Growth inhibitor for fungi of genus malassezia

A growth inhibitor using hibiscus flower, English ivy, royal jelly, and Scutellaria root extracts, along with hydrolyzed keratin, effectively inhibits Malassezia fungi growth, addressing the lack of effective treatments for skin diseases.

JP2025168458APending Publication Date: 2025-11-07TAISHO PHARMACEUTICAL CO LTD
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Patent Information

Application Number
JP2025145287
Authority / Receiving Office
JP · JP
Patent Type
Applications
Current Assignee / Owner
Priority Date
2020-08-19
Filing Date
2025-09-02
Publication Date
2025-11-07

AI Technical Summary

Technical Problem

There is a lack of effective drugs to inhibit the proliferation of Malassezia fungi, particularly Malassezia globosa and Malassezia restricta, which are associated with skin diseases such as seborrheic dermatitis, eczema, and acne.

Method used

A growth inhibitor comprising hibiscus flower extract, English ivy leaf/stem extract, royal jelly extract, Scutellaria root extract, and N-[2-hydroxy-3-(trimethylammonio)propyl] chloride hydrolyzed keratin solution is developed to inhibit the growth of Malassezia fungi.

Benefits of technology

The inhibitor effectively suppresses the growth of Malassezia fungi, including Malassezia globosa, thereby reducing symptoms and preventing diseases like tinea versicolor, seborrheic dermatitis, and acne.

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Abstract

To provide a growth inhibitor for fungi of the genus Malassezia.SOLUTION: There is provided a growth inhibitor for fungi of the genus Malassezia comprising, as an active ingredient, at least one selected from the group consisting of hibiscus flower extract, Hedera helix leaf / stem extract, royal jelly extract, Rubus suavissimus leaf extract, Scutellaria baicalensis root extract, and N-[2-hydroxy-3-(trimethylammonio)propyl] chloride hydrolyzed keratin solution. The growth inhibitor is preferably applied to skin or hair.SELECTED DRAWING: None
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Description

[Technical Field]

[0001] The present invention relates to a growth inhibitor against fungi of the genus Malassezia. [Background technology]

[0002] Malassezia is a yeast-like fungus that normally inhabits human skin. It is a lipophilic fungus that requires high quality ingredients. Depending on the condition of the host, it can cause tinea versicolor, seborrheic dermatitis, etc. Bacteria that cause or exacerbate skin diseases such as eczema, Malassezia folliculitis, atopic dermatitis, psoriasis, and acne Currently, the genus Malassezia is classified into 18 species, and M alassezia globosa and Malassezia restricta are skin This bacterial species is always detected from the skin of patients with skin diseases and healthy individuals (Non-patent Documents 1 and 2). Among the above diseases, for example, therapeutic agents for seborrheic dermatitis include topical steroids and non-steroidal anti-inflammatory drugs. Known anti-inflammatory topical agents include steroids and antifungal agents such as ketoconazole (Non-patent Document 3 ). [Prior art documents] [Non-patent literature]

[0003] [Non-Patent Document 1] Persononia Vol.41,56-70,2018 [Non-patent document 2] Med.Mycol.J. Vol.54(No.1),39-44,2013 [Non-patent document 3] Jpn.J.Med.Mycol.Vol.46(No.3),163-167,2005 Summary of the Invention [Problem to be solved by the invention]

[0004] However, the fungi of the genus Malassezia, especially Malassezia detected on human skin, Directly against sezia globosa and Malassezia restricta There have been few reports of drugs that effectively inhibit proliferation. Therefore, it is important to treat, improve, and prevent diseases and symptoms associated with Malassezia fungi. There is a demand for active ingredients that can do this. In order to solve the above-mentioned problems in the prior art, the present invention provides a method for treating fungi of the genus Malassezia. The objective of the present invention is to provide a proliferation inhibitor that inhibits the growth of mitochondrial cells. [Means for solving the problem]

[0005] As a result of extensive research to solve the above problems, the present inventors have discovered a hibiscus flower extract, English: English: English: English: English: English: Ivy leaf / stem extract, royal jelly extract, tiancha extract, scutellaria root extract , N-[2-hydroxy-3-(trimethylammonio)propyl] chloride hydrolyzed keratin At least one selected from the group consisting of fungi of the genus Malassezia, particularly Malassezia It has been found that this compound is suitable for a new application in that it can inhibit the growth of B. lassezia globosa. The present invention was completed.

