Scalp-derived peptide with antimicrobial activity against hair loss-inducing harmful microorganisms

Abstract

One aspect of the present invention relates to a peptide having antibacterial activity against scalp bacteria, an antibacterial composition comprising same, and an antibacterial formulation comprising same. The peptide composition having the ability to regulate the scalp microbiome of the present invention exhibits antibacterial activity against scalp bacteria, thereby contributing to effectively improving the microbial balance of the scalp. Such antibacterial activity can promote the health of the scalp environment and provide a positive effect on preventing hair loss and alleviating scalp-related problems.

Description

Scalp-derived peptides with antibacterial effects against hair loss-causing bacteria

[0001] One example of the present invention relates to a peptide having antibacterial activity against scalp fungi; an antibacterial composition comprising the same; and an antibacterial preparation comprising the same.

[0002] With the recent increase in interest in scalp health, research on the scalp's microbial ecosystem, or microbiome, is actively underway. The scalp microbiome consists of a variety of bacteria and fungi, and these microorganisms play a crucial role in maintaining the scalp's physiological balance. While a healthy scalp is maintained through a balance between beneficial and harmful bacteria, excessive growth of certain harmful bacteria can lead to various scalp problems, such as dandruff, seborrheic dermatitis, and hair loss.

[0003] Some scalp harmful bacteria thrive in environments with high sebum production, inducing an inflammatory response that can damage hair follicles. They also degrade sebum to produce harmful metabolites, exacerbating scalp inflammation. This imbalance in the scalp microbiome is a major cause of various scalp abnormalities, including hair loss. Consequently, various approaches to hair loss treatment and prevention are being studied. In addition to existing drug treatments, various hair loss treatments are being actively developed, including new formulations, protein and antibody drugs, and cell therapies. In particular, the need for treatments with fewer side effects and greater patient convenience is growing, leading to a shift from the traditional low-cost drug market to a premium market focused on high-priced products.

[0004] Existing scalp care products and treatments primarily work by inhibiting microbial growth. However, long-term use can damage beneficial bacteria or lead to resistance issues. Therefore, a new approach is needed that selectively targets specific harmful bacteria while maintaining the balance of the scalp microbiome.

[0005] The purpose of the present invention is to provide a peptide having antibacterial activity against scalp fungi, comprising an amino acid sequence of sequence number 1 or sequence number 2.

[0006] In addition, the present invention aims to provide an antibacterial composition comprising the above peptide.

[0007] In addition, the present invention aims to provide an antibacterial preparation comprising the above antibacterial composition.

[0008] To achieve the above purpose, the present invention provides a peptide having antibacterial activity against scalp fungi, comprising an amino acid sequence of sequence number 1 or sequence number 2.

[0009] In one embodiment of the present invention, the scalp fungus may be Malassezia furfur, Cutibacterium acnes, or Staphylococcus epidermidis.

[0010]

[0011] In addition, the present invention provides an antibacterial composition comprising the peptide.

[0012] In one embodiment of the present invention, the composition may have antibacterial activity against scalp-derived Malassezia furfur, Cutibacterium acnes, or Staphylococcus epidermidis.

[0013] In another embodiment of the present invention, the composition may have an effect of preventing, alleviating or treating hair loss.

[0014] In another embodiment of the present invention, the hair loss may be selected from the group consisting of androgenetic alopecia, alopecia areata, telogen effluvium, traumatic alopecia, trichotillomania, pressure alopecia, anagen effluvium, pityriasis alopecia, syphilitic alopecia, seborrheic alopecia, symptomatic alopecia, and congenital alopecia.

[0015]

[0016] In addition, the present invention provides an antibacterial preparation comprising the antibacterial composition.

[0017] In one embodiment of the present invention, the formulation may be an external skin preparation.

