Chankabietra and Mauje is applied, there is a tendency to suppress the release of free fatty acids caused by adrenaline.

Effects of the invention The solvent extract of Matico and Bordo has a clear effect of promoting the decomposition of adipose tissue, and the decomposition promoting effect is
It is far superior to oolong tea, which has traditionally been considered to be relatively effective.

Therefore, by administering the adipose tissue decomposing agent of the present invention, obesity and hyperlipidemia can be effectively improved.

In addition, since these are made from natural plants,
Highly safe.

Claims (1)

[Claims] 1. Piper angustifolium (PIPER
ANGUSTIFOLIUM) or/and BOLDEA FRAGRANS
An adipose tissue decomposition agent whose active ingredient is a solvent extract of. 2. The adipose tissue decomposition agent according to claim 1, wherein the solvent extract is a hot water or/and alcohol extract.