JPS60190719A - Antitumor agent - Google Patents

Abstract

PURPOSE:An antitumor agent containing (-)-epigallocatechin as an active component. CONSTITUTION:An antitumor agent effective to suppress the mutation can be prepared by using (-)-epigallocatechin gallate (EGCg) which is one of the tea catechins constituting socalled tea tannin, as an active component. EGCg can be separated from tea leaves. Although it is soluble in water, it can be dissolved in an oil easily by dissolving in a small amount of ethanol in advance. It can be administered orally or parenterally, singly or in combination with a carrier. Dose: 1-3g/day for oral administration and 0.5-1.5g/day for parenteral administration.

Description

DETAILED DESCRIPTION OF THE INVENTION The present invention relates to an antitumor agent, and more specifically, an antitumor agent containing (-) epigallocatechin gallate (hereinafter abbreviated as EGCg) among tea catechins, which are the main constituents of so-called tea tannins, as an active ingredient. The present invention relates to an antitumor agent.

The present inventors have previously conducted research on anti-mutagenic factors in the environment, and have added Bacillus subtilis to tea extract.
lus 5ubtilis) NI G1125 histidine auxotroph strain and the same methionine auxotroph strain, and as a result of intensive research, it was determined that EGCg is the substance that exhibits this anti-mutagenic effect. .

In other words, the above-mentioned Bacillus subtilis is a DNA polymerase ■temperature-sensitive strain that causes spontaneous mutations at a high frequency, but EGCg has the effect of strongly inhibiting this mutation, so it also has antitumor effects (anticancer effects, etc.). You can expect it.

Therefore, the present inventors conducted further research and found that this substance not only suppresses mutational activity in microorganisms, but also
- It was found that formation of III tumor acid was significantly suppressed in rats transplanted with sarcoma pieces induced by methylcholanthrene, and the present invention was completed based on this finding.

The present inventors discovered for the first time that the main components of the tea drinking solution, which has been enjoyed since ancient times, has anti-mutagenic activity against microorganisms and has an anti-cancer effect against transplanted cancers in animals. That's true.

EGCg can be produced from tea leaves, for example, by the method described in Japanese Patent Application No. 58-12096'3. Although EGCg is water-soluble, it can be easily mixed with oil by dissolving it in a small amount of ethanol in advance.

Experimental results showing the effectiveness of EGCg as an antitumor agent are shown below.

(2) Acute toxicity test When EGCg was orally administered to 6-week-old male ICR mice, the LDso after 1 week was 2314 mg/kg. Furthermore, 5-week-old female ICR mice were given 11M EGCg.
When administered intracavitally, the LDso after 1 week was 150/
It was kg.

2) Tumor Suppression Test A group of five 6-week-old Wis ter strain male rats were each subcutaneously implanted with a sarcoma 7tm square induced with 20-methylcholanthrene in the lumbar region. E from 7 days after transplantation
Dissolve GCU in water and prepare “C25■/+tg, 50■/kg”
It was administered intraperitoneally at a rate of Administration is once a day every other day for a total of 9
I went around.

It was dissected on the 27th day after transplantation, and the weight of the sarcoma was measured. The results are shown in Table 1. As is clear from the table, 800g25■
Tumor formation was significantly suppressed in the EGCg/kg administration group and the EGCg 50/kg administration group compared to the non-administration group.

Table 1 - T * Tumor suppression rate - It may also be administered alone or in combination with a pharmaceutically acceptable carrier. The daily dose of EGCg is 1 to 3 g orally, and 0.5 to 1.5 g per day parenterally.
Approximately 5 g is appropriate.

The formulations are shown below as examples, but the formulations are not limited to these.

Example I EGCg 100■ Light silicic anhydride 80■ Crystalline cellulose 140■ Lactic acid appropriate amount Magnesium stearate 2mg The above composition is molded into one tablet according to a conventional method.

Example 2 EGCg, 100 ■ Polyethylene glycol 4000 1 g Both the above components were mixed with 10 mj of distilled water! The drug is dissolved in water and lyophilized in a vial to make an intravenous injection, which is then dissolved at the time of use.

Patent applicant: Mitsui Norin Co., Ltd.

Claims (1)

[Claims] (-)An antitumor agent containing epigallocatechin gallate as an active ingredient.