[0006] That is, the present invention provides: (1) Hibiscus flower extract, English ivy leaf / stem extract, royal jelly extract, Cha extract, Scutellaria root extract, N-[2-hydroxy-3-(trimethylammonium chloride and (v) propyl) hydrolyzed keratin solution. a growth inhibitor for fungi of the genus Malassezia, comprising: (2) The antifungal agent for the skin and / or hair against the fungus of the genus Malassezia according to (1) antiproliferative agents, (3) The fungus in the genus Malassezia is Malassezia globosa (1 ) or (2), is. [Effects of the Invention]

[0007] The present invention makes it possible to provide a growth inhibitor for fungi of the genus Malassezia. Ta. DETAILED DESCRIPTION OF THE INVENTION

[0008] The growth inhibitor of the fungus of the genus Malassezia of the present invention contains hibiscus flower extract, Ukizu leaf / stem extract, royal jelly extract, Tencha extract, Scutellaria root extract, chloride N-[2-hydroxy-3-(trimethylammonio)propyl] hydrolyzed keratin solution and containing at least one selected from the group consisting of: The above drugs are generally used in pharmaceuticals, quasi-drugs, or cosmetics. Any quality product can be used as appropriate.

[0009] The hibiscus flower extract of the present invention is derived from the plant Roselle (scientific name: Hibiscus sabdariffa) belonging to the Malvaceae family. The extract is extracted from the flowers of the plant (Dalifax dariffa). The extraction method for the extract is not particularly limited. The extraction can be carried out according to a conventional method. The extraction solvent used for the extraction can be a polar solvent, a non-polar solvent, or both. Any solvent can be used, for example, water, ethanol, propylene glycol, , 3-butylene glycol, and mixtures thereof can be used. The extracted solution may be used as is, or may be concentrated, diluted, filtered, or decolorized with activated carbon, etc., as necessary. The extracted solution may be concentrated, deodorized, precipitated with ethanol, or the like. It may also be used as a dried product obtained by treatment such as shrink drying, spray drying, or freeze drying. Commercially available products can also be used.

[0010] The use of hibiscus flower extract in the growth inhibitor of Malassezia fungi of the present invention When provided as a drug, quasi-drug, cosmetic or reagent, the amount of each ingredient in the composition is It is preferably 0.0001 mass % to 20 mass %, more preferably 0.001 mass %. The content is 10% by mass to 10% by mass.

[0011] The English ivy leaf / stem extract of the present invention is derived from the plant English ivy (scientific name: English: English ivy) belonging to the Araliaceae family. The extract is extracted from the leaves and stems of the plant Hedera helix. The extraction solvent used for extraction is not limited to a specific solvent, and can be carried out according to a conventional method. Both polar and non-polar solvents can be used, such as water, ethanol, and propylene glycol. Cholesterol, 1,3-butylene glycol, and mixtures thereof can be used. The extract may be used as it is, or may be concentrated, diluted, filtered, treated with activated carbon, etc., as required. It is also possible to use the extracts which have been subjected to bleaching, deodorization, ethanol precipitation, etc. The resulting solution was concentrated to dryness, spray-dried, freeze-dried, etc., and used as a dried product. Alternatively, commercially available products can be used.

[0012] The growth inhibitor of the genus Malassezia according to the present invention is an ivy leaf / stem extract. When provided as a drug, quasi-drug, cosmetic, or reagent, the amount of the compounded product is Each of these is preferably 0.0001% by mass to 20% by mass based on the total composition. The content is more preferably 0.001% by mass to 10% by mass.

[0013] The royal jelly extract of the present invention is derived from European honeybee (Apis mellifera L.) or It is produced in vivo from pollen and nectar of honeybees (Apis indika Radoszkowski) and secreted into the pharynx. The extract is extracted from the secretions of the mandibular gland or mandibular gland. There are no particular limitations, and extraction can be carried out according to a conventional method. Either polar or non-polar solvents can be used, such as water, ethanol, propylene glycol, etc. ethylene glycol, 1,3-butylene glycol, and mixtures thereof can be used. The extract may be used as it is, or may be concentrated, diluted, filtered, activated, or the like, as needed. It is also possible to use those that have been subjected to treatments such as decolorization with carbon or the like, deodorization, and ethanol precipitation. The extracted solution is concentrated to dryness, spray dried, freeze dried, etc., and the dried product is Alternatively, commercially available products may be used.

