Use of the composition
Patent Information
- Application Number
- CN202611317499.8
- Authority / Receiving Office
- CN · China
- Patent Type
- Applications(China)
- Current Assignee / Owner
- Filing Date
- 2026-08-28
- Publication Date
- 2026-09-25
AI Technical Summary
[0014]本申请的有益效果包括:当将中长链脂肪酸甘油三酯与神经酸以特定质量比组合使用时,在改善过敏和/或湿疹、特别是缓解瘙痒和降低类胰蛋白酶含量方面呈现出协同作用,其组合使用的效果优于单独使用相同量的中长链脂肪酸甘油三酯的效果或单独使用相同量的神经酸的效果,也优于单独使用相同量的中长链脂肪酸甘油三酯+单独使用相同量的神经酸的效果之和。例如,当中长链脂肪酸甘油三酯与神经酸以3:1至1000:1的质量比使用时,组合物能够协同地缓解瘙痒和/或降低类胰蛋白酶含量,从而改善过敏和/或湿疹。优选地,当中长链脂肪酸甘油三酯与神经酸以4.63:1至667:1的质量比使用时,或者以55.6:1至667:1的质量比使用时,或者以111:1至667:1的质量比使用时,或者以333:1至667:1的质量比使用时,所述组合物能够协同地缓解瘙痒和/或降低类胰蛋白酶含量,从而改善过敏和/或湿疹。
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Figure CN122805628A_ABST
Abstract
Description
Technical Field
[0001] This application relates to the use of the composition, and in particular to its use in the preparation of products for improving eczema. Background Technology
[0002] Eczema is an inflammation of the epidermis and superficial dermis caused by a variety of internal and external factors. In the acute phase, the skin lesions are mainly papulovesicles with a tendency to ooze, while in the chronic phase, lichenification is the main feature, and it is prone to recurrence. In recent years, the global incidence of eczema has been on the rise, affecting about 2.0% of adults and 4.0% of children. The pathogenesis of eczema is closely related to the interaction between many factors such as genetic background, environmental factors, skin barrier dysfunction, microbial imbalance, immune dysregulation and skin inflammation (Zhang Aili, Xu Na, Wang Juan, et al. Peripheral serum levels of 25-hydroxyvitamin D, IL-4, IL-10 and IL-17 in adult eczema and their clinical significance [J]. Guizhou Medical Journal, 2026, 50(03): 467-473).
[0003] In view of the above problems, it is of great significance to develop ways to effectively improve eczema. Summary of the Invention
[0004] This application is made in view of the aforementioned problems existing in the prior art.
[0005] In one aspect, this application relates to the use of a composition in the preparation of a product for improving eczema, wherein the composition comprises a medium- and long-chain fatty acid triglyceride and nervonic acid, and the mass ratio of the medium- and long-chain fatty acid triglyceride to the nervonic acid is from 3:1 to 1000:1.
[0006] In some embodiments, the mass ratio of the medium- and long-chain fatty acid triglycerides to the nervonic acid is from 4.63:1 to 667:1.
[0007] In some embodiments, the mass ratio of the medium- and long-chain fatty acid triglycerides to the nervonic acid is from 55.6:1 to 667:1.
[0008] In some embodiments, the mass ratio of the medium- and long-chain fatty acid triglycerides to the nervonic acid is from 111:1 to 667:1.
[0009] In some embodiments, the mass ratio of the medium- and long-chain fatty acid triglycerides to the nervonic acid is 167:1 to 667:1.
[0010] In some embodiments, the mass ratio of the medium- and long-chain fatty acid triglycerides to the nervonic acid is from 333:1 to 667:1.
[0011] In some embodiments, the eczema is allergic eczema.
[0012] In some embodiments, the improvement of eczema includes relieving itching and / or reducing trypsin levels.
[0013] In some embodiments, the composition is used in such a quantity that the intake of the medium- and long-chain fatty acid triglycerides is 2.25 g to 30.0 g per day.
[0014] The beneficial effects of this application include: when medium- and long-chain fatty acid triglycerides and nervonic acid are used in combination at a specific mass ratio, they exhibit a synergistic effect in improving allergies and / or eczema, particularly in relieving itching and reducing trypsin levels. The combined effect is superior to the effect of using the same amount of medium- and long-chain fatty acid triglycerides alone or using the same amount of nervonic acid alone, and also superior to the sum of the effects of using the same amount of medium- and long-chain fatty acid triglycerides alone plus the same amount of nervonic acid alone. For example, when medium- and long-chain fatty acid triglycerides and nervonic acid are used at a mass ratio of 3:1 to 1000:1, the composition can synergistically relieve itching and / or reduce trypsin levels, thereby improving allergies and / or eczema. Preferably, when the long-chain fatty acid triglycerides and nervonic acid are used in a mass ratio of 4.63:1 to 667:1, or in a mass ratio of 55.6:1 to 667:1, or in a mass ratio of 111:1 to 667:1, or in a mass ratio of 333:1 to 667:1, the composition can synergistically relieve itching and / or reduce trypsin levels, thereby improving allergies and / or eczema. Attached Figure Description
[0015] To more clearly illustrate the technical solutions of this application, the accompanying drawings required for describing the embodiments will be briefly described below. It should be understood that these drawings are only for the purpose of facilitating a better understanding of this application by those skilled in the art, and are not intended to limit the scope of this application.
