Use of stearyl nitrile in the preparation of a medicament for the treatment of eczema

Abstract

The application belongs to the technical field of medicines, and provides application of stearyl cyanide in preparation of medicines for treating eczema, wherein the mass concentration of the stearyl cyanide is 1.29%-11.58%. The application shows that the stearyl cyanide can be used for treating eczema and has no obvious side effects.

Description

Technical Field

[0001] This invention belongs to the field of pharmaceutical technology, and in particular relates to the use of stearonitrile in the preparation of drugs for treating eczema. Background Technology

[0002] Eczema is a common inflammatory skin disease affecting the epidermis and superficial dermis, caused by a variety of internal and external factors. It is characterized by intense itching, polymorphic skin lesions, symmetrical distribution, a tendency to ooze, a chronic course, and a high recurrence rate. Traditional Chinese medicine literature describes eczema as "infiltrating sores," "ear sores," "hydrangea wind," "four-bend wind," and "milk rash," which are similar to Western medical terms such as acute eczema, periauricular eczema, scrotal eczema, atopic dermatitis, and infantile eczema. In recent years, the incidence of eczema has been on the rise.

[0003] Eczema is caused by the interaction of multiple factors. Some types of eczema are closely related to genetics. Many studies have confirmed that environmental factors are one of the important reasons for the increased prevalence of eczema. The environment includes both the group environment and the individual environment. Group environmental pathogenic factors refer to large-scale outdoor air, water, soil, radiation sources, large areas of allergenic pollen vegetation, and large areas of airborne allergenic bacteria. The individual microenvironment refers to the individual's living environment. Since people spend about two-thirds of their time indoors, the individual microenvironment has a more significant impact on eczema. Some types of eczema are related to microbial infections. These microorganisms include Staphylococcus aureus, Malassezia, and airborne fungi such as Alternaria, Cladosporium, Penicillium, Aspergillus fumigatus, Fusarium, Penicillium chrysogenum, Aspergillus niger, and Rhizopus nigricans. In addition, human food is extremely diverse, generally divided into plant, animal, and mineral categories. Modern foods also frequently use chemically synthesized ingredients such as saccharin, acetic acid, citric acid, flavorings, and synthetic dyes. These foods can trigger allergic reactions, leading to eczema. Drug-related factors are also a major cause of some types of eczema, especially drug eruptions. Eczema can also be caused by neuropsychiatric factors such as distress, fatigue, anxiety, tension, emotional excitement, and insomnia, as well as climatic and physical factors such as sunlight, ultraviolet radiation, cold, humidity, dryness, and friction. Furthermore, chronic gastrointestinal diseases, chronic alcoholism, intestinal parasites, metabolic disorders, and endocrine imbalances are all causes of eczema.

[0004] Currently, there are various medications available for treating eczema, such as 999 Piyanping, a compound preparation containing hormones and antifungal components. It has anti-inflammatory, anti-allergic, and antipruritic effects and can be used to treat various types of eczema, including hand eczema, scrotal eczema, and chronic eczema. It can reduce inflammation, relieve itching, and promote the resolution of rashes. However, 999 Piyanping is a corticosteroid, and frequent use may cause side effects such as skin atrophy, telangiectasia, or secondary skin infections in the affected area. Summary of the Invention

[0005] To address the aforementioned issues, this invention proposes the application of stearonitrile in the preparation of drugs for treating eczema, demonstrating that stearonitrile can be used to treat eczema without significant side effects.

[0006] To achieve the above objectives, the technical solution adopted by the present invention is as follows: The use of stearonitrile in the preparation of drugs for treating eczema.

[0007] Furthermore, the mass concentration of the stearonitrile is 1.29%-11.58%.

[0008] Compared with the prior art, the present invention has the following beneficial effects: This invention demonstrates that the stearonitrile component has no obvious side effects and is highly safe; it can effectively relieve thickened skin, acute and chronic scratching, and chronic scratching in the ears of mice; it can also improve skin lesion symptoms and, to some extent, improve inflammatory hyperplasia. Attached Figure Description

[0009] Figure 1 A trend graph was created to compare the weight of mice after continuous topical administration of stearonitrile for 6 days and daily recording. Figure 2 A trend graph comparing the thickness of mouse ear skin recorded daily for 6 consecutive days of topical application of stearonitrile. Figure 3 The trend chart shows the number of ear scratches recorded 30 minutes immediately after the last challenge and administration of the drug (stearonitrile). Figure 4 The trend chart shows the number of ear scratches recorded 30 minutes after the last challenge and drug administration (stearonitrile). Figure 5 The images show the comparison of mouse ears taken after the final challenge and administration of the drug (stearonitrile); Figure 6 The image shows a comparison of histopathological changes observed after mice were sacrificed following the final challenge and administration of stearonitrile, ear tissue was fixed, embedded, sectioned, and stained with hematoxylin and eosin (HE). Detailed Implementation

[0010] The technical solutions of the embodiments of the present invention will be clearly and completely described below with reference to the accompanying drawings. Obviously, the described embodiments are only some embodiments of the present invention, and not all embodiments. Based on the embodiments of the present invention, all other embodiments obtained by those of ordinary skill in the art without creative effort are within the scope of protection of the present invention.

[0011] I. Experimental Objective A mouse model of eczema induced by DNCB was established, and the effect of stearonitrile on improving eczema symptoms was evaluated.

[0012] II. Instruments and Reagents 1. Instruments: analytical balance, weighing paper, pipette.

[0013] 2. Reagents: 999 Piyanping (Dex-dexamethasone), stearonitrile.

