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Compound with functions of blocking cholesterol esterification and lowering cholesterol

A cholesteryl ester and compound technology, applied in the field of compounds, can solve the problems of poor human body tolerance, myocardial damage, skin flushing, etc., and achieve the effects of increased effectiveness, stable action and wide adaptability

Inactive Publication Date: 2010-11-03
向定元
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Existing cholesterol-lowering drugs include bile cross-linking agents, niacinazines, and statins. Although they all have definite curative effects, they all have some defects in clinical use: the role of statins is to inhibit the cholesterol itself. Synthesis, has no inhibitory effect on the cholesterol absorbed in food, and clinically shows that the cholesterol-lowering effect is not high (called the ceiling effect), and sometimes even has no therapeutic effect on some people. In addition, statins also have many side effects
Bile cross-linking agents are a class of drugs that only affect the absorption of cholesterol but not the synthesis of cholesterol in the body. Some of them are not effective, and there are side effects such as constipation and poor human tolerance.
Niacinazide drugs have skin flushing after medication, and combined medication can cause myocardial damage and other side effects

Method used

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  • Compound with functions of blocking cholesterol esterification and lowering cholesterol
  • Compound with functions of blocking cholesterol esterification and lowering cholesterol
  • Compound with functions of blocking cholesterol esterification and lowering cholesterol

Examples

Experimental program
Comparison scheme
Effect test

Embodiment Construction

[0022] 1. Preparation and detection of cholestane submicroemulsion:

[0023] Prescription composition: 5α-cholesterane, soybean oil for injection, medium chain oil for injection, lecithin for injection, puloxamer F127, oleic acid, glycerin, water.

[0024] Process: Dissolve 5α-cholesterane in soybean oil, add medium-chain oil and oleic acid and mix to obtain an oil phase, add appropriate amount of lecithin, glycerin, and puloxamer into water and ultrasonically disperse it as the water phase, and vortex After mixing the oil phase and water phase, high-speed shearing for 3 minutes to obtain colostrum, high-pressure homogenizer for 2-3 cycles. Boil for 30 minutes to sterilize. Particle size and zeta potential were measured by Malvern particle size analyzer.

[0025] 2. The lipid-lowering effect of cholesterol liposome on high-fat-fed rabbit model.

[0026] A. Replication of animal model of atherosclerosis:

[0027] Adaptive feeding for 1 week, after observing no abnormality, ...

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PUM

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Abstract

The invention relates to a compound, in particular to the compound with the functions of blocking cholesterol esterification and lowering cholesterol. R in the basