Application of schefflera octophylla in preparation of medicine for treating skin itch

Abstract

The invention discloses application of schefflera octophylla in preparation of a medicine for treating skin itch, and belongs to the technical field of application and development of traditional Chinese medicinal materials. The invention finds that the schefflera octophylla and the extract thereof have the patent medicine potential for treating the skin itch for the first time, can be used for preparing the medicine for treating the skin itch, and opens up a new way for treating the skin itch. Embodiments prove that the Schefflera octophylla extract can reduce the scratching frequency of mice and improve the mouse skin itch behavior induced by a compound 48 / 80 (65mmol / L), and powerfully prove that the Schefflera octophylla extract disclosed by the invention has an obvious itch relieving effect on the itch mice.

Description

Technical Field

[0001] The invention relates to the technical field of application and development of Chinese medicinal materials, and more particularly to the application of Schefflera arborvitae in preparing a medicine for treating skin itching. Background Art

[0002] Pruritus refers to a common skin disease with only itching of the skin without primary skin damage. It can be caused by certain diseases, drugs, cold, wool allergies and other stimuli, and is a neurological dysfunction skin disease. Patients may experience local or systemic itching of the skin. Due to the itching, patients will scratch repeatedly, causing the skin to become red, rough, and raised. In severe cases, secondary injuries such as bleeding and lichenification occur, causing the patient to suffer unbearable pain. In recent years, the prevalence of itchy skin has shown a clear upward trend, seriously affecting people's daily life and physical and mental health.

[0003] At present, the pathogenesis of pruritus is still unclear, clinical treatment is difficult, and there is no specific method. The most commonly used drugs are H1 receptor blockers, such as chlorpheniramine maleate tablets, ebastine tablets, desloratadine citrate tablets, etc. However, the pruritus will be relieved after taking the medicine, and it will be aggravated after stopping the medicine. After taking the medicine, symptoms such as drowsiness, fatigue, and inattention will often appear. Antibiotics and hormones can cause dysbacteriosis, etc., and the side effects of immunosuppressants are relatively large.

[0004] Because Chinese medicine adopts the principle of dialectical treatment and has the characteristics of multi-link, multi-pathway and integrated regulation, Chinese medicine has a long history of treating skin itching. For example, Compound Sophora flavescens Decoction (30g each of Sophora flavescens and wild chrysanthemum, 20g of Cynanchum chinense, 15g each of Kochia scoparia, Cnidium monnieri, Stemona bulb, Saposhnikovia divaricata, Artemisia capillaris, and Polygonum multiflorum), Compound Cynanchum chinense Decoction (30g of Cynanchum chinense, 15g each of Sophora flavescens, Artemisia capillaris, Rubia cordifolia, Dictamni bark, Agastache rugosa, Lilium leucophylla, Rheum officinale, Coptis chinensis, and Cnidium monnieri), Compound Hibiscus bark Decoction (30g each of Hibiscus bark, Stemona bulb, Calamine, Psoralea corylifolia, and wild chrysanthemum, 15g each of Pittosporum tobira bark, Angelica dahurica, and Atractylodes macrocephala, 10g each of Beehive, Sichuan pepper, and Leonurus japonicus) and other decocted and used for whole-body washing have a significant improvement effect on local itching. However, the above-mentioned Chinese herbal decoctions are generally prescription drugs, and when used, doctors are generally required to select the ingredients of the drug composition according to the actual situation of the patient. Although there are also Chinese patent medicines, due to the fact that Chinese herbal compound has many flavors and ingredients, and the Chinese herbal ingredients work synergistically to exert therapeutic effects, direct pharmacodynamic evaluation of the Chinese herbal compound cannot clarify the effective ingredients and their mechanisms of action in the treatment of diseases. In addition, due to the complex preparation, it is inconvenient in actual use, which seriously limits its promotion and application worldwide.

[0005] It is of great significance to develop a new drug for treating skin pruritus. Schefflera octophylla (Lour.) Harms is the fresh branches and leaves of Schefflera octophylla (Lour.) Harms of the Araliaceae family. It is mainly used to treat influenza, traumatic injuries and the like. In the Flora of China, there are a few records of the medicinal use of Schefflera octophylla. According to literature reports, it mainly contains triterpenoid components, such as lupane-type, oleanane-type, ursane-type pentacyclic triterpenoids, and volatile oils. At present, there are no reports on the use of Schefflera octophylla in the treatment of skin pruritus. Therefore, it is necessary to conduct in-depth research on it, which is of great significance to provide ideas for the prevention and treatment of skin pruritus and the development of new drugs. Summary of the invention

[0006] In view of the above problems, the present invention provides an application of Schefflera arborvitae in preparing a medicine for treating skin itching.

[0007] In order to achieve the above object, the present invention adopts the following technical solution:

[0008] Application of Schefflera arborvitae in preparing medicine for treating skin itching.

[0009] Specifically, the Schefflera arborvitae extract is used in the preparation of a drug for treating skin itching, wherein the Schefflera arborvitae extract is a water extract or an organic solvent extract of fresh branches and leaves of Schefflera arborvitae.

[0010] Preferably, the Schefflera arborvitae aqueous extract is prepared by the following steps: (31) chopping fresh branches and leaves of Schefflera arborvitae, boiling them with distilled water, filtering, and collecting the filtrate; (32) boiling the filter residue after filtering in step (31) again with distilled water, filtering, and collecting the filtrate; (33) boiling the filter residue after filtering in step (32) again with distilled water, filtering, and collecting the filtrate; (34) combining the filtrates of steps (31), (32), and (33), concentrating, and collecting the concentrate to obtain the aqueous extract.

[0011] Preferably, the solid-to-liquid ratio of the raw material drug and distilled water in step (31) is 1 kg: 8-12 L.

[0012] Preferably, the solid-to-liquid ratio of the filter residue to distilled water in step (32) and step (33) is 1 kg:8-12 L.

[0013] Preferably, the boiling time in step (31), step (32) and step (33) is 30 to 60 minutes.

[0014] Preferably, the concentrated solution in step (34) is: the mass of the raw material drug corresponding to each 1 mL of the concentrated solution volume is 1.6 g.

[0015] Preferably, the Schefflera arborvitae organic solvent extract is prepared by the following steps: (61) chopping fresh branches and leaves of Schefflera arborvitae, adding 30-50% ethanol solution, heating and reflux, filtering, and collecting the filtrate; (62) adding 30-50% ethanol solution to the filter residue after filtering in step (61), heating and reflux, filtering, and collecting the filtrate; (63) adding 30-50% ethanol solution to the filter residue after filtering in step (62), heating and reflux, filtering, and collecting the filtrate; (64) combining the filtrates of step (61), step (62) and step (63), concentrating under reduced pressure, and collecting the concentrate to obtain the product.

[0016] Preferably, in step (61), the solid-to-liquid ratio of the raw material drug to the 30-50% ethanol solution is 1 kg:8-12 L.

[0017] Preferably, the solid-to-liquid ratio of the filter residue and the 30-50% ethanol solution in step (62) and step (63) is 1 kg:8-12 L.

[0018] Preferably, the heating reflux temperature in step (61), step (62) and step (63) is 80-85° C. and the time is 30-60 min.

[0019] Preferably, the concentrated solution in step (64) is: the mass of the raw material drug corresponding to each 1 mL of the concentrated solution is 1.6 g.

[0020] Another object of the present invention is to provide a medicine for treating skin itching, comprising the above-mentioned Schefflera arborvitae extract.

[0021] Preferably, the drug further comprises other pharmaceutically active ingredients and / or excipients.

[0022] Preferably, the auxiliary materials include any one or more of sodium lauryl sulfate, ethylparaben, and glycerol.

[0023] Preferably, the dosage form of the drug includes lotion, ointment, paste, patch, spray, and liniment.

[0024] It can be seen from the above technical scheme that the present invention provides a new application of Schefflera arborvitae - application in the preparation of drugs for treating skin itching. The present invention first discovered that Schefflera arborvitae and its extracts have the potential to be used as medicines for treating skin itching, and can be used to prepare drugs for treating skin itching, opening up a new way for the treatment of skin itching. The examples prove that the Schefflera arborvitae extract can reduce the number of scratching times in mice and improve the skin itching behavior of mice induced by compound 48 / 80 (65mmol / L), which strongly proves that the Schefflera arborvitae extract of the present invention has a significant antipruritic effect on itchy mice.

