CN111991378A - Application of hydroxy-alpha-sanshool in preparing blood sugar regulating medicine - Google Patents
Application of hydroxy-alpha-sanshool in preparing blood sugar regulating medicine Download PDFInfo
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- CN111991378A CN111991378A CN202010973574.2A CN202010973574A CN111991378A CN 111991378 A CN111991378 A CN 111991378A CN 202010973574 A CN202010973574 A CN 202010973574A CN 111991378 A CN111991378 A CN 111991378A
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- sanshool
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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
- A61K31/16—Amides, e.g. hydroxamic acids
- A61K31/164—Amides, e.g. hydroxamic acids of a carboxylic acid with an aminoalcohol, e.g. ceramides
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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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/48—Drugs for disorders of the endocrine system of the pancreatic hormones
- A61P5/50—Drugs for disorders of the endocrine system of the pancreatic hormones for increasing or potentiating the activity of insulin
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Abstract
The invention discloses an application of hydroxy-alpha-sanshool in preparing a medicament for regulating blood sugar, which is an oral preparation prepared from the hydroxy-alpha-sanshool and pharmaceutically acceptable auxiliary materials or carriers, and can be used as the medicament for regulating blood sugar, and the effects of the oral preparation comprise improving the pancreatic beta cell function of human or animals and reducing the blood sugar of the human or animals. The content of hydroxy-alpha-sanshool in the blood sugar-regulating drug can be 0.1 to 100 percent by mass, and the administration dosage can be easily determined by a person skilled in the art according to actual conditions. The invention can obviously reduce the blood sugar of a metabolic syndrome model mouse by orally administering the hydroxyl-alpha-sanshool, and simultaneously, the HOMA-beta index is obviously increased, which indicates that the hydroxyl-alpha-sanshool can treat diabetes.
Description
Technical Field
The invention relates to the field of medicines, discloses an effect of reducing blood sugar by improving pancreatic beta cell function of hydroxy-alpha-sanshool, provides a medicine for treating diabetes with definite curative effect and controllable quality, and can meet the requirement of clinical application. Experiments prove that the hydroxy-alpha-sanshool can obviously reduce the blood sugar of a metabolic syndrome model mouse caused by high-fat and high-cholesterol diet and protect the function of islet beta cells.
Background
Epidemiological studies show that with the increasing living standard of people and the change of dietary habits, the incidence rate and the death rate of diabetes mellitus are continuously increased all over the world, and the onset age is gradually younger.
The etiology and pathogenesis of type 2 diabetes are currently unclear, with its prominent pathophysiological features being a decrease (or relative decrease) in insulin secretion resulting from a decrease in the ability of insulin to regulate glucose metabolism (insulin resistance) coupled with a defect in islet beta cell function. The goal of diabetes therapy is to prevent chronic complications, improve the quality of life of patients and prolong life span through good metabolic control including blood glucose. The pharmacotherapy of hyperglycemia is based on correcting two major pathophysiological changes that lead to elevated blood glucose in humans — insulin resistance and impaired insulin secretion. Although diabetes mellitus has been increasingly paid attention to, the diabetes mellitus is still a hotspot and a difficult point of research in the medical field, and the active and deep development of research on prevention and treatment of atherosclerosis has important practical significance.
Zanthoxylum bungeanum (Zanthoxylum bungeanum Maxim.) is a small deciduous tree of Rutaceae and Zanthoxylum genus, and has effects of warming middle-jiao and activating qi-flowing, dispelling cold, relieving pain, and killing parasite. Modern pharmacology indicates that the pepper is mainly applied to the treatment of cardiovascular and cerebrovascular systems, anti-inflammation and analgesia, digestive systems, bacteriostasis, disinsection and the like. The applicant previously combined a High Performance Liquid Chromatography (HPLC) to separate the active components from the Zanthoxylum bungeanum extract and combined UV to analyze the UV absorption of the active components. The main active ingredients of the pepper are identified to be Hydroxy-alpha sanshool (H alpha SS), Hydroxy-beta sanshool (H beta SS) and Hydroxy-gamma sanshool (H gamma SS), the three substances have similar structures, and the content of the H alpha SS is the highest (80.22%). Studies have demonstrated that H α SS improves lipid metabolism and reduces inflammatory responses, but its therapeutic effects on diabetes are lacking.
