Novel compound with efficient mosquito repelling and itching relieving effects and application thereof

Abstract

The invention relates to the technical field of biological medicines, in particular to a novel compound with efficient mosquito-repelling and itching-relieving effects, the compound is composed of bioactive peptide and N, N-diethyl-2-hydroxy-2-phenylacetamide, and the bioactive peptide and the N, N-diethyl-2-hydroxy-2-phenylacetamide are combined to form the compound. Wherein the bioactive peptide comprises peptide fragments of which the sequences are as follows: SEQ NO: 1: Cys-Arg-Val-Leu-Pro (CRVLP), SEQ NO: 2: Gly-Asn-Phe-Thr-Ser (GNPTS) and SEQ NO: 3: Lys-Met-His-Glu-Tyr (KMHEY). The invention also discloses a preparation method of the bioactive peptide. The used components are relatively high in safety, so that the potential skin adverse reaction risk is reduced. The bioactive peptide is composed of natural amino acids, and has good biocompatibility and low toxicity. Safety evaluation on the N, N-diethyl-2-hydroxy-2-phenylacetamide shows that the N, N-diethyl-2-hydroxy-2-phenylacetamide has small harm to human skin and body under normal use concentration, and has a remarkable effect on relieving itching.

Description

Technical Field

[0001] The invention belongs to the technical field of biomedicine and chemistry, and specifically relates to a novel compound with high-efficiency mosquito-repelling and itching-relieving effects and application thereof. Background Art

[0002] In the hot summer, mosquito infestation has become a major problem in people's daily lives. Mosquito bites not only cause discomfort symptoms such as itching, redness and swelling of the skin, but may also spread a variety of diseases, such as malaria, dengue fever, Japanese encephalitis, etc., which seriously threaten human health. In order to deal with mosquito bites, a variety of mosquito repellent and anti-itch products have emerged on the market. However, most of these products have various problems.

[0003] Common mosquito repellent products such as mosquito coils and mosquito repellent liquids often rely on chemically synthesized mosquito repellents, such as DEET. Although these chemicals can repel mosquitoes to a certain extent, they may irritate human skin and may even cause allergic reactions if used for a long time. In addition, some mosquito repellent products made from natural plant extracts, such as lemon eucalyptus oil, often do not have a long-lasting mosquito repellent effect and need to be used frequently.

[0004] In terms of anti-itch products, common ones include calamine lotion, glucocorticoid ointment, etc. Although these products can relieve itching symptoms to a certain extent, they often have problems such as slow onset and insignificant effects. Moreover, for some severe allergic reactions caused by mosquito bites, these conventional anti-itch products may not be able to effectively control the symptoms.

[0005] Therefore, developing a safe, efficient and long-lasting mosquito repellent and antipruritic product has become an urgent problem to be solved in the current biomedicine and chemical technology fields. Summary of the invention

[0006] The novel compound of the present invention is composed of the following components: a novel compound with high-efficiency mosquito repelling and itching relieving effects, characterized in that the compound is composed of bioactive peptides and N,N-diethyl-2-hydroxy-2-phenylacetamide.

[0007] Furthermore, the bioactive peptide sequence CRVLP specifically binds to the mosquito olfactory receptor protein OR35, thereby interfering with the mosquito's recognition of human odor and achieving a mosquito repellent effect.

[0008] Furthermore, the bioactive peptide sequence GNPTS can reduce the inflammatory response and achieve an antipruritic effect by inhibiting the activity of enzymes such as phosphatases and proteases injected into the skin when mosquitoes bite.

[0009] Furthermore, the bioactive peptide sequence KMHEY regulates the immune system's response to mosquito bites by binding to the FcεRI receptor on the surface of immune cells, reduces allergic reactions, and relieves symptoms of itching and redness.

[0010] Furthermore, the N,N-diethyl-2-hydroxy-2-phenylacetamide exerts mosquito repellent and anti-inflammatory effects and relieves itching and redness symptoms by interfering with the mosquito olfactory receptor protein OR83b and inhibiting the activation of the inflammation-related pathway NF-κB.

