Application of vanillyl-beta-D-glucopyranoside in preparation of liver injury drugs

Abstract

The invention belongs to the technical field of medicines, and particularly relates to application of vanillyl-beta-D-glucopyranoside in preparation of a medicine for treating liver injury. The invention provides the application of vanillyl-beta-D-glucopyranoside in the aspect of preparing the liver injury medicine for the first time. The vanillyl-beta-D-glucopyranoside is Vanillyl-beta-D-glucopyranoside (the molecular formula of the vanillyl-beta-D-glucopyranoside is C14H20O8, the molecular formula of the vanillyl-beta-D-glucopyranoside is C14H20O8 According to the present invention, the drug A has the molecular weight of 316.3, hereinafter referred to as VA, and the drug VA does not show toxicity in the investigated concentration range (6.25-100 [mu] M), can significantly improve the cell survival rate of acetaminophen induced damaged parenchymal hepatic cells AML-12 at the investigated concentration of 6.25-25 [mu] M, has significant liver protection effect, and has good application prospects in the preparation of the drugs for prevention and treatment of liver injury.

Description

Technical Field

[0001] The invention belongs to the field of medical technology, and specifically relates to application of vanillyl-β-D-pyranoglucoside in preparing liver injury medicines. Background Art

[0002] The liver is the largest substantial organ in the human body, and undertakes key functions such as metabolism, immune regulation, and detoxification. Liver damage caused by viral hepatitis, alcohol and drug toxic liver disease, systemic diseases, and the subsequent liver fibrosis, cirrhosis, and liver failure have become common diseases that seriously endanger human health. Chemical liver injury refers to liver damage induced by various chemical substances (including drugs) and their metabolites, and is one of the main causes of acute liver injury. At present, more than 1,100 marketed drugs known worldwide have been found to have potential hepatotoxicity. The most common liver-damaging drugs in China are mainly antipyretic and analgesic acetaminophen (APAP), anti-tuberculosis drugs (isoniazid, rifampicin), etc. At present, there is a lack of specific treatment methods for chemical liver injury in clinical practice. The principle of treatment is to protect liver function, and prevention is still the focus. Therefore, finding drugs that have a protective effect on the liver for the prevention and treatment of liver injury is of great significance for controlling the development of liver diseases.

[0003] Vanillyl-β-D-pyranoglucoside belongs to the phenolic glycosides, which are widely found in natural medicines and have a variety of physiological activities. For example, it can bind to receptors in the skin, increase the solubility of drugs, and increase the retention time of internal active drugs in the skin; in cosmetics, vanillyl-β-D-pyranoglucoside is used as a thermal agent and can be used in slimming products, breast enhancement products, skin care products, etc. to provide a sense of warmth, which may help promote blood circulation and product absorption.

[0004] There are currently no reports on the use of vanillyl-β-D-pyranoglucoside as a drug for the prevention and treatment of liver damage. Summary of the invention

[0005] In order to solve the above problems, the present invention provides the use of vanillyl-β-D-pyranoglucoside in the preparation of liver injury drugs.

[0006] This is achieved specifically through the following technical solutions:

[0007] Application of vanillyl-β-D-glucopyranoside (VA) in the preparation of liver injury drugs, wherein the vanillyl-β-D-glucopyranoside has a molecular formula of C 14 H 20 O 8 ; The molecular weight is 316.3. The structural formula of the vanillyl-β-D-pyranoglucoside is as follows:

[0008]

[0009] A medicine for preventing and treating liver damage, containing vanillyl-β-D-pyranoglucoside

[0010] Furthermore, the liver injury drug is a drug for preventing and treating liver injury.

[0011] The above-mentioned drugs for treating liver damage include oral preparations or injection preparations. The oral preparations can be any one or more of granules, capsules, tablets, powders, pills, and sustained-release preparations.

[0012] The VA used in the present invention can be extracted from plants (such as Artemisia grandis) or chemically synthesized, and the prepared medicine can contain other drugs for preventing and treating liver damage and drug excipients or carriers. The medicine can be prepared into any pharmaceutical preparation suitable for clinical use, mainly including liquid preparations, granules, tablets, granules, capsules, capsules, dripping pills, sustained-release preparations or injections. The administration form of the preparation mainly includes oral administration or injection.

[0013] The chemical name of VA in the present invention is vanillyl-β-D-pyranoglucoside, and its molecular formula is C 14 H 20 O 8 , molecular weight is 316.3, scientific name Vanillyl-β-D-glucopyranoside, structural formula is Figure 1 .

[0014] The beneficial effect of the present invention is that the present invention provides for the first time the use of vanillyl-β-D-pyranoglucoside in the preparation of liver injury drugs. Vanillyl-β-D-pyranoglucoside is Vanillyl-β-D-glucopyranoside (molecular formula: C 14 H 20 O 8 ; molecular weight is 316.3, hereinafter referred to as VA). The drug VA showed no toxicity within the investigated concentration range (6.25-100 μM), and could significantly improve the cell survival rate of AML-12 hepatocytes damaged by acetaminophen at the investigated concentration of 6.25-25 μM, had a significant liver-protecting effect, and had good application prospects in the preparation of drugs for the prevention and treatment of liver damage. BRIEF DESCRIPTION OF THE DRAWINGS

[0015] Figure 1 is the chemical structure of VA;

[0016] Figure 2 The following is the result of the effect of different concentrations of VA on the survival rate of normal AML-12 liver cells. Indicates (n=3).

