JPH05238942A - Antiulcerous agent - Google Patents

Abstract

PURPOSE:To provide an antiulcerous agent containing as an active ingredient the organic solvent extract or organic solvent aqueous solution extract of Hypericum erectum thumb used as external agents for hemostasis, swellings, etc., also as decoctions for menoxenia, sedation, etc. CONSTITUTION:This antiulcerous agent contains as an active ingredient the organic solvent extract or organic solvent aqueous solution extract of Hypericum erectum Thumb, the extract being obtained by grinding the whole grasses of the Hypericum erectum Thumb preferably collected in the seasons ranging from summer to autumn after dried or not dried and subsequently extracting the ground product at the ordinary temperature or at a heated temperature. The extract is extremely low toxic and highly safe. This agent has an activity to prevent especially acute gastritis models, and exhibits remarkable effects on aspirin or ethanol induced tunica mucosa lesions of stomack, especially on the latter lesions. Namely, the agent has a prevention factor-reinforcing action.

Description

Detailed Description of the Invention

[0001]

TECHNICAL FIELD The present invention relates to an antiulcer agent. More specifically, it relates to an anti-ulcer agent containing an extract from a plant as an active ingredient.

[0002]

BACKGROUND OF THE INVENTION To date, many compounds having antiulcer activity have been reported, but most of them have been synthesized by chemical means, and due to their nature, various side effects due to continuous administration are observed. The situation is unavoidable.

[0003]

SUMMARY OF THE INVENTION It is an object of the present invention to provide an antiulcer agent containing an extract from a plant, which has no side effect, as an active ingredient.

[0004]

The object of the present invention is as follows.
This is achieved by an anti-ulcer drug containing an organic solvent extract or an organic solvent aqueous solution extract of Hypericum perforatum as an active ingredient.

Hypericum perforatum, which is a perennial plant distributed in all parts of Japan except Hokkaido, grows naturally in sunny places in the wilderness and mountains, and has a height of about 40 cm.
Around September, bright yellow flowers are attached to the branches. by the way,
The whole plant is used externally for hemostasis, swelling, etc., and as a decoction for menstrual irregularities, analgesia, etc., but it is not known at all to have an anti-ulcer effect.

[0006] In the present invention, preferably, whole plants of Hypericum perforatum collected from summer to autumn are pulverized after drying or undried, and an organic solvent extract or an organic solvent aqueous solution extract at room temperature or under heating is used as an extract. Used as an active ingredient in ulcer drugs. As the organic solvent, alcohols such as methanol and ethanol are preferably used, and when used as an aqueous solution thereof, the concentration is about 10% or more, preferably about 50 to 75%.

The extract was obtained as a dark brown to brown powder, and its acute toxicity test was conducted using male Wistar rats. No oral death of 5000 mg / kg (po) was observed and no toxicity was observed. Was confirmed to be extremely low and safe.

[0008] These extracts can be provided in the form of medicine or food. When used as a medicine,
It is provided in the form of powder, granules, tablets, dragees, capsules, liquids, etc., and when used as food, gum,
It is provided in the form of candies, jellies, confectionery, beverages, and the like.

[0009]

The organic solvent extract or organic solvent aqueous solution extract of Hypericum perforatum exhibits antiulcer action. That is, a preventive effect was observed against an acute gastritis model, and a remarkable effect was observed against aspirin gastric mucosal lesions, ethanol gastric mucosal lesions, and particularly ethanol gastric mucosal lesions, which suggests that it has a protective factor-enhancing effect. Conceivable.

[0010]

EXAMPLES The present invention will now be described with reference to examples.

EXAMPLE [0011] Dried whole plant of Hypericum perforatum was crushed, 100 g of each was added to 1 L of 75% ethanol aqueous solution, 50% ethanol aqueous solution or 25% ethanol aqueous solution, and shaken at 40 ° C for 24 hours. After that, the insoluble matter was separated by filtration, and the solvent was removed under reduced pressure, and the extract I (1
5.7 g), extract II (19.6 g) and extract III (19.8 g) were obtained.

These extracts were prepared into 2% or 20% suspensions with 0.5% aqueous sodium carboxymethylcellulose solution, and then used in rats (6 weeks old male Crj: Wister purchased and quarantine-acclimated for 1 week). 5 ml / kg (2% suspension
The ulcer-inducing agent was pretreated by oral gavage at a ratio of 100 mg / kg and 1000 mg / kg for a 20% suspension). The control group was administered with 0.5% aqueous sodium carboxymethyl cellulose solution at the same dose.

Aspirin Action on gastric mucosal lesions: Aspirin suspended in 0.5% sodium carboxymethylcellulose aqueous solution after fasting rats for 24 hours and water for 24 hours
Oral administration of 125 mg / kg twice every 2 hours, and 3 hours after the end of the second administration, the rats were killed by exsanguination under ether anesthesia, the stomach was excised, and simple fixation in 1% formalin solution was performed to ulcer. The presence or absence of the occurrence was visually observed and the length of the lesion was measured. The test substance was the first aspirin administration 1
Oral administration was performed before the time.

The results obtained are shown in Table 1 below. From these results, a considerable inhibitory effect is observed in the 1000 mg / kg pretreatment group of Extracts I and II as compared with the control group. (Margins below) Table 1 Pretreatment liquid concentration of test substance (mg / kg) Ulcer length (mm) Suppression rate (%) Control 52 Extract I 1000 10 80.8 100 40 23.1 Extract II 1000 25 51.9 100 48 7.7 Extract Thing III 1000 35 32.7 100 40 23.1

Effect on ethanol gastric mucosal lesion: After fasting and starvation of rats for 24 hours, 1.0 ml of absolute ethanol was orally administered, and 1 hour later, the animals were killed by exsanguination under ether anesthesia, and the stomach was excised and placed in 1% formalin solution. After simple fixation, the presence or absence of an ulcer was visually observed and the length of the lesion was measured. The test substance was orally administered 1 hour before the administration of ethanol.

The results obtained are shown in Table 2 below. From these results, a suppressive effect is observed in a dose-dependent manner in the pretreatment group of all extracts. Table 2 Pretreatment liquid concentration of test substance (mg / kg) Ulcer length (mm) Suppression rate (%) Control 135 Extract I 1000 0 100 100 60 55.6 Extract II 1000 5 96.3 100 85 37.0 Extract III 1000 37 72.6 100 103 23.7

Claims (1)

[Claims] 1. An anti-ulcer agent comprising an organic solvent extract of Hypericum perforatum or an organic solvent aqueous solution extract as an active ingredient.