[0014] The use of royal jelly extract in the growth inhibitor of Malassezia fungi of the present invention When provided as a drug, quasi-drug, cosmetic or reagent, the amount of each ingredient in the composition is It is preferably 0.0001 mass % to 20 mass %, more preferably 0.001 mass %. The content is 10% by mass to 10% by mass.

[0015] The Tencha extract of the present invention is derived from the plant name Tencha (scientific name: Rubus suavissimus) belonging to the Rosaceae family. The extract is extracted from the leaves. The extraction method for the extract is not particularly limited, and can be carried out according to a conventional method. The extraction solvent used for extraction can be either a polar solvent or a non-polar solvent. Also usable are water, ethanol, propylene glycol, 1,3-butylene glycol, and the like. The extract can be prepared by adding ethanol, glycerol, or a mixture thereof. It may be used as is, or may be concentrated, diluted, filtered, decolorized with activated carbon, deodorized, or ethanolized, if necessary. The extracted solution may be concentrated to dryness, sprayed, or the like. It may be used as a dried product obtained by drying, freeze-drying, or the like. You can also be there.

[0016] Amount of Tiancha extract in the growth inhibitor of Malassezia fungi of the present invention When provided as a drug, quasi-drug, cosmetic or reagent, It is preferably 0.0001% by mass to 20% by mass, and more preferably 0.001% by mass to It is 10% by mass.

[0017] The Scutellaria root extract of the present invention is derived from Scutellaria root (scientific name: Scutellaria baicalensis) which belongs to the Lamiaceae family. The extract is extracted from the roots of the plant (Prunus ensis). The extraction method for the extract is not particularly limited, and it is usually The extraction solvent used for extraction can be polar solvent, non-polar solvent, or the like. Any solvent can be used, for example, water, ethanol, propylene glycol, 1, 3-butylene glycol and mixtures thereof can be used. The resulting solution may be used as is, or may be concentrated, diluted, filtered, decolorized with activated carbon, etc., or It is also possible to use the extract after deodorization, ethanol precipitation, etc. Furthermore, the extracted solution can be concentrated. It may also be used as a dried product obtained by treatment such as drying, spray drying, or freeze drying. Commercially available products can also be used.

[0018] Amount of Scutellaria root extract in the growth inhibitor of Malassezia fungi of the present invention When provided as a drug, quasi-drug, cosmetic or reagent, It is preferably 0.0001% by mass to 20% by mass, and more preferably 0.001% by mass to It is 10% by mass.

[0019] The hydrolyzed N-[2-hydroxy-3-(trimethylammonio)propyl] chloride of the present invention The dekeratinized solution is extracted while maintaining the amino acid balance of keratin protein derived from wool. This is a cationized form of purified α-keratose. If necessary, the extract may be concentrated, diluted, filtered, decolorized with activated carbon or the like, deodorized, or precipitated with ethanol. Furthermore, the extracted solution may be concentrated to dryness, spray-dried, frozen, etc. It may be used as a dried product after drying or other treatment. can.

[0020] The growth inhibitor of the fungus of the genus Malassezia of the present invention is The amount of hydrolyzed keratin solution used is the same as that of pharmaceuticals, When provided as a quasi-drug, cosmetic or reagent, each of them is preferably 0.05g based on the total composition. It is 0.0001% by mass to 20% by mass, and more preferably 0.001% by mass to 10% by mass. be.

[0021] The fungi of the genus Malassezia of the present invention include Malassezia globos a, Malassezia restricta, Malassezia furfur , Malassezia sympodialis, Malassezia pachy dermatis, etc., but preferably Malassezia globo It is sa.

[0022] The growth inhibitor of the present invention against Malassezia fungi, preferably for human skin It is used for the skin (including the scalp) or hair. [Example]

[0023] The present invention will be explained in more detail below with reference to examples and test examples. The present invention is not limited to these examples.