[0016] Figure 1 A typical graph showing the total movement distance of zebrafish after sample treatment is presented, where the black line represents the slow movement distance, the green line represents the medium movement distance, and the red line represents the fast movement distance. Detailed Implementation
[0017] To provide a clearer understanding of the technical features, objectives, and beneficial effects of this application, the technical solution of this application is described in detail below with reference to specific embodiments and accompanying drawings. It should be understood that these embodiments are for illustrative purposes only and are not intended to limit the scope of this application. Unless otherwise specifically defined, all technical and scientific terms used herein have the same meaning as commonly understood by one of ordinary skill in the art. Furthermore, unless otherwise stated, all methods, steps, techniques, and operations not specifically detailed can and have been performed in a manner commonly known and understood by one of ordinary skill in the art.
[0018] In this application, unless otherwise specified, the temperature is room temperature (e.g., 25°C), the atmosphere is air, and the pressure is normal pressure (e.g., 1 atmosphere).
[0019] In this application, the term "medium-chain fatty acid" refers to fatty acids with 6 to 12 carbon atoms in their carbon chain, such as hexanoic acid, heptanoic acid, octanoic acid, nonanoic acid, decanoic acid, undecanoic acid, and dodecanoic acid. The term "long-chain fatty acid" refers to fatty acids with 14 or more carbon atoms in their carbon chain, generally 14 to 30 carbon atoms, such as myristic acid, palmitic acid, oleic acid, linoleic acid, stearic acid, linolenic acid, arachidonic acid, eicosapentaenoic acid, docosapentaenoic acid, and docosahexaenoic acid. The terms "medium-chain fatty acid triglyceride" (MCT) and "long-chain fatty acid triglyceride" (LCT) refer to the esterification products of medium-chain fatty acids and long-chain fatty acids with glycerol, respectively. The term "medium- and long-chain fatty acid triglycerides" refers to triglycerides that contain both medium-chain fatty acid residues and long-chain fatty acid residues in their molecular structure.
[0020] This application relates to compositions comprising medium- and long-chain fatty acid triglycerides and nervonic acid, products comprising the above compositions, the use of the above compositions in the preparation of products for improving allergies and / or eczema, and the use of the above compositions or products for non-therapeutic purposes in improving allergies and / or eczema. The application will be described in detail below.
[0021] In one aspect, this application provides the use of a composition for non-therapeutic purposes to improve allergies and / or eczema. The composition comprises medium- and long-chain fatty acid triglycerides and nervonic acid, wherein the mass ratio of the medium- and long-chain fatty acid triglycerides to nervonic acid is from 3:1 to 1000:1.
[0022] As used in this article, "medium- and long-chain triglycerides" (MLCT) refers to triglycerides with one or two medium-chain fatty acids attached to the glycerol backbone, and the remainder being long-chain fatty acids. High doses of medium-chain triglycerides (MCT) can easily induce gastrointestinal discomfort, and long-term use may also pose a risk of ketoacidosis or ketoacidosis; while long-chain triglycerides (LCT) have lower absorption efficiency. Compared with LCT or MCT, natural or synthetic medium- and long-chain triglycerides have unique composition, structure and metabolic characteristics, and are therefore closely related to a variety of beneficial physiological functions. Early studies have shown that the fatty acid composition of medium- and long-chain triglycerides is closer to that of breast milk, which can improve the digestion and absorption of fat, increase the utilization efficiency of fat-soluble nutrients, inhibit the accumulation of body fat, and provide energy quickly and stably (Yuan Tinglan, Wei Wei, Ye Xingwang, et al. Research progress on medium- and long-chain triglycerides in breast milk [J]. Journal of Food and Biotechnology, 2022, 41(6):10). Furthermore, even with the same total fatty acid composition, differences in the molecular structure of triglycerides can significantly affect their biological functions. For example, mouse experiments have shown that mice fed a diet containing medium- and long-chain triglyceride structure esters exhibit effects such as thermoregulation, inhibition of visceral fat accumulation, alteration of gut microbiota, and regulation of lipid metabolism compared to mice fed a diet containing a physically mixed vegetable oil formula with the same fatty acid composition (Yuan T, Cheng X, Shen L, Liu Z, Ye X, Yan Z, Wei W, Wang X. Novel Human Milk Fat Substitutes Based on Medium- and Long-Chain Triacylglycerol Regulate Thermogenesis, Lipid Metabolism, and Gut Microbiota Diversity in C57BL / 6J Mice. J Agric Food Chem. 2024 Mar 27;72(12):6213-6225). However, there are currently no reports on the correlation between medium- and long-chain triglycerides and allergies or eczema.
