Application of oroxylum indicum general flavone in preparation of medicine for treating atopic dermatitis
By using total flavonoids from Oroxylum indicum to prepare a topical formulation, the problems of local adverse reactions and poor efficacy of existing drugs for treating atopic dermatitis have been solved, achieving a safe and effective treatment for dermatitis.
Patent Information
- Authority / Receiving Office
- CN · China
- Patent Type
- Applications(China)
- Current Assignee / Owner
- SOUTHERN MEDICAL UNIVERSITY
- Filing Date
- 2026-02-13
- Publication Date
- 2026-05-19
AI Technical Summary
Existing medications for treating atopic dermatitis suffer from problems such as local adverse reactions, poor efficacy, and high costs, necessitating the development of new topical treatments that are safer and more cost-effective.
Using total flavonoids from Oroxylum indicum as the active ingredient, topical preparations such as ointments, creams, and gels are formulated, containing pharmaceutical excipients such as gel matrix, transdermal penetration enhancers, pH adjusters, preservatives, and stabilizers, for the treatment of atopic dermatitis.
It significantly reduces skin inflammation, erythema, and edema, improves skin barrier function, reduces mast cell infiltration, has high safety, does not affect organ indices in mice, and provides a new treatment approach.
Smart Images
Figure CN122056935A_ABST
Abstract
Description
Technical Field
[0001] This invention belongs to the field of biomedical technology, and in particular relates to the application of total flavonoids from Oroxylum indicum in the preparation of drugs for treating atopic dermatitis. Background Technology
[0002] Atopic dermatitis (AD) is a common, chronic, relapsing, inflammatory skin disease characterized by intense itching, dry skin, and eczematous lesions. The prevalence of atopic dermatitis has been increasing significantly in recent years, particularly impacting the quality of life and mental health of children, and placing a long-term burden on patients' families. The pathogenesis of this disease is complex, involving the interaction of multiple factors, including skin barrier dysfunction, immune dysregulation, and skin microbiota imbalance.
[0003] Currently, the treatment of atopic dermatitis follows a stepwise approach, with topical therapy as the foundation, primarily using topical corticosteroids. While corticosteroids are first-line anti-inflammatory drugs, long-term use can cause local adverse reactions such as skin atrophy and pigmentation changes, and patient compliance is often reduced due to "steroid phobia." Topical calcineurin inhibitors such as tacrolimus and pimecrolimus are suitable for sensitive areas and long-term maintenance therapy, but initial irritation and potential safety concerns exist. Recently approved topical PDE4 inhibitors like criborone and JAK inhibitors such as ruxolitinib cream offer new treatment options, but their long-term efficacy, safety, and cost-effectiveness still require further clinical data validation. Systemic therapy includes immunosuppressants, biologics such as dupilumab, and JAK inhibitors, mainly used for moderate to severe cases. Despite the variety of existing therapies, clinical practice still faces challenges such as adverse drug reactions, poor response rates in 30-50% of patients, disease recurrence, and high treatment costs. Therefore, developing novel topical therapeutic drugs from natural products that have multiple mechanisms of action, higher safety, and better cost-effectiveness has significant clinical implications and application prospects. Summary of the Invention
[0004] To address the aforementioned technical problems, this invention provides the application of total flavonoids from *Oroxylum indicum* in the preparation of drugs for treating atopic dermatitis. Experimental results demonstrate that total flavonoids from *Oroxylum indicum* can significantly alleviate skin inflammation, erythema, and edema symptoms in atopic dermatitis model animals, effectively improving skin barrier function. Simultaneously, total flavonoids from *Oroxylum indicum* can reduce the number of mast cell infiltrations without affecting organ indices in mice, providing a new theoretical basis and technical approach for topical treatment of atopic dermatitis and the research of novel drugs.
[0005] To achieve the above objectives, the present invention provides the following solution: On the one hand, the present invention provides the application of total flavonoids from Oroxylum indicum in the preparation of medicaments for treating atopic dermatitis.
[0006] In the technical solution of the present invention, the total flavonoids of Oroxylum indicum are flavonoid compounds extracted from Oroxylum indicum, including baicalin, baicalin, oroxylum indicum glycoside A, oroxylum indicum glycoside B, salicornin, and salicornin-7-O-glucuronide, etc.
[0007] Preferably, the drug is a topical preparation.
[0008] Preferably, the topical preparation includes ointments, creams, gels, liniments, film-forming agents, and sprays.
[0009] Preferably, the topical preparation further includes medically acceptable pharmaceutical excipients.
