TW201509414A - Use of flavonoids in manufacturing compositions for wound healing - Google Patents

Abstract

The present invention provides a use of a flavonoid in manufacturing a composition for wound healing, preferably a non-glycosylated flavone. Particularly, the present invention is directed to the use in treating skin disorders such as trauma, burns, chronic wounds, especially a wound healing in diabetic patient.

Description

Use of flavonoid compounds for the preparation of wound healing compositions

The present invention relates to a novel use of a compound for the preparation of a wound healing composition, and in particular, to a novel use of a flavonoid compound for the preparation of a wound healing composition.

Flavonoids are broadly defined as a series of compounds having two phenolic hydroxyl-containing benzene rings interconnected by a central three carbon atom, having the structure of Formula I:

Usually found in fruits, vegetables, tea, wine, seeds or plant roots. Although not a vitamin, it has been shown to have antioxidant and anti-inflammatory effects; it has also been shown to resist or slow the formation of tumors, relieve pain, slow down cardiovascular disease or dementia.

Flavonoid compounds include flavones and flavonols. Flavonoids also include sugar Flavonoids and non-glycosylated flavonoids.

U.S. Patent No. 6,471,973 B2, issued Oct. 29, 2002, discloses the disclosure of flavonoid compounds in cosmetics, but does not mention other effects. U.S. Patent No. 6,451,837 B1, issued Nov. 17, the disclosure of which is incorporated herein by reference.

It is an object of the present invention to provide novel uses of flavonoids for the preparation of wound healing compositions.

In one aspect, the invention provides the use of a compound for the preparation of a wound healing composition, wherein the compound is a compound having the structure of the following formula I or an isomer thereof: Wherein A is a hydrogen atom, R or -OH; and n1 and n2 are the same or different and are one of integers from 0 to 4, wherein the sum of n1 and n2 is at most 4; n3 and n4 are the same or different and are 0 to 5 One of the integers, wherein the sum of n3 and n4 is at most 5; wherein R, R ₁ , R ₂ , R ₃ or R ₄ is defined as a hydrogen atom, an alkyl group having 1 to 30 carbon atoms, and contains 1-30 A mercapto group of an alkyl group of one carbon atom, a hydrocarbon chain having 1 to 30 carbon atoms; or a pharmaceutically acceptable ester or salt thereof.

According to the invention, the wound healing composition is for use in wound healing Skin symptoms of trauma, burns and chronic wounds, especially wound healing in diabetic patients.

According to an embodiment of the invention, wherein the compound is a flavone, especially a non-glycosylated flavone.

According to a preferred embodiment of the present invention, the non-glycosylated flavonoid compound is cirsimaritin having the following structure:

The above and other aspects of the present invention will be apparent from the following description of the preferred embodiments of the invention. Spirit and scope.

Unless defined otherwise, all technical and scientific terms used herein have the same meaning as the ones of ordinary skill in the art.

The singular forms "a", "an", "the" and "the" are used in the plural. Therefore, for example, when referring to "a component", it includes a plurality of such components and those having ordinary knowledge in the field. Know the equivalent.

The invention provides the use of a compound for the preparation of a wound healing composition, wherein the compound is a compound having the structure of the following formula I or an isomer thereof:

Wherein A is a hydrogen atom, R or -OH; and n1 and n2 are the same or different and are one of integers from 0 to 4, wherein the sum of n1 and n2 is at most 4; n3 and n4 are the same or different and are 0 to 5 One of the integers, wherein the sum of n3 and n4 is at most 5; wherein R, R ₁ , R ₂ , R ₃ or R ₄ is defined as a hydrogen atom, an alkyl group having 1 to 30 carbon atoms, and contains 1-30 a thiol group of an alkyl group of one carbon atom, a hydrocarbon chain having 1 to 30 carbon atoms; or a pharmaceutically acceptable ester or salt thereof.

According to the invention, the compound is a flavone, especially a non-glycosylated flavone. The non-glycosylated flavonoid compound is cirsimaritin having the following structure:

According to the invention, the composition comprises a pharmaceutically acceptable carrier.

According to the invention, the composition comprises a suitable excipient to form a composition in the form of a topical pharmaceutical, cosmetic or pharmaceutical material.

According to the invention, wherein the composition further comprises a therapeutic agent, such as other anti-inflammatory agents, antibacterial agents or other therapeutic agents.

The term "skin symptoms" as used herein includes wounds or sores, including skin injuries such as skin cuts, lacerations, stab wounds, and abrasions. According to the present invention, the compounds exhibit healing effects on skin symptom wounds of trauma, burns and chronic wounds, especially for wounds in diabetic patients, such as chronic wounds in diabetic patients.

The term "treatment" as used herein, including "treatment" or "promotion", means to ameliorate symptoms.