Disclosure of Invention
Aiming at the defects of the prior art, the invention provides the application of the hydroxy-alpha-sanshool in preparing the medicine for regulating blood sugar.
Specifically, one embodiment of the present invention adopts the following technical solutions:
the invention provides application of hydroxy-alpha-sanshool in preparing a medicament for regulating blood sugar.
The application of the hydroxy-alpha-sanshool in preparing the medicine for regulating the blood sugar comprises the application of the hydroxy-alpha-sanshool in preparing the medicine for reducing the blood sugar;
on the other hand, the application of the hydroxy-alpha-sanshool in preparing the medicine for improving the function of the islet beta cells is included.
When the hydroxy-alpha-sanshool is applied to the preparation of the blood sugar regulating medicine, the blood sugar regulating medicine can also comprise pharmaceutically acceptable auxiliary materials or carriers.
When the hydroxy-alpha-sanshool is used for preparing the blood sugar regulating medicament, the blood sugar regulating medicament can be an oral preparation.
When the hydroxy-alpha-sanshool is applied to the preparation of the blood sugar regulating medicine, the weight percentage content of the hydroxy-alpha-sanshool in the blood sugar regulating medicine can be 0.1 to 100 percent.
Preferably, the content of the hydroxy-alpha-sanshool in the medicament for regulating blood sugar is 50 to 90 percent by mass.
More preferably, the content of the hydroxy-alpha-sanshool in the medicament for regulating blood sugar is 75 to 85 percent by mass.
The dosage to be administered can be readily determined by one skilled in the art based on the actual circumstances.
The structure of the compound, namely the hydroxy-alpha-sanshool, is shown as a formula 1:
compared with the prior art, the invention has at least the following beneficial effects: the invention uses the hydroxyl-alpha-sanshool to prepare the medicine for regulating blood sugar, and the medicine can improve the function of islet beta cells of human beings or animals and reduce the blood sugar of human beings or animals.
Drawings
FIG. 1 is a graph showing the fasting blood glucose levels of three groups of mice;
FIG. 2 is a graph showing the results of HOMA-beta values of three groups of mice;
wherein, Control is a normal diet Control group (n is 4), Model is a metabolic syndrome Model group made by high-fat high-cholesterol diet, and H alpha SS group is high-fat high-cholesterol diet plus 80 ug/g/day of hydroxyl-alpha-sanshool. Denotes independent samples between groups T-test p < 0.05.
Detailed Description
In order to make the objects, technical solutions and advantages of the present invention more apparent, the present invention is further described in detail with reference to the following embodiments. It should be understood that the specific embodiments described herein are merely illustrative of the invention and are not intended to limit the invention.
The invention relates to extraction and identification of a compound hydroxy-alpha-sanshool shown as a formula 1, which is characterized in that a high-purity active component is separated from a low-polarity component of pepper by means of a medium-pressure column chromatography system (MPLC) and preparative liquid chromatography (Pre-HPLC); the active component is confirmed to be hydroxy-alpha-sanshool by comparing with a reference substance through ultraviolet spectrum, liquid phase retention time and mass spectrum analysis.
The invention discloses the effect of hydroxyl-alpha-sanshool on protecting the function of islet beta cells and reducing blood sugar by researching the influence of the hydroxyl-alpha-sanshool on the blood sugar and the function of the islet beta cells of a metabolic syndrome model mouse.
The invention can obviously reduce the blood sugar of a metabolic syndrome model mouse by orally administering the hydroxyl-alpha-sanshool, and simultaneously, the HOMA-beta index is obviously increased, which indicates that the hydroxyl-alpha-sanshool can treat diabetes.