[0010] In another aspect, the present invention provides a topical preparation for treating atopic dermatitis, comprising total flavonoids from Oroxylum indicum, adjuvants, and medically acceptable pharmaceutical excipients.
[0011] Preferably, the topical preparation comprises total flavonoids from Oroxylum indicum, a gel matrix, a transdermal penetration enhancer, a pH adjuster, a preservative, a stabilizer, and water.
[0012] Preferably, the gel matrix is selected from one or more of carbomer 940, carbomer 934, carbomer 980, hydroxypropyl methylcellulose, sodium carboxymethyl cellulose, sodium alginate, gelatin, agar and propylene glycol; Preferably, the transdermal penetration enhancer is selected from one or more of diethanol glycol, diethylene glycol monoethyl ether, lolocaramide, squalene, oleic acid, and isopropyl myristate. Preferably, the stabilizer is selected from one or more of disodium EDTA, ascorbic acid, benzophenone, and titanium dioxide.
[0013] In the technical solution of the present invention, there is no particular limitation on the type of pH adjuster, and specific examples include triethanolamine, ethylenediamine, laurylamine, ammonia, sodium bicarbonate, sodium hydroxide, potassium hydroxide, etc.; the above-listed examples can be used alone or in any combination.
[0014] In the technical solution of the present invention, there is no particular limitation on the type of preservative, but specific examples include phenoxyethanol, benzoic acid, butylated hydroxyanisole, etc.; the above-listed preservatives can be used alone or in any combination.
[0015] Preferably, the topical preparation comprises, by mass fraction, 0.1%~1% total flavonoids from Oroxylum indicum, 18%~22% gel matrix, 3%~6% transdermal penetration enhancer, 3%~6% pH adjuster, 0.5%~1% preservative, 0.5%~1% stabilizer, and the balance being water.
[0016] Preferably, the topical preparation comprises, by mass fraction, 0.1% to 1% total flavonoids from Oroxylum indicum, 20% gel matrix, 5% transdermal penetration enhancer, 5% pH adjuster, 1% preservative, 1% stabilizer, and the remainder being water.
[0017] Preferably, the atopic dermatitis is 1-chloro-2,4-dinitrobenzene (DNCB)-induced atopic dermatitis.
[0018] The present invention has the following technical effects: This invention, through animal experiments, demonstrates that total flavonoids from *Oroxylum indicum* can significantly improve skin inflammation, erythema, and edema symptoms in a mouse model of DNCB-induced atopic dermatitis, effectively improve skin barrier function, and significantly reduce mast cell infiltration without affecting organ indices. Therefore, total flavonoids from *Oroxylum indicum* exhibit good therapeutic activity against atopic dermatitis and possess a certain degree of safety. They can be used as active ingredients in the preparation of drugs for treating atopic dermatitis, providing a theoretical basis for the treatment of atopic dermatitis and offering technical insights for the research of novel drugs for atopic dermatitis. Attached Figure Description
[0019] Figure 1 Methods for designing DNCB-induced AD mouse model and drug intervention experiments.
[0020] Figure 2 The skin morphology of mice in each treatment group was measured on days 3, 5, 7, 9, 11, and 12 after modeling.
[0021] Figure 3 The changes in body weight of mice in each treatment group; compared with the model group, P <0.001.
[0022] Figure 4 The results of skin dryness / desquamation assessment for mice in each treatment group are shown. Compared with the blank control group, ### P <0.001; compared with the model group, P <0.001.
[0023] Figure 5 The results of skin bleeding / rashes assessment for mice in each treatment group are shown. Compared with the blank control group, ### P <0.001; compared with the model group, * P <0.05, P <0.001.
[0024] Figure 6 The results of skin ulceration / epidermal shedding assessment in mice of each treatment group are shown. Compared with the blank control group, ### P <0.001; compared with the model group, P <0.05, P <0.001.
[0025] Figure 7 The results of skin edema assessment for mice in each treatment group are shown. Compared with the blank control group, ### P <0.001; compared with the model group, P <0.001.
[0026] Figure 8 The organ index results for mice in each treatment group include heart, liver, lungs, and kidneys. Detailed Implementation
[0027] The following embodiments are merely some, not all, of the embodiments of the present invention. Therefore, the detailed descriptions of the embodiments provided below are not intended to limit the scope of the claimed invention, but merely to illustrate selected embodiments. All other embodiments obtained by those skilled in the art based on the embodiments of the present invention without inventive effort are within the scope of protection of the present invention.
[0028] In this invention, unless otherwise specified, all equipment and raw materials are commercially available or commonly used in the industry. The methods described in the following embodiments are conventional methods in the art, unless otherwise specified.