[0024] (Test Example 1: Growth inhibition test of Malassezia globosa) To evaluate the growth inhibitory effect on Malassezia globosa, the following methods were used. Tested by the method. (Test medium preparation) The medium was prepared so that the final concentrations were as follows: Artificial sebum 2, which mimics human scalp sebum % (triolein 58.6%, glyceryl distearate 15.6%, palmitic acid 6. 1%, Myristic Acid 2.2%, Pentadecanoic Acid 1.5%, Oleic Acid 4.7%, Squalene 11.3% mixture of lactic acid bacteria, glucose 1%, bile salt 0.8%, yeast extract 0.2%, glycerin monosterate 0.05%, glycerin 1%, After mixing with 1% self-emulsifying glyceryl monostearate and sterilizing, Chromoagar Candida (Kanto A specified amount of chemicals was added and used. (Preparation of inoculum solution) Malassezia globosa was pre-cultured in modified LNA medium (32 After the mixture was left to stand at ℃ for 3 days, the resulting test bacteria were collected with a sterile loop, suspended in PBS, and washed. After washing, the bacterial suspension was diluted to a bacterial count of approximately 10 7Inoculate the sample diluted with PBS to CFU / mL It was used as a bacterial solution. (Test substance preparation) Hibiscus flower extract, English ivy leaf / stem extract, royal jelly extract, Tencha Extract, Scutellaria root extract, N-[2-hydroxy-3-(trimethylammonio)propionate] chloride Hydrolyzed keratin solution and 1,3-butylene glycol were diluted 4 times with purified water. The hibiscus flower extract used was organic <hibiscus> ( Maruzen Pharmaceuticals), and English ivy leaf / stem extract is English ivy extract BG-J (Maruzen Pharmaceuticals) Royal jelly extract is Royal Jelly Extract B (manufactured by Ichimaru Falcos), and Tencha The extract is Sweet Tea Extract BGW (Maruzen Pharmaceuticals), and the Scutellaria root extract is Scutellaria root Extract BG-JC (Maruzen Pharmaceuticals). Pharmaceutical), N-[2-hydroxy-3-(trimethylammonio)propyl] chloride hydrolysis The keratin liquid is Proticute C Alpha (manufactured by Ichimaru Falcos). (Antibacterial test) A sterile 24-well plate was placed in each well of a flat-bottom plate. As a positive control, 200 μL of purified water was added to each sample, and then the artificial sebum solution was added. 300 μL of the medium was added to each well and mixed quickly. After the medium solidified, 10 μL of the inoculum was added to the center of the medium. The bacteria were cultured at 32°C for 3 days. The chromogenic enzyme substrate contained in Chromoagar Candida The bacteria that have grown in the positive control and solvent control will turn red, so the growth of the bacteria in each well will be compared. The growth was visually compared, and the survival rate of the bacteria was set at 0%, 25% and 100% for the positive control. The evaluation was done on a five-point scale: 50%, 75%, and 100%.

[0025] (Test results) Table 1 shows the average survival rates of bacteria tested in duplicate.

[0026] [Table 1]

[0027] As can be seen from Table 1, hibiscus flower extract, English ivy leaf / stem extract, and Yar Jelly Extract, Tencha Extract, Scutellaria Baicalensis Extract, Chloride N-[2-Hydroxy-3- (trimethylammonio)propyl] hydrolyzed keratin solution was a solvent control. It has been confirmed that the growth inhibitory effect is stronger than that of 1,3-butylene glycol, and it has been shown to be effective against hibiscus flowers. Extract, English Ivy Leaf / Stem Extract, Royal Jelly Extract, Tencha Extract, Gracilaria Extract, N-[2-hydroxy-3-(trimethylammonio)propyl] chloride hydrolyzed At least one selected from the group consisting of Malassezia globulus and keratinized liquid It was suggested that it has an inhibitory effect on the proliferation of osa. [Industrial Applicability]

[0028] The growth inhibitor of the genus Malassezia of the present invention inhibits the abnormal growth of Malassezia fungi. It is expected to suppress the bacteria and normalize the imbalance of normal bacteria on the skin, scalp, and hair. The growth inhibitor of the fungus of the genus Malassezia of the present invention can Fungal diseases, such as tinea versicolor, seborrheic dermatitis, Malassezia folliculitis, and atopic dermatitis Cosmetics, quasi-drugs, and other products for the treatment, improvement, and prevention of skin diseases and symptoms such as psoriasis and acne. It can be used in the pharmaceutical field.

Claims

1. Hibiscus flower extract, English ivy leaf / stem extract, royal jelly extract, tench Extract, Scutellaria root extract, N-[2-hydroxy-3-(trimethylammonio) chloride propyl] hydrolyzed keratin solution as an active ingredient.

1. A growth inhibitor against fungi of the genus Malassezia, comprising:

2. The antifungal agent against the fungus of the genus Malassezia according to claim 1, which is for skin and / or hair. A growth inhibitor.

3. The fungus of the genus Malassezia is Malassezia globosa.

3. The growth inhibitor according to claim 1 or 2.

Citation Information

Patent Citations

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    JP2019043855A