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Method for screening out active natural medicines by using immobilization model of alpha-glucosaccharase

A technology of glucosidase and natural medicine, applied in the field of new drug screening chemical process, can solve the problems such as the false positive phenomenon of N-terminal inhibitor and the difference of pharmacological effect of enzyme inhibitor cannot be ruled out.

Inactive Publication Date: 2005-10-26
SHANGHAI UNIV
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Problems solved by technology

The traditional in vitro enzyme inhibitor activity test cannot rule out the false positive phenomenon of N-terminal inhibitors, which makes the pharmacological effects of enzyme inhibitors in vivo and in vitro different.

Method used

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0016] The specific process and steps of this embodiment are as follows:

[0017] 1. Immobilization of α-glucosidase: use trihydroxymethylphosphine as a crosslinking agent and chitosan as a carrier to immobilize α-glucosidase;

[0018] 2. Make an inhibitor screening model: put the above-mentioned immobilized α-glucosidase into a chromatographic column with a diameter of 0.8 cm and a length of 8 cm, and add p H 6.8 Potassium phosphate buffer solution, stored at 4°C, constitutes a screening model;

[0019] 3. Validation of the model: Use the representative α-glucosidase inhibitor acarbose to verify the validity of the screening model. Insert the lower end of the column into a small tube with a plunger tightly, and insert a syringe into the upper end of the column. After the buffer solution in the medium was pressed down to about 0.4cm from the top of the column, 50μl of 4-nitrophenyl-α-D-glucopyranoside (0.116mol / L) and a certain amount of acarbose solution (250mg / L), gently ...

Embodiment 2

[0026] The specific process and steps of this embodiment are basically the same as those of the above-mentioned embodiment 1, except that in step 5, the screening object of the immobilized enzyme screening model is the traditional Chinese medicine Guangxi jerky. The reaction system is a mixture of methanol and pH3.6 buffer in a ratio of 1:2. Table 2 lists the data of the immobilized enzyme screening model for screening D.

[0027] Table 2 Immobilized enzyme screening model screening data of blood in Guangxi (n=5)

[0028] Inhibitory dose (mg)

[0029] The above data show that Dried Blood from Guangxi has a significant and strong inhibitory effect on α-glucosidase, which is consistent with the literature reports.

[0030] In addition, as a reference, the experimental data obtained by screening the immobilized enzyme screening model with acarbose, which is a representative α-glucosidase inhibitor, are listed in Table 3.

[0031] Inhibitory ...

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Abstract

This invention relates to a method of screening active natural medicines by immobilization model of alpha-glucosaccharase. It belongs to chemical craft domain of new drug screening, characters: immobilizing alpha-glucosaccharase, make screening model of its inhibitor, and validate model efficiency efficaciously of representative alpha-glucosaccharase inhibitor acarbose. We use this model to select Huzhang and Xuehe, first fix the alpha-glucosaccharase, enclose it into chromatographic column with pH=6.8 KxH3-xPO4 buffer solution at 4Deg.C. When selecting Huzhang and Xuehe, we add 4-nitrobenzene- alpha -galactopyranose, Huzhang and Xuehe, and then collect the buffer solution eluted, test its absorption in the Ultraviolet spectrophotometer, count the suppression rate by formulae, draw work curve of the corresponding suppression solution density, obtain half suppression solution density IC50 at the point of 50% suppression rate, as the thereunder of selection material activity.

Description

technical field [0001] The invention relates to a method for screening active natural medicines by using an immobilized α-glucosidase model, and belongs to the technical field of new drug screening chemical technology. Background technique [0002] α-glucosidase can catalyze the hydrolysis of α-1.4-glucosidic bonds, and hydrolyze oligosaccharides such as maltose and sucrose in the small intestine. Inhibiting the activity of α-glucosidase can slow down the production and absorption of glucose, reduce the peak blood sugar after meals, adjust the blood sugar level, and regulate the production of fat while regulating glucose metabolism. α-glucosidase inhibitors have become a research hotspot in medicinal chemistry in recent years. The traditional method for screening α-glucosidase inhibitors is to use free α-glucosidase simultaneously with its substrate (4-nitrophenyl-α-D-glucopyranoside (PNPG)) and with the inhibitory agent effect. [0003] It is reported that when the α-glu...

Claims

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Application Information

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IPC IPC(8): C12Q1/18
Inventor 雍克岚吕敬慈卢大胜陈旭顾慧娟
Owner SHANGHAI UNIV
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