[0025] In addition, Schefflera arborvitae resources are abundant, the extraction and preparation methods are simple and easy, and the sources of Schefflera arborvitae are convenient and easy to obtain, so it can be used for large-scale preparation of Schefflera arborvitae medicinal materials and their extracts; it has low cost and little pollution, which is conducive to large-scale production under the conditions of energy conservation and emission reduction, and has good industrialization prospects. BRIEF DESCRIPTION OF THE DRAWINGS

[0026] Figure 1 : The itch frequency of mice in each group, * represents P<0.05 compared with the blank group, ** represents P<0.01 compared with the blank group;

[0027] Figure 2 : Morphological images of subcutaneous cells of mice in each group (×100 μm), purple: mast cells;

[0028] Figure 3 : Subcutaneous mast cell count results of mice in each group, * represents P < 0.05 compared with the blank group, ** represents P < 0.01 compared with the blank group. DETAILED DESCRIPTION

[0029] The technical solutions in the embodiments of the present invention are described clearly and completely below. Obviously, the described embodiments are only part of the embodiments of the present invention, not all of the embodiments. Based on the embodiments of the present invention, all other embodiments obtained by ordinary technicians in this field without creative work are within the scope of protection of the present invention.

[0030] The reagents involved in the embodiments of the present invention are all purchased from commercial channels, and the methods not mentioned are conventional experimental methods and will not be described in detail here.

[0031] Example 1 Preparation of Schefflera affine extract

[0032] Take 1kg of fresh Schefflera arborvitae branches and leaves, chop them into 0.5cm pieces, add 8L of distilled water, heat and boil them for 60min, filter them through 200 mesh, and collect the filtrate; add 8L of distilled water to the residue and heat and boil them for 60min, filter them, and collect the filtrate; add 8L of distilled water to the residue and heat and boil them for 45min, filter them, and collect the filtrate; combine the filtrates three times and concentrate them to 1.6g / mL (m 新鲜枝叶 / v 提取液 ) and you’ll get it.

[0033] Example 2 Preparation of Schefflera arboricola Extract

[0034] Take 1kg of fresh Schefflera arborvitae branches and leaves, chop them into 0.5cm pieces, add 10L of distilled water, heat and boil them for 45min, filter them through 200 mesh, and collect the filtrate; add 10L of distilled water to the residue, heat and boil them for 45min, filter them, and collect the filtrate; add 10L of distilled water to the residue, heat and boil them for 45min, filter them, and collect the filtrate; combine the filtrates three times and concentrate them to 1.6g / mL (m 新鲜枝叶 / v 提取液 ) and you’ll get it.

[0035] Example 3 Preparation of Schefflera arboricola Extract

[0036] Take 1kg of fresh Schefflera arborvitae branches and leaves, chop them into 0.5cm pieces, add 12L of distilled water, heat and boil for 30min, filter through 200 mesh, and collect the filtrate; add 12L of distilled water to the residue, heat and boil for 30min, filter, and collect the filtrate; add 12L of distilled water to the residue, heat and boil for 30min, filter, and collect the filtrate; combine the filtrates three times and concentrate to 1.6g / mL (m 新鲜枝叶 / v 提取液 ) and you’ll get it.

[0037] Example 4 Preparation of Schefflera arboricola Extract

[0038] Take 1kg of fresh Schefflera arborvitae branches and leaves, chop them into 0.5cm pieces, add 8L of 50% ethanol solution, heat to 80℃, reflux extract for 40min, filter through 200 mesh, and collect the filtrate; add 8L of 50% ethanol solution to the residue, heat to 80℃, reflux extract for 40min, filter, and collect the filtrate; add 8L of 50% ethanol solution to the residue, heat to 80℃, reflux extract for 40min, filter, and collect the filtrate; combine the filtrates for three times, concentrate under reduced pressure to recover ethanol, and continue to concentrate to 1.6g / mL (m 新鲜枝叶 / v 提取液 ) and you’ll get it.