[0018] In another embodiment of the present invention, the external skin preparation may be selected from the group consisting of a cream, a gel, an ointment, a skin emulsifier, a skin suspension, a transdermal patch, a drug-containing bandage, a lotion, a hair tonic, a hair cream, a hair lotion, a hair shampoo, a hair rinse, a hair conditioner, a hair spray, a hair aerosol, a pomade, a powder gel, a hair pack, a hair treatment, an eyebrow hair growth agent, an eyelash hair growth agent, an eyelash nutrition agent, and a combination thereof.

[0019] In another embodiment of the present invention, the formulation may have antibacterial activity against scalp-derived Malassezia furfur, Cutibacterium acnes or Staphylococcus epidermidis.

[0020] In another embodiment of the present invention, the formulation may have an effect of preventing, alleviating or treating hair loss.

[0021] In another embodiment of the present invention, the hair loss may be selected from the group consisting of androgenetic alopecia, alopecia areata, telogen effluvium, traumatic alopecia, trichotillomania, pressure alopecia, anagen effluvium, pityriasis alopecia, syphilitic alopecia, seborrheic alopecia, symptomatic alopecia, and congenital alopecia.

[0022]

[0023] In addition, the present invention aims to provide a scalp fungal antibacterial method using the composition.

[0024] In addition, the present invention aims to provide a method for preventing, alleviating or treating hair loss using the composition.

[0025] In addition, the present invention aims to provide an antibacterial use of the composition against scalp fungi.

[0026] In addition, the present invention aims to provide a composition for use in preventing, alleviating or treating hair loss.

[0027] The peptide of the present invention, which possesses scalp microbiome-regulating properties, exhibits antibacterial activity against harmful bacteria, thereby contributing to effectively improving scalp microbial balance. This antibacterial activity can improve the scalp environment, promoting scalp health and providing positive effects in preventing hair loss and alleviating scalp-related problems.

[0028] Additionally, peptide therapeutics have the advantages of higher biocompatibility and target specificity compared to synthetic compound therapeutics, lower risk of side effects, and lower possibility of developing resistance.

[0029] It should be understood that the effects of the present invention are not limited to the effects mentioned above, but include all effects that can be inferred from the detailed description of the present invention or the composition of the invention described in the claims.

[0030] Figure 1 is LC-MS 2 This diagram illustrates the scalp peptidome analysis workflow.

[0031] Figure 2 illustrates a workflow for discovering scalp-derived peptide candidates with scalp microbiome modulating capabilities.

[0032] Figure 3 illustrates a method for verifying the antibacterial activity of a peptide using a well diffusion assay.

[0033] Figure 4 shows the microorganisms that make up the scalp microbiome.

[0034] Figure 5 shows the results of screening for antibacterial activity of peptides against scalp resident bacteria and harmful bacteria.

[0035] Figure 6 shows the results of measuring the inhibitory concentration (IC50) of a peptide against scalp resident bacteria and harmful bacteria.

[0036] Hereinafter, the present invention will be described in detail.

[0037] To achieve the above purpose, the present invention provides a peptide having antibacterial activity against scalp fungi, comprising an amino acid sequence of sequence number 1 or sequence number 2.

[0038] As used herein, the term "scalp flora" refers to the collective collection of various microorganisms found on the scalp. This includes both "scalp resident flora," which normally reside on the scalp and contribute to maintaining its health, and "harmful bacteria," which can cause scalp diseases by overproliferating under certain conditions, such as changes in the scalp environment or a weakened immune system. Scalp flora generally includes various microorganisms, including bacteria, fungi, and yeast.

[0039] As used herein, the term "antibacterial" refers to the action or activity of inhibiting or eliminating the growth of bacteria, fungi, and other microorganisms. Antibacterial activity may include direct microbial sterilization and bacteriostatic activity that inhibits microbial growth. Antibacterial activity is expressed through various chemical or biological mechanisms and may be selective for specific microorganisms or have a broad antibacterial spectrum. The peptides described herein and antibacterial compositions containing them may be useful in preventing or improving hair loss by regulating the microbial balance of the scalp.

