Application of succinic acid and salt or ester of succinic acid in preparation of monoamine oxidase inhibitor
A technology of monoamine oxidase and succinate, which is applied in the direction of active ingredients of esters, medical preparations containing active ingredients, organic active ingredients, etc., can solve the problems of few types of monoamine oxidase inhibitors and obvious toxic and side effects, and achieve low biological toxicity, high efficiency effect
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Embodiment 1
[0024] Embodiment 1 Preparation of monoamine oxidase A and monoamine oxidase B solutions
[0025] Preparation of MAO solution:
[0026] Firstly, Wistar aged male rats (Shanghai Experimental Animal Center, Chinese Academy of Sciences) were killed by myelotomy, and the liver was removed under aseptic conditions, washed in pre-cooled potassium phosphate buffer (0.2mol / L pH 7.4), and kept at -85 Store under the condition of ℃ until use. Homogenize the liver tissue (5g) in 0.3mol / L sucrose solution at a volume ratio of 1:40 (w / v), and homogenize until it is basically uniform. Centrifuge the homogenate at low temperature and high speed at 1000×g for 10 minutes , retain the supernatant, and then centrifuge the supernatant at 10,000×g for 30 minutes to retain the precipitate. During the whole process, the temperature should be controlled within the range of 0-4°C.
[0027] Then resuspend the precipitate in 4mL 0.3mol / L sucrose solution, mix thoroughly, add to 40mL 1.2mol / L sucrose s...
Embodiment 2
[0030] Example 2 In vitro determination of the inhibitory effect of succinic acid on monoamine oxidase
[0031] Wherein the MAO solution, MAO-A solution and MAO-B solution are prepared in Example 1.
[0032] Preparation of succinic acid solution: prepare succinic acid solutions with different concentration gradients, the concentration of which is 0.1mg / mL~20mg / mL.
[0033] Substrate configuration: prepare 1 mmol / L kynuramine (kynurenine, Sigma, USA).
[0034] 1. Inhibition of monoamine oxidase (MAO) by succinate
[0035] Add 100 μL potassium phosphate (0.1mol / L pH 7.4) buffer solution, 30 μL test sample (the above succinic acid solution), 20 μL MAO solution and 30 μL 1 mmol / L substrate (the above kynuramine solution) to the 96-well microtiter plate. solution), mix for 30s. At the wavelength of 360nm, measure the absorbance value of the mixed solution at the beginning (A 1 ), and then measure the absorbance value at 37°C for 40 minutes (A 2 ); the absorbance value of the b...
Embodiment 3
[0046] Embodiment 3 In vitro determination of the inhibitory effect of monoethyl succinate on monoamine oxidase
[0047] Wherein said MAO solution, MAO-A solution and MAO-B solution are prepared in Example 1, and the determination method is the same as in Example 2.
[0048] Determination results: When the concentration of monoethyl succinate is 0.1mg / mL, it has in vitro inhibitory effect on MAO, MAO-A, and MAO-B, and when the concentration reaches 0.5mg / mL, the in vitro inhibitory effect on the three is even greater. Significantly, and the inhibition rate increased with the increase of concentration.
[0049] When the concentration of monoethyl succinate is 0.5mg / mL to 10mg / mL, the inhibition rate of MAO is 6.33% to 67.3%, and its IC 50 It is 42.2μmol / L.
[0050] When the concentration of monoethyl succinate was 0.5 mg / mL to 20 mg / mL, the inhibition rate of MAO-A was 12.76% to 74.73%, and its IC 50 was 40.6μmol / L; the inhibition rate to MAO-B was 22.17% to 80.88%, and its ...
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