[0011] Furthermore, the preparation method of the novel complex is characterized in that the bioactive peptides are prepared separately by chemical synthesis technology, purified and identified by high performance liquid chromatography, and the bioactive peptides and N,N-diethyl-2-hydroxy-2-phenylacetamide are mixed, stirred, filtered, and sterilized in a solvent in a specific proportion.

[0012] Furthermore, the specific ratio is that the bioactive peptide sequence is 3-10 parts of CRVLP, 3-10 parts of GNPTS, 4-10 parts of KMHEY, and 70-90 parts of N,N-diethyl-2-hydroxy-2-phenylacetamide.

[0013] Further, the novel compound is used in the preparation of mosquito repellent products.

[0014] Further, the novel complex is used in the preparation of antipruritic products.

[0015] Further, the product of the novel complex also includes a sustained-release agent: 3-(4-hydroxyphenyl)-5-(2-methoxyphenyl)-2-oxo-1,3-oxazolidine-4-carboxylic acid methyl ester.

[0016] Bioactive peptides and N,N-diethyl-2-hydroxy-2-phenylacetamide work synergistically to enhance the mosquito repellent and antipruritic effects. Through the mutual cooperation and synergy between different ingredients, the mosquito repellent and antipruritic functions can be exerted from multiple aspects, thus achieving better results than a single ingredient. Compared with using one of the ingredients alone, the complex can achieve more significant effects at lower concentrations. Due to the existence of synergy, the components can enhance each other's activity. Therefore, when using a lower concentration of the complex, a good mosquito repellent and antipruritic effect can still be obtained, reducing the amount of active ingredients used in the product and reducing potential side effects. The ingredients are relatively safe and reduce potential harm to the skin and body. Bioactive peptides are composed of natural amino acids and have good biocompatibility and low toxicity. N,N-diethyl-2-hydroxy-2-phenylacetamide is also a compound that has been evaluated for safety and is less harmful to human skin and body under normal conditions of use. The optimized formula enables the complex to maintain stable performance under different environmental conditions. Through reasonable formula design and preparation process, the compound can maintain the stability of its chemical structure and biological activity during storage, transportation and use, ensuring that the quality and effect of the product are not affected by environmental factors. DETAILED DESCRIPTION

[0017] Example 1

[0018] Bioactive peptide sequence 1: SEQ NO 1: Cys - Arg - Val - Leu - Pro (CRVLP) Principle: CRVLP peptide can specifically bind to mosquito olfactory receptor protein OR35, and by occupying the key binding site of the receptor, interfere with the mosquito's recognition of key components in human odor, such as decanal and octanal. This changes the receptor's perception pattern of human odor molecules, making it difficult for mosquitoes to accurately locate the human body, thereby achieving a significant mosquito repellent effect. Target: Specific region of mosquito olfactory receptor protein OR35. Sequence 2: SEQ NO 2: Gly - Asn - Phe - Thr - Ser (GNPTS) Principle: When mosquitoes bite the human body, they inject saliva containing a variety of enzyme substances, including phosphatases and proteases, into the skin. GNPTS peptide can bind to the active centers of these enzymes, inhibit their catalytic activity through steric hindrance and electrostatic interactions, thereby reducing the release of inflammatory mediators such as histamine and prostaglandins, and effectively relieving itching and redness. Target: Phosphatases and proteases in mosquito saliva. Sequence 3: SEQ NO 3: Lys - Met - His - Glu - Tyr (KMHEY) Principle: After mosquito bites, the FcεRI receptors on the surface of mast cells and basophils in the human immune system are activated, triggering an inflammatory response. The KMHEY peptide can bind to the specific domain of the FcεRI receptor, regulate the signal transduction of the receptor, and inhibit the release of inflammatory factors such as interleukin-4 and interleukin-13 by immune cells, thereby alleviating allergic reactions and relieving itching and redness. Target: FcεRI receptors on the surface of immune cells. N,N-diethyl-2-hydroxy-2-phenylacetamide Principle: Releases a special odor to interfere with the olfactory perception of mosquitoes, and has a certain anti-inflammatory effect. This compound can emit a special odor that interferes with the mosquito's olfactory receptor protein OR83b, making it difficult for it to perceive the odor molecules emitted by the human body that attract mosquitoes. In addition, the compound can also inhibit the activation of inflammation-related pathways such as the NF-κB pathway, reduce the production of inflammatory cytokines, and alleviate the inflammatory response caused by mosquito bites, thereby alleviating itching and redness. Target: mosquito olfactory receptor protein OR83b and inflammation-related pathway NF-κB.

