Isoflavone compound curing atherosclerosis through strengthening reverse cholesterol transport mechanism and composite thereof

A cholesterol reverse transport and atherosclerosis technology, applied in the direction of drug combinations, organic active ingredients, medical preparations containing active ingredients, etc., can solve the problem that the regulation mechanism has not been fully understood

Inactive Publication Date: 2008-06-25
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

This is mainly because the mechanism of positive cholesterol transport regulated by LDLR was first revealed and generally accepted, while the mechanism related to the reverse cholesterol transport process has only been revealed in recent years, and there are still many regulatory mechanisms that have not yet been fully understood. figure out

Method used

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  • Isoflavone compound curing atherosclerosis through strengthening reverse cholesterol transport mechanism and composite thereof
  • Isoflavone compound curing atherosclerosis through strengthening reverse cholesterol transport mechanism and composite thereof
  • Isoflavone compound curing atherosclerosis through strengthening reverse cholesterol transport mechanism and composite thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0052] Example 1 Preparation and structure identification of red cloverin

[0053] A) preparation of red cloverin

[0054] The dried flowering branches and leaves of leguminous plant red clover (Trifolium pratense L.) were purchased from Hunan Jiuhui Modern Chinese Medicine Co., Ltd., and compounds 1 (60 mg), 2 (52 mg), 3 (1.6 g), 4 (3.6 g), 5 (41 mg), 6 (52 mg), 7 (49 mg) and 8 (38 mg).

[0055] Among them, component 5 (referred to as F5) showed good up-regulation activity in the high-density lipoprotein receptor expression up-regulator screening model, and it was determined by EI-MS and ESI-MS; 3 OD 3 and CD 3 COCD 3 as solvent, carried out 1 H-NMR, 13 The determination of C-NMR, HSQC, HMBC and NOESY and the corresponding spectrum analysis identified the compound as 4'-methoxy-3',5,7-trihydroxy isoflavone, namely red cloverin.

[0056] Compound F5 is a white powder, which is easily soluble in methanol, acetone, and DMSO, but hardly soluble in water. Its physical and ...

Embodiment 2

[0066] Example 2 Screening model for up-regulators of high-density lipoprotein receptor expression Determination of red cloverin and genistein up-regulating high-density lipoprotein receptor expression activity

[0067] A) Construction of recombinant expression plasmid pGL3-CLAP

[0068] Strains and cell lines

[0069] E. coli DH5α was used for genetic manipulation of plasmid DNA. Liver cancer BEL-7402 cell line (purchased from Shanghai Wuli Biotechnology Co., Ltd.) was used to construct a screening model for human high-density lipoprotein receptor expression upregulators.

[0070] plasmid

[0071] pGEM-T (purchased from Promega) was used for cloning of PCR products. pGL3-Basic (purchased from Promega Company) is a reporter gene vector containing a firefly (Photinus pyralis) luciferase coding gene without a promoter, and is used for cloning of human high-density lipoprotein receptor regulatory sequence.

[0072] pGL3-control (purchased from Promega) contains SV40 promoter ...

Embodiment 3

[0097] Example 3 Effect of red cloverin on high-density lipoprotein receptors in liver cancer cells HepG2

[0098] A) Semi-quantitative RT-PCR method was used to study the effect of red clover on the transcription level of human high-density lipoprotein receptor before and after acting on HepG2 cells

[0099] ① Extraction of total cellular RNA

[0100] Human hepatoma cells HepG2 at 5×10 5 Inoculate 60mm cell culture plates at 37°C, 5% CO 2 After culturing for 24 hours under conditions, rinse the cells twice with ice-cold PBS, add serum-free MEM-EBSS medium containing 2.08M (DMSO content: 0.1%) red cloverin, and add 0.1% DMSO to the control plate corresponding medium. 37°C, 5% CO 2 After culturing under the condition for 24 hours, the total RNA of the cells was extracted with Trizol reagent (Invitrogen) (the specific operation steps were carried out according to the instructions of the kit). After the total cellular RNA was extracted, the integrity of the riboso...

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Abstract

The invention relates to the application of isoflavones red clover (form 1) and genistein (form 2). The invention is utilized for the preparation of medicine through strengthening the reverse cholesterol transport processed treatment and / or preventing the atherosclerosis. The medicine of strengthing the reverse cholesterol transport processed treatment and / or preventing the atherosclerosis comprises the medicine presented the liveness through the up-regulation of the high density lipoprotein receptor CLA-1 / SR-BI and the ATP cassette antigen ABCA1. The invention also relates to the drug composition of strengthening the reverse cholesterol transport processed treatment and / or preventing the atherosclerosis, the active constituents efficient chosen from the isoflavones red clover (form 1) and genistein (form 2) provided on the drug composition and optional carrier which is able to be adopted by the pharmacy.

Description

field of invention [0001] The present invention relates to the use of isoflavone compounds red cloverin (formula 1) and genistein (formula 2) for the preparation of drugs for treating and / or preventing atherosclerosis by enhancing cholesterol reverse transport mechanism, wherein said Drugs that enhance cholesterol reverse transport mechanism to treat and / or prevent atherosclerosis include drugs that up-regulate the expression activity of high-density lipoprotein receptor CLA-1 / SR-BI and drugs that up-regulate the expression activity of ATP-binding cassette transporter ABCA1. The present invention also relates to a pharmaceutical composition for treating and / or preventing atherosclerosis by enhancing the reverse cholesterol transport mechanism, which contains a therapeutically effective amount of cloverin (formula 1) and genistein (formula 2) active ingredient and optional pharmaceutically acceptable carrier. Background of the invention [0002] Cardiovascular disease has be...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/352A61P9/10A61P3/06
Inventor 司书毅洪斌姜威杨媛张忠兵高洁郑智慧王娟杨轶鲍羿高磊赵桂玉王丽非
Owner MEDICINE & BIOENG INST OF CHINESE ACAD OF MEDICAL SCI
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