[0014] 3. Animals: Female C57BL / 6 mice, 6-8 weeks old, were purchased from the SPF-grade Laboratory Animal Center of Xi'an Jiaotong University. They were routinely housed in separate cages in a pathogen-free environment, maintaining a room temperature of 20-25℃, relative humidity of 40%, 10-14 hours of lighting daily, and ensuring adequate nutritional food and fresh drinking water. All experimental protocols were approved by the Animal Experiment Ethics Committee of the School of Medicine, Xi'an Jiaotong University, China.

[0015] III. Experimental Procedure 1. Establishment of a mouse model of eczema Sample preparation: Weigh an appropriate amount of DNCB powder using a precision balance, dissolve it in acetone, and prepare solutions with mass fractions of 0.5% DNCB, 1% DNCB, and 2% DNCB. Store the solutions at -20°C for later use.

[0016] Medium concentration for human use (stearic acid mass fraction of 3.86%). The low concentration is 1 / 3 of the medium concentration (stearic acid mass fraction is 1.29%). The high concentration is three times that of the medium concentration (stearic acid mass fraction is 11.58%).

[0017] The above liquid reference standard was accurately measured using a pipette and added to the oil matrix to prepare the test sample of the corresponding concentration for later use.

[0018] Model induction: Mice were randomly divided into blank control group (NC), model control group (Vehicle), positive drug group (999 Piyanping / Dex), low concentration stearonitrile group (stearonitrile 1.29%), medium concentration stearonitrile group (stearonitrile 3.86%), and high concentration stearonitrile group (stearonitrile 11.58%).

[0019] To establish an AD mouse model, DNCB solution was applied topically: Five days prior to sensitization, the mice's abdomens were shaved, and 2% DNCB (50 μL acetone) was applied topically to the abdominal skin once daily for three consecutive days. On day 8, 1% DNCB (25 μL acetone) was applied topically to the mice's ears (for behavioral testing) once daily for three consecutive days. Acetone was used alone to sensitize and stimulate the mice, serving as a control. All drug interventions began on the day of the first stimulation, applied once daily for six consecutive days.

[0020] 2. Pharmacodynamic studies ① Record the daily weight of the mice; ② Measure the ear thickness of the mice with digital calipers before and after each stimulation to evaluate the ear swelling of the mice; ③ Record the scratching of the ears for 30 minutes and count the number of scratches; ④ Take photos and compare the effects of topical administration on ear lesions in mice; ⑤ After taking photos, the mouse ear was taken, fixed, sectioned, and stained with hematoxylin and eosin (HE) to observe the pathological changes of tissue inflammation.

[0021] IV. Experimental Results and Discussion ① Apply the medication continuously for 6 days and record the mouse's weight daily. The results are as follows: Figure 1 As shown.

[0022] Depend on Figure 1 It was found that modeling did not cause a decrease in mouse body weight, and administration of the stearonitrile component did not cause a significant change in mouse body weight. The body weight of mice in the 999 Piyanping group began to decrease from day 5. These results confirm that the stearonitrile component did not cause a significant decrease in body weight and has a high safety profile.

[0023] ② Apply the medication continuously for 6 days and record the skin thickness of the mouse ears daily. The results are as follows: Figure 2 As shown.

[0024] Depend on Figure 2 It can be seen that from the 3rd day after stimulation and administration, the skin thickness of the model group mice showed significant differences, and 999 Piyanping significantly inhibited the thickening caused by modeling; on the 6th day after administration, administration of the stearonitrile component showed significant improvement in ear skin thickness.

[0025] ③-1 Immediately after the last challenge and drug administration, record the number of times the mouse scratches its ear 30 minutes later. The results are as follows: Figure 3 As shown.

[0026] Depend on Figure 3 It was found that the model caused obvious scratching in mice; the stearonitrile component showed a certain inhibitory effect, but no dose-dependent effect was observed.

[0027] ③-2 Eight hours after the last challenge and drug administration, the number of times mice scratched their ears for 30 minutes was recorded. The results are as follows: Figure 4 As shown.

[0028] Depend on Figure 4 It can be seen that modeling caused obvious scratching in mice; administration of the stearonitrile component had an ameliorative effect on chronic scratching.

[0029] ④ After the final challenge and drug administration, photographs were taken of the mice's ears for comparison. The results are as follows: Figure 5 As shown.

[0030] Depend on Figure 5 It was found that the model caused significant wrinkling and desquamation of the mouse ears; administration of the stearonitrile component partially improved the skin lesion symptoms.

[0031] ⑤ After the final challenge and drug administration, the mice were sacrificed, ear tissue was collected, fixed and embedded, sectioned, and stained with hematoxylin and eosin (HE) to observe histopathological changes. The results are as follows: Figure 6 As shown.

[0032] Depend on Figure 6 It was found that the skin of the ears of the model group mice was significantly thickened, accompanied by severe edema and inflammatory infiltration. The stearonitrile component could improve the inflammatory proliferation to some extent.

[0033] Conclusion: Based on the above pharmacodynamic test results of DNCB-induced eczema in mice, stearonitrile applied topically for 6 consecutive days did not cause significant changes in mouse weight, indicating high safety; and it could effectively relieve thickened skin on the ears and acute and chronic scratching in mice.

[0034] Although the present invention has been described in detail with reference to the foregoing embodiments, those skilled in the art can still modify the technical solutions described in the foregoing embodiments or make equivalent substitutions for some of the technical features. Any modifications, equivalent substitutions, improvements, etc., made within the spirit and principles of the present invention should be included within the protection scope of the present invention.

Claims

1. Use of stearyl nitrile in the manufacture of a medicament for the treatment of eczema.

2. Use of stearyl cyanide for the manufacture of a medicament for the treatment of eczema according to claim 1, characterized in that, The mass concentration of the stearyl nitrile is 1.29%-11.58%.

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