[0040] As used herein, the term "peptide" means a polymer composed of two or more amino acids linked by peptide bonds.

[0041] The peptide of the present invention can be obtained by various methods widely known in the art. For example, the peptide can be produced using polynucleotide recombination and protein expression systems, in vitro synthesis via chemical synthesis such as peptide synthesis, and cell-free protein synthesis, but is not limited to these production methods.

[0042] In addition, a protecting group may be bonded to the N-terminus or C-terminus of the peptide to obtain better chemical stability, enhanced pharmacological properties (half-life, absorbability, potency, efficacy, etc.), altered specificity (e.g., broad biological activity spectrum), and reduced antigenicity. For example, the protecting group may be an acetyl group, a fluorenyl methoxy carbonyl group, a formyl group, a palmitoyl group, a myristyl group, a stearyl group, or polyethylene glycol (PEG), but any component that can modify the peptide, particularly enhance the stability of the peptide, may be included without limitation. The 'stability' refers not only to stability in vivo, which protects the peptide of the present invention from attack by in vivo protein cleavage enzymes, but also to storage stability (e.g., room temperature storage stability).

[0043] The peptide of the present invention is composed of, but is not limited to, the amino acid sequence of SEQ ID NO: 1 (RKLW) or the amino acid sequence of SEQ ID NO: 2 (RQLW), and may be a peptide composed of an amino acid sequence having a homology or identity of 70%, 75%, 80%, 90%, 95%, 96%, 97%, 98%, or 99% or more.

[0044]

[0045] In one embodiment of the present invention, the scalp fungus may be Malassezia furfur, Cutibacterium acnes, or Staphylococcus epidermidis.

[0046] Among the scalp-derived microorganisms used herein, "Malassezia furfur" is a lipid-dependent yeast-like fungus that exists in the sebaceous gland secretions of the scalp and is known as a major pathogen associated with dandruff. "Cutibacterium acnes" is a normal flora commonly found in the sebaceous glands of the skin and scalp, and is known as a strain that affects the microbial ecosystem of hair follicles and sebaceous glands. In addition, "Staphylococcus epidermidis" is a gram-positive coccus that exists as a normal flora of the scalp and skin and can affect skin barrier function and microbial balance.

[0047]

[0048] In addition, the present invention provides an antibacterial composition comprising the peptide.

[0049] In one embodiment of the present invention, the composition may have antibacterial activity against scalp-derived Malassezia furfur, Cutibacterium acnes, or Staphylococcus epidermidis.

[0050] In another embodiment of the present invention, the composition may have an effect of preventing, alleviating or treating hair loss.

[0051] As used herein, the term "hair loss" refers to the absence of hair in areas where hair would normally be present, and includes a decrease in the number of hairs compared to normal. The term "hair loss" includes both non-scarring and scarring alopecia, depending on whether hair follicles are destroyed.

[0052] The term "prevention" in the present invention means reducing the risk of contracting a disease or disorder, and means any act of inhibiting or delaying the onset of a disease by preventing the progression of one or more clinical symptoms of the disease in a subject who is exposed to or susceptible to the disease but has not yet contracted the disease or shown symptoms of the disease.

[0053] The term "palliation" in the present invention refers to alleviating the symptoms of a disease or disorder, and encompasses any action that suppresses or reduces one or more clinical signs of the disease, thereby reducing the severity of the symptoms or alleviating discomfort. This refers to any action that improves a patient's quality of life by reducing the frequency, duration, or severity of symptoms, even if the underlying cause of the disease is not eliminated.

[0054] The term "treatment" in the present invention means alleviating a disease or disorder, and includes all acts that improve or beneficially change the symptoms of a disease by preventing or reducing the progression of the disease or one or more of its clinical symptoms.

