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Applications of five-ring triterpenoid compounds as oxidized squalene cyclase inhibitors

A technology of pentacyclic triterpenoids and oxidized dogfish, which is applied in the field of medicine and can solve the problems of toxicity, side effects, formation and malformation of lens epithelial cells.

Inactive Publication Date: 2014-11-12
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

These OSC inhibitors are all substrate analog inhibitors. Although they can effectively inhibit the biosynthesis of cholesterol, they can also cause a variety of side effects, including: skin and epididymal tissue lesions, cataract formation, and abnormal toxicity.
For example, the OSC inhibitor U18666A is toxic to lens epithelial cells and may lead to cataract formation (Toxicol. Pathol. 29, 174-179)

Method used

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  • Applications of five-ring triterpenoid compounds as oxidized squalene cyclase inhibitors
  • Applications of five-ring triterpenoid compounds as oxidized squalene cyclase inhibitors
  • Applications of five-ring triterpenoid compounds as oxidized squalene cyclase inhibitors

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] Blood lipid lowering effect of commercially available oleanolic acid tablets on patients with hyperlipidemia

[0040] Method: 30 patients with hyperlipidemia were subjected to a clinical trial of lowering blood lipid of commercially available oleanolic acid tablets in patients with hyperlipidemia. None of the subjects used any lipid-lowering drugs or related health care products. The subjects took oleanolic acid tablets orally after meals every day, 3 times a day, 4 tablets at a time, 20mg / tablet, administered 7 days a week, for 1 week continuously. 24 hours after the last administration, fast overnight, take blood, take appropriate amount of blood, routinely prepare serum, observe blood lipid related indicators: serum total cholesterol (TC), triglyceride (TG), high-density lipoprotein cholesterol (HDL -C) and low-density lipoprotein cholesterol (LDL-C).

[0041] Results: Table 1 shows the effect of oleanolic acid tablets on lowering blood lipids of 3 hyperlipidemia p...

Embodiment 2

[0046] Effects of commercially available oleanolic acid tablets on relevant physiological indicators in patients with hyperlipidemia

[0047] Method: 30 patients with hyperlipidemia were subjected to a clinical trial of lowering blood lipid of commercially available oleanolic acid tablets in patients with hyperlipidemia. None of the subjects used any lipid-lowering drugs or related health care products. The subjects took oleanolic acid tablets orally after meals every day, 3 times a day, 4 tablets at a time, 20mg / tablet, administered 7 days a week, for 1 week continuously. 24 hours after the last administration, fast overnight, take blood, take appropriate amount of blood, routinely prepare serum, observe relevant physiological indicators: alanine aminotransferase (ALT), aspartate aminotransferase (AST), glutamyl transpeptidase (GGT) ), creatine kinase (CK), urea (BUN), creatinine (Cr), uric acid (UA), C-reactive protein (CRP) and hypersensitive C-reactive protein (HsCRP).

...

Embodiment 3

[0053] Lipid-lowering effects of oleanolic acid, 3-acetyloleanolic acid, ursolic acid, and 3-acetylursolic acid on hyperlipidemic rats

[0054] Method: SD rats (200-220g, male) were adaptively fed for 1 week, and randomly divided into 2 groups: 6 normal control groups fed with standard diet and 36 model groups fed with high-fat diet. No intervention factors were applied to the normal control group. The model group was fed with high-fat diet (2% cholesterol, 0.5% sodium cholate, 3% lard, 0.2% propylthiouracil, 94.3% basic powder feed) for 2 weeks to form a high-fat model, and then randomly divided into vehicle group (6 rats) (fed with vehicle), atorvastatin calcium group (6 rats), oleanolic acid group (6 rats), 3-acetyl oleanolic acid group (6 rats), ursolic acid group ( 6) and 3-acetylursolic acid group (6). In addition to the normal control group, there were 7 groups in total. Among them, the atorvastatin calcium group was fed with 5 mg / kg / d of atorvastatin calcium, the ol...

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PUM

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Abstract

The invention relates to the field of medicines, and particularly relates to applications of five-ring triterpenoid compounds shown as general formulas (I), (II) or (III) or pharmaceutical acceptable salts or esters thereof as oxidized squalene cyclase inhibitors, especially applications in the field of preparation of anti-hypercholesterolemia medicines, anti-hyperlipidemia medicines, medicines for treating heart and cerebral vessels and antitumor medicines, and other fields. The R1 to R6 are defined in the specification.

Description

technical field [0001] The invention relates to the field of medicines, in particular to the use of a series of pentacyclic triterpenoids as oxidized squalene cyclase inhibitors, especially in the preparation of anti-hypercholesterolemia drugs, anti-hyperlipidemia drugs, and anti-cardiovascular and cerebrovascular diseases. Drugs, anti-tumor drugs, anti-mycotic drugs, anti-parasitic infection drugs, anti-gallstones and anti-diabetic drugs, etc. Background technique [0002] Many epidemiological studies have shown that hypercholesterolemia is one of the three major risk factors for atherosclerotic diseases, such as myocardial infarction, angina pectoris and cerebral infarction. Therefore, for the prevention or treatment of cardiovascular and cerebrovascular diseases related to atherosclerosis, it is very important to properly control the cholesterol level in the blood. At present, the drugs used clinically to lower blood cholesterol levels mainly include: drugs that can capt...

Claims

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Application Information

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IPC IPC(8): A61K31/56A61P3/06A61P9/10A61P9/00A61P33/00A61P1/16A61P35/00A61P3/10A61P31/10
Inventor 孙宏斌陈冬寅柳军邓洁徐畅
Owner CHINA PHARM UNIV
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