Materials and methods
1. Experimental materials:
1.1 animal and feed
Experimental animals: 6 weeks old C57/BL male mice, SPF grade, purchased from Wydorubio laboratory animals Inc.
Feed: basal diet and high-fat high-cholesterol model diet, purchased from Nantong Terofen feed science and technology Co.
1.2 drugs and reagents
PBS:Invitrogen。
Blood glucose test paper: roche excellence test paper.
Insulin Elisa kit: mouse Insulin ELISA kit (cat # 10-1247-01) from Mercodia.
1.3 Equipment
Low temperature refrigerator (-80 ℃ C.: Thermo, USA).
A constant-temperature incubator: Shanghai-Heng scientific instruments Ltd.
Washing the plate machine: BIO-RAD, USA.
Enzyme-linked immunosorbent assay instrument BIO-RAD, USA.
Glucometer Accu, Swizerland.
A high-speed refrigerated centrifuge: anhui Zhongzhongjia scientific instruments, Inc.
2. The experimental method comprises the following steps:
2.1 preparation of mouse metabolic syndrome model
From Woods Shuicho laboratory animals Co., Ltd, 14 healthy mice male SPF grade C57/L6 were purchased. After 2 weeks of adaptive feeding, the animals were divided into 4 normal diet Control groups (Control group), 4 metabolic syndrome Model groups (Model group), and 6 hydroxy- α -sanshool groups (H α SS group). The Model group and the H.alpha.SS group were given a high-fat high-cholesterol Model diet (15% fat + 1.25% cholesterol + 0.5% bile salt), the H.alpha.SS group was given H.alpha.SS intragastric administration of 80 ug/g/day, and the Model group was given the same volume of solvent as a control. The mice are fed in SPF-level experimental centers of national key laboratories of Sichuan university, and can be lighting-controlled, the light and the shade of the mice are 12 hours each day, the indoor temperature is 22 ℃, and the humidity is 55%. The feed and the drinking water are replaced every two days during the breeding period, and the padding is replaced every four days. Body weight was measured weekly. Intervention + high fat feeding for 16 weeks. All experimental procedures and operations comply with the requirements of the rules of experimentation and the animal ethics committee.
2.2 high fat diet
Purchased from southbound telofen technologies ltd, diet type Paigen model diet (TP28640), high-fat high-sugar containing 15% fat + 1.25% cholesterol + 0.5% bile salts.
2.3 determination of index
Tail vein blood glucose: at the end of 16 weeks of the experiment, after three groups of mice had an empty stomach for 12 hours, the tip of the tail was cut off by about 5mm, and the tail portion was massaged from the tail to the tip portion, so that blood flowed out from the severed end. Allowing blood to flow out by itself. Discarding the first drop of blood, collecting the second drop of blood, and detecting the concentration of glucose in the peripheral venous snow by a rapid glucometer. After blood collection is finished, disinfection and hemostasis are carried out.
Fasting insulin: at the end of the 16 th week of the experiment, three groups of mice fasted for 12 hours, weighed and recorded, anesthetized with ether, bled from the heart, and centrifuged to separate the serum. Fasting Insulin levels were determined in mice by reference to the Mouse Insulin ELISA kit method and the results are shown in Table 1.
2.4 HOMA-beta value calculation formula
HOMA- β ═ 20 × fasting insulin levels (FINS, μ U/mL)/(fasting blood glucose levels (FPG, mmol/L) -3.5) (%)
TABLE 1 fasting blood glucose, fasting insulin and HOMA-beta results
Note:*representing Model set vs. Control set, p<0.05,#Denotes the comparison of the H.alpha.SS team with the Model team, p<0.05。
As shown in Table 1, the blood sugar of mice in a metabolic syndrome model can be obviously reduced by orally administering the hydroxy-alpha-sanshool, and the HOMA-beta index is obviously increased, which indicates that the hydroxy-alpha-sanshool can treat diabetes.