[0023] As is known in the art, medium- and long-chain fatty acid triglycerides are produced by using edible vegetable oils and MCTs as raw materials, through transesterification by lipases, followed by processes such as distillation, decolorization, and deodorization.
[0024] This application does not have any particular requirements regarding the medium- and long-chain triglycerides used; medium- and long-chain triglycerides commonly used in the art can be used. Medium- and long-chain triglycerides can be used in pure form or in a non-pure form rich in medium- and long-chain triglycerides. For example, the medium- and long-chain triglycerides used in the compositions of this application can be medium- and long-chain triglycerides with a single composition (i.e., each molecular chain has the same long-chain fatty acid residues and the same medium-chain fatty acid residues), or a mixture of multiple medium- and long-chain triglycerides with two or more different compositions (i.e., each molecular chain has different long-chain fatty acid residues and / or different medium-chain fatty acid residues).
[0025] In some embodiments, the medium- and long-chain fatty acid triglycerides used in this application may contain C6-C6. 12 (e.g., C6, C7, C8, C9, C) 10 C 11 C 12 (or the range defined by either or both) fatty acid residues and C 14 ~C 30 (e.g., C) 14 C 15 C 16 C 17 C 18 C 19 C 20 C 21 C 22 C 23 C 24 C 25 C 26 C 27 C 28 C 29 C 30 (or the range defined by either C6-C6) fatty acid residues. In some examples, C6-C6... 12 Fatty acid residues can originate from one or more of the following: hexanoic acid, heptanoic acid, octanoic acid, nonanoic acid, decanoic acid, undecanoic acid, and lauric acid, etc. C 14 ~C 30 Fatty acid residues can be derived from one or more of the following: myristic acid, palmitic acid, heptadecanic acid, oleic acid, linoleic acid, stearic acid, nonadecanic acid, eicosapentaenoic acid, docosahexaenoic acid, docosapatraenoic acid, docosahexaenoic acid, tricarboxylic acid, tetracarboxyenoic acid, docosapentaenoic acid, docosahexaenoic acid, arachidonic acid, etc. In some examples, C6~C... 12 The fatty acid residues may be derived from one or more of the following: hexanoic acid, caprylic acid, decanoic acid, and lauric acid. In some examples, C... 14 ~C 30Fatty acid residues may be derived from one or more of the following: myristic acid, palmitic acid, oleic acid, linoleic acid, stearic acid, linolenic acid, arachidonic acid, eicosapentaenoic acid, docosapentaenoic acid, and docosahexaenoic acid.
[0026] In some embodiments, the medium- and long-chain fatty acid triglycerides used in this application have C6~C6... 12 Fatty acid residues and C 14 ~C 30 The unit weight ratio of fatty acid residues can be from 0.124 to 2.000. For example, in the medium- and long-chain fatty acid triglycerides used in this application, C6~C 12 Fatty acid residues and C 14 ~C 30 The unit weight ratio of fatty acid residues may be 0.124, 0.125, 0.130, 0.140, 0.150, 0.160, 0.170, 0.180, 0.190, 0.200, 0.300, 0.400, 0.500, 0.600, 0.700, 0.800, 0.900, 1.000, 1.100, 1.200, 1.300, 1.400, 1.500, 1.600, 1.700, 1.800, 1.900, 2.000, or within the range defined by any two of these.
[0027] As used in this article, the term "nervonic acid" (NA) refers to a long-chain monounsaturated fatty acid (chemical name: cis-15-tetracosenoic acid, ω-9), named for its close association with the nervous system. Nervonic acid has neuroprotective, blood glucose regulating, anti-inflammatory, and cognitive function improving functions, and has shown therapeutic potential in the prevention and treatment of nervous system diseases, cancer, obesity, diabetes, and other diseases (Gao Yunqi, Zhang Yi, Zhou Mengzhou, et al. Research progress on biosynthesis, purification and nutritional application of nervonic acid [J]. Food Science, 2026, 47(05):13-25), but its role in allergies and eczema is not yet clearly understood.
[0028] To date, further research is needed to determine whether combining medium- and long-chain triglycerides with nervonic acid can synergistically improve the efficacy of allergies and / or eczema.
[0029] There are no particular restrictions on the source of nervonic acid used in this application, and it can generally be obtained through natural extraction and artificial preparation. For example, nervonic acid extracted from natural plants, such as nervonic acid extracted from plant seed oils, can be used. Plant sources that can be used to extract nervonic acid include, but are not limited to, garlic fruit, Acer truncatum, rapeseed, and hemp seeds. Alternatively, nervonic acid produced and extracted by certain oil-producing microalgae or other microorganisms can also be used. In addition, nervonic acid can also be prepared artificially (e.g., chemical synthesis or biosynthesis). For example, nervonic acid can be artificially synthesized from inexpensive raw materials such as erucic acid through reactions such as esterification and reduction. Preferably, the nervonic acid used in this application is nervonic acid extracted from plant sources.
[0030] In addition, nervonic acid can also be obtained through commercial channels, such as commercially available nervonic acid products from companies like Wuhan Pushida, Shaanxi Fuheng Biotechnology, and Shandong Yuanlitai.
[0031] In some embodiments, the mass ratio of medium- and long-chain fatty acid triglycerides to nervonic acid in the compositions of this application is from 3:1 to 1000:1. When medium- and long-chain fatty acid triglycerides and nervonic acid are used in combination in the above-mentioned mass ratio range, the compositions of this application show a significant synergistic effect in improving allergies and / or eczema, particularly in relieving itching and / or reducing trypsin-like enzyme levels. As an example, the mass ratio of medium- and long-chain fatty acid triglycerides to nervonic acid can be 3.0:1, 3.1:1, 3.2:1, 3.3:1, 3.4:1, 3.5:1, 3.6:1, 3.7:1, 3.8:1, 3.9:1, 4.0:1, 4.1:1, 4.2:1, 4.3:1, 4.4:1, 4.5:1, 4.63:1, 4.7:1, 4.8:1, 4.9:1, 5.0:1, 5.2:1, 5.5:1, 5.8:1, 6.0:1, 6.5:1, 7 0:1, 7.5:1, 8.0:1, 8.5:1, 9.0:1, 9.5:1, 10.0:1, 11:1, 12:1, 13:1, 14:1, 15:1, 16:1, 17:1, 18:1, 19:1, 20:1, 22:1, 24:1, 28:1, 32:1, 34:1, 35:1, 36:1, 38:1, 40:1, 42:1, 44:1, 45:1, 46:1, 48:1, 50:1, 52:1, 55.6:1, 58:1 60:1, 62:1, 65:1, 68:1, 70:1, 72:1, 75:1, 78:1, 80:1, 82:1, 85:1, 88:1, 90:1, 92:1, 95:1, 98:1, 100:1, 105:1, 111:1, 115:1, 120:1, 125:1, 130:1, 140:1, 150:1, 160:1, 167:1, 170:1, 180:1, 190:1, 200:1, 220:1, 240:1, 26 0:1, 280:1, 300:1, 320:1, 333:1, 360:1, 380:1, 400:1, 420:1, 450:1, 480:1, 500:1, 520:1, 560:1, 580:1, 600:1, 620:1, 640:1, 660:1, 667:1, 680:1, 700:1, 750:1, 800:1, 850:1, 900:1, 950:1 or 1000:1, or within the range defined by any two of the above.
[0032] Preferably, the mass ratio of medium- and long-chain fatty acid triglycerides to nervonic acid is 4.63:1 to 667:1. Alternatively, preferably, the mass ratio of medium- and long-chain fatty acid triglycerides to nervonic acid is 55.6:1 to 667:1. Alternatively, preferably, the mass ratio of medium- and long-chain fatty acid triglycerides to nervonic acid is 111:1 to 667:1. Alternatively, preferably, the mass ratio of medium- and long-chain fatty acid triglycerides to nervonic acid is 167:1 to 667:1. Alternatively, preferably, the mass ratio of medium- and long-chain fatty acid triglycerides to nervonic acid is 333:1 to 667:1. When medium- and long-chain fatty acid triglycerides and nervonic acid are used in combination within the above-mentioned mass ratio ranges, the synergistic effect of the composition of this application in improving allergies and / or eczema, particularly relieving itching and / or reducing trypsin levels, is more pronounced.
[0033] In some embodiments, the composition of this application may consist of medium- and long-chain fatty acid triglycerides and nervonic acid, for example, in any mass ratio or mass ratio range of the medium- and long-chain fatty acid triglycerides and nervonic acid described above.
[0034] In some embodiments, the product includes or is a pharmaceutical product.
[0035] In some embodiments, the product is a pharmaceutical product. This invention does not place particular requirements on the dosage form of the pharmaceutical product; commonly used pharmaceutical dosage forms in the art can be used. As examples, the pharmaceutical product of this invention can be a solid dosage form, such as powders, granules, tablets, capsules, drop pills, or pills; a semi-solid dosage form, such as ointments, creams, eye ointments, or gels; or a liquid dosage form, such as oral liquid preparations, such as syrups, mixtures, suspensions, or emulsions. Those skilled in the art will readily understand that, depending on the dosage form and application scenario, the pharmaceutical product may also include various pharmaceutically permissible excipients. Furthermore, the pharmaceutical product of this invention can be prepared using methods commonly employed in the art, which will not be elaborated upon here.
[0036] In some embodiments, the compositions described in this application may be added to a product as a beneficial ingredient.
[0037] In some embodiments, the content of medium- and long-chain fatty acid triglycerides may be from 0.1% to 30.0% based on the dry basis weight of the product. As an example, the content of medium- and long-chain fatty acid triglycerides may be 0.1%, 0.15%, 0.2%, 0.25%, 0.3%, 0.35%, 0.4%, 0.45%, 0.5%, 0.55%, 0.6%, 0.65%, 0.7%, 0.75%, 0.8%, 0.85%, 0.9%, 0.95%, 1.0%, 1.5%, 2.0%, 2.5%, 3.0%, 3.5%, 4.0%, 4.5%, 5.0%, 5.5%, 6.0%, 6.5%, 7.0%, 7.5%, 8.0%, 8.5%, 9.0%, 9.5%, 10.0%, 10.5%, 11.0%, 11.5%, or 12%. 0, 12.5, 13.0, 13.5, 14.0, 14.5, 15.0, 15.5, 16.0, 16.5, 17.0, 17.5, 18.0, 18.5, 19.0, 19.5, 20.0, 20.5, 21.0, 21.5, 22.0, 22.5, 23.0, 23.5, 24.0, 24.5, 25.0, 25.5, 26.0, 26.5, 27.0, 27.5, 28.0, 28.5, 29.0, 29.5, 30.0% (dry basis mass), or within the range defined by any two of the above. Furthermore, in a further embodiment, the nervonic acid content is calculated proportionally.
[0038] In other embodiments, the nervonic acid content may be from 0.1% to 30.0% based on the dry basis weight of the product. As an example, the nervonic acid content may be 0.1%, 0.15%, 0.2%, 0.25%, 0.3%, 0.35%, 0.4%, 0.45%, 0.5%, 0.55%, 0.6%, 0.65%, 0.7%, 0.75%, 0.8%, 0.85%, 0.9%, 0.95%, 1.0%, 1.5%, 2.0%, 2.5%, 3.0%, 3.5%, 4.0%, 4.5%, 5.0%, 5.5%, 6.0%, 6.5%, 7.0%, 7.5%, 8.0%, 8.5%, 9.0%, 9.5%, 10.0%, 10.5%, 11.0%, 11.5%, 12.0%, based on the weight of the product. 12.5, 13.0, 13.5, 14.0, 14.5, 15.0, 15.5, 16.0, 16.5, 17.0, 17.5, 18.0, 18.5, 19.0, 19.5, 20.0, 20.5, 21.0, 21.5, 22.0, 22.5, 23.0, 23.5, 24.0, 24.5, 25.0, 25.5, 26.0, 26.5, 27.0, 27.5, 28.0, 28.5, 29.0, 29.5, 30.0% by dry weight, or within the range defined by any two of the above.
[0039] In some embodiments, the non-therapeutic purpose refers to a non-medical therapeutic purpose (e.g., nutritional and / or health care purpose), such as for preparing a product for preventing allergies and / or eczema or for relieving one or more symptoms of allergies and / or eczema.
[0040] In some embodiments, the method for improving allergies and / or eczema includes preventing allergies and / or eczema, or relieving one or more symptoms of allergies and / or eczema. For example, preventing allergies and / or eczema includes, for instance, preventing the occurrence or development of allergies and / or eczema; and, for example, relieving one or more symptoms of allergies and / or eczema includes, for instance, relieving or reducing itching, and / or reducing trypsin levels.
[0041] In some embodiments, the improvement of allergies and / or eczema may include relieving itching and / or reducing trypsin levels.
[0042] In some implementations, there are no particular limitations on the subjects (recipients) who are improving allergies and / or eczema, and may include, for example, infants, toddlers, children, adolescents, adults, young adults, middle-aged people, and / or the elderly. As used herein, the term “infant” refers to a person aged from birth to 12 months; the term “toddler” refers to a person aged 1 to 3 years; the term “child” refers to a person aged 3 to 7 years; the term “adolescent” refers to a person aged 7 to 17 years; the term “adult” refers to a person aged 18 years or older; the term “young adult” refers to a person aged 18 to 40 years; the term “middle-aged person” refers to a person aged 41 to 65 years; and the term “elderly person” or “senior person” refers to a person aged 65 years or older.
[0043] As described above, when medium- and long-chain fatty acid triglycerides and nervonic acid are used in combination at a specific mass ratio (e.g., any mass ratio or range described above), the composition according to this application exhibits a synergistic effect in improving allergies and / or eczema, particularly in relieving itching and reducing trypsin-like enzyme levels.
