JPS58167512A - Antitrichophytic agent - Google Patents

Abstract

PURPOSE:The titled stably usable agent, containing osthole as an active constituent, and having an antimicrobial activity against trichophytes. CONSTITUTION:An antitrichophytic agent containing osthole of the formula as an active constituent. In formulating the agent, the osthole is mixed with a liquid carrier, e.g. water, an alcohol or glycol ether, and used as a drug, e.g. tincture, or kneaded with a wax, e.g. polyethylene glycol 4000 or spermaceti wax, or another ointment base and used as an ointment for external application to an affected part. The content of the active constituent osthole is suitably 0.1-5wt% in general, and the osthole is the well-known compound and is obtained by extraction from Cnidium monnieri Cusson which is a Chinese herbal medicine used as an anti-inflammatory, astringent and invigorating drug with a non-aqueous solvent, e.g. methanol or ether.

Description

[Detailed description of the invention] The present invention relates to an antiwhitening agent.

That is, one aspect of the present invention is an anti-fungal agent containing osthol represented by the following structural formula as an active ingredient.

Snake seeds are a Chinese herbal medicine that is mainly used as an anti-inflammatory, astringent, and tonic agent. The present inventors have discovered that Chinese snake seeds contain the above-mentioned ostol, and that this ostole has anti-white-bacteria activity. I discovered that it has. The present invention was completed based on this knowledge.

It has been found that the known compound used as an active ingredient in the present invention can be obtained by extracting it from Chinese chives using a non-aqueous solvent such as methanol-ether. Incidentally, Ostole is not contained in the Taiwanese snake roe.

Here is a specific example of obtaining ostole from china seedlings from China. It is as follows.

Methanol λo for Chinese snake roe tKy! After 70 days at room temperature, the P-filtered extract was concentrated in vacuo to obtain 3 g of methanol extract. This methanol extract:
13gi! -diethyl ether j! and water i. Add ti and divide between ether and water. Ether layer/10g-
and 7 qg of aqueous phase were obtained.

This etheric layer? was subjected to silica gel force column chromatography - n-hexane:chloroform di/:
Each fraction obtained was eluted with an eluent of / and analyzed using the paper disk method to extract Trichophyton, a type of Bacillus aeruginosa, and Mentaglophytes IFO. tg09(Trichophy
tonmentagrophytesIFOsg09)
Ostol was isolated from the main active fraction by a recrystallization method using a mixed solvent of chloroform and n-hexane. Yield: 3a, 271; 10 The fact that the component isolated from the above-mentioned main active fraction is osthole - its melting point: g. tC-infrared pure absorption spectrum (chloroform solution 'Q): /7/gcm-' (C=O), i
toscm-'CC=O), /zt2Crn-' (aromatic C=C). Ultraviolet absorption spectrum: methanol λnm3-22. -21g+-Z'lg (should
er). maX mass spectrum: molecular ion peak (m+/e)
lI, elemental analysis: actual value C7. ? ．． M24, H Otsu. Island I
．． Since the predicted content was C7.7.7j4, H4, ≦θ, it was identified as ostole.

Ostol's antibacterial activity against white fungi. Minimum inhibitory concentration CM determined by agar plate dilution method. I. C,) (mcノ/
The antibacterial activity of osthole against other microorganisms is shown in the minimum inhibitory concentration (M, I, C.) (mc9/ml) determined by the agar plate dilution method. , as shown in Table 2.0 From the above test results, it is recognized that ostol exhibits particularly high antibacterial activity against the fungus Lepidoptera, and is suitable as an active ingredient of an anti-fungal agent.

Next, we will discuss the toxicity test of osthole.We prepared an olive oil suspension of 0 osthole and added this suspension to DDY.
It was intraperitoneally injected into male mice (6 weeks old, average weight: 1 mouse) and observed for 1 day.

The results are shown in Table 3 below -LD. teeth/
It is permitted to exceed 97 kg for 000 m.

Ostol/undecylenic acid 0. -1 + salicylic acid 0. +2, P-polyethylene glycol 400
J? ．． When an ointment with the composition of polyethylene glycol 40003 was applied to the palm of a human being, no change was observed even after a week had passed.

From the results of the above tests, it is confirmed that Ostol can be used stably as an antifungal agent.

The antibacterial agent of the present invention is prepared by mixing ostol with a liquid carrier such as water, alcohols, glycol ethers, etc. to prepare a solution (for example, a tincture) or using ostol as a wax (for example, polyethylene glycol 4000.
Mix it with other ointment bases (such as spermaceti) and apply it externally to the affected area as an ointment.

The content of osthole in the antiwhitening fungal agent of the present invention can be appropriately selected, but is usually 0. /-1 weight coefficient is appropriate.

Next, examples of the present invention will be shown, but the present invention is not limited thereto.

Example 1 Osthole 7 parts by weight, diethyl sebacate J parts by weight monoglycol salicylate! Part by weight - Polyethylene glycol 400j4' Part by weight, Polyethylene glycol 4000
No. 31 was mixed uniformly to obtain an ointment. Apply this ointment externally to the affected area.

Example 2 Osthole/parts by weight, diethyl sepacate IO parts by weight,
74 tincture was obtained by mixing 0 parts by weight of glycol salicylate, 4 parts by weight of mechetinole, and 39 parts by weight of ethanol.This tincture was applied externally to the affected area.

Claims (1)

[Scope of Claims] An anti-white fungus product containing ostol represented by the following structural formula as an active ingredient.