CN114028383A - Composition for preventing and treating rheumatoid arthritis and application - Google Patents
Composition for preventing and treating rheumatoid arthritis and application Download PDFInfo
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- CN114028383A CN114028383A CN202111595228.6A CN202111595228A CN114028383A CN 114028383 A CN114028383 A CN 114028383A CN 202111595228 A CN202111595228 A CN 202111595228A CN 114028383 A CN114028383 A CN 114028383A
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- hydroxyphenyl
- acrolein
- brazilein
- rheumatoid arthritis
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- 206010039073 rheumatoid arthritis Diseases 0.000 title claims abstract description 26
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
- A61K31/35—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
- A61K31/352—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom condensed with carbocyclic rings, e.g. methantheline
-
- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23L—FOODS, FOODSTUFFS, OR NON-ALCOHOLIC BEVERAGES, NOT COVERED BY SUBCLASSES A21D OR A23B-A23J; THEIR PREPARATION OR TREATMENT, e.g. COOKING, MODIFICATION OF NUTRITIVE QUALITIES, PHYSICAL TREATMENT; PRESERVATION OF FOODS OR FOODSTUFFS, IN GENERAL
- A23L33/00—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof
- A23L33/10—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof using additives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/11—Aldehydes
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23V—INDEXING SCHEME RELATING TO FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES AND LACTIC OR PROPIONIC ACID BACTERIA USED IN FOODSTUFFS OR FOOD PREPARATION
- A23V2002/00—Food compositions, function of food ingredients or processes for food or foodstuffs
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- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Organic Chemistry (AREA)
- Rheumatology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Epidemiology (AREA)
- General Chemical & Material Sciences (AREA)
- Engineering & Computer Science (AREA)
- Immunology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pain & Pain Management (AREA)
- Physical Education & Sports Medicine (AREA)
- Mycology (AREA)
- Nutrition Science (AREA)
- Food Science & Technology (AREA)
- Polymers & Plastics (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
The invention discloses a composition, which comprises brazilein and 3- (4-hydroxyphenyl) acrolein with equal mass, and can be used for preparing anti-inflammatory drugs, in particular to the application in drugs for resisting rheumatoid arthritis. When the compound of the present invention is used as a medicament, it may be used as it is or in the form of a pharmaceutical composition. The pharmaceutical composition can also be used in a compound form with other medicines, contains 0.1-99%, preferably 0.5-90% of the compound and the balance of pharmaceutically acceptable auxiliary materials, and is prepared into a medicinal carrier and/or an excipient which are nontoxic and inert to human and animals and are commonly used in pharmaceutical preparations. The research of the invention finds that the combined use of the brazilein and the 3- (4-hydroxyphenyl) acrolein can obviously inhibit the expression of proinflammatory factors IL-6 and IL-8 in MH7A cells induced by TNF alpha, and the inhibition effect of the combination is obviously superior to the effect of the single use of the brazilein and the 3- (4-hydroxyphenyl) acrolein when the brazilein and the 3- (4-hydroxyphenyl) acrolein are mixed for use.
Description
Technical Field
The invention belongs to the technical field of medicines, and particularly relates to a composition of brazilein and 3- (4-hydroxyphenyl) acrolein, and a new application of a pharmaceutical composition taking the composition as an active ingredient in preparation of drugs, health products and functional foods for preventing and treating rheumatoid arthritis.
Technical Field
Rheumatoid Arthritis (RA) is a systemic autoimmune disease which is mainly characterized by chronic inflammation of symmetrical synovial membranes of small joints, and has the main pathological characteristics that chronic inflammation of synovial membranes gradually grows to form pannus, so that invasion and damage to cartilage and bone joints are caused, the joints are straightened and deformed in late stage, and the muscular atrophy is accompanied, so that the Rheumatoid arthritis is one of the main causes of incapability loss of sick people and limb disability. And also causes severe damage to the heart, lungs, skin, eyes, kidneys, blood vessels, and the like. Worldwide, about 1% of the population suffers from this disease, with a higher incidence in people of european asian descent. If not effectively controlled, RA will cause irreversible damage to the patient's joints, and therefore RA seriously affects the quality of life and health of the patient.