[0055] In another embodiment of the present invention, the hair loss may be selected from the group consisting of androgenetic alopecia, alopecia areata, telogen effluvium, traumatic alopecia, trichotillomania, pressure alopecia, anagen effluvium, pityriasis alopecia, syphilitic alopecia, seborrheic alopecia, symptomatic alopecia, and congenital alopecia.

[0056]

[0057] In addition, the present invention provides an antibacterial preparation comprising the antibacterial composition.

[0058] As used herein, the term "formulation" refers to a preparation containing one or more active ingredients mixed in an appropriate pharmaceutical or chemical composition to achieve a specific functional purpose. It encompasses various types depending on its physical form and method of application. Formulations may be provided in solid, liquid, or semi-solid forms, and are categorized into oral, injectable, or externally applied forms, depending on the intended use and site of application.

[0059] In one embodiment of the present invention, the formulation may be an external skin preparation.

[0060] In particular, the term "topical skin preparation" as used herein refers to a preparation applied to human skin to provide a specific functional effect. Such topical skin preparations are used for antibacterial, moisturizing, anti-inflammatory, or other therapeutic and cosmetic purposes, and can contribute to maintaining or improving scalp health by including the composition of the present invention.

[0061] In another embodiment of the present invention, the external skin preparation may be selected from the group consisting of a cream, a gel, an ointment, a skin emulsifier, a skin suspension, a transdermal patch, a drug-containing bandage, a lotion, a hair tonic, a hair cream, a hair lotion, a hair shampoo, a hair rinse, a hair conditioner, a hair spray, a hair aerosol, a pomade, a powder gel, a hair pack, a hair treatment, an eyebrow hair growth agent, an eyelash hair growth agent, an eyelash nutrition agent, and a combination thereof.

[0062] In another embodiment of the present invention, the formulation may have antibacterial activity against scalp-derived Malassezia furfur, Cutibacterium acnes or Staphylococcus epidermidis.

[0063] In another embodiment of the present invention, the formulation may have an effect of preventing, alleviating or treating hair loss.

[0064] In another embodiment of the present invention, the hair loss may be selected from the group consisting of androgenetic alopecia, alopecia areata, telogen effluvium, traumatic alopecia, trichotillomania, pressure alopecia, anagen effluvium, pityriasis alopecia, syphilitic alopecia, seborrheic alopecia, symptomatic alopecia, and congenital alopecia.

[0065]

[0066] When the antibacterial composition according to the present invention is a pharmaceutical composition, it can be used for antibacterial purposes against scalp-derived Malassezia furfur, Cutibacterium acnes, or Staphylococcus epidermidis. It can contain the peptide as an active ingredient, and can also contain a pharmaceutically acceptable carrier. The pharmaceutically acceptable carrier is one commonly used in formulations, and includes, but is not limited to, saline solution, sterile water, Ringer's solution, buffered saline, cyclodextrin, dextrose solution, maltodextrin solution, glycerol, ethanol, liposomes, and the like, and can further contain other conventional additives such as antioxidants and buffers, if necessary. In addition, diluents, dispersants, surfactants, binders, lubricants, etc. can be additionally added to formulate the composition into injectable formulations such as aqueous solutions, suspensions, emulsions, pills, capsules, granules, or tablets. Regarding suitable pharmaceutically acceptable carriers and formulations, each ingredient can be preferably formulated using the methods disclosed in Remington's literature. The pharmaceutical composition of the present invention has no particular limitations on the formulation, but can be formulated into injections, inhalants, topical skin preparations, or oral intake preparations.

[0067] The pharmaceutical composition of the present invention can be administered orally or parenterally (e.g., intravenously, subcutaneously, through the skin, nasal cavity, or respiratory tract) depending on the intended method, and the dosage varies depending on the patient's condition and weight, the degree of disease, the drug form, the route of administration, and the time of administration, but can be appropriately selected by a person skilled in the art.

