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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 cholesterol uptake, but they can only reduce the heart rate by 20% to 40%. Vascular events (Shah PK. Emerging non-statin LDL-lowering therapies for dyslipidemia and atherosclerosis. Rev Cardiovase Med, 2003, 4(3): 136-141), and currently statins have been found to be toxic to the liver and heart

Method used

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

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0043] Example 1: Activity of evodiamine on ABCA1 up-regulation screening model

[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 the luciferase reporter gene of pGL3-BasicVector (Promega Company) to obtain the recombinant plasmid pGL3-ABCA1. pGL3-ABCA1 and pcDNA3 were co-transfected into human liver cancer cell HepG2, and a stable transfected cell line was obtained by G418 screening, which was named ABCA1-LUC HepG2 cells. The up-regulation activity of the drug on receptor gene expression was indirectly reflected by measuring the change of its fluorescence intensity. .

[0045]Determination of cell luciferase expression activity: Luciferase expression activity was determined using a luciferase detection kit Luciferase Assay System (Promega). The bioluminescent reaction catalyzed by firefly luciferase is as follows:

[0046]

[0047] ABCA1-LUC HepG2 cells in...

Embodiment 2

[0056] Example 2: Activity of evodiamine on CLA1 up-regulation screening model

[0057] CLAP-LUC HepG2 cells (invention patent 200410029902.4, human high-density lipoprotein receptor expression up-regulator screening model) were mixed with 5×10 4 Each cell / well was seeded in a 96-well cell culture plate. After the cells had adhered to the wall for about 6 hours, the medium was replaced with 200 μl / well of serum-free MEM containing a series of diluted concentrations of evodiamine and evodiamine- EBSS medium (Hyclone; because the people who built the model used two different mediums, 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 the regulation of ABCA1 sequences have partially identical regulatory elements; both compounds are dosed in parallel). Note that the final concentration of DMSO in each concentration well is kept at 0.1% (and added at the same time as the drug ...

Embodiment 3

[0067] Example 3: Agonist activity of evodiamine on PPARγ

[0068] A) Effects 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 by our laboratory (Patent No. 200710061911.5, new xanone compounds and their preparation methods and uses), the ligand-binding domain (LBD) of PPARγ and the DNA-binding domain of the 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 into the upstream of the reporter gene to construct the reporter plasmid pG5-promotor-GAL4 (GAL4 for short).

[0070] The GAL4 reporter plasmid and the constructed recombinant plasmid pBIND-PPARγ-LBD were subjected to 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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