The pathogenesis of RA is not quite clear at present, but rheumatoid arthritis fibroblast-like synoviocytes (RAFLSs), mononuclear macrophages and T cells play an important role in the development of inflammation of rheumatoid arthritis, wherein the RAFLS not only can respond to the inflammation, but also can directly secrete proinflammatory factors (IL-6, IL-8, IL 1-beta, TNF alpha and the like), and further destroys joints and cartilage through the formation of pannus and the induction of osteoclast generation. Therefore, the control of inflammation and joint destruction by regulating the secretion of inflammatory factors of RAFLSs is an important means for treating RA.
Currently, RA drugs clinically comprise biological and non-biological drugs, and besides, non-steroidal anti-inflammatory drugs, glucocorticoids and the like. Although most of the drugs have obvious curative effect clinically, the drugs have the defects of toxic and side effects of liver and kidney in different degrees, or large individual difference of drug effect and the like. Therefore, the search for safe and effective RA therapeutic drugs is still of great significance.
Disclosure of Invention
The invention aims to provide an anti-RA composition and application thereof in preparing anti-inflammatory drugs, in particular anti-RA drugs, health products or functional foods. In order to achieve the purpose, the invention provides the following technical scheme:
a composition comprising brazilein (CAS:474-07-7) and 3- (4-hydroxyphenyl) acrolein (CAS: 2538-87-6).
Furthermore, the composition comprises, by mass, 0.5-99.5% of brazilein and 0.5-99.5% of 3- (4-hydroxyphenyl) acrolein.
Further, the composition comprises 50% of brazilein and 50% of 3- (4-hydroxyphenyl) acrolein by mass fraction.
The invention also provides an application of any one of the compositions in preparing anti-inflammatory drugs.
Furthermore, the anti-inflammatory drug is an anti-rheumatoid arthritis drug.
Furthermore, the prepared anti-inflammatory drug is an anti-rheumatoid arthritis drug.
Further, the prepared anti-rheumatoid arthritis medicine comprises: 0.1-99% of the composition by mass fraction and pharmaceutically acceptable auxiliary materials.
Further, the prepared anti-rheumatoid arthritis medicine comprises: 0.5-90% of composition by mass fraction and pharmaceutically acceptable auxiliary materials
Further, the prepared anti-inflammatory drug is any pharmaceutically acceptable preparation.
Further, the formulations include, but are not limited to: solid formulations as well as liquid formulations.
The invention also discloses a pharmaceutical preparation for treating rheumatoid arthritis, which comprises the composition and pharmaceutically acceptable auxiliary materials.
The invention also discloses an application of any one of the compositions in preparing health products or functional foods.
The invention has the beneficial effects that:
according to the invention, a mature cell line MH7A of Rheumatoid Arthritis Fibroblasts (RAFLSs) is used, an in-vitro rheumatoid arthritis cell model is established through TNF alpha induction, the anti-RA activity of the composition is detected, the composition can effectively inhibit MH7A cells from secreting proinflammatory factors IL-6 and IL-8, and when the two are mixed for use, the inhibition effect of the composition is obviously superior to the effect of the brazilein and the 3- (4-hydroxyphenyl) acrolein which are used independently.
When the compound of the present invention is used as a medicament, it may be used as it is or in the form of a pharmaceutical composition. The pharmaceutical composition can also be used in a compound form together with other medicines, contains 0.1-99%, preferably 0.5-90% of the compound, and the balance of the compound is pharmaceutically acceptable, and is prepared into a medicinal carrier and/or an excipient which are nontoxic and inert to human and animals and are commonly used in pharmaceutical preparations. The pharmaceutical composition of the present invention is used in the form of a dose per unit body weight. Can be made into solid preparation (tablet, capsule, granule, powder, etc.) or liquid preparation (injection, solution, suspension, emulsion, syrup, etc.) by using different medicinal adjuvants. The medicament of the invention can be administered orally and in the form of injection (intravenous injection, intravenous drip, intramuscular injection, subcutaneous injection, intraperitoneal injection, etc.).
Drawings
FIG. 1 shows that the combination of brazilein and 3- (4-hydroxyphenyl) acrolein inhibits TNF α -induced expression of IL-6 and IL-8 in MH7A cells, wherein S1 represents brazilein and G9 represents 3- (4-hydroxyphenyl) acrolein.
Detailed Description
The present invention is further illustrated by the following examples, which should not be construed as limiting the invention thereto. In each example, a conventional method is not specifically described, and reagents and drugs used in each example are commercially available.
