A kind of enzyme inhibitor and its application
A technology of inhibitor and urease, which is applied in the direction of medical preparations containing active ingredients, organic chemistry, pharmaceutical formulas, etc., can solve the problems of epigastric distension and pain, high cost of medication, antibiotic resistance, etc.
- Summary
- Abstract
- Description
- Claims
- Application Information
AI Technical Summary
Problems solved by technology
Method used
Image
Examples
Embodiment 1
[0024] Add 25 μL urease solution (10 U / mL), 25 μL (3R,3aR,6S,7aS,E)-4-hydrazine-2-isoamyl-3,6-dimethyloctahydrobenzo to a 96-well plate Furan-3-ol (1) and (3R,3aR,6S,7aS,Z)-4-hydrazine-2-isoamyl-3,6-dimethyloctahydrobenzofuran-3-ol (2) The mixture (each accounted for 50%) (0.25μM, 0.50μM, 1.00μM, 2.00μM, 4.00μM, prepared with DMSO-phosphate buffer solution), co-cultivated at 37°C for 30min, added 50μL of phosphate buffer containing urea 25mmol Solution, co-incubated at 37°C for 30min, then added 50μL A reagent (127mM phenol and 0.168mM sodium nitroprusside) and 50μL B reagent (125mM NaOH and 11.3mM NaOCl), co-incubated at 37°C for 30min, measured at 620nm Absorbance values. Set up blank group, normal control group, positive control group (acetohydroxamic acid) in addition, calculate the half inhibitory concentration IC of inhibitor to urease 50 0.79μM, positive control group acetohydroxamic acid IC 50 is 18.2 μM.
Embodiment 2
[0026] Add 25 μL urease solution (10 U / mL), 25 μL (2Z,3R,3aR,4E,6S,7aS)-4-hydrazine-3,6-dimethyl-2-(3-methyl Butenyl) octahydrobenzofuran-3-ol (3) and (2Z,3R,3aR,4Z,6S,7aS)-4-hydrazine-3,6-dimethyl-2-(3-methyl Butenyl) octahydrobenzofuran-3-ol (4) mixture (50% each) (0.25 μM, 0.50 μM, 1.00 μM, 2.00 μM, 4.00 μM, prepared with DMSO-phosphate buffer solution), in Co-cultivate at 37°C for 30 min, add 50 μL of phosphate buffer solution containing 25 mmol of urea, and co-cultivate at 37°C for 30 min, then add 50 μL of reagent A (127 mM phenol and 0.168 mM sodium nitroprusside) and 50 μL of reagent B (125 mM NaOH and 11.3 mM NaOCl), co-cultivated at 37°C for 30 min, and measured the absorbance value at 620 nm. A blank group, a normal control group, and a positive control group (acetohydroxamic acid) were also set up, and the half inhibitory concentration IC of the inhibitor to urease was calculated. 50 0.78μM, positive control group acetohydroxamic acid IC 50 is 18.2 μM.
PUM
Login to View More Abstract
Description
Claims
Application Information
Login to View More