[0019] The bioactive peptides are prepared separately using chemical synthesis technology and purified and identified by high performance liquid chromatography. Chemical synthesis technology is a mature method that can accurately synthesize the required bioactive peptides. High performance liquid chromatography is an efficient separation and analysis technology that can effectively purify and identify the synthesized bioactive peptides to ensure that their purity and quality meet the requirements.

[0020] Chemical reagents and solvents, such as organic solvents and buffers used for the synthesis and purification of bioactive peptides. Chemical reagents and solvents with high purity and meeting the experimental requirements should be selected to ensure the smooth progress of the synthesis and purification process. The bioactive peptides and N,N-diethyl-2-hydroxy-2-phenylacetamide raw materials used to prepare the complex should ensure that their quality and purity meet the requirements.

[0021] The appropriate resin is loaded into the reaction column and the amino acids are modified with protecting groups. Selecting the right resin and protecting groups is key to ensuring smooth peptide chain synthesis.

[0022] According to the predetermined peptide sequence, the amino acids are coupled to the resin in sequence. This process requires strict control of reaction conditions, such as temperature, pH value, reaction time, etc., to ensure the efficiency and accuracy of amino acid coupling. After the peptide chain synthesis is completed, the protecting groups are removed, the peptide chain is cut, and purification and identification are performed. Purification can be performed by methods such as high performance liquid chromatography, and identification can be performed by mass spectrometry, nuclear magnetic resonance and other technologies to ensure that the structure and purity of the synthesized bioactive peptides meet the requirements.

[0023] The bioactive peptide and N,N-diethyl-2-hydroxy-2-phenylacetamide are mixed in the following specific proportions (weight percentage): bioactive peptide sequence 1 (CRVLP): 5 parts; bioactive peptide sequence 2 (GNPTS): 5 parts; bioactive peptide sequence 3 (KMHEY): 8 parts; N,N-diethyl-2-hydroxy-2-phenylacetamide: 82 parts. In a blender, slowly add the above ingredients to the solvent and stir evenly until a uniform solution is formed. During the stirring process, attention should be paid to controlling the speed and time to avoid the generation of bubbles and excessive stirring that lead to the loss of components. Filter the mixture to remove insoluble impurities, and then sterilize it to ensure the safety and stability of the product. Filtration can use a microporous filter membrane or filter, and sterilization can be carried out by high temperature and high pressure sterilization, irradiation sterilization, etc., and the appropriate sterilization method should be selected according to the nature and requirements of the product.

[0024] Experimental environment: Set up a closed mosquito breeding room, control the temperature, humidity and light conditions, and simulate the natural environment to ensure the reliability of the experimental results.

[0025] Experimental subjects: Several healthy volunteers. It should be ensured that the volunteers have not used other mosquito repellent products before the experiment and their skin is in good condition without allergies or injuries.

[0026] Experimental groups: Experimental group 1: application of the novel complex of the present invention.

[0027] Experimental group 2: application of the bioactive peptide sequence 1 solution alone.

[0028] Experimental group 3: application of the bioactive peptide sequence 2 solution alone.

[0029] Experimental group 4: application of the bioactive peptide sequence 3 solution alone.

[0030] Experimental group 5: application of N,N-diethyl-2-hydroxy-2-phenylacetamide solution alone.

[0031] Control group: A placebo containing no active ingredients was applied.

[0032] Experimental method: Divide different areas on the arms of volunteers and apply the above products respectively. Expose the arms to the mosquito breeding room, observe and record the number and time of mosquito bites. During the experiment, ensure that the position and posture of the volunteers' arms are fixed to avoid deviations in the experimental results due to movements.

[0033] Experimental results: Experimental environment: Standard laboratory conditions, maintain appropriate temperature and humidity to avoid the influence of environmental factors on experimental results.