Brazilein (English name: Brazilin), CAS:474-07-7, molecular weight: 286.28, appearance: red powder, dissolved in DMSO.
3- (4-hydroxyphenyl) acrolein (English name: 3- (4-hydroxyphenyl) acrylamide), CAS:2538-87-6, molecular weight: 148.16, appearance: white powder, dissolved in DMSO.
The following composition consisted of brazilein and 3- (4-hydroxyphenyl) acrolein.
Example 1
The brasilein and 3- (4-hydroxyphenyl) acrolein composition inhibited TNF alpha-induced IL-6 and IL-8 expression in MH7A cells.
Preparing a reagent: 10. mu.g of TNF α was purchased from Peprotech, dissolved in 200. mu.L of 5% trehalose in PBS, and the TNF α concentration was 50. mu.g/mL. 2.5mg of brazilin was weighed and added with 62.5. mu.L of MSO to prepare a 40mg/mL brazilin solution. 2.5mg of 3- (4-hydroxyphenyl) acrolein was weighed and added with 62.5. mu.L of DMSO to prepare a 40mg/mL 3- (4-hydroxyphenyl) acrolein solution. The cytokine TNF α is diluted 1:2000 in the desired volume of medium, e.g., 1mL DMEM medium with 0.5 μ L TNF α (50 μ g/mL) to make up DMEM medium containing TNF α to a final concentration of 25 ng/mL. Brazilian hematoxylin and 3- (4-hydroxyphenyl) acrolein solutions are diluted in DMEM medium containing 25ng/mL of TNF alpha according to a ratio of 1:2000, for example, 0.5 mu L of 200mg/mL Brazilian hematoxylin solution and 0.5 mu L of 200mg/mL 3- (4-hydroxyphenyl) acrolein solution are added to 1mL of DMEM medium containing 25ng/mL of TNF alpha respectively or simultaneously, and compound single and composition (mass ratio 1:1) solutions are prepared.
MH7A cells were induced by 25ng/mL TNF α, and the cells were incubated with brazilein and 3- (4-hydroxyphenyl) acrolein alone and in a composition solution (1: 1 by mass) for 24 hours, and cell culture medium supernatants were collected. The concentrations of IL-6 and IL-8 in the culture supernatant (Elisakutaki) were determined according to the instructions of the Human IL-6 and Human IL-8 ELISAKit kits. The results show that the anti-inflammatory activity of the 3- (4-hydroxyphenyl) acrolein is not obvious when the 3- (4-hydroxyphenyl) acrolein is used alone, but the brazilin and 3- (4-hydroxyphenyl) acrolein composition can obviously inhibit the expression of IL-6 and IL-8 of MH7A cells, and the inhibition effect is obviously better than the effect when the two are used respectively, for example, the anti-inflammatory activity of the brazilin used alone is not as good as the effect when the brazilin is used alone at 5 mu g/mL and is used together with the 3- (4-hydroxyphenyl) acrolein at 5 mu g/mL. Brazilian hematoxylin can inhibit the expression of inflammatory factors IL-6 and IL-8 in a dose-dependent mode when being used alone, but has obvious cytotoxicity at high concentration. When the concentration of the brazilian sappan is 20 mug/mL alone, the cell viability is 48% + -0.9, and when the cell viability is 84% + -3.7 under the same dosage (the concentration of the brazilian sappan is 10 mug/mL plus the total 20 mug/mL of the 10 mug/mL of the 3- (4-hydroxyphenyl) acrolein), the combination of the two can effectively inhibit the level of inflammatory factors and exert the anti-inflammatory activity, and can also obviously reduce the cytotoxicity caused by the brazilian sappan (as shown in figure 1).
According to the results of fig. 1, it is known that the brazilein and 3- (4-hydroxyphenyl) acrolein composition can obviously inhibit the expression of IL-6 and IL-8 of MH7A cells, and the inhibition effect is obviously better than the effect of the two when the two are used respectively. The brazilein can be used independently for inhibiting the expression of inflammatory factors IL-6 and IL-8 in a dose-dependent manner, but has obvious cytotoxicity under high concentration, and under the combined condition of the two, the brazilein not only can effectively inhibit the level of the inflammatory factors and exert anti-inflammatory activity, but also can obviously reduce the cytotoxicity caused by the brazilein.
