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Traditional Chinese medicine monomer component medicine for inhibiting PCSK9 target, and application of polydatin in preparation of PCSK9 target inhibition medicines

A technology of polydatin and drugs, which is applied in the field of traditional Chinese medicine monomer components, can solve problems such as adverse reactions and restrictions on the use of insulin resistance regulation, and achieve the effect of improving metabolic disorders

Inactive Publication Date: 2016-05-04
SUN YAT SEN UNIV
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AI Technical Summary

Problems solved by technology

Insulin sensitizers such as pioglitazone and biguanides are commonly used in existing drugs for improving insulin resistance. The clinical effects of these drugs need to be further improved. response, so that their use in the regulation of insulin resistance is also limited

Method used

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  • Traditional Chinese medicine monomer component medicine for inhibiting PCSK9 target, and application of polydatin in preparation of PCSK9 target inhibition medicines
  • Traditional Chinese medicine monomer component medicine for inhibiting PCSK9 target, and application of polydatin in preparation of PCSK9 target inhibition medicines
  • Traditional Chinese medicine monomer component medicine for inhibiting PCSK9 target, and application of polydatin in preparation of PCSK9 target inhibition medicines

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Experimental program
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Embodiment Construction

[0028] 1. Materials and methods

[0029] 1.1 Insulin resistance cell model and polydatin intervention

[0030] HepG2 cells were purchased from ATCC and cultured in 25mM DMEM high-glucose medium (Gbico, Invitrogen Corporation,) plus 10% fetal bovine serum (Hyclone) at 37°C and 5% CO2. When the cells grew to a density above 80%, they were digested with 0.25% trypsin-EDTA (Gibco, USA), and passaged at a ratio of 1:3, once every 2 days. Palmitic acid (PA, Sigma, USA) used for modeling was added to 0.1M NaOH solution and dissolved at 70°C, then mixed with 20% BSA (BSA, lowfreefattyacid, MPBiomedical, USA) in a certain volume, and the mixture was heated at 55 ℃ water bath for 1 hour, and stored at -20 ℃ in the form of 10mM stock solution after cooling. HepG2 cell drug treatment group was pretreated with polydatin (Beijing Weiye Kechuang) for 1 hour, and then added 0.25mM palmitic acid to continue culture for 24 hours. The normal control group was added with 5% BSA as a control.

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Abstract

The invention relates to a traditional Chinese medicine monomer component medicine capable of relatively specifically influencing a pro-protein convertase subtilisin / kexin 9 (PCSK9) target and improving insulin resistance, and an application of the medicine especially polydatin in the preparation of PCSK9 target inhibition medicines. The polydatin can relatively specifically inhibit the expression and activity of the PCSK9 in insulin resisting hepatocytes in order to improve the insulin induced metabolism disorder; and polydatin molecules can be combined with the active pocket of a PCSK9 crystal structure, and can form stable hydrogen bonds together with a plurality of amino acid residues.

Description

[technical field] [0001] The invention relates to a traditional Chinese medicine monomer component drug that can relatively specifically affect the target of proprotein convertase subtilisin 9 (PCSK9) and improve insulin resistance, and the drug, especially polydatin, is used in the preparation of proprotein convertase subtilisin 9 (PCSK9) target inhibitory drug application. [Background technique] [0002] Diabetes is one of the diseases with the fastest-growing morbidity worldwide, and the third-highest mortality disease after cardiovascular diseases and tumors. The World Health Organization estimates that by 2030, the number of diabetic patients worldwide may exceed 360 million, of which 90% to 95% are type 2 diabetes. China is the second largest country with diabetes in the world. The "Prevalence of Diabetes in China's Population" released by the internationally authoritative journal "New England Journal of Medicine" in 2010 shows that the age-standardized incidence of d...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/7034A61P3/10A61P5/50
Inventor 黄河清王雨李婕叶建涛刘培庆
Owner SUN YAT SEN UNIV
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