Application of vitisinol D in the preparation of xanthine oxidase inhibitory drugs
A technology of xanthine oxidase and drugs, which is applied in the direction of drug combinations, active ingredients of heterocyclic compounds, and pharmaceutical formulations, can solve problems such as hindering hypoxanthine and xanthine metabolism, aggravating glucose metabolism disorders, and uric acid metabolism disorders. Good xanthine oxidase inhibitory activity, avoid stomach pain, clear pharmacological effect
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Embodiment 1
[0021] The application of Vitisinol D in the preparation of xanthine oxidase inhibitory drugs, the inhibition of xanthine oxidase is manifested by inhibiting the activity of xanthine oxidase, reducing the generation of uric acid in the body, and treating hyperuricemia, gout, diabetic nephropathy, heart disease, etc. Prevention and treatment of diseases related to xanthine oxidase activity, such as vascular diseases.
[0022] The molecular formula of the Vitisinol D is C 28 h 22 o 6 , the chemical name is (+)-(1R,5S,6S,7S)-6-(3,5-Dihydroxyphenyl)-7-(4-hydroxyphenyl)-4-[(1E)-2-(4-hydroxyphenyl) ethenyl]bicyclo[3.2.1]oct-3-ene-2,8-dione, its structural formula is:
[0023]
[0024] The xanthine oxidase inhibitory drug is made of Vitisinol D as an active ingredient and other pharmaceutical excipients or carriers;
[0025] The xanthine oxidase inhibitory drug is an oral agent or an injection; wherein, the oral agent is any one or more of granules, capsules, tablets, powders,...
experiment example 1XO
[0028] Experimental example 1XO inhibitory activity test:
[0029] At 25°C, using a 96-well plate with a total reaction volume of 200 μL, first add 50 μL of enzyme solution (the final concentration of the reaction is 0.05 U / mL), 50 μL of sample solution, and after incubating at 25 °C for 15 minutes, add 50 μL of xanthine base solution (final concentration 150 μmol / L) to start the reaction. After incubating at 25°C for 20 min, 50 μL of 1 mol / L hydrochloric acid solution was added to terminate the reaction. Absorbance values were detected at 290 nm. Take the difference between this value and the OD value at the time of incubation for 0 min as the final detection result; detect the blank sample in the same way (that is, without the test drug, replace the sample solution with PBS containing 5% DMSO to determine the maximum reactivity of the enzyme) OD value, and the inhibition rate of each extract was calculated according to the following formula: inhibition rate (%)=(1-test s...
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