[0068] The composition according to the present invention is administered in a pharmaceutically effective amount. In the present invention, "pharmaceutically effective amount" means an amount sufficient to treat a disease with a reasonable benefit / risk ratio applicable to medical treatment. The effective dosage level may be determined based on the type and severity of the patient's disease, the activity and sensitivity of the drug to the drug, the time of administration, the route of administration and excretion rate, the duration of treatment, concomitant drugs, and other factors well known in the medical field. The composition according to the present invention may be administered as an individual therapeutic agent or in combination with other therapeutic agents, may be administered sequentially or simultaneously with conventional therapeutic agents, and may be administered singly or in multiple doses. It is important to take all of the above factors into consideration and administer an amount that achieves the maximum effect with the minimum amount without causing side effects, and this can be easily determined by those skilled in the art.

[0069] When the antibacterial composition according to the present invention is a cosmetic composition, it can be used for antibacterial purposes against scalp-derived Malassezia furfur, Cutibacterium acnes, or Staphylococcus epidermidis. The cosmetic composition may include a cosmetically effective amount of the peptide and a cosmetically acceptable carrier, wherein the cosmetically effective amount means an amount sufficient to achieve the aforementioned hair loss prevention or hair growth promotion effect.

[0070] The cosmetic composition of the present invention may contain commonly used auxiliary agents such as hydrophilic or lipophilic gelling agents, hydrophilic or lipophilic active agents, preservatives, antioxidants, solvents, fragrances, fillers, blocking agents, pigments, deodorants, and dyes.

[0071] In one embodiment, the cosmetic composition of the present invention may be a formulation for external use on the skin, and the formulation for external use on the skin may be selected from the group consisting of hair tonic, hair cream, hair lotion, hair shampoo, hair rinse, hair conditioner, hair spray, hair aerosol, pomade, powder gel, hair pack, hair treatment, eyebrow hair growth agent, eyelash hair growth agent, and eyelash nutrient.

[0072]

[0073] When the antibacterial composition according to the present invention is a food composition, it can be used for antibacterial purposes against scalp-derived Malassezia furfur, Cutibacterium acnes, or Staphylococcus epidermidis. The food composition of the present invention includes all forms such as functional foods, nutritional supplements, health foods, food additives, and feeds, and is intended for consumption by humans or animals, including livestock. The above-mentioned type of food composition can be prepared in various forms according to conventional methods known in the art.

[0074] The above type of food composition can be manufactured in various forms according to conventional methods known in the art. General foods include, but are not limited to, beverages (including alcoholic beverages), fruits and processed foods thereof (e.g., canned fruits, bottled fruits, jams, marmalades, etc.), fish, meats and processed foods thereof (e.g., ham, sausages, corned beef, etc.), breads and noodles (e.g., udon, buckwheat noodles, ramen, spagate, macaroni, etc.), fruit juices, various drinks, cookies, taffy, dairy products (e.g., butter, cheese, etc.), edible plant oils, margarine, vegetable proteins, retort foods, frozen foods, various seasonings (e.g., soybean paste, soy sauce, sauces, etc.), etc., which may include a composition containing the above peptide as an active ingredient.

[0075]

[0076] To facilitate understanding of the present invention, the following examples will be described in more detail. However, these examples are intended only to exemplify the content of the present invention and are not intended to limit the scope of the present invention. These examples are provided to more fully explain the present invention to those with average knowledge in the technical field to which the invention pertains.

[0077]

[0078] Example

[0079] Example 1. In silico exploration of scalp-derived peptides with scalp microbiome-regulating capabilities.

[0080] LC-MS 2 The scalp peptidome analysis workflow consists of the following specific steps (Figure 1). First, a scalp surface tissue biopsy is performed, collecting tissue from the scalp of both the non-hair loss and hair loss groups. Samples from the non-hair loss and hair loss groups are stored in separate containers to prevent mixing. The collected samples undergo a concentration and desalination process, which removes impurities and concentrates the peptide components, making them readily available for analysis.