[0044] In some embodiments, when the composition described in this application is used to improve allergies and / or eczema, particularly to relieve itching and reduce trypsin levels, the dosage may be such that the intake of medium- and long-chain triglycerides is 2.25 g to 30 g per day, for example, 2.25, 2.50, 2.75, 3.00, 3.25, 3.50, 3.75, 4.00, 4.25, 4.50, 4.75, 5.00, 5.25, 5.50, 5.75, 6.00, 6.25, 6.50, 6.75, 7.00, 7.25, 7.50, 7.75, 8.00, 8.25, 8.50, 8.75, 9.00, 9.25, 9.50, 9.75, 10.0, 10.5, 11.0, 11.5, 1 2.0, 12.5, 13.0, 13.5, 14.0, 14.5, 15.0, 15.5, 16.0, 16.5, 17.0, 17.5, 18.0, 18.5, 19.0, 19.5, 20.0, 20.5, 21.0, 21.5, 22.0, 22.5, 23.0, 23.5, 24.0, 24.5, 25.0, 25.5, 26.0, 26.5, 27.0, 27.5, 28.0, 28.5, 29.0, 29.5, 30.0 g, or within any two of the above ranges. Furthermore, in a further embodiment, the intake of nervonic acid is calculated proportionally.
[0045] Example
[0046] The present application will be more easily understood by referring to the following embodiments, which are only used to illustrate certain aspects and implementation methods of the present application and are not intended to limit the present application.
[0047] Unless otherwise stated, all materials used in this embodiment are commercially available or conventional materials.
[0048] Medium- and long-chain triglycerides (MLCT): Medium- and long-chain fatty acid edible oil purchased from Yihai Kerry Food Industries Co., Ltd. was used, in which the purity of MLCT was 61±10% (by mass) and the production batch number was 20250804. Nervonic acid (NA): Purchased from Fuheng Biotechnology, purity 94.91% (by weight), production batch number FH20240120; Loratadine: purchased from Peking University Medicine Co., Ltd., tablets, batch number 241203; 1-Chloro-2,4-Dinitrobenzene (DNCB): Purchased from Shanghai Aladdin Biochemical Technology Co., Ltd., batch number F2518064; Wild-type AB strain zebrafish: bred and provided by the fish breeding center of Hangzhou Huante Biotechnology Co., Ltd.
[0049] Example 1: Determination of the maximum tolerated concentration of a single sample
[0050] Wild-type AB strain zebrafish, 4 days post-fertilization (4 dpf), were randomly selected and enclosed in 6-well plates with a volume of 3 mL per well. Thirty zebrafish were treated in each well. Each group was tested in triplicate.
[0051] Water-soluble samples (concentrations shown in Table 1) were administered to establish single-sample groups (single-component MLCT and single-component), while a normal control group (naïve, no treatment) and a model control group (eczema model, no administration) were also set up. Except for the normal control group, each experimental group received water-soluble DNCB to establish a zebrafish eczema model. After treatment at 28℃ for 21 h, except for the normal control group, each experimental group received water-soluble high-concentration DNCB. After further treatment at 28℃ for 3 h, the maximum tolerated concentration (MTC) of the single sample against the model zebrafish was determined.
[0052] Table 1. Experimental results for the maximum detectable concentration (n = 30)
[0053] As shown in Table 1, the MTC of medium- and long-chain fatty acid triglycerides is 2000 μg / mL, and the MTC of nervonic acid is 125 μg / mL.
[0054] Example 2: Evaluation of the efficacy of the sample in improving eczema - behavioral (pruritus) efficacy
[0055] Wild-type AB strain zebrafish with 4 dpf were randomly selected and placed in 6-well plates with a volume of 3 mL per well. Thirty zebrafish were treated. Each group was set up in triplicate.
[0056] Water-soluble samples (concentrations shown in Table 2) were administered to establish experimental groups (formulas 1 to 7 (MLCT + NA)) and single-sample groups (single-component MLCT or single-component NA). Loratadine at a concentration of 187.5 ng / mL was administered as a positive control group. Simultaneously, a normal control group (naïve, no treatment) and a model control group (eczema model, no medication) were established. Except for the normal control group, each group received water-soluble DNCB to establish a zebrafish eczema model. After treatment at 28℃ for 21 h, except for the normal control group, each group received a high concentration of water-soluble DNCB. After further treatment at 28℃ for 3 h, 10 zebrafish from each experimental group were randomly selected and placed in a 96-well plate (1 zebrafish / well, 200 μL / well). Behavioral data for each group were collected over 20 min using a behavioral analyzer (Zebra Lab 3.22.3.31, Viewpoint, France). The total movement distance of the zebrafish was analyzed, and the statistical analysis results of this index were used to evaluate the efficacy of the samples in improving eczema. Statistical results are expressed as mean ± standard error (SE). Statistical analysis was performed using SPSS software. P < 0.05 indicates that the difference is statistically significant.
