Application of isosalicin in preparation of liver injury medicine

Abstract

The invention belongs to the technical field of medicines, and particularly relates to application of isosalicin in preparation of liver injury medicines. The invention provides the application of the isosalicin in the aspect of preparing the liver injury medicine for the first time. The isosalicin is isosalicin (the molecular formula is C13H18O7; the compound has a molecular weight of 286.28, hereinafter referred to as IS), and the medicine IS does not show toxicity in an 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 a significant liver protection effect, and has a good application prospect in preparation of medicines for preventing and treating liver injury.

Description

Technical Field

[0001] The invention belongs to the field of medical technology, and particularly relates to the application of isosalicin in the preparation of 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] Isosalicin belongs to the phenolic glycosides and is widely found in natural medicines. Its isomer salicin has anti-inflammatory, anti-tumor, anticoagulant and anti-platelet aggregation effects, making it a natural substitute for aspirin. In the cosmetics industry, it is used to relieve skin irritation, reduce redness and swelling, promote the shedding of dead skin cells and inhibit acne formation. In terms of food and health care, salicin can also be used as a natural dietary supplement. However, the activity of isosalicin has rarely been reported, and there is currently no report on the use of isosalicin as a drug for the prevention and treatment of liver damage. Summary of the invention

[0004] In order to solve the above problems, the present invention provides the use of isosalicin in preparing liver injury medicines.

[0005] This is achieved specifically through the following technical solutions:

[0006] Application of isosalicin (hereinafter referred to as IS) in the preparation of liver injury drugs, wherein the molecular formula of isosalicin is C 13 H 18 O7; molecular weight is 286.28. The structural formula of isosalicin is as follows:

[0007]

[0008] A medicine for preventing and treating liver damage, containing isosalicin.

[0009] Furthermore, the liver injury drug is a drug for preventing and treating liver injury.

[0010] 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.

[0011] The IS used in the present invention can be extracted from plants (such as Pedicularis dawangensis) 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.

[0012] The chemical name of IS in the present invention is isosalicin (2-hydroxybenzylβ-D-glucopyranoside) and its molecular formula is C 13 H 18 O7, molecular weight is 286.28; scientific name is Isosalicin, structural formula is Figure 1 .

[0013] The beneficial effect of the present invention is that the present invention provides for the first time the use of isosalicin in the preparation of liver injury drugs. 13 H 18 O7; molecular weight is 286.28, hereinafter referred to as IS), the drug IS shows no toxicity within the investigated concentration range (6.25-100 μM), can significantly improve the cell survival rate of AML-12 hepatic parenchymal cells damaged by acetaminophen at the investigated concentration of 6.25-25 μM, has a significant liver-protecting effect, and has good application prospects in the preparation of drugs for the prevention and treatment of liver damage. BRIEF DESCRIPTION OF THE DRAWINGS

[0014] Figure 1 It is the chemical structure of IS.

[0015] Figure 2 The following is the result of the effect of different concentrations of IS on the survival rate of normal AML-12 liver cells. Indicates (n=3).

[0016] Figure 3 The following is the result of the effect of different concentrations of IS 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

[0017] 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.

[0018] Example 1 demonstrates the toxic effect of IS on normal hepatocytes AML-12

[0019] Experimental method: CCK-8 method to detect cell viability

[0020] AML-12 cells were cultured in a high-glucose medium DMEM 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 in a 5% CO2 incubator. AML-12 cells in the logarithmic growth phase were digested with 0.25% trypsin, and the cell density was adjusted to 3×10 with culture medium (10% FBS + 1% double antibody + 1% ITS + 40 ng / mL DXMS). 4 / mL, inoculated into 96-well plates, and the cells were divided into a control group (CON) and a drug group (6.25, 12.5, 25, 50, 100 μM). Each group had 3 replicate wells, 100 μL of cell suspension in each well, and a blank group with no cells but only culture medium was set up. After culturing for 24 hours at 37°C and 5% CO2 saturated humidity, the corresponding concentration of drugs was added and incubated for 24 hours. Subsequently, 10 μL of CCK-8 was added to each well, and the culture was continued for 1 hour under the same culture conditions. The absorbance (A) at 450 nm of each well was measured by an enzyme reader, and the cell survival rate was calculated according to the following formula:

[0021]

[0022] Experimental results ( Figure 2 ) It can be concluded that IS has no effect on the survival rate of normal liver cells AML-12 at a concentration of 6.25-100 μM. This shows that IS has no cytotoxicity to AML-12 cells at a concentration of 6.25-100 μM.

[0023] Example 2 demonstrates that IS protects normal hepatocytes from acetaminophen-induced liver injury

[0024] Experimental method: CCK-8 method to detect cell viability

[0025] The culture conditions were the same as those in Experiment 1, and the cells were divided into a control group (CON), a model group (APAP, 10mM), and a drug-treated group (6.25, 12.5, 25μM). Each group had 3 replicate wells, 100μL of cell suspension in each well, and a blank group with no cells but only culture medium was set up. After culturing for 24 hours at 37°C and 5% CO2 saturated humidity, APAP serum-free culture medium with a final concentration of 10mM was added to each well of the remaining groups except the control group and incubated for 24 hours. The drug-treated group was also incubated with drugs of corresponding concentrations. Subsequently, 10μL of CCK-8 was added to each well, and the culture was continued for 1 hour under the same culture conditions. The absorbance (A) at 450nm of each well was measured by an enzyme reader, and the cell survival rate was calculated according to the following formula:

[0026]

[0027] Experimental results ( Figure 3 ) It can be concluded that IS can significantly improve the survival rate of AML-12 hepatocytes damaged by acetaminophen in a concentration range of 6.25-25 μM, and it is concentration-dependent. This shows that IS has a good liver-protecting effect and has a good application prospect in the preparation of drugs for preventing and treating liver damage. In summary, the present invention provides for the first time the use of IS in the preparation of drugs for preventing and treating liver damage.

[0028] 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. The use of isosalicin in the preparation of liver injury drugs, characterized in that: The molecular formula of isosalicin is C 13 H 18 O7; molecular weight is 286.

28.

2. The use of isosalicin in the preparation of liver injury drugs according to claim 1, characterized in that: The structural formula of isosalicin is as follows:

3. The use of isosalicin in the preparation of liver injury drugs according to claim 1, 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 isosalicin.

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.

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