JPH05139968A - Agent for promoting medullasin activity - Google Patents

Abstract

PURPOSE:To obtain the subject promoting agent having low toxicity and useful as an agent for the treatment and prevention of infectious diseases, cancers, etc., by using a docosahexaenoic acid compound as an active component. CONSTITUTION:The objective promoting agent is produced by adding and mixing a docosahexaenoic acid compound such as docosahexaenoic acid glyceride to a carrier for oral administration such as an excipient (e.g. lactose), a binder (e.g. PVA), a lubricant and a colorant. The dose of the compound is preferably 0.5-10g/day.

Description

Detailed Description of the Invention

[0001]

BACKGROUND OF THE INVENTION 1. Field of the Invention The present invention relates to an agent for promoting medalacin activity, which promotes production of medalacin by granulocytes.

[0002]

BACKGROUND ART Granulocytes are cells producing medalacin, which is a serine protease. It is known that granulocyte medalacin has medalacin activity and is deeply involved in a wide range of biological defense mechanisms including the expression of inflammation, especially chronic inflammation (Biochemistry, 59 (10), 1111, (1987). Further, it has been revealed that it also activates NK cells, that is, Natural Killer cells, which are a kind of lymphocytes capable of damaging cancer cells. However, there are still few biological defense mechanism promoting actions with few side effects and anti-cancer agents, and there is no therapeutic agent or preventive agent mediated by medalacin activation.

[0003]

Therefore, an object of the present invention is to provide a drug which is less toxic to cells and is effective in treating and preventing cancer and infectious diseases by a new mechanism of promoting medalacin activity. Is.

[0004]

Means for Solving the Problems As a result of intensive studies to solve the above problems, the present inventors have found that docosahexaenoic acid (DHA) promotes the production of medalacin by granulocytes, and completed the present invention. did. That is, the present invention is DH
Provided is a medalacin activity promoter containing Group A as an active ingredient.

The medalacin activity promoter of the present invention contains DHAs as active ingredients. As DHAs, DHA, D
Including HA esters, DHA glycerides, DHA phospholipids, DHA choline compounds, DHA nicotinic acid compounds, and DHA amino acid compounds having increased water solubility are included. A preferred specific example is DHA ethyl ester, and it is expected that this substance has a strong promoting activity and is particularly effective for the treatment and prevention of cancer and infectious diseases. It also has the following advantages. 1) A drug with a new mechanism of promoting granulocyte production of medalacin, which is less cytotoxic than conventional drugs, and 2) has a mechanism of action different from that of conventional anti-cancer drugs and anti-infective drugs. Yes, it can be expected to be effective in combination with these or reduce side effects.

The DHAs used in the present invention are commercially available and can be extracted from animals, algae and microorganisms in the natural world by a known method.

The dose of DHA, which is the active ingredient of the inhibitor of the present invention, is preferably 0.1-50 g / day, more preferably
It is 0.5-10 g / day. As the administration method, oral administration, intravenous administration, enteral administration and the like can be performed. For oral administration, tablets, capsules, granules, powders,
For parenteral administration, a liquid preparation or the like can be prepared in the form of injection, suppository, external preparation and the like. As an orally administered carrier, usually used emulsifiers, excipients, binders, lubricants, coloring agents and the like can be used. Examples of the excipient include lactose, sucrose, starch, talc, magnesium stearate, crystalline cellulose, methyl cellulose, carboxymethyl cellulose, glycerin, sodium alginate, gum arabic, etc., and polyvinyl alcohol, polyvinyl ether, ethyl cellulose, arabic as a binder. Rubber, shellac, sucrose and the like can be used, and other coloring agents and disintegrating agents can be used. The tablets may be coated by a commonly known method. In addition, liquids are aqueous or oily suspensions, emulsifiers, solutions, syrups,
It may be an elixir agent or the like and is prepared by a commonly used method. In the case of preparing an injection, an emulsifier, a pH buffer, a stabilizer, an isotonic agent, a local anesthetic, etc. are added to the DHAs of the present invention, and a subcutaneous, intramuscular or intravenous injection is manufactured by a conventional method. can do. As the base for the production of suppositories, oily bases such as cacao butter, polyethylene glycol, lanolin, fatty acid triglyceride, witepsol and the like can be used.

[0008]

INDUSTRIAL APPLICABILITY According to the present invention, there is provided a medalacin activity-promoting agent which can promote the production of medalacin by granulocytes, which is effective for infectious diseases and cancer diseases.

Hereinafter, the present invention will be described more specifically by way of examples, but the present invention is not limited to these examples. It should be noted that, in the following examples, a method known in the art for measuring medaracin activity (J. Clin. Invest.
2)).

[0010]

【Example】

[Selection diagram] None. Example 1 A ddy mouse (male, 6 weeks old) was used, and a control mouse was fed with 4 g of powder feed every day. On the other hand, the experimental group had 5% or 10% DHA ethyl ester (97%
Purity) was added and the animals were bred for 2 weeks. Thereafter, blood was sacrificed and collected from each group of mice, granulocytes were collected, and the medalasin activity thereof was measured. The numbers in Table 1 indicate the medalacin activity (unit) contained by 10 ⁸ granulocytes. From this result, it was shown that DHA ethyl ester promotes the medalasine activity of granulocytes in a dose-dependent manner.

─────────────────────────────────────────────────── ─── Continuation of front page (51) Int.Cl. ⁵ Identification number Office reference number FI technical display location // C07C 69/587 8018-4H

Claims (1)

[Claims] 1. A medalacin activity promoter comprising docosahexaenoic acids as an active ingredient.