[0057] In Table 2, the parameters are as follows: Total movement distance = The total distance the zebrafish moves in 20 minutes, in millimeters (mm); The reduction in total movement distance compared to the model control group = the total movement distance of zebrafish in the model control group – the total movement distance of zebrafish in the single sample group or experimental group, in mm; Synergistic reduction = Total reduction in movement distance of the experimental group compared to the model control group – Sum of total reduction in movement distance of the individual sample group at the corresponding concentration compared to the model control group, in mm; Synergy coefficient = (Total reduction in movement distance of the experimental group compared to the model control group) / (Sum of total reductions in movement distance of the individual sample groups at the corresponding concentrations compared to the model control group); Unit dose synergy factor = synergy factor / sum of MLCT and NA doses.
[0058] The results are shown in Table 2 and Figure 1 As shown.
[0059] Following the above method, zebrafish were administered different doses of MLCT and NA to evaluate their effects on behavioral (pruritus) improvement. The dosages are shown in Table 2, and the experimental results are shown in Table 2 and... Figure 1 As shown.
[0060] Table 2. Results of the experiment evaluating the efficacy of the samples in improving eczema (behavioral (pruritus)).
[0061] From Table 2 and Figure 1 The results showed that, compared with the model control group, both the positive control drug (loratadine) and the single-component NA (18.0 μg / mL and 108 μg / mL) were effective in improving eczema. Specifically, compared with the model control group, the total movement distance (mm) of zebrafish decreased, while the single-component MLCT had no effect on improving eczema. Furthermore, compared with the model control group, the combination of MLCT and NA (formulas 1 to 7) also showed an effect on improving eczema. P <0.05), specifically reflected in the total movement distance of zebrafish, and there is a synergistic effect between the two. For example, compared with the model control group, the total movement distance (mm) of formulations 3, comparative examples 2 and 4 in Table 2 decreased by 540 mm, 185 mm and 198 mm respectively. The reduction in total movement distance in formulation 3 is greater than the sum of the reductions in comparative examples 2 and 4 (383 mm). Similarly, formulations 1 to 2 and 4 to 7 also show a synergistic effect, that is, MLCT and nervonic acid have a synergistic effect in improving the efficacy of eczema when the ratio is 4.63:1 to 667:1.
[0062] On the other hand, regarding the synergy coefficient, the synergy coefficient of Formula 3 is the ratio of the reduction in total movement distance (mm) of Formula 3 to the sum of the reductions in total movement distance (mm) of Comparative Examples 1 and 4, i.e., synergy coefficient 1.84 > 1, indicating a synergistic effect between MLCT and nervonic acid, which can synergistically reduce the total movement distance (mm). Similarly, Formulas 1 to 2 and 4 to 7 also show a synergistic effect between MLCT and nervonic acid, which can synergistically reduce the total movement distance (mm). That is, Formulas 1 to 7 with MLCT:nervonic acid mass ratios of 4.63:1 to 667:1 have a synergistic effect in improving eczema (synergy coefficients are all greater than 1).
[0063] On the other hand, the synergy coefficient, formula 3>formula 6>formula 7>formula 4>formula 2>formula 1=formula 5, preferably, in the direction of improving the efficacy of eczema, the preferred mass ratio of MLCT:nervonic acid is in the range of 333:1 to 667:1 (synergy coefficient greater than 1.4).
[0064] Example 3: Efficacy of Samples in Improving Eczema - Evaluation of Trypsin Activity Level
[0065] Wild-type AB strain zebrafish with 4 dpf were randomly selected and placed in 6-well plates with a volume of 3 mL per well. Thirty zebrafish were treated. Each group was set up in triplicate.
[0066] Water-soluble samples (concentrations shown in Table 2) were administered to establish experimental groups (formulas 1 to 7 (MLCT + NA)) and single-sample groups (single-component MLCT or single-component NA). Loratadine at a concentration of 187.5 ng / mL was administered as a positive control group. Simultaneously, a normal control group (naïve, no treatment) and a model control group (eczema model, no medication) were established. Except for the normal control group, each group received water-soluble DNCB to establish a zebrafish eczema model. After treatment at 28℃ for 21 h, except for the normal control group, each group received water-soluble high-concentration DNCB. After further treatment at 28℃ for 3 h, zebrafish samples from each experimental group were collected according to the trypsin-like protein kit (catalog number ml286418V, Shanghai Enzyme-Link Biotechnology Co., Ltd., China). Data were collected using a multi-functional microplate reader (SPARK, TECAN, Austria) and the trypsin content in each experimental group was analyzed. The statistical analysis results of this index were used to evaluate the efficacy of the samples in improving eczema (trypsin content). Statistical results are expressed as mean ± SE. Statistical analysis was performed using SPSS software. P < 0.05 indicates that the difference is statistically significant.