[0039] Example 5 Preparation of Schefflera affine extract

[0040] Take 1kg of fresh Schefflera arborvitae branches and leaves, chop them into 0.5cm pieces, add 12L of 30% ethanol solution, heat to 85℃, reflux extract for 60min, filter through 200 mesh, and collect the filtrate; add 12L of 30% ethanol solution to the residue, continue to heat to 85℃, reflux extract for 60min, filter, and collect the filtrate; add 12L of 30% ethanol solution to the residue, continue to heat to 85℃, reflux extract for 60min, filter, and collect the filtrate; combine the filtrates for three times, concentrate under reduced pressure to recover ethanol, and continue to concentrate to 1.6g / mL (m 新鲜枝叶 / v 提取液 ) and you’ll get it.

[0041] Efficacy test

[0042] Experimental animals: ICR mice, male, 20 g, SPF grade, purchased from Changsha Tianqin Biotechnology Co., Ltd., production license number: SCXK (Xiang) 2022-0011).

[0043] Test samples: Schefflera arborvitae extracts prepared in Example 3 (denoted as EZC), Example 4 (denoted as EZC-30), and Example 5 (denoted as EZC-50).

[0044] Experimental method: 45 ICR mice were taken, and after 3 days of adaptive feeding, they were weighed and numbered, and randomly divided into groups, with 5 mice in each group, and divided into: blank group, dexamethasone acetate group (positive control group), high dose of Schefflera affine water extract (EZC-high group, 80 g medicinal material / kg mouse), low dose of Schefflera affine water extract (EZC-low group, 40 g medicinal material / kg mouse), high dose of 30% ethanol extract of Schefflera affine (EZC-30-high group, 80 g medicinal material / kg mouse), low dose of 30% ethanol extract of Schefflera affine (EZC-30-low group, 40 g medicinal material / kg mouse), high dose of 50% ethanol extract of Schefflera affine (EZC-50-high group, 80 g medicinal material / kg mouse), and low dose of 50% ethanol extract of Schefflera affine (EZC-50-low group, 40 g medicinal material / kg mouse). The high-dose group of extracts corresponds to the extract concentration of the embodiment, and the low-dose solution is diluted 1 times with pure water at the concentration of the high-dose solution.

[0045] The day before the experiment, hair was removed from the back of the mouse neck with clippers to an area of ​​about 2cm×2cm, and mice with undamaged skin were selected for the experiment. Each dose group applied 1ml of the corresponding lotion to the depilated area, and the positive control group applied 0.2g of dexamethasone acetate to each mouse. The drug was administered continuously for 5 days and 5 days. One hour after the last administration, 50μL of compound 48 / 80 (65mmol / L) was subcutaneously injected into the back of the neck of each group of mice, and the scratching reaction of the mice was immediately observed within 30 minutes. It was calculated as a single attack, that is, from the time the hind limbs were lifted to touch the injection site of the itch-inducing agent to the time the hind limbs were put back on the ground or in the mouth. The whole process was regarded as one scratch, and the number of scratches was counted and recorded. The results are shown in the figure. Figure 1 .

[0046] Depend on Figure 1 It can be seen that compared with the blank group, dexamethasone acetate can significantly reduce the number of scratching times of mice, the high and low dose groups of Schefflera affine water extract and the high and low dose groups of 50% alcohol extract can significantly reduce the number of scratching times of mice and improve the itchy behavior of mouse skin induced by compound 48 / 80 (65mmol / L) (p<0.05).

[0047] After the observation, the skin was taken, fixed in 4% formaldehyde, stained with toluidine blue, and the number of mast cells was counted. The results are shown in Figure 2-3 .

[0048] like Figure 2-3 As shown, dexamethasone acetate can significantly reduce the number of subcutaneous mast cells (purple). The low-dose group of Schefflera chinensis water extract (EZC-low group) and the low-dose group of 50% alcohol extract (EZC-50-low group) can significantly reduce the number of subcutaneous mast cells in mice (p<0.05), indicating that Schefflera chinensis water extract and alcohol extract have the effect of inhibiting the release of itch-related particles from mast cells.

[0049] The extracts provided in Examples 1 to 5 above can be further prepared into external preparations according to a pharmaceutically acceptable method. The external preparations can be ointments, pastes, patches, lotions, sprays, liniments, etc. Here, the external lotion is used as an example for description.