[0017] Figure 3 The following is the result of the effect of different concentrations of VA on the survival rate of AML-12 hepatocytes damaged by acetaminophen. Compared with the control group, ### P<0.001; compared with the model group, **P<0.01. DETAILED DESCRIPTION

[0018] The specific embodiments of the present invention are further described in detail below, but the present invention is not limited to these embodiments, and any improvement or substitution based on the basic spirit of the present embodiment still falls within the scope of protection required by the claims of the present invention.

[0019] Example 1 shows the toxic effect of VA on normal hepatocytes AML-12

[0020] Experimental method: CCK-8 method to detect cell viability

[0021] The cells were cultured in DMEM medium containing 10% fetal bovine serum, 100 kU / L penicillin and 100 mg / L streptomycin, 1% insulin-transferrin-selenium (ITS), and 40 ng / mL dexamethasone (DXMS) at 37°C and 5% CO. 2 AML-12 cells were cultured in an incubator. AML-12 cells in the logarithmic growth phase were taken, digested with 0.25% trypsin, and the cell density was adjusted to 3×10 with culture medium (10% FBS + 1% double antibody + 1% ITS + 40ng / mL DXMS). 4 / mL, inoculated into 96-well plates, and divided into control group (CON) and drug group (6.25, 12.5, 25, 50, 100μM). Each group has 3 replicate wells, 100μL cell suspension in each well, and a blank group with no cells but only culture medium was set up. 37℃, 5% CO 2 Culture for 24 hours under saturated humidity conditions. Add drugs of corresponding concentrations and incubate for 24 hours. Then, add 10 μL CCK-8 to each well and continue to culture for 1 hour under the same culture conditions. Measure the absorbance (A) of each well at 450 nm with an ELISA instrument, and calculate the cell survival rate according to the following formula:

[0022]

[0023] Experimental results ( Figure 2 ) It can be concluded that VA has no effect on the survival rate of normal liver cells AML-12 at a concentration of 6.25-100 μM. This shows that VA has no cytotoxicity to AML-12 cells at a concentration of 6.25-100 μM.

[0024] Example 2 demonstrates that VA protects normal hepatocytes from acetaminophen-induced liver damage

[0025] Experimental method: CCK-8 method to detect cell viability

[0026] The culture conditions were the same as those in Experiment 1. The cells were divided into a control group (CON), a model group (APAP, 10 mM), and a drug group (6.25, 12.5, 25 μM). Each group had 3 replicate wells, with 100 μL of cell suspension in each well, and a blank group with no cells but only culture medium was set up. 37°C, 5% CO 2 After culturing for 24 hours under saturated humidity conditions, APAP serum-free culture medium with a final concentration of 10mM was added to each well of the other groups except the control group and incubated for 24 hours. The drug-treated group was also incubated with drugs of corresponding concentrations. Subsequently, 10μL CCK-8 was added to each well and cultured for 1 hour under the same culture conditions. The absorbance (A) at 450nm of each well was measured by an ELISA instrument, and the cell survival rate was calculated according to the following formula:

[0027]

[0028] Experimental results ( Figure 3 ) It can be concluded that within the concentration range of 6.25-25 μM, VA can significantly improve the survival rate of AML-12 hepatocytes induced by acetaminophen, and it is concentration-dependent. This shows that VA has a good liver-protecting effect and has a good application prospect in the preparation of drugs for the prevention and treatment of liver damage. In summary, the present invention provides for the first time the use of VA in the preparation of drugs for the prevention and treatment of liver damage.

[0029] It is obvious to those skilled in the art that the present invention is not limited to the details of the exemplary embodiments described above, and that the present invention can be implemented in other specific forms without departing from the spirit or essential features of the present invention. Therefore, the embodiments should be regarded as exemplary and non-restrictive from all points of view, and the scope of the present invention is defined by the appended claims rather than the above description, and it is intended that all changes falling within the equivalent meaning and scope of the claims be included within the scope of protection of the present invention.

Claims

1. Use of vanillyl-β-D-pyranoglucoside in the preparation of liver injury drugs, characterized in that: The vanillyl-β-D-pyranoglucoside is Vanillyl-β-D-glucopyranoside, with a molecular formula of C 14 H 20 O8; molecular weight is 316.

3.

2. The use of the vanillyl-β-D-pyranoglucoside according to claim 1 in the preparation of a liver injury drug, characterized in that: The structural formula of the vanillyl-β-D-glucopyranoside is as follows:

3. The use of the vanillyl-β-D-pyranoglucoside according to claim 1 in the preparation of a liver injury drug, characterized in that: The liver injury drug is a drug for preventing and treating liver injury.

4. A drug for preventing and treating liver damage, characterized in that: Contains vanillyl-β-D-glucopyranoside.

5. The drug for preventing and treating liver damage according to claim 4, characterized in that: The medicine for treating liver injury includes oral preparations or injection preparations.

6. The drug for preventing and treating liver damage according to claim 5, characterized in that: The oral preparation is any one of granules, capsules, tablets, powders, pills, and sustained-release preparations.

Images