The term "patient" as used herein includes humans, and animals, particularly mammals.

As used herein, the term "pharmaceutically acceptable carrier" refers to diluents, excipients, and the like, which are commonly used in the art of pharmaceutics for the preparation of pharmaceutical compositions. According to the invention, it can be formulated into a form of a pharmaceutical, cosmetic or medical material. According to the invention, it may be in the form of a topical application, for example in the form of a spray. The spray form comprises a spray and a liquid; or a semi-solid or solid form, preferably a solid form having a dynamic viscosity greater than that of water. Appropriate formula Including, but not limited to, suspensions, emulsions, creams, ointments, liniments, and the like. Preferably, it is in the form of an ointment. The pharmaceutical compositions of the present invention may also contain emollients, perfumes or pigments in any form to enhance their acceptability for a variety of uses.

As used herein, the term "therapeutically effective amount" means a dose effective to treat a wound in the treatment of symptoms. According to the needs of the patient or the wound, the appropriate dosage can be used according to the technical or clinical knowledge commonly used in general medicine, and can be adjusted according to the manner of administration and the treatment, including age, weight, symptom, treatment effect, administration mode and treatment time. .

The invention is described in the above description of the invention and the following examples, which are not intended to limit the scope of the invention.

Example 1 Establishment of animal test mode

Rats weighing 300 g were induced by hyperglycemia (65 mg/kg, ip administration) with streptozotocin (STZ). Successfully induced hyperglycemic animals (300 mg/DL) were selected, and the hyperglycemic animals were subjected to a diabetic wound healing test two months after the symptoms of hyperglycemia were produced. High-glycemic animals weighing less than 300 grams were eliminated and randomized. The animals were anesthetized with pentobarbital and shaved and sterilized on the back. Immediately above the animal's back, the animal's skin was removed by a circular knife with a diameter of 1 cm from the midpoint of the two sides of the humerus at 4, 6, and 8 cm.

Test wounds were applied to each animal's wound, and the new epidermis was removed after the end of the experiment.

The area of the zeroth day was the original wound area after three areas of each rat's back were analyzed by image pro. The original wound area was subtracted from the wound area at each time point and divided by the original wound area as the percentage of wound healing. The average percentage of wound healing in each rat was counted as the degree of healing of each wound. There were only 6 rats in each group in each test. Data are expressed as mean ± standard error (SEM). The test results are calculated by the t-test of the control group. Value, P < 0.05 indicates a significant difference, expressed as *.

The 0.5% aflatoxanthin composition was prepared in the form of an ointment, and the mice treated by the above were treated as follows. The results of the wound healing on the 9th, 11th, 13th, and 15th days after the application were compared with the untreated control group as follows. The effects are all significantly different. Further calculation of the number of days required for wound healing (CT50 value) also showed significant differences.

%: percentage of wound healing CT50: wound half-closure time*: p<0.05 animal number: n=6

From the experimental results, it is known that flavonoids in the compound of the present invention has a therapeutic effect on chronic wound healing in diabetic patients.

Claims (10)

Use of a compound for the preparation of a wound healing composition, wherein the compound is a compound having the structure of the following formula I or an isomer thereof: Wherein A is a hydrogen atom, R or -OH; and n1 and n2 are the same or different and are one of integers from 0 to 4, wherein the sum of n1 and n2 is at most 4; n3 and n4 are the same or different and are 0 to 5 One of the integers, wherein the sum of n3 and n4 is at most 5; wherein R, R ₁ , R ₂ , R ₃ or R ₄ is defined as a hydrogen atom, an alkyl group having 1 to 30 carbon atoms, and contains 1-30 A mercapto group of an alkyl group of one carbon atom, a hydrocarbon chain having 1 to 30 carbon atoms; or a pharmaceutically acceptable ester or salt thereof. According to the use of claim 1, wherein the wound healing is wound healing of skin symptoms of trauma, burns and chronic wounds. According to the use of claim 1, wherein the wound healing refers to wound healing in a diabetic patient. According to the use of claim 1, wherein the wound healing is chronic wound healing in a diabetic patient. The use according to claim 1, 2, 3 or 4, wherein the compound is a flavone. The use according to claim 5, wherein the compound is a non-glycosylated flavone. According to the use of claim 6, wherein the compound is cirsimaritin having the following structure: The use according to claim 1, wherein the compound comprises a suitable excipient to form a composition for external use, a cosmetic form or a pharmaceutical material. The use according to claim 5, wherein the compound comprises a suitable excipient to form a composition in the form of an external pharmaceutical form, a cosmetic form or a medicinal material. The composition according to claim 7, wherein the compound comprises a suitable excipient to form a composition in the form of a pharmaceutical preparation for external use, a cosmetic form or a pharmaceutical material.