Example 2
Preparation of injection preparation:
80mg of each of brazilein and 3- (4-hydroxyphenyl) acrolein was weighed in a ratio of 1:1, dissolved in 2 ml of propylene glycol, and the resulting solution was filtered and aseptically filled in an ampoule.
Example 3
Preparation of powder:
adding excipient into the mixed preparation of brazilein and 3- (4-hydroxyphenyl) acrolein with the mass ratio of 1:1 and the weight ratio of the excipient of 9:1, and preparing into powder.
Example 4
Preparation of tablets:
mixing brazilein and 3- (4-hydroxyphenyl) acrolein at a mass ratio of 1:1, adding excipient at a weight ratio of the mixture to the excipient of 1:1, granulating and tabletting.
Example 5
Preparation of oral liquid preparation:
the oral liquid is prepared by mixing brazilein and 3- (4-hydroxyphenyl) acrolein in a mass ratio of 1:1 according to a conventional oral liquid preparation method.
The scope of the present invention is not limited thereto, and any person skilled in the art can easily conceive of changes or substitutions within the technical scope of the present invention, and the present invention is intended to be covered thereby. Therefore, the protection scope of the present invention shall be subject to the protection scope of the claims.
Claims (10)
1. A composition, comprising:
brazilein and 3- (4-hydroxyphenyl) acrolein.
2. The composition of claim 1, wherein:
the mass fraction of brazilein is 0.5-99.5%, and the mass fraction of 3- (4-hydroxyphenyl) acrolein is 0.5-99.5%.
3. Use of a composition according to claim 1 or 2 for the preparation of an anti-inflammatory medicament.
4. The use of claim 3, wherein:
the anti-inflammatory medicine prepared is an anti-rheumatoid arthritis medicine.
5. The use of claim 4, wherein:
the prepared medicine for resisting rheumatoid arthritis comprises the following components:
0.1-99% by mass of the composition; and
pharmaceutically acceptable adjuvants.
6. The use of claim 5, wherein:
the prepared medicine for resisting rheumatoid arthritis comprises the following components:
0.5-99% by mass of the composition; and
pharmaceutically acceptable adjuvants.
7. Use of a composition according to any one of claims 3 to 6 in the preparation of an anti-inflammatory medicament, wherein:
the prepared anti-inflammatory drug is any pharmaceutically acceptable preparation.
8. The use of claim 7, wherein;
the preparation comprises the following components:
solid formulations as well as liquid formulations.
9. A pharmaceutical formulation for the treatment of rheumatoid arthritis, wherein:
comprising the composition of claim 1 or 2 and a pharmaceutically acceptable excipient.
10. Use of the composition according to claim 1 or 2 for the preparation of a health product or functional food.
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| Application Number | Priority Date | Filing Date | Title |
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| CN202111595228.6A CN114028383A (en) | 2021-12-24 | 2021-12-24 | Composition for preventing and treating rheumatoid arthritis and application |
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| CN202111595228.6A CN114028383A (en) | 2021-12-24 | 2021-12-24 | Composition for preventing and treating rheumatoid arthritis and application |
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| CN114028383A true CN114028383A (en) | 2022-02-11 |
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|---|---|---|---|---|
| CN104055875A (en) * | 2014-05-27 | 2014-09-24 | 登封市科创商务咨询有限公司 | Traditional Chinese medicinal liquor for treating rheumatoid |
| CN104274489A (en) * | 2013-06-05 | 2015-01-14 | 楼兰花 | Combined medicine for treating tumors |
-
2021
- 2021-12-24 CN CN202111595228.6A patent/CN114028383A/en active Pending
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104274489A (en) * | 2013-06-05 | 2015-01-14 | 楼兰花 | Combined medicine for treating tumors |
| CN104055875A (en) * | 2014-05-27 | 2014-09-24 | 登封市科创商务咨询有限公司 | Traditional Chinese medicinal liquor for treating rheumatoid |
Non-Patent Citations (2)
| Title |
|---|
| EUI-GIL JUNG ET AL.,: "Brazilin isolated from Caesalpinia sappan L.inhibits rheumatoid arthritis activity in a type-II collagen induced arthritis mouse model", 《BMC COMPLEMENTARY AND ALTERNATIVE MEDICINE》 * |
| THANYALUCK PHITAK ET AL.,: "The effects of p-hydroxycinnamaldehyde from Alpinia galanga extracts on human chondrocytes", 《PHYTOCHEMISTRY》 * |
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