CN113197907B - Application of gardenia acetic acid and derivatives thereof in preparing medicine for treating diabetes - Google Patents
Application of gardenia acetic acid and derivatives thereof in preparing medicine for treating diabetes Download PDFInfo
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- CN113197907B CN113197907B CN202110688279.7A CN202110688279A CN113197907B CN 113197907 B CN113197907 B CN 113197907B CN 202110688279 A CN202110688279 A CN 202110688279A CN 113197907 B CN113197907 B CN 113197907B
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- gardenia
- acetic acid
- derivatives
- treating diabetes
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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
- A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
- A61K31/575—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of three or more carbon atoms, e.g. cholane, cholestane, ergosterol, sitosterol
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
Abstract
The present invention provides aAn application of gardenia acetic acid shown as a formula I and derivatives thereof in preparing a medicament for treating diabetes,
wherein R is 1 Or R 2 Each independently selected from hydrogen, hydroxy or C 1 ‑C 4 An alkyl group; r 3 、R 4 、R 5 、R 6 、R 7 Or R 8 Each independently selected from hydrogen or C 1 ‑C 4 An alkyl group; the gardenia acetic acid and the derivative thereof provided by the invention have a very good inhibition effect on alpha-glucosidase, the inhibition rate reaches 91.32%, and the gardenia acetic acid and the derivative thereof can be used as potential drugs for treating diabetes.
Description
Technical Field
The invention belongs to the field of medical application, and particularly relates to application of gardenia acetic acid and derivatives thereof in preparation of a medicine for treating diabetes.
Background
Diabetes mellitus is a disease of endocrine metabolism characterized by hyperglycemia due to defective insulin secretion or impaired biological action thereof. If the organism is in a high blood sugar state for a long time, various complications such as limb gangrene, renal failure, cardiovascular and cerebrovascular diseases and the like can be caused. Diabetes has become the third largest disease that endangers human health. Among them, type 2 diabetes is common and is mainly treated by oral hypoglycemic drugs.
The alpha-glucosidase inhibitor is a novel oral hypoglycemic medicament, and can competitively inhibit the activity of the alpha-glucosidase in the small intestine, inhibit or delay the absorption of glucose in the intestinal tract, and further play a role in reducing blood sugar. The alpha-glucosidase inhibitor commonly used in clinic comprises miglitone, acarbose and the like.
Gardenia acetic acid, also called gardenia acetic acid B or gardenia acetic acid.
The gardenia acetic acid is an active ingredient separated from gardenia. The gardenia has the effects of purging fire, relieving restlessness, clearing away damp-heat, cooling blood and removing toxicity. Few reports are currently made on the efficacy of gardenia acetic acid.
Disclosure of Invention
Aiming at the technical problems, the invention provides application of gardenia acetic acid and derivatives thereof in preparing a medicament for treating diabetes.
One technical scheme of the invention provides application of gardenia acetic acid and derivatives thereof in preparing medicines for treating diabetes.
In a further improved scheme, the gardenia acetic acid and the gardenia acetic acid derivatives can be prepared into a pharmaceutical composition with a pharmaceutically acceptable carrier.
The prepared pharmaceutical composition can be administered orally, transdermally, intramuscularly, subcutaneously, etc.
When the gardenia acetic acid and the gardenia acetic acid derivatives are orally taken, the gardenia acetic acid and the gardenia acetic acid derivatives can be prepared into any orally acceptable preparation form, including but not limited to tablets, capsules and the like. Among these, carriers for tablets generally include lactose and corn starch, and additionally, lubricating agents such as magnesium stearate may be added. Diluents for use in capsules typically include lactose and dried corn starch. Optionally, some sweetener, aromatic or colorant may be added into the above oral preparation.
When topically applied to the skin, the gardenia acetic acid and derivatives thereof provided by the present invention can be formulated into suitable ointment or cream formulations, wherein the active ingredient is suspended or dissolved in one or more carriers. Carriers that may be used in ointment formulations include, but are not limited to: mineral oil, liquid petrolatum, white petrolatum, propylene glycol, polyethylene oxide, polypropylene oxide, emulsifying wax and water; creams carriers that may be used include, but are not limited to: mineral oil, sorbitan monostearate, tween 60, cetyl esters wax, cetearyl alcohol, 2-octyldodecanol, benzyl alcohol and water.
The gardenia acetic acid and the derivatives thereof of the present invention can also be administered in the form of a sterile injectable preparation, including a sterile injectable aqueous or oleaginous suspension or a sterile injectable solution, and can also be in a lyophilized form. Among the carriers and solvents that may be employed are water, ringer's solution and isotonic sodium chloride solution. In addition, the sterilized fixed oil may also be employed as a solvent or suspending medium, such as a monoglyceride or diglyceride.
In a further improved scheme, the gardenia acetic acid and the gardenia acetic acid derivatives are applied to the preparation of alpha-glucosidase inhibitor drugs.