[0029] In the following embodiments: Total flavonoids from Oroxylum indicum were purchased from Chengdu Pusi Biotechnology Co., Ltd. (purity ≥50%). Dexamethasone cream was purchased from Guangdong CR Shunfeng Pharmaceutical Co., Ltd. (National Drug Approval Number H44024170).
[0030] The preparation method of the total flavonoids cream from *Oroxylum indicum* is as follows: Dissolve 1 mg of total flavonoids from Oroxylum indicum in 20 µL of DMSO, shake well, add 100 mg or 1 g of cream base and mix thoroughly to obtain an Oroxylum indicum total flavonoids cream with a mass fraction of approximately 0.1% or 1%.
[0031] The cream base formulation consists of: 20% sodium carboxymethyl cellulose (gel base), 5% diethylene glycol monoethyl ether (transdermal penetration enhancer), 5% triethanolamine (pH adjuster), 1% phenoxyethanol (preservative), 1% disodium EDTA (stabilizer), and the remainder is distilled water.
[0032] Example 1 This example investigated how total flavonoids from *Oroxylum indicum* alleviated the clinical manifestations and pathological changes of DNCB-induced atopic dermatitis. The details are as follows: 1. Establish an animal model of atopic dermatitis (AD). Eight-week-old female Balb / c mice (purchased from Guangdong Provincial Animal Experiment Center) were randomly divided into four groups: Control group, Model group, Model + 0.1% total flavonoids from Oroxylum indicum group, Model + 1% total flavonoids from Oroxylum indicum group, and Model + dexamethasone group. The mice were housed in a pathogen-free environment with a 12-hour light-dark cycle and unrestricted access to food and water.
[0033] For experimental design methods of DNCB-induced AD mice and drug intervention, please refer to [link to relevant documentation]. Figure 1 The specific procedures are as follows: Hair removal was performed on the backs of mice one day in advance. Mice in the Model group and the treatment group were sensitized to the back skin with 100 μL of 2% DNCB solution on Day 1 and Day 2. On Days 5, 7, and 9, the back skin was sensitized again with 100 μL of 1% DNCB solution. From Day 1 to Day 12, mice in the treatment group were treated daily with an ointment containing total flavonoids from *Oroxylum indicum* or dexamethasone ointment. Mice were sacrificed on Day 12. After sacrifice, blood was collected from the eyes, and the back skin and organs were collected for subsequent experiments.
[0034] 2. Observation indicators: The weight of mice was recorded daily, and the severity of the inflammation in each treatment group was assessed by evaluating the thickness of the skin on the back and the atopic dermatitis score. To determine the severity of dermatitis, the severity of the skin inflammation on the back of the mice was scored according to the atopic dermatitis scoring criteria, which included four parts: edema / exudation, scarring / dryness, erythema / hemoptysis, and desquamation / erosion. The scores represented the severity as follows: 0 (none); 1 (mild <20%); 2 (moderate 20%-60%); 3 (severe >60%).
[0035] 3. Organ Index Analysis On Day 12, mice were euthanized by cervical dislocation. The hearts, livers, lungs, and kidneys of mice in each treatment group were harvested and weighed. The organ index was calculated using the following formula: Organ Index = (Organ weight / Animal body weight) × 100%.
[0036] Figure 2The skin morphology of mice in each treatment group was shown on days 3, 5, 7, 9, 11, and 12 after modeling. The figures show that DNCB significantly induced atopic dermatitis symptoms in mice; while 0.1% and 1% concentrations of total flavonoids from *Oroxylum indicum* and the positive control drug dexamethasone effectively alleviated dermatitis symptoms and improved skin damage. Furthermore, the therapeutic effect of total flavonoids from *Oroxylum indicum* was superior to that of the positive control drug dexamethasone.
[0037] Figure 3 The figure shows the changes in body weight of mice in each treatment group. It can be seen from the figure that 0.1% and 1% concentrations of total flavonoids from *Oroxylum indicum* did not significantly affect mouse body weight, while dexamethasone significantly reduced mouse body weight. This result suggests that total flavonoids from *Oroxylum indicum* may be safer than the positive control drug dexamethasone.
[0038] Figure 4 The results of the assessment of dry / scaly skin in mice in each treatment group are shown in the figure. It can be seen from the figure that DNCB can significantly induce dry and scaly skin symptoms in mice; while 0.1% and 1% concentrations of total flavonoids from Oroxylum indicum can effectively alleviate the above symptoms; the positive control drug dexamethasone has no significant effect on improving dry and scaly skin symptoms in mice.
