Anti-inflammatory soothing composition and application thereof

Abstract

The invention discloses an anti-inflammatory soothing composition which is composed of 100-270 parts of synephrine, 2-100 parts of geniposide and 8-100 parts of beta-glucan, and the three effective active components are utilized to effectively relieve skin inflammation through multi-dimensional and multi-path mechanisms such as inhibition of generation of inflammatory mediators, regulation of immune response, enhancement of skin barrier function and promotion of skin repair. The invention also determines the optimal compatibility proportion of the three active matters when the three active matters exert the anti-inflammatory and soothing effects, and ensures the high efficiency and safety of the composition. The anti-inflammatory soothing composition can be used in the fields of medicines and cosmetics, and has high market promotion value. The invention also discloses an application of the anti-inflammatory soothing composition in preparation of a product for treating and / or preventing skin inflammation.

Description

Technical Field

[0001] This invention relates to an anti-inflammatory and soothing composition and its application. Background Technology

[0002] Under normal physiological conditions, the skin's inflammatory response is a self-protective mechanism of the body against external stimuli, such as pathogen invasion, physical damage, or chemical irritation. It helps to remove harmful substances and promote wound healing. However, excessive or persistent inflammation can not only damage the skin barrier, leading to symptoms such as dry skin, erythema, and itching, but may also trigger a series of inflammatory skin diseases, such as acne, eczema, psoriasis, and allergic reactions, seriously affecting skin health and the patient's quality of life.

[0003] Skin inflammation is closely related to the excessive release of inflammatory mediators, such as interleukins, tumor necrosis factor, and prostaglandins. These mediators can activate inflammatory signaling pathways and exacerbate the inflammatory response. Studies have found that antioxidants can reduce inflammatory responses by scavenging free radicals and reducing oxidative stress. Furthermore, inhibiting key enzymes in inflammatory signaling pathways, such as cyclooxygenase (COX) and 5-lipoxygenase (5-LOX), can effectively control the production of inflammatory mediators and reduce skin inflammation.

[0004] Skin inflammation depends not only on the control of inflammatory mediators but also on factors such as the repair of the skin barrier function and the regulation of immune cells. For example, strengthening the skin barrier function and reducing the penetration of external irritants can effectively prevent inflammation. At the same time, regulating skin immune cells, such as inhibiting activated T cells and macrophages and reducing the infiltration of inflammatory cells, is also an important part of anti-inflammatory and soothing strategies.

[0005] Based on the above research findings, the synergistic effect of antioxidants, key enzyme inhibitors, barrier repair components, and immunomodulators can comprehensively and effectively suppress skin inflammation, achieving anti-inflammatory and soothing effects. This strategy not only alleviates skin inflammation symptoms and promotes skin repair but also prevents recurrent inflammation, providing new ideas and methods for the treatment and management of inflammatory skin diseases. Summary of the Invention

[0006] The purpose of this invention is to overcome the shortcomings of the prior art and provide an anti-inflammatory and soothing composition. Utilizing two effective ingredients derived from natural Chinese medicine and a polysaccharide, this composition regulates skin immune cells, such as inhibiting activated neutrophils and reducing the infiltration of inflammatory cells, thus exhibiting good anti-inflammatory and soothing effects. Furthermore, the optimal ratio of the three active ingredients to exert their anti-inflammatory and soothing effects has been determined. This anti-inflammatory and soothing composition can be used in the pharmaceutical and cosmetic fields and has high market promotion value.

[0007] Another object of the present invention is to provide an anti-inflammatory and soothing composition for use in products for treating and / or preventing skin inflammation.

[0008] One technical solution to achieve the above objective is: an anti-inflammatory and soothing composition, which, by weight, consists of 100-270 parts of synephrine, 2-100 parts of geniposide, and 8-100 parts of β-glucan.

[0009] In the aforementioned anti-inflammatory and soothing composition, the mass ratio of synephrine, geniposide, and β-glucan is 2.04:0.10:0.86.

[0010] The above-mentioned anti-inflammatory and soothing composition, wherein the synephrine, geniposide, and β-glucan are obtained by chemical synthesis or by extraction and purification from natural plants and animals.

[0011] The present invention also provides the use of the above-described anti-inflammatory and soothing composition in products for treating and / or preventing skin inflammation.

[0012] The above-mentioned anti-inflammatory and soothing compositions are used in the context of pharmaceuticals and cosmetics.

[0013] The above-described anti-inflammatory and soothing composition is used in cases where the skin inflammation includes acne, eczema, psoriasis, and allergic skin reactions.