[0067] Following the method described above, zebrafish were administered different doses of MLCT and NA to evaluate their efficacy in improving trypsin-like protease activity levels. The dosages and results are shown in Table 3.
[0068] Table 3. Evaluation results of the samples' efficacy in improving eczema (trypsin activity level) (n = 10)
[0069] As shown in Table 3, compared with the model control group, the positive control group and the single-component NA (18.0 μg / mL and 108 μg / mL) both showed efficacy in improving eczema. Specifically, compared with the model control group, the zebrafish trypsin content (ng / mgprot) was reduced, while the single-component MLCT showed no efficacy in improving eczema. Furthermore, compared with the model control group, the combination of MLCT and NA (formulas 1 to 7) also showed efficacy in improving eczema. P<0.05), specifically reflected in the decrease in zebrafish trypsin content, and a synergistic effect between the two. For example, compared with the model control group, the trypsin content (ng / mgprot) of formulations 1, 1, and 4 in Table 3 decreased by 0.28 ng / mgprot, 0.06 ng / mgprot, and 0.07 ng / mgprot, respectively. The decrease in trypsin content in formulation 1 was greater than the sum of the decreases in 1 and 4 (0.13 ng / mgprot). Similarly, formulations 2 to 7 also showed a synergistic effect, that is, MLCT and nervonic acid have a synergistic effect in improving eczema when the ratio is 4.63:1 to 667:1.
[0070] On the other hand, regarding the synergistic coefficient, the synergistic coefficient of Formula 1 is the ratio of the reduction in trypsin content (ng / mgprot) in Formula 1 to the sum of the reductions in trypsin content (ng / mgprot) in Comparative Examples 1 and 4, i.e., synergistic coefficient 2.15 > 1, indicating a synergistic effect between MLCT and nervonic acid, which can synergistically reduce trypsin content (ng / mgprot). Similarly, for Formulas 2 to 7, the conclusion that there is a synergistic effect between MLCT and nervonic acid, which can synergistically reduce trypsin content (ng / mgprot) can also be drawn. That is, Formulas 1 to 7 with MLCT:nervonic acid mass ratios of 4.63:1 to 667:1 have a synergistic effect in improving eczema (synergistic coefficients are all greater than 1).
[0071] On the other hand, regarding the synergy coefficient, formula 3 > formula 6 > formula 1 > formula 7 > formula 4 > formula 2 > formula 5, preferably, in the direction of improving the efficacy of eczema, the preferred mass ratio of MLCT:nervonic acid is 55.6:1 to 667:1 (synergy coefficient greater than 1.4), further preferably 111:1 to 667:1 (synergy coefficient greater than 1.5), and most preferably 167:1 to 667:1 (synergy coefficient greater than 2).
[0072] Finally, it should be noted that the above embodiments are only used to illustrate the technical solutions of this application, and are not intended to limit them. Although this application has been described in detail with reference to the foregoing embodiments, those skilled in the art should understand that modifications can still be made to the technical solutions described in the foregoing embodiments, or equivalent substitutions can be made to some of the technical features. Such modifications or substitutions do not cause the essence of the corresponding technical solutions to deviate from the spirit and scope of the technical solutions of the embodiments of this application.
Claims
1. The use of the composition in the preparation of a product for improving eczema, characterized in that, The composition comprises medium- and long-chain fatty acid triglycerides and nervonic acid, and the mass ratio of the medium- and long-chain fatty acid triglycerides to the nervonic acid is from 3:1 to 1000:
1.
2. The use according to claim 1, characterized in that, The mass ratio of the medium- and long-chain fatty acid triglycerides to the nervonic acid is from 4.63:1 to 667:
1.
3. The use according to claim 1, characterized in that, The mass ratio of the medium- and long-chain fatty acid triglycerides to the nervonic acid is from 55.6:1 to 667:
1.
4. The use according to claim 1, characterized in that, The mass ratio of the medium- and long-chain fatty acid triglycerides to the nervonic acid is from 111:1 to 667:
1.
5. The use according to claim 1, characterized in that, The mass ratio of the medium- and long-chain fatty acid triglycerides to the nervonic acid is 167:1 to 667:
1.
6. The use according to claim 1, characterized in that, The mass ratio of the medium- and long-chain fatty acid triglycerides to the nervonic acid is 333:1 to 667:
1.
7. The use according to any one of claims 1 to 6, characterized in that, The eczema described is allergic eczema.
8. The use according to any one of claims 1 to 6, characterized in that, The improvement of eczema includes improving itching and / or reducing trypsin levels.
9. The use according to any one of claims 1 to 6, characterized in that, The composition is used in such a quantity that the intake of the medium- and long-chain fatty acid triglycerides is 2.25 g to 30.0 g per day.