Although the invention has been described herein with reference to illustrative embodiments thereof, it should be understood that numerous other modifications and embodiments can be devised by those skilled in the art that will fall within the spirit and scope of the principles of this disclosure.
Claims (8)
1. Application of hydroxy-alpha-sanshool in preparing medicine for regulating blood sugar is provided.
2. Use of hydroxy- α -sanshool according to claim 1 for the preparation of a medicament for regulating blood glucose, characterized in that it is used for the preparation of a medicament for lowering blood glucose.
3. Use of hydroxy- α -sanshool according to claim 1 for the preparation of a medicament for regulating blood glucose, characterized in that the hydroxy- α -sanshool is used for the preparation of a medicament for improving pancreatic β -cell function.
4. The use of hydroxy- α -sanshool for the preparation of a medicament for regulating blood glucose according to claim 1, wherein the medicament for regulating blood glucose further comprises a pharmaceutically acceptable adjuvant or carrier.
5. The use of hydroxy- α -sanshool according to claim 1 for the preparation of a medicament for regulating blood glucose, wherein the medicament for regulating blood glucose is an oral formulation.
6. The use of hydroxy- α -sanshool in the manufacture of a medicament for regulating blood glucose according to claim 1, wherein the amount of hydroxy- α -sanshool in the medicament for regulating blood glucose is from 0.1% to 100% by weight.
7. The use of hydroxy- α -sanshool in the manufacture of a medicament for regulating blood glucose according to claim 1, wherein the amount of hydroxy- α -sanshool in the medicament for regulating blood glucose is from 50% to 90% by weight.
8. The use of hydroxy- α -sanshool in the manufacture of a medicament for regulating blood glucose according to claim 1, wherein the amount of hydroxy- α -sanshool in the medicament for regulating blood glucose is 75% to 85% by weight.
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| Application Number | Priority Date | Filing Date | Title |
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| CN202010973574.2A CN111991378A (en) | 2020-09-16 | 2020-09-16 | Application of hydroxy-alpha-sanshool in preparing blood sugar regulating medicine |
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| CN202010973574.2A CN111991378A (en) | 2020-09-16 | 2020-09-16 | Application of hydroxy-alpha-sanshool in preparing blood sugar regulating medicine |
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Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN113907283A (en) * | 2021-10-22 | 2022-01-11 | 西华大学 | Reduction process of heterocyclic amine in barbecued meat product |
| CN114053254A (en) * | 2021-12-13 | 2022-02-18 | 成都中医药大学 | Combined medicine for treating diabetes and/or hyperlipidemia |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN108567852A (en) * | 2018-07-04 | 2018-09-25 | 四川省中医药科学院 | A kind of pharmaceutical composition of prevention diabetic neuropathy |
-
2020
- 2020-09-16 CN CN202010973574.2A patent/CN111991378A/en active Pending
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN108567852A (en) * | 2018-07-04 | 2018-09-25 | 四川省中医药科学院 | A kind of pharmaceutical composition of prevention diabetic neuropathy |
Non-Patent Citations (3)
| Title |
|---|
| WEILI LI等: "Chemical profiles and screening of potential α-glucosidase inhibitors from", 《INDUSTRIAL CROPS & PRODUCTS》 * |
| 任廷远: "花椒麻素对试验大鼠蛋白质合成与分解代谢影响的机制研究", 《西南大学博士学位论文》 * |
| 黄金敏等: "《药物化学》", 31 August 2019 * |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN113907283A (en) * | 2021-10-22 | 2022-01-11 | 西华大学 | Reduction process of heterocyclic amine in barbecued meat product |
| CN114053254A (en) * | 2021-12-13 | 2022-02-18 | 成都中医药大学 | Combined medicine for treating diabetes and/or hyperlipidemia |
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Application publication date: 20201127 |
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