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Application of 3-aryl coumarin compound

An aryl coumarin and compound technology, which is applied in the directions of active ingredients of heterocyclic compounds, drug combinations, metabolic diseases, etc., can solve the problems of poor therapeutic effect, large side effects, and single action target.

Inactive Publication Date: 2021-01-05
INST OF PHARMACY SHANDONG PROV ACAD OF MEDICAL SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] In terms of the treatment of vascular calcification, there is currently no means to reverse vascular calcification, but a variety of interventions can be used to slow or delay the progression of vascular calcification, such as controlling traditional risk factors such as hyperglycemia, blocking AGEs production, AGEs / RAGE However, these interventions still have the disadvantages of single target, large side effects, and poor therapeutic effect. Therefore, the treatment of vascular calcification is the difficulty and hot spot of current research.
In recent years, a variety of natural products have been reported to have the effect of protecting blood vessels. Coumarin and flavonoids have attracted much attention in recent years because of their good AGEs production inhibition, anti-oxidation and anti-inflammatory activities. Among them, umbelliferone, quercetin Cortex, soybean isoflavones, etc. are considered to have good blood vessel protection effects and have been studied and reported many times, but because of their weak activity, or side effects such as cytotoxicity and carcinogenicity, it is difficult to directly make medicines

Method used

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  • Application of 3-aryl coumarin compound
  • Application of 3-aryl coumarin compound
  • Application of 3-aryl coumarin compound

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] Example 1: Determination of the toxicity of two compounds to cells

[0028] (1) Human aortic vascular smooth muscle cells of 2-8 generations were cultured, a single cell suspension was made into a culture medium containing 10% fetal bovine serum, and 5000 cells per well were inoculated into a 96-well plate with a volume of 200 ul per well.

[0029] (2) Set up 7 groups, namely: normal group, Ⅰ-6.25ug, Ⅰ-12.5ug, Ⅰ-25ug, Ⅱ-6.25ug, Ⅱ-12.5ug, Ⅱ-25ug. Six replicate wells were set up for each drug group. The same as the general culture conditions, culture 24h, 48h.

[0030] (3) After the incubation, add 20ul of MTT solution (5mg / ml, prepared with PBS) to each well.

[0031] Continue to incubate for 4 hours, terminate the culture, carefully aspirate and discard the culture supernatant in the well, for suspension cells, centrifuge and then aspirate and discard the culture supernatant in the well. Add 150ul DMSO to each well and shake for 10 minutes to fully melt the crystals....

Embodiment 2

[0036] Example 2: Calcification induction of human vascular smooth muscle cells

[0037] (1) Preparation of calcification induction solution

[0038] Weigh 20 mg of bovine serum albumin and dissolve it in 50 mmol / L PBS (pH7.4) to prepare a buffer solution of bovine serum albumin in PBS (pH7.4) with a final concentration of 10 mg / mL. Weigh 79.2 mg of glucose, dissolve it in 2 ml of distilled water, and prepare a glucose solution with a final concentration of 0.2 mol / L. The above two solutions were mixed and filtered, and 0.02% double antibody was added to prevent bacterial growth. The above mixed solution was incubated at 37°C for 14 days, and the excitation wavelength and emission wavelength were set to 350nm and 420nm respectively using a fluorescence spectrophotometer, and the measured fluorescence intensity of AGE was as follows:

[0039]

[0040] (2) Calcification induction of human aortic smooth muscle

[0041] Human aortic vascular smooth muscle cells (HAVSMCs) wer...

Embodiment 3

[0044] Example 3: Determination of the inhibitory effect of two compounds on the activity of alkaline phosphatase in calcified cells

[0045] 1. Determination principle of alkaline phosphatase activity in vitro

[0046] Alkaline phosphatase is widely distributed in the bones, intestines, kidneys, liver, placenta and other tissues of the human body. Under alkaline conditions, Para-nitrophenyl phosphate (pNPP) can generate para-nitrophenol under the action of alkaline phosphatase. Para-nitrophenol is a yellow product under alkaline conditions, and the absorbance can be detected at 400-415nm. The deeper the yellow color of the product, the higher the alkaline phosphatase activity and the higher the absorbance value, otherwise the lower the enzyme activity.

[0047] 2. Preparation of reaction solution

[0048] (1) Reagent preparation: Take out all reagents and return to room temperature for use.

[0049] (2) Preparation of chromogenic substrate solution: Take a tube of chromog...

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Abstract

The invention discloses application of 3-arylcoumarin compounds shown in a structural formula I and / or a structural formula II in preparation of a medicine for preventing and / or treating diabetic vascular calcification, and belongs to the field of medicine production.

Description

technical field [0001] The invention relates to the field of medicine production, and specifically provides the application of 3-arylcoumarin compounds in the preparation of diabetes and related vascular calcification medicines. Background technique [0002] Diabetes mellitus is a chronic, multifactorial metabolic disorder characterized by hyperglycemia, insulin resistance, and pancreatic β-cell dysfunction. Diabetic patients are very prone to cardiovascular diseases. Cardiovascular complications are the main cause of death in diabetic patients. This has a great relationship with vascular calcification, and vascular calcification is widely present in patients with diabetes. Compared with the general population, the index of vascular calcification in diabetic patients is significantly higher, mainly in coronary arteries and lower extremity vessels, and vascular calcification is also closely related to the prognosis of atherosclerosis and heart failure. Vascular calcification...

Claims

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Application Information

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IPC IPC(8): A61K31/37A61P9/14A61P9/10A61P3/10
CPCA61K31/37A61P3/10A61P9/10A61P9/14
Inventor 孙捷李雨霏牟艳玲王晓静王兵
Owner INST OF PHARMACY SHANDONG PROV ACAD OF MEDICAL SCI
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