[0081] Afterwards LC-MS 2 Samples are analyzed using an analyzer to obtain MS spectra data. MS spectra measure the mass-to-charge ratio (m / z) of peptides in a sample, allowing for the identification of peptide structures and properties. The acquired MS spectra data undergo a denovosequencing process, which directly decode the amino acid sequence of the peptides from the MS spectra. This process constructs a scalp peptidome library.

[0082] Based on the constructed peptide library, in silico analysis is performed to predict the functionality of each peptide. This process utilizes an AI-based predictive model to assess the potential bioactivity of each peptide, with a particular focus on peptides with the ability to regulate the scalp microbiome. The predicted results are used to select bioactive peptides. Finally, the activity of the selected functional peptides is verified and screened in the laboratory, thereby identifying effective scalp-derived peptides capable of regulating the scalp microbiome.

[0083]

[0084] The process of discovering scalp-derived peptide candidates with scalp microbiome regulation ability proceeded through the following steps (Fig. 2).

[0085] In the initial analysis phase, De novosequencing was performed, resulting in a total of 198,384 peptides. This process applied strict criteria specific to each analysis software. For PEAKS software, only peptides with a De novo score greater than 55 were selected, and for Novor software, only peptides with a De novo score greater than 50 were selected. Through this quality control, 16,475 reliable peptide sequences were obtained.

[0086] In the next step, anti-inflammatory peptides (AIPs) were selected using an in-house prediction model called pQSAR v0.1. Only peptides with an AIP score exceeding 0.5 were selected. This process eliminated 14,694 non-AIPs, yielding 1,781 scalp-derived functional peptides predicted to have anti-inflammatory activity.

[0087] In the final experimental data analysis step, we analyzed the statistical significance between the non-hair loss (NA) and hair loss (AA) groups. A p-value less than 0.05 was considered statistically significant, and 1,778 non-significant peptides were excluded. Finally, two peptides showing significant differences were selected: RKLW (Arg-Lys-Leu-Trp; SEQ ID NO: 1) and RQLW (Arg-Gln-Leu-Trp; SEQ ID NO: 2).

[0088]

[0089] The two peptides selected in this manner are classified as potential bioactive peptides (Potential BPs) for hair loss prevention (anti-alopecia) and are expected to be effective in regulating the scalp microbiome. Through this systematic and step-by-step screening process, two peptides, RKLW (Arg-Lys-Leu-Trp) and RQLW (Arg-Gln-Leu-Trp), were identified from an initial pool of 198,384 peptides, and were predicted to be effective in preventing or alleviating hair loss.

[0090]

[0091] Example 2. In vitro efficacy verification of a peptide that regulates the scalp microbiome.

[0092] The antimicrobial activity of the two peptides was verified using the well diffusion assay. The well diffusion assay is a standardized experimental method for quantitatively assessing the antimicrobial activity of peptides. By measuring the size of the inhibition zone, the strength of antimicrobial activity can be objectively assessed.

[0093] The process for verifying the antimicrobial activity of peptides using the well diffusion assay was as follows (Fig. 3). First, hard agar (1.5%) and soft agar (0.75%) were prepared separately, and the hard agar was poured into a petri dish to form a base medium layer. Next, the soft agar and target microorganisms were mixed and overlaid on the hard agar. Wells were created in this double-layer medium, and each well was injected with the peptide sample to be verified or a control.

[0094] After culturing, the zone of inhibition formed around each well was observed. If an inhibition zone was formed, it meant that there was an anti-microbial effect, and if no inhibition zone was formed, it was judged as no effect.

[0095] Referring to the microorganisms that compose the scalp microbiome (Fig. 4, Suzuki et al. Microorganisms 2021, 9(10), 2132), two bacterial species (Staphylococcus epidermidis, Cutibacterium acnes) and one fungal species (Malassezia furfur), which are the main constituent microorganisms of the scalp microbiome, were selected as targets for antibacterial activity screening (Table 1).