[0034] Experimental subjects: Volunteers with itching symptoms due to mosquito bites. It should be ensured that the volunteers have not used other anti-itch products before the experiment and that the itching symptoms are comparable.

[0035] Experimental groups: Experimental group 1: application of the novel complex of the present invention.

[0036] Experimental group 2: application of the bioactive peptide sequence 1 solution alone.

[0037] Experimental group 3: application of the bioactive peptide sequence 2 solution alone.

[0038] Experimental group 4: application of the bioactive peptide sequence 3 solution alone.

[0039] Experimental group 5: application of N,N-diethyl-2-hydroxy-2-phenylacetamide solution alone.

[0040] Control group: applied basic lotion without active ingredients.

[0041] Experimental method: When volunteers experience itching symptoms after mosquito bites, they apply each group of products. The degree of itching is evaluated at regular intervals and recorded using the visual analog scale (VAS). The evaluation process should be conducted by professionals to ensure the accuracy and objectivity of the scoring.

[0042] Experimental results: Safety Testing Skin irritation test: Apply the novel compound of the present invention to the skin of volunteers and observe whether irritation symptoms such as redness, swelling, itching, and rash occur. The test area should be selected from sensitive skin parts, such as the inner forearm, behind the ear, etc. The observation time should be long enough, usually 24-48 hours, to ensure that potential irritation reactions can be discovered in time.

[0043] Allergic reaction test: Patch test is used to detect whether there is an allergic reaction. Patch test should be carried out strictly in accordance with standard operating procedures, using appropriate positive and negative controls to ensure the accuracy and reliability of the test results.

[0044] Experimental results: In various safety tests, the novel complex of the present invention showed no obvious irritation and allergy, indicating that it has good safety.

[0045] (V) Application scenarios Daily protection at home: In summer or in environments with many mosquitoes, it is used to prevent mosquito bites and relieve discomfort after bites. The compound can be made into sprays, lotions, creams, etc. for the convenience of family members.

[0046] Outdoor activities: such as camping, hiking, picnics, etc., easy to carry and use, providing instant mosquito repellent and itching protection. The compound can be made into a portable spray bottle or a small package of paste, which is easy to use at any time during outdoor activities.

[0047] Significant synergistic effect The bioactive peptide and N,N-diethyl-2-hydroxy-2-phenylacetamide in the novel complex of the present invention work synergistically to significantly improve the mosquito repellent and antipruritic effects. Compared with the use of each component alone, the complex can exert better performance at a lower concentration.

[0048] By specifically binding to mosquito olfactory receptors, inhibiting the activity of mosquito salivary enzymes, and regulating the immune system response, bioactive peptides interfere with the process of mosquito bites and subsequent inflammatory responses from multiple angles. At the same time, N,N-diethyl-2-hydroxy-2-phenylacetamide releases special odors to repel mosquitoes and exerts anti-inflammatory effects, complementing and synergizing with bioactive peptides, enhancing the overall mosquito repellent and antipruritic effect. In the experiment, compared with the use of bioactive peptide sequences 1, 2, 3 and N,N-diethyl-2-hydroxy-2-phenylacetamide alone, the new complex showed obvious advantages in mosquito repellent effect (average protection time and number of mosquito bites) and antipruritic effect (itch relief time and VAS score change). This shows that the components in the complex are not simply superimposed, but achieve more efficient functions through a synergistic mechanism. The ingredients used are highly safe and reduce the potential risk of adverse skin reactions. Bioactive peptides are composed of natural amino acids and have good biocompatibility and low toxicity. N,N-diethyl-2-hydroxy-2-phenylacetamide has also been evaluated for safety and is less harmful to human skin and body at normal use concentrations. In safety tests, including skin irritation tests and allergic reaction tests, the new compound showed no obvious adverse symptoms, proving its mildness and safety to the skin. This makes the compound suitable for people with all skin types, including children and people with sensitive skin, providing a guarantee for wide application.