[0039] Figure 5 The results of the assessment of bleeding / rashes on the skin of mice in each treatment group are shown in the figure. It can be seen from the figure that DNCB can significantly induce bleeding and rashes on the skin of mice; while 0.1% and 1% concentrations of total flavonoids from Oroxylum indicum and the positive control drug dexamethasone can effectively alleviate the above symptoms; and the improvement effect of total flavonoids from Oroxylum indicum is better than that of the positive control drug dexamethasone.
[0040] Figure 6 The results of the evaluation of skin ulceration / epidermal shedding in mice in each treatment group are shown in the figure. It can be seen from the figure that DNCB can significantly induce skin ulceration and epidermal shedding symptoms in mice; while 0.1% and 1% concentrations of total flavonoids from Oroxylum indicum and the positive control drug dexamethasone can effectively alleviate the above symptoms; and the improvement effect of total flavonoids from Oroxylum indicum is better than that of the positive control drug dexamethasone.
[0041] Figure 7 The results of edema assessment of the skin of mice in each treatment group are shown in the figure. It can be seen from the figure that DNCB can significantly induce edema symptoms in the skin of mice; while 0.1% and 1% concentrations of total flavonoids from Oroxylum indicum and the positive control drug dexamethasone can effectively alleviate the above symptoms; and the improvement effect of total flavonoids from Oroxylum indicum is better than that of the positive control drug dexamethasone.
[0042] Figure 8The organ index results for mice in each treatment group are shown in the figure. It can be seen from the figure that the 0.1% and 1% concentrations of total flavonoids from Oroxylum indicum and the positive control drug dexamethasone did not have a significant effect on the heart, liver, lungs and kidneys of mice with atopic dermatitis, further suggesting that total flavonoids from Oroxylum indicum have high safety.
[0043] The above description is only a preferred embodiment of the present invention. It should be noted that for those skilled in the art, several improvements and modifications can be made without departing from the principle of the present invention, and these improvements and modifications should also be considered within the scope of protection of the present invention.
Claims
1. Application of total flavonoids from Oroxylum indicum in the preparation of drugs for treating atopic dermatitis.
2. The application according to claim 1, characterized in that, The total flavonoids from *Oroxylum indicum* are flavonoid compounds extracted from *Oroxylum indicum*, including baicalin, baicalin, oroxylum indicum A, oroxylum indicum B, salicornin, and salicornin-7-O-glucuronide.
3. The application according to claim 1, characterized in that, The drug is a topical preparation; Preferably, the topical preparation includes ointments, creams, gels, liniments, film-forming agents, and sprays. Preferably, the topical preparation further includes medically acceptable pharmaceutical excipients.
4. A topical preparation for treating atopic dermatitis, characterized in that, Including total flavonoids from Oroxylum indicum, auxiliaries, and medically acceptable pharmaceutical excipients.
5. The topical preparation according to claim 4, characterized in that, The topical preparation comprises total flavonoids from Oroxylum indicum, a gel matrix, a transdermal penetration enhancer, a pH adjuster, a preservative, a stabilizer, and water.
6. The topical preparation according to claim 5, characterized in that, The gel matrix is selected from one or more of carbomer 940, carbomer 934, carbomer 980, hydroxypropyl methylcellulose, sodium carboxymethyl cellulose, sodium alginate, gelatin, agar and propylene glycol.
7. The topical preparation according to claim 5, characterized in that, The transdermal penetration enhancer is selected from one or more of diethanol glycol, diethylene glycol monoethyl ether, lolocaramide, squalene, oleic acid, and isopropyl myristate.
8. The topical preparation according to claim 5, characterized in that, The stabilizer is selected from one or more of disodium EDTA, ascorbic acid, benzophenone, and titanium dioxide.
9. The topical preparation according to claim 4, characterized in that, The topical preparation, by mass fraction, comprises 0.1%–1% total flavonoids from Oroxylum indicum, 18%–22% gel matrix, 3%–6% transdermal penetration enhancer, 3%–6% pH adjuster, 0.5%–1% preservative, 0.5%–1% stabilizer, and the balance being water; Preferably, the topical preparation comprises, by mass fraction, 0.1% to 1% total flavonoids from Oroxylum indicum, 20% gel matrix, 5% transdermal penetration enhancer, 5% pH adjuster, 1% preservative, 1% stabilizer, and the remainder being water.
10. The application according to claim 1 or the topical preparation according to claim 4, characterized in that, The atopic dermatitis mentioned is 1-chloro-2,4-dinitrobenzene (DNCB)-induced atopic dermatitis.