[0096] [Table 1] Scalp Microbiome Information

[0097]

[0098]

[0099] Among the microorganisms present on the scalp, Malassezia is a lipid-dependent yeast that possesses numerous lipolytic enzyme genes that break down sebum. This is due to Malassezia's lack of fatty acid synthesis genes, making it dependent on external lipid sources. Malassezia possesses 14 lipase and 9 phospholipase genes, most of which are believed to be secreted enzymes. These enzymes break down scalp lipids to produce fatty acids, which can cause skin irritation and inflammation. They also promote excessive production of the stratum corneum, which can lead to dandruff and scalp itching and redness.

[0100] Staphylococcus and Cutibacterium are major microbial genera in the scalp flora. Under normal conditions, they play a crucial role in skin health, including maintaining scalp pH and preventing the invasion of other harmful bacteria. However, changes in the scalp environment can disrupt the balance of these microorganisms, leading to various problems.

[0101] Malassezia furfur is a yeast commonly found on the scalp. It is a major cause of dandruff and seborrheic dermatitis. While normally present on the scalp, it can overgrow due to environmental factors such as excessive sebum production and humidity. It breaks down skin lipids to produce fatty acids, which can cause skin irritation and inflammation. It promotes excessive production of the stratum corneum, which can lead to dandruff and scalp itching and redness.

[0102] Staphylococcus epidermidis is a normal flora of the skin and scalp, and is generally nonpathogenic. It plays a vital role in skin health, maintaining skin pH and preventing the invasion of other harmful bacteria. It can cause opportunistic infections in those with a weakened immune system or a compromised skin barrier. Its ability to form biofilms makes it a major cause of medical device-related infections. On the scalp, it interacts with acne bacteria to help maintain skin homeostasis, but it can also invade sebaceous glands and cause inflammation.

[0103] Cutibacterium acnes is a common, normal flora found in the sebaceous glands of the skin and scalp, playing a crucial role in skin health. While generally non-pathogenic, it can cause inflammatory skin conditions like acne in cases of excessive sebum production or a weakened immune system. It is also found on the scalp and is known to affect the microbial ecosystem of hair follicles and sebaceous glands.

[0104] We aimed to verify the antibacterial effects of peptides against the three types of scalp harmful bacteria and resident bacteria mentioned above (Fig. 5). The subjects of the experiment were Cutibacterium acnes ATCC 6919, a bacterium that causes scalp inflammation; Malassezia furfur ATCC 14521T, a fungus that causes dandruff and seborrheic dermatitis; and Staphylococcus epidermidis ATCC 12228, a normal scalp resident bacteria. The antibacterial activities of two types of peptides, RKLW (Arg-Lys-Leu-Trp) and RQLW (Arg-Gln-Leu-Trp), were evaluated against these strains.

[0105] The antibacterial activity of each peptide was measured using the well diffusion method. The peptides were diluted to four concentrations of 50, 25, 12.5, and 6.25 mg / ml, respectively, and appropriate controls were set to ensure the reliability of the experiment. Fluconazole (0.5 mg / ml) was used as a positive control against the fungus M. furfur, and nisin (2 mg / ml) was used as a positive control against the bacteria S. epidermidis and C. acnes. Distilled water was set as a negative control. Six wells were created in each medium, and peptides and controls were treated at different concentrations, respectively.

[0106] The RKLW peptide showed the strongest antibacterial activity against M. furfur, as confirmed by the distinct clear ring formed around the well (indicated by the yellow arrow) in Figure 5. Weak antibacterial activity was also observed against S. epidermidis (yellow arrow), but the size of the inhibition zone was relatively smaller than that of M. furfur.

[0107] In contrast, the RQLW peptide did not exhibit significant antibacterial activity against any of the three strains under the same concentration conditions. In particular, neither peptide formed any inhibition zone around the well against C. acnes.

