Novel application of rutaecarpine compound

A technology of compound and application, which is applied in the field of new application of rutaecarpine compounds, can solve problems such as incurability, achieve good anti-atherosclerosis effect, and have broad application prospects

Active Publication Date: 2012-09-26
MEDICINE & BIOENG INST OF CHINESE ACAD OF MEDICAL SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But these things can slow down the progress of the disease, but they can't cure AD
Statins, which are widely used clinically, mainly achieve anti-atherosclerosis by inhibiting the biosynthesis of cholesterol and enhancing the LDL receptor regulation pathway of peripheral cells to choleste

Method used

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  • Novel application of rutaecarpine compound
  • Novel application of rutaecarpine compound
  • Novel application of rutaecarpine compound

Examples

Experimental program
Comparison scheme
Effect test

Example Embodiment

[0043] Example 1: The activity of evodia in the screening model of ABCA1 upregulator

[0044] ABCA1 up-regulator screening model principle: insert the upstream regulatory sequence of ABCA1 (ref|NT_008470.18|Hs9_8627, -819bp~+67bp) into the upstream of pGL3-BasicVector (Promega) luciferase reporter gene to obtain the recombinant plasmid pGL3-ABCA1, pGL3-ABCA1 and pcDNA3 were co-transfected into human hepatocarcinoma cell HepG2, and the stable transfected cell line was obtained by G418 screening, named ABCA1-LUC HepG2 cell. The change in fluorescence intensity was measured to indirectly reflect the upregulation activity of the drug on receptor gene expression .

[0045] Determination of cellular luciferase expression activity: The luciferase expression activity was determined using the Luciferase Assay System (Promega). The bioluminescence reaction catalyzed by firefly luciferase is as follows:

[0046]

[0047] Divide ABCA1-LUC HepG2 cells to 5×10 4 Cells / well were inoculated in a 9...

Example Embodiment

[0056] Example 2: The activity of evodiaeine on CLA1 upregulator screening model

[0057] The CLAP-LUC HepG2 cells (invention patent 200410029902.4, screening model of human high-density lipoprotein receptor expression up-regulator) were used as 5×10 4 Cells / well were seeded in a 96-well cell culture plate. After the cells adhered to the wall for about 6 hours, the medium was replaced with a serum-free MEM- containing a series of dilutions of evodia and evodia lactone at 200μl / well. EBSS medium (Hyclone; because of the two different mediums used by the people who built the model, it has been continued; because CLA1 is also involved in reverse cholesterol transport (RCT), up-regulating CLA1 and ABCA1 will be beneficial against AS, and it will be regulated by ABCA1 The sequence has partially identical regulatory elements; the two compounds are added in parallel). Note that the final concentration of DMSO in the wells of each concentration is maintained at 0.1% (added at the same ti...

Example Embodiment

[0067] Example 3: The agonistic activity of evodia subine on PPARγ

[0068] A) The effect of compounds on PPARγ transcriptional activation

[0069] The nuclear receptor PPARγ has two main domains: ligand binding domain (LBD) and DNA binding domain (DBD), each of which has independent functions. Using the PPARγ agonist model constructed in our laboratory (patent number 200710061911.5, new xanthone compounds and their preparation methods and uses), the ligand binding domain (LBD) of PPARγ and the DNA binding domain of yeast cell transcription factor GAL4 (DBD) was constructed as a fusion expression vector pBIND-PPARγ-LBD. The corresponding elements of 5×GAL4 were artificially synthesized and inserted upstream of the reporter gene to construct the reporter plasmid pG5-promotor-GAL4 (abbreviated as GAL4).

[0070] The GAL4 reporter plasmid and the constructed recombinant plasmid pBIND-PPARγ-LBD were tested by Lipofectamine TM 2000 (Invitrogen) mediated co-transfection of HepG2 cells,...

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Abstract

The invention relates to a composition containing a rutaecarpine compound and a novel application thereof, specifically to a compound selected from the formula 1-formula 2 or its combined medicine and stimulant and a novel application thereof. The novel application is the application for preparing the stimulant for raising ABCA1, CLA-1/SR-B1 and LXRalpha and activating PPARgamma and the application for preparing a medicine for treating and/or preventing atherosclerotic.

Description

field of invention [0001] The present invention relates to a new application of rutaecarpine (rutaecarpine, Rut), rutaecarpine (Evodine) or combination. The evodiamine compound is used for development and anti-atherosclerotic diseases. The present invention also relates to the use of the evodiamine compound for preparing ABCA1, CLA1, LXRα up-regulators and PPARγ agonists. Background of the invention [0002] Atherosclerosis (AS) is a kind of ischemic cardiovascular and cerebrovascular diseases. In recent years, the incidence of cardiovascular and cerebrovascular diseases has shown an obvious upward trend, and the death toll caused by the disease accounts for 1 / 3 of the global death toll. Clinical AS treatment drugs include vasodilation drugs, blood lipid adjustment drugs, antiplatelet drugs and so on. However, although these requirements can slow down the disease process, they cannot cure AD. Statins, which are widely used clinically, mainly achieve anti-atherosclerosis...

Claims

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Application Information

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IPC IPC(8): A61K31/519A61K31/366A61P9/10
CPCC07D471/14A61P9/10A61P43/00
Inventor 司书毅许艳妮刘祺蒋建东洪斌李卓荣姜威贺晓波徐扬李永臻来芳芳巫晔翔李霓王智敏刘伟
Owner MEDICINE & BIOENG INST OF CHINESE ACAD OF MEDICAL SCI
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