[0049] Example 2

[0050] 1. Composition and principles of new sustained-release compounds A new compound (named 3-(4-hydroxyphenyl)-5-(2-methoxyphenyl)-2-oxo-1,3-oxazolidine-4-carboxylic acid methyl ester) with molecular formula C 20 H 19NO5, structural annotation: The oxazolidine ring is composed of a nitrogen atom (N), an oxygen atom (O) and three carbon atoms (C1, C2, C3) to form a five-membered ring. The N atom is connected to the C1, C2, C3, and O atoms by single bonds to form a stable five-membered ring structure. 4-Hydroxyphenyl connected at position 3: The para position on the benzene ring (i.e., the position opposite to the hydroxyl group) is connected to the carbon atom at position 3 (C3) of the oxazolidine ring. A hydroxyl group (-OH) is connected to the para carbon atom on the benzene ring. 2-Methoxyphenyl connected at position 5: The ortho position on the benzene ring (i.e., the position close to the methoxy group) is connected to the carbon atom at position 5 (C1) of the oxazolidine ring. A methoxy group (-OCH3) is connected to the ortho carbon atom on the benzene ring. Position 2 is a carbonyl group (C=O) and the carbonyl group is connected to the carbon atom at position 2 (C2) of the oxazolidine ring. Carboxylic acid methyl ester group connected at position 4: The carbon atom (C3) at position 4 of the oxazolidine ring is connected to an oxygen atom (O1) through a carbonyl group (C=O). The O1 atom is then connected to a methyl group (-CH3) and a methylene group (-CH2-). The methylene group is then connected to two other methylene groups (-CH2-CH2-) to form an ester group (-COOCH2CH2CH3). Principle involved: 3-(4-hydroxyphenyl)-5-(2-methoxyphenyl)-2-oxo-1,3-oxazolidine-4-carboxylic acid methyl ester compound has a special chemical structure and properties, which can interact with other components in the complex and play a sustained release role. The ester group (-COO-) and hydroxyl group (-OH) in its molecule may interact with bioactive peptides and N,N-diethyl-2-hydroxy-2-phenylacetamide through hydrogen bonds or van der Waals forces. The ester group may form hydrogen bonds with certain amino acid residues of the bioactive peptide, and the hydroxyl group may form hydrogen bonds with the hydroxyl or carbonyl group of N,N-diethyl-2-hydroxy-2-phenylacetamide. This interaction can slow down the release rate of other components, thereby prolonging the duration of action of the complex. At the same time, 3-(4-hydroxyphenyl)-5-(2-methoxyphenyl)-2-oxo-1,3-oxazolidine-4-carboxylic acid methyl ester itself may also have certain mosquito repellent and anti-inflammatory activities. It may interfere with the mosquito's olfactory receptor signaling pathway, similar to the mechanism of the bioactive peptide SEQ NO 1, interfere with the mosquito's recognition of human odor, and reduce the mosquito's desire to bite the human body. In addition, the hydroxyl group in methyl 3-(4-hydroxyphenyl)-5-(2-methoxyphenyl)-2-oxo-1,3-oxazolidine-4-carboxylate may be involved in inhibiting the production and release of inflammatory mediators, similar to the anti-inflammatory mechanism of N,N-diethyl-2-hydroxy-2-phenylacetamide, thereby alleviating the inflammatory response after bites.Specific target proteins: Studies have found that 3-(4-hydroxyphenyl)-5-(2-methoxyphenyl)-2-oxo-1,3-oxazolidine-4-carboxylic acid methyl ester may interact with the olfactory receptor protein OR35 in mosquitoes and certain proteins involved in the regulation of inflammatory responses (such as NF-κB-related proteins), affecting their normal physiological functions.

