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Application of baicalein and derivative 6,7-diacetyl radix scutellariae thereof

A technology of diacetyl baicalein and its derivatives, which is applied in the direction of medical preparations containing active ingredients, drug combinations, and pharmaceutical formulas, etc., to achieve the effect of improving bioavailability

Inactive Publication Date: 2016-10-12
PEKING UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0006] However, oral administration of baicalein has a wide range of hepatic and intestinal first-pass effects, mainly manifested in the glucuronidation and sulfation metabolic reactions of phase II metabolism

Method used

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  • Application of baicalein and derivative 6,7-diacetyl radix scutellariae thereof
  • Application of baicalein and derivative 6,7-diacetyl radix scutellariae thereof
  • Application of baicalein and derivative 6,7-diacetyl radix scutellariae thereof

Examples

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Embodiment 1

[0036] Example 1. Pharmacodynamic test of 6,7-diacetylbaicalein in preventing and treating hyperuricemia and the kidney damage caused by it

[0037] 1. Computer simulation predicts the combination of XOR and baicalein

[0038] Software: SYBYL 6.92, Chimera, Microsoft Excel, database: Protein Data Bank. Download the three-dimensional structure of the protein Xanthine Dehydrogenase from Bovine Milk with InhibitorTEI-6720Bound (PDB ID: 1N5X) from the PDB database (which contains the structure of the original ligand TEI). The ligand and receptor were split with Chimera and the receptor protein was saved as a file in PDB format. Use SYBYL software to draw the ligand TEI structure and save it in mol2 format. Put the 2 pdb and 1 mol2 files into a new folder for later use. Open the SYBYL software, import the 1N5X.pdb file (including meta-ligands), delete the B chain, and leave only the A chain as the docking material. Select the natural ligand TEI, and generate an active site pock...

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Abstract

The invention discloses application of baicalein and a derivative 6,7-diacetyl radix scutellariae thereof to preparation of medicine for treating hyperuricemia and / or preparation of medicine for treating renal injury caused by hyperuricemia. The baicalein and the derivative 6,7-diacetyl radix scutellariae thereof can remarkably lower the uric acid level, the creatinine level and the urea nitrogen level of hyperuricemia , and the 6,7-diacetyl radix scutellariae has a remarkable protection function on the kidney. The baicalein has a first-pass effect of liver sausage, the derivative 6,7-diacetyl radix scutellariae of the baicalein can inhibit the first-pass effect of liver sausage, and bioavailability is improved.

Description

technical field [0001] The present invention relates to the use of baicalein and its derivative 6,7-diacetylbaicalein. Background technique [0002] 1. General characteristics of baicalein and its derivative 6,7-diacetylbaicalein [0003] The structural formula of baicalein is shown in formula I: [0004] [0005] Traditional medicine Scutellaria baicalensis is the dry root of Lamiaceae plant Scutellaria baicalensis Georgi. "The Pharmacopoeia of the People's Republic of China" records that Scutellaria baicalensis has the effects of "clearing away heat and dampness, purging fire and detoxification, stopping bleeding, and preventing miscarriage", and is one of the commonly used drugs in traditional Chinese medicine. Baicalein is one of the flavonoids with the highest content in Scutellaria baicalensis. Its chemical name is 5,6,7-trihydroxyflavone. The National Pharmacopoeia Committee officially named it baicalein (English name is baicalein). Studies have shown that after...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/352A61P19/06A61P13/12
CPCA61K31/352
Inventor 周虹杨宝学孟晓璐
Owner PEKING UNIV
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