[0108] Additionally, the antibacterial activity of RKLW and RQLW peptides against M. furfur ATCC 14521T, S. epidermidis ATCC 12228, and C. acnes ATCC 6919 was evaluated using a broth microdilution assay (Fig. 6). Each graph shows the antibacterial activity of RKLW and RQLW peptides against the peptide concentration used (log 10[compound], μg / μL) and the reaction ratio (%) were shown, and the antibacterial activity was analyzed by comparing the IC50 values. As a result, it was confirmed that not only the RKLW peptide but also the RQLW peptide showed antibacterial activity against M. furfur. In addition, RKLW showed weak antibacterial activity against S. epidermidis and C. acnes, and the IC50 values ​​tended to be lower for RKLW than for RQLW.

[0109] That is, RKLW had a higher overall antibacterial activity against all three strains compared to RQLW, and it was confirmed that it had a strong inhibitory effect, especially with a lower IC50 value with respect to the strain causing scalp inflammation.

[0110] Therefore, RKLW peptide (SEQ ID NO: 1) and RQLW peptide (SEQ ID NO: 2) were selected as final candidates, and these peptides exhibited selective antimicrobial properties, exhibiting antimicrobial activity against scalp pathogens M. furfur and C. acnes, as well as scalp resident bacteria S. epidermidis. This selective antimicrobial spectrum suggests their potential as therapeutic agents capable of targeting specific pathogenic strains without significantly disrupting the normal microbial balance of the scalp.

[0111]

[0112] The foregoing description of the present invention is provided for illustrative purposes only. Those skilled in the art will readily appreciate that the present invention can be readily modified into other specific forms without altering the technical spirit or essential characteristics of the present invention. Therefore, the embodiments described above should be understood as illustrative in all respects and not restrictive.

Claims

1. A peptide having antibacterial activity against scalp fungi, comprising an amino acid sequence of sequence number 1 or sequence number 2.

2. A peptide according to claim 1, characterized in that the scalp fungus is Malassezia furfur, Cutibacterium acnes or Staphylococcus epidermidis.

3. An antibacterial composition comprising the peptide of any one of claims 1 or 2.

4. An antibacterial composition according to claim 3, characterized in that the composition has antibacterial activity against scalp-derived Malassezia furfur, Cutibacterium acnes, or Staphylococcus epidermidis.

5. An antibacterial composition according to claim 3, characterized in that the composition has an effect of preventing, alleviating, or treating hair loss.

6. An antibacterial composition according to claim 5, wherein the hair loss is selected from the group consisting of androgenetic alopecia, alopecia areata, telogen effluvium, traumatic alopecia, trichotillomania, pressure alopecia, anagen effluvium, pityriasis alopecia, alopecia syphilitica, alopecia seborrheica, symptomatic alopecia, and congenital alopecia.

7. An antibacterial preparation comprising the antibacterial composition of claim 3.

8. In claim 7, the preparation is an antibacterial preparation for external use on the skin.

9. In claim 8, the skin external preparation is an antibacterial preparation selected from the group consisting of creams, gels, ointments, skin emulsifiers, skin suspensions, transdermal patches, drug-containing bandages, lotions, hair tonics, hair creams, hair lotions, hair shampoos, hair rinses, hair conditioners, hair sprays, hair aerosols, pomades, powder gels, hair packs, hair treatments, eyebrow hair tonics, eyelash hair tonics, eyelash nutrients, and combinations thereof.

10. An antibacterial preparation according to claim 7, characterized in that it has antibacterial activity against scalp-derived Malassezia furfur, Cutibacterium acnes or Staphylococcus epidermidis.

11. An antibacterial agent according to claim 7, characterized in that it has an effect of preventing, alleviating or treating hair loss.

12. An antibacterial agent according to claim 11, wherein the hair loss is selected from the group consisting of androgenetic alopecia, alopecia areata, telogen effluvium, traumatic alopecia, trichotillomania, pressure alopecia, anagen effluvium, pityriasis alopecia, alopecia syphilitica, alopecia seborrheica, symptomatic alopecia, and congenital alopecia.

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