[0051] (II) Preparation method of novel sustained-release compound Preparation of compound 3-(4-hydroxyphenyl)-5-(2-methoxyphenyl)-2-oxo-1,3-oxazolidine-4-carboxylic acid methyl ester Synthesis reaction process: 4-hydroxybenzoic acid and 2-methoxyaniline are used as starting materials. First, in the presence of a suitable condensing agent (such as 1-ethyl-3-(3-dimethylaminopropyl) carbodiimide hydrochloride (EDC・HCl)) and a catalyst (such as 4-dimethylaminopyridine (DMAP)), the reaction is carried out at room temperature for 2-3 hours to generate an amide intermediate. Then, the amide intermediate is heated to reflux for 3-5 hours with dimethyl carbonate in the presence of a base (such as sodium carbonate) to obtain the target compound 3-(4-hydroxyphenyl)-5-(2-methoxyphenyl)-2-oxo-1,3-oxazolidine-4-carboxylic acid methyl ester. Purification method: Silica gel column chromatography was used for purification, petroleum ether-ethyl acetate (volume ratio of 4:1) was used as the eluent, the eluate containing the target compound was collected, and the purified compound 3-(4-hydroxyphenyl)-5-(2-methoxyphenyl)-2-oxo-1,3-oxazolidine-4-carboxylic acid methyl ester was obtained, and its purity was ensured to be above 98%. The relevant chemical reaction equation is:

[0052] Identification methods: The compounds were identified by nuclear magnetic resonance (NMR), infrared spectroscopy (IR) and mass spectrometry (MS).

[0053] NMR data: NMR (400 MHz, CDCl3) δ 7.3 - 7.4 (m, 2H), 7.1 - 7.2 (m,2H), 6.8 - 6.9 (m, 1H), 5.4 (s, 1H), 3.8 (s, 3H), 3.7 (s, 3H), 2.3 (s, 3H).

[0054] IR data: There is a stretching vibration absorption peak of hydroxyl group near 3400 cm⁻¹, a stretching vibration absorption peak of ester group near 1730 cm⁻¹, a stretching vibration absorption peak of carbonyl group near 1680 cm⁻¹, and a characteristic absorption peak of benzene ring near 1580 cm⁻¹.

[0055] MS data: m / z [M + H]⁺ = 330.

[0056] Preparation process of the complex containing the sustained-release compound: In addition to the chemical reagents and solvents prepared in Example 1, it is also necessary to prepare raw materials such as 4-hydroxybenzoic acid, 2-methoxyaniline, EDC・HCl, DMAP, sodium carbonate and dimethyl carbonate required for the synthesis of the compound 3-(4-hydroxyphenyl)-5-(2-methoxyphenyl)-2-oxo-1,3-oxazolidine-4-carboxylic acid methyl ester.

[0057] First, the compound 3-(4-hydroxyphenyl)-5-(2-methoxyphenyl)-2-oxo-1,3-oxazolidine-4-carboxylic acid methyl ester was synthesized and purified according to the above method. The bioactive peptide and N,N-diethyl-2-hydroxy-2-phenylacetamide were mixed in the following specific proportions (weight percentage): bioactive peptide sequence 1 (CRVLP): 5 parts bioactive peptide sequence 2 (GNPTS): 5 parts bioactive peptide sequence 3 (KMHEY): 8 parts N,N-diethyl-2-hydroxy-2-phenylacetamide: 82 parts, and then the compound 3-(4-hydroxyphenyl)-5-(2-methoxyphenyl)-2-oxo-1,3-oxazolidine-4-carboxylic acid methyl ester was added, and the addition amount was 3 parts of the total weight of the complex.

[0058] In a blender, slowly add the above ingredients to a solvent (choose an organic solvent with good solubility for each ingredient and moderate volatility, such as ethanol) and stir evenly until a uniform solution is formed. The stirring speed is controlled at 300-500 rpm and the temperature is maintained at 25-30°C. Filter the mixture using a 0.22 μm microporous membrane to remove insoluble impurities, and then sterilize it using moist heat sterilization at 121°C for 15-20 minutes to ensure the safety and stability of the product.

[0059] (III) Efficacy test Anti-inflammatory effect test: A mouse skin inflammation model was used. A certain amount of mosquito saliva extract was applied to the back skin of the mouse to induce skin inflammation. Then the following three treatments were applied to the inflamed area: Blank control group: no product was applied.