[0050] A medicine for treating skin itching is prepared according to the following method:

[0051] Weigh 1600g of fresh branches and leaves of Schefflera arborescens, crush them, add water equivalent to 12 times of its total weight for the first time, boil for 1.0h, and collect the filtrate; add water equivalent to 12 times of its total weight to the residue, boil for 1.0h, and collect the filtrate; add water equivalent to 12 times of its total weight to the residue, boil for 1.0h, and collect the filtrate. Combine the filtrates obtained from the three decoctions and concentrate to a relative density of 1.6g medicinal material / mL (70℃);

[0052] Add 6 g of sodium lauryl sulfate, 1 g of ethylparaben and 10 g of glycerol to the obtained concentrate, mix and stir thoroughly until dissolved, add purified water to a total volume of 1000 ml, and fill in portions to obtain the product.

[0053] The above-mentioned sodium lauryl sulfate, ethylparaben and glycerin can all be purchased on the market, and the added amounts meet the requirements of relevant standards.

[0054] The various embodiments in this specification are described in a progressive manner, and each embodiment focuses on the differences from other embodiments. The same or similar parts between the various embodiments can be referenced to each other.

[0055] The above description of the disclosed embodiments enables one skilled in the art to implement or use the present invention. Various modifications to these embodiments will be apparent to one skilled in the art, and the general principles defined herein may be implemented in other embodiments without departing from the spirit or scope of the present invention. Therefore, the present invention will not be limited to the embodiments shown herein, but rather to the widest scope consistent with the principles and novel features disclosed herein.

Claims

1. Application of Schefflera arborvitae in preparing medicine for treating skin itching.

2. Use of Schefflera arborvitae extract in the preparation of a drug for treating skin itching, characterized in that: The Schefflera arboricola extract is a water extract or an organic solvent extract of fresh branches and leaves of Schefflera arboricola.

3. The use according to claim 2, characterized in that: The Schefflera affine water extract is prepared by the following steps: (31) chopping fresh branches and leaves of Schefflera arboricola, adding distilled water, boiling, filtering, and collecting the filtrate; (32) boiling the filter residue after filtering in step (31) again with distilled water, filtering, and collecting the filtrate; (33) boiling the filter residue after filtering in step (32) again with distilled water, filtering, and collecting the filtrate; (34) The filtrates from step (31), step (32) and step (33) are combined, concentrated, and the concentrated solution is collected to obtain.

4. The use according to claim 3, characterized in that: The solid-liquid ratio of the raw material drug and distilled water in step (31) is 1kg:8-12L, and the solid-liquid ratio of the filter residue and distilled water in steps (32) and (33) is both 1kg:8-12L.

5. The use according to claim 3, characterized in that: The boiling time in step (31), step (32) and step (33) is 30 to 60 minutes; The concentrate in step (34) is as follows: the mass of the raw material drug corresponding to each 1 mL of the concentrate volume is 1.6 g.

6. The use according to claim 2, characterized in that: The Schefflera arborvitae organic solvent extract is prepared by the following steps: (61) Chopping fresh branches and leaves of Schefflera arboricola into small pieces, adding 30-50% ethanol solution, heating and refluxing, filtering, and collecting the filtrate; (62) adding 30-50% ethanol solution to the filter residue after filtering in step (61), heating and refluxing, filtering, and collecting the filtrate; (63) adding 30-50% ethanol solution to the filter residue after filtering in step (62), heating and refluxing, filtering, and collecting the filtrate; (64) The filtrates from step (61), step (62) and step (63) are combined, concentrated under reduced pressure, and the concentrate is collected to obtain.

7. The use according to claim 6, characterized in that: The solid-liquid ratio of the raw material drug and the 30-50% ethanol solution in step (61) is 1kg:8-12L, and the solid-liquid ratio of the filter residue and the 30-50% ethanol solution in steps (62) and (63) is both 1kg:8-12L.

8. The use according to claim 6, characterized in that: The heating reflux temperature in step (61), step (62) and step (63) is 80-85° C. and the time is 30-60 min. The concentrate in step (64) is as follows: the mass of the raw material drug corresponding to each 1 mL of the concentrate volume is 1.6 g.

9. A drug for treating skin itching, characterized in that: The medicine comprises the Schefflera arboricola extract as described in any one of claims 2-8.

10. A drug for treating skin itching according to claim 9, characterized in that: The dosage forms of the medicine include lotion, ointment, paste, patch, spray and liniment.

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