The invention has the beneficial effects that: the gardenia acetic acid and the derivatives thereof provided by the invention have a very good inhibition effect on alpha-glucosidase, the inhibition rate reaches 91.32%, and the gardenia acetic acid and the derivatives thereof can be used as potential medicines for treating diabetes.
Drawings
FIG. 1 is a statistical chart of inhibition results.
Detailed Description
Test example 1: alpha-glucosidase inhibitory Activity test
1.1 Experimental materials
The reagents used in this experiment were as follows:
TABLE 1 test reagents
1.2 Experimental methods
(1) Substrate PNPG solution: accurately weighing 0.3766g PNPG, dissolving with a proper amount of 0.1mol/L phosphate buffer solution (pH 6.8), accurately metering the volume to 50mL by using a volumetric flask, preparing a solution of 25mmol/L, and diluting the solution to a substrate solution of 3.0 mmol/L.
(2) Preparing an enzyme solution of alpha-glucosidase: dissolving lyophilized enzyme powder (enzyme activity is 50U/mg) with 0.01mol/L phosphate buffer solution (pH 6.8) to obtain 2U/mL solution, and diluting to obtain 1.0mU/mL enzyme solution.
(3) Preparing an inhibitor control solution (luteolin standard): accurately weighing 0.0010g of luteolin standard, accurately metering the volume to 10mL by using a volumetric flask, preparing 1000 mu g/mL of luteolin standard mother liquor, and respectively diluting the mother liquor into 30 mu g/mL of standard solution.
(4) 0.2mol/L of Na 2 CO 3 : weighing 2.16g Na 2 CO 3 Adding a proper amount of purified water into a beaker for dissolving, fixing the volume to 100mL, and storing at 4 ℃.
(5) The measurement method is adjusted according to test conditions such as Masao Hattori. Experiment ofThe reactions were loaded in 96-well plates at the doses in table 2, 3 replicates per group. Sequentially adding PBS buffer solution, inhibitor solution and substrate according to the table, mixing well, keeping the temperature in 37 ℃ water bath for 30min, taking out after finishing, adding enzyme solution in 37 ℃ water bath, mixing well, reacting in 37 ℃ water bath for 40min, adding 150 mu L of 0.2mol/L Na after finishing 2 CO 3 The reaction was stopped with the solution.
Because PNPG can be hydrolyzed under the action of alpha-glucosidase to generate glucose and PNP, PNP has maximum absorption at 405nm, corresponding absorbance is measured, and the inhibition rate of the alpha-glucosidase of each sample can be calculated according to a formula.
The following are the formula of inhibition (formula 1) and the reactant addition table (table 2):
inhibition rate = (1- (a) S -A SB )/(A C -A CB ) 100% (equation (1))
(wherein, A) S Absorbance of sample group, A SB Absorbance of sample blank, A C Absorbance of control group, A CB Absorbance for blank control group)
TABLE 2 amounts of reactants added
1.3 results of the experiment
The positive control drug, the triterpenes and the flavonoids are respectively tested to obtain data, and then the inhibition rate of each compound is calculated by the formula (1). The results of the inhibition rate obtained by the experiment are shown in fig. 1.
The inhibition rate of gardenia acetic acid on alpha-glucosidase is up to 91.32%, which is obviously superior to that of positive control drugs and other extracts. Therefore, the gardenia acetic acid has better application prospect in the aspect of treating diabetes.
Claims (3)
1. Use of gardenia acetic acid as sole active ingredient for the preparation of a medicament for the treatment of diabetes.
2. The use of claim 1, wherein said gardenia acetic acid and a pharmaceutically acceptable carrier are formulated into a pharmaceutical composition.
3. The use of claim 1, wherein the medicament for the treatment of diabetes is an α -glucosidase inhibitor.
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN202110688279.7A CN113197907B (en) | 2021-06-21 | 2021-06-21 | Application of gardenia acetic acid and derivatives thereof in preparing medicine for treating diabetes |
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| Application Number | Priority Date | Filing Date | Title |
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| CN202110688279.7A CN113197907B (en) | 2021-06-21 | 2021-06-21 | Application of gardenia acetic acid and derivatives thereof in preparing medicine for treating diabetes |
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| CN113197907A CN113197907A (en) | 2021-08-03 |
| CN113197907B true CN113197907B (en) | 2023-03-14 |
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Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101422465A (en) * | 2007-10-30 | 2009-05-06 | 上海市新文达生物科技有限公司 | Use of ursolic acid and plant extract containing the same |
Family Cites Families (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105124078A (en) * | 2015-10-12 | 2015-12-09 | 青岛恒波仪器有限公司 | Gardenia blood-glucose-reducing and lipid-reducing healthcare tea and preparing method thereof |
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- 2021-06-21 CN CN202110688279.7A patent/CN113197907B/en active Active
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101422465A (en) * | 2007-10-30 | 2009-05-06 | 上海市新文达生物科技有限公司 | Use of ursolic acid and plant extract containing the same |
Non-Patent Citations (1)
| Title |
|---|
| 栀子主要成分研究概述;徐克明;《实用中医药杂志》;20100930;第26卷(第9期);669-670 * |
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