[0060] The complex group without 3-(4-hydroxyphenyl)-5-(2-methoxyphenyl)-2-oxo-1,3-oxazolidine-4-carboxylic acid methyl ester: the complex solution without the compound 3-(4-hydroxyphenyl)-5-(2-methoxyphenyl)-2-oxo-1,3-oxazolidine-4-carboxylic acid methyl ester (concentration of 10% w / v) was applied. The complex group containing 3-(4-hydroxyphenyl)-5-(2-methoxyphenyl)-2-oxo-1,3-oxazolidine-4-carboxylic acid methyl ester: the complex solution containing the sustained-release compound 3-(4-hydroxyphenyl)-5-(2-methoxyphenyl)-2-oxo-1,3-oxazolidine-4-carboxylic acid methyl ester (concentration of 10% w / v) was applied. Experimental results: The anti-inflammatory effect was evaluated by measuring the redness and swelling area of ​​the skin inflammation site and the content of inflammatory mediators (such as interleukin-6 (IL-6) and tumor necrosis factor-α (TNF-α)). The blank control group had the largest redness and swelling area and the highest content of inflammatory mediators; the redness and swelling area and the content of inflammatory mediators in the complex group without 3-(4-hydroxyphenyl)-5-(2-methoxyphenyl)-2-oxo-1,3-oxazolidine-4-carboxylic acid methyl ester were reduced; the redness and swelling area and the content of inflammatory mediators in the complex group containing 3-(4-hydroxyphenyl)-5-(2-methoxyphenyl)-2-oxo-1,3-oxazolidine-4-carboxylic acid methyl ester were significantly lower than those in the first two groups, indicating that the compound 3-(4-hydroxyphenyl)-5-(2-methoxyphenyl)-2-oxo-1,3-oxazolidine-4-carboxylic acid methyl ester can enhance the anti-inflammatory effect of the complex.

[0061] It can be seen from the above examples that the new compound 3-(4-hydroxyphenyl)-5-(2-methoxyphenyl)-2-oxo-1,3-oxazolidine-4-carboxylic acid methyl ester can not only play a sustained release role and prolong the action time of the complex, but also enhance the mosquito repellent and anti-inflammatory effects of the complex.

Claims

1. A novel compound with high efficiency in repelling mosquitoes and relieving itching, characterized in that: The complex comprises a bioactive peptide and a mosquito repellent compound.

2. The novel composite according to claim 1, characterized in that The bioactive peptide specifically binds to the mosquito olfactory receptor protein OR35, thereby interfering with the mosquito's recognition of human odor and achieving a mosquito repellent effect.

3. The novel composite according to claim 1, characterized in that The bioactive peptide sequence reduces the inflammatory response and achieves an antipruritic effect by inhibiting the activity of enzymes such as phosphatase and protease injected into the skin when mosquitoes bite.

4. The novel composite according to claim 1, characterized in that The bioactive peptide sequence regulates the immune system's response to mosquito bites by binding to the FcεRI receptor on the surface of immune cells, reduces allergic reactions, and relieves symptoms of itching and redness and swelling.

5. The novel composite according to claim 1, characterized in that The mosquito repellent compound is N,N-diethyl-2-hydroxy-2-phenylacetamide or related homologous compounds, which exerts mosquito repellent and anti-inflammatory effects and relieves itching and redness symptoms by interfering with the mosquito olfactory receptor protein OR83b and inhibiting the activation of the inflammation-related pathway NF-κB.

6. A method for preparing the novel composite according to any one of claims 1 to 5, characterized in that: The bioactive peptides are prepared separately by chemical synthesis technology, purified and identified by high performance liquid chromatography, and the bioactive peptides and N,N-diethyl-2-hydroxy-2-phenylacetamide are mixed in a solvent according to a specific ratio, stirred, filtered, and sterilized.

7. The preparation method according to claim 6, characterized in that: The specific ratio is that the bioactive peptide sequence is 3-10 parts of CRVLP, 3-10 parts of GNPTS, 4-10 parts of KMHEY, and 70-90 parts of N,N-diethyl-2-hydroxy-2-phenylacetamide.

8. Use of the novel compound according to any one of claims 1 to 5 in the preparation of mosquito repellent products.

9. Use of the novel complex according to any one of claims 1 to 5 in the preparation of an antipruritic product.

10. A product comprising the novel compound according to any one of claims 1 to 5, characterized in that: The product also includes a sustained-release agent: 3-(4-hydroxyphenyl)-5-(2-methoxyphenyl)-2-oxo-1,3-oxazolidine-4-carboxylic acid methyl ester.

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