Method for screening phosphodiesterase (PDE) inhibitor

Abstract

The invention provides a method for screening a phosphodiesterase (PDE) inhibitor. The method comprises the following steps of: after the reaction of extracts of the traditional Chinese medicine with the PDE sample, detecting the activity of the PDE, and judging target points with selective action for inhibiting the activity of the PDE; and judging the effective ingredients for inhibiting the PDE according to the change of finger print of the extracts of the traditional Chinese medicine, thus screening the selective phosphodiesterase inhibitor. The method comprises the steps of preparation of extracts of the traditional Chinese medicine, preparation of PDE samples, cell incubation, detection of the activity of PDE and detection of finger print of extract samples of the traditional Chinese medicine; the preparation of the PDE samples comprises preparation of PDE samples of animal tissues, preparation of PDE samples of animal skeletal muscle and preparation of PDE samples of animal neutrophilic granulocyte.

Description

technical field [0001] The invention belongs to the field of screening of traditional Chinese medicine components, and in particular relates to a method for screening phosphodiesterase (PDE) inhibitors; the method detects the activity of the PDE after reacting Chinese medicine extracts with PDE samples respectively, and judges the selection for inhibiting the activity of PDE Sexual action targets; and then according to the changes in the fingerprints of traditional Chinese medicine extracts, the active ingredients that inhibit PDE are judged, so as to screen out selective phosphodiesterase inhibitors. Background technique [0002] Phosphodiesterase (PDE for short) is a key component in cAMP / PKA and cGMP / PKG signaling pathways. According to the specificity, sensitivity, enzyme kinetics and amino acid sequences of agonists and inhibitors, 11 PDE family members have been discovered and identified in mammalian tissue cells, and each member encodes 1 to 4 different genes. Splic...

AI Technical Summary

Problems solved by technology

Due to the large number of traditional Chinese medicines and complex components, this method of screening PDE inhibitors from traditional Chinese medicines has the disadvantages of high cost, difficulty, long cycle, and heavy workload, which seriously limits the screening of PDE-specific inhibitors with special pharmacological activity in the field. It is imperative to design a new and rapid technology for screening PDE-specific inhibitors from complex components of traditional Chinese medicines for clinical application

[0006] In addition, since there are more than 50 kinds of PDE proteins, both purification and cloning expression require a lot of long-term work

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