[0014] In the technical solution of the anti-inflammatory and soothing composition and its application of the present invention, synephrine is one of the effective components of the extracts of the traditional Chinese medicines *Citrus aurantium* and *Citrus reticulata*, and has anti-inflammatory, antioxidant, and blood circulation-promoting effects. Gardenoside, derived from the traditional Chinese medicine *Gardenia jasminoides*, has significant anti-inflammatory, analgesic, and antibacterial effects. β-glucan is a polysaccharide widely found in fungi, yeasts, oats, and other plants, and has powerful immunomodulatory, anti-inflammatory, and skin barrier-repairing functions.

[0015] The anti-inflammatory and soothing composition of this invention utilizes three effective active ingredients to effectively suppress skin inflammation through multiple dimensions and pathways, including inhibiting the production of inflammatory mediators, regulating immune responses, enhancing skin barrier function, and promoting skin repair. We have also determined the optimal ratio of the three active ingredients to achieve their anti-inflammatory and soothing effects, ensuring the composition's high efficacy and safety. This provides a scientific basis for the appropriate dosage of this composition in products, significantly increasing product effectiveness and reducing usage costs.

[0016] This anti-inflammatory and soothing composition is not only applicable to the pharmaceutical field, such as the preparation of drugs for treating inflammatory skin diseases, but also applicable to the cosmetic field, such as the preparation of skin care products that are anti-inflammatory, soothing, and repair sensitive skin. It has broad market prospects and extremely high promotional value. BRIEF DESCRIPTION OF THE DRAWINGS

[0017] Figure 1 A quantitative map of neutrophil migration in zebrafish (Tg(mpx:dsRED)) with red fluorescent labeling of neutrophils by a single component;

[0018] Figure 2 Phenotypic diagram of neutrophil migration in zebrafish (Tg(mpx:dsRED)) with single-component red fluorescent labeling of neutrophils.

[0019] Figure 3 A three-dimensional structural diagram constructed for the D-optimal design model;

[0020] Figure 4 A quantitative graph showing the effect of different ratios of anti-inflammatory and soothing compositions on neutrophil migration in zebrafish (Tg(mpx:dsRED)) with red fluorescent labeling.

[0021] Figure 5 Phenotypic diagram of neutrophil migration in zebrafish (Tg(mpx:dsRED)) with different ratios of anti-inflammatory and soothing compositions. Detailed Implementation

[0022] To enable those skilled in the art to better understand the technical solution of the present invention, its specific embodiments are described in detail below with reference to the accompanying drawings:

[0023] An embodiment of the present invention provides an anti-inflammatory and soothing composition, comprising, by weight, 100-270 parts synephrine, 2-100 parts geniposide, and 8-100 parts β-glucan. Synephrine, geniposide, and β-glucan are prepared by chemical synthesis or by extraction and purification from natural plants and animals. Commercially available products can be used for synephrine, geniposide, and β-glucan.

[0024] Biological evaluation of individual components of the anti-inflammatory and soothing composition was conducted by observing neutrophil migration in zebrafish, and the anti-inflammatory and soothing effects of individual components were verified.

[0025] Please see Figure 1 and Figure 2 In this experiment, zebrafish were labeled with neutrophil red fluorescent markers (Tg(mpx:dsRED)). The zebrafish were reared according to *The Zebrafish Book*. The water temperature was maintained at approximately 28.5℃, with 14 hours of light and 10 hours of darkness daily, and feeding twice a day, morning and evening. The night before embryo collection, one female and two male zebrafish were placed in a spawning tank, separated by a partition, and placed in a dark environment. The following morning, after the lights were turned on, the partition was removed, and the embryos were collected after spawning. The embryos were placed in egg water and cultured in a 28.5℃ illuminated incubator.

[0026] On the day of embryo collection, at approximately 7-8 hpf, thoroughly change and wash the embryos, removing any embryos in poor condition, and replace with fresh egg water. Continue incubation at 28.5℃ until 3 dpf (during incubation, promptly remove any unsuitable embryos and replace with fresh egg water daily).

[0027] The 3dpf zebrafish were randomly divided into groups of 15:

[0028] 1) Control group: containing zebrafish and standard dilution water.

[0029] 2) Model group: Contains zebrafish and modeling agent (copper sulfate solution).

[0030] 3) Synephrine group: Contains zebrafish, modeling agent (copper sulfate solution), and 0.1 mg / mL synephrine;

[0031] 4) Geniposide: Contains zebrafish, modeling agent (copper sulfate solution), and 1 mg / mL of geniposide;

[0032] 5) β-glucan: Contains zebrafish, modeling agent (copper sulfate solution) and 1 mg / mL of β-glucan.

[0033] After mixing thoroughly, cover with the culture plate panel and wrap with aluminum foil, then incubate in a biochemical incubator at 28°C in the dark for 2 hours.

[0034] Neutrophil red fluorescent labeling (Tg(mpx:dsRED)) in zebrafish allows neutrophils to emit red fluorescence, enabling direct observation of neutrophil migration and other behaviors in live zebrafish under a stereofluorescence microscope. After incubation, zebrafish with normal phenotype and behavior were randomly selected, fixed with 3% methylcellulose, and observed and photographed under a stereofluorescence microscope. All zebrafish photographs were taken under identical instrument and environmental conditions, and the zebrafish positions were kept consistent.

[0035] Quantitative results of the effects of different ratios of anti-inflammatory and soothing compositions on zebrafish neutrophil migration, such as... Figure 1 As shown, the phenotypic results are as follows Figure 2 As shown.

[0036] from Figure 1 and Figure 2 As can be seen, the anti-inflammatory effects of using synephrine, geniposide, and β-glucan alone are shown in Table 1 below:

[0037] name concentration Anti-inflammatory effect (%) Synephrine 0.1 mg / mL 56.41 Gardenin 1mg / mL 38.81 β-glucan 1mg / mL 44.92

[0038] The different masses of synephrine, geniposide, and β-glucan in the anti-inflammatory and soothing composition are shown in Table 2 below.

[0039] Table 2. Compatibility ratios of synephrine, geniposide, and β-glucan:

[0040] name Synephrine Gardenin β-glucan Compatibility ratio 1 1.46 0.74 0.80 Compatibility ratio 2 1.09 1.00 0.91 Compatibility ratio 3 1.96 0.10 0.94 Compatibility ratio 4 1.87 0.62 0.51 Compatibility ratio 5 1.54 1.00 0.46 Compatibility ratio 6 1.88 1.00 0.12 Compatibility ratio 7 2.22 0.42 0.36 Compatibility ratio 8 2.17 0.73 0.10 Compatibility ratio 9 1.61 0.39 1.00 Compatibility ratio 10 2.29 0.10 0.61 Compatibility ratio 11 2.62 0.28 0.10

[0041] Based on the mass ratios in Table 2, prepare anti-inflammatory and soothing compositions with compatibility ratios of 1-11.

[0042] Please see Figure 3 Using the D-optimal design mathematical calculation method, under the premise of keeping the total amount of the anti-inflammatory and soothing composition fixed, the changes in efficacy and activity are correlated by the changes in the compatibility ratio of each component in the anti-inflammatory and soothing composition, and a corresponding mathematical model is constructed to explore the relationship between the compatibility ratio of each component in the anti-inflammatory and soothing composition and the efficacy. A three-dimensional structural diagram is constructed to predict the optimal compatibility ratio range and the optimal compatibility ratio. Figure 3 In the diagram, A represents the mass ratio of synephrine; B represents the mass ratio of geniposide; and C represents the mass ratio of β-glucan. From a numerical modeling perspective, the three components of the anti-inflammatory and soothing composition were designed to coordinate their compatibility. It was predicted that the optimal anti-inflammatory and soothing effect would be achieved when the compatibility ratio of synephrine:geniposide:β-glucan = 2.04:0.10:0.86.

[0043] Then, by observing the migration of neutrophils in zebrafish, the biological evaluation of anti-inflammatory and soothing compositions with different ratios was conducted, and the anti-inflammatory and soothing effects of the optimal ratio of anti-inflammatory and soothing compositions were verified.

[0044] Effects of different ratios of anti-inflammatory and soothing compositions on neutrophil migration in zebrafish (Tg(mpx:dsRED)):

[0045] Please see Figure 4 In this experiment, zebrafish were labeled with neutrophil red fluorescent markers (Tg(mpx:dsRED)). The zebrafish were reared according to *The Zebrafish Book*. The water temperature was maintained at approximately 28.5℃, with 14 hours of light and 10 hours of darkness daily, and feeding twice a day, morning and evening. The night before embryo collection, one female and two male zebrafish were placed in a spawning tank, separated by a partition, and placed in a dark environment. The following morning, after the lights were turned on, the partition was removed, and the embryos were collected after spawning. The embryos were placed in egg water and cultured in a 28.5℃ illuminated incubator.

[0046] On the day of embryo collection, at approximately 7-8 hpf, thoroughly change and wash the embryos, removing any embryos in poor condition, and replace with fresh egg water. Continue incubation at 28.5℃ until 3 dpf (during incubation, promptly remove any unsuitable embryos and replace with fresh egg water daily).

[0047] The 3dpf zebrafish were randomly divided into groups of 15:

[0048] a) Normal control group: containing zebrafish and standard dilution water.

[0049] b) Model control group: containing zebrafish and modeling agent (copper sulfate solution).

[0050] c) Test group of test substances: containing zebrafish, modeling agent (copper sulfate solution) and test substances of different concentrations.

[0051] After mixing thoroughly, cover with the culture plate panel and wrap with aluminum foil, then incubate in a biochemical incubator at 28°C in the dark for 2 hours.

[0052] Neutrophil red fluorescent labeling (Tg(mpx:dsRED)) in zebrafish allows neutrophils to emit red fluorescence, enabling direct observation of neutrophil migration and other behaviors in live zebrafish under a stereofluorescence microscope. After incubation, zebrafish with normal phenotype and behavior were randomly selected, fixed with 3% methylcellulose, and observed and photographed under a stereofluorescence microscope. All zebrafish photographs were taken under identical instrument and environmental conditions, and the zebrafish positions were kept consistent.

[0053] Quantitative results of the effects of different ratios of anti-inflammatory and soothing compositions on zebrafish neutrophil migration, such as... Figure 4 As shown, the phenotypic results are as follows Figure 5 As shown.

[0054] Experimental results showed that, compared with the model control group, all anti-inflammatory and soothing compositions with different ratios significantly inhibited the migration of neutrophils in zebrafish. Furthermore, the optimal ratio, namely synephrine:geniposide:β-glucan = 2.04:0.10:0.86, exhibited significantly better anti-inflammatory and soothing effects on zebrafish than other ratios. The anti-inflammatory effects of the anti-inflammatory and soothing compositions with different ratios are shown in Table 3.

[0055] Table 3. Anti-inflammatory effects of anti-inflammatory and soothing compositions with different formulation ratios:

[0056]

[0057]

[0058] As shown in Table 3, the anti-inflammatory effect is significantly enhanced when the mass ratio of synephrine, geniposide, and β-glucan is 2.04:0.10:0.86. The anti-inflammatory and soothing composition of this invention can be used in the preparation of drugs and cosmetics for the treatment and / or prevention of skin inflammation, including acne, eczema, psoriasis, and allergic skin reactions.

[0059] Finally, following the above method, the anti-inflammatory and soothing effects of the anti-inflammatory and soothing composition and its individual components were evaluated by observing the migration of neutrophils in zebrafish. The anti-inflammatory and soothing results are shown in Table 4.

[0060] Table 4. Anti-inflammatory effects of individual components and anti-inflammatory soothing compositions:

[0061]

[0062] As shown in Table 4, compared with individual components, the anti-inflammatory effect was significantly improved when the mass ratio of synephrine, geniposide, and β-glucan was 2.04:0.10:0.86.

[0063] In summary, the anti-inflammatory and soothing composition of this invention utilizes three effective active ingredients to achieve effective management and soothing of skin inflammation through multi-dimensional and multi-pathway mechanisms, including inhibiting the production of inflammatory mediators, regulating immune responses, enhancing skin barrier function, and promoting skin repair. We have also determined the optimal ratio of the three active ingredients to exert their anti-inflammatory and soothing effects, ensuring the composition's high efficacy and safety. This anti-inflammatory and soothing composition has high market potential in the pharmaceutical and cosmetic fields.

[0064] Those skilled in the art should recognize that the above embodiments are merely illustrative of the present invention and are not intended to limit the present invention. Any variations or modifications to the above embodiments that are within the spirit and essence of the present invention will fall within the scope of the claims of the present invention.

Claims

1. An anti-inflammatory soothing composition, characterized in that: The invention comprises 100 to 270 parts of synephrine, 2 to 100 parts of gardenia glycoside and 8 to 100 parts of beta-glucan in parts by weight.

2. An anti-inflammatory soothing composition according to claim 1, characterized in that: The mass ratio of synephrine, gardenoside and β-glucan is 2.04:0.10:0.

86.

3. An anti-inflammatory soothing composition according to claim 1, characterized in that: The synephrine, gardenia glycoside and beta-glucan are prepared by chemical synthesis or extraction and purification of natural animals and plants.

4. Use of the anti-inflammatory soothing composition according to any one of claims 1 to 3 in products for treating and / or preventing skin inflammation.

5. The use of the anti-inflammatory soothing composition according to claim 4, characterized in that: The products include medicines and cosmetics.

6. The use of the anti-inflammatory soothing composition according to claim 4, characterized in that: The skin inflammation includes acne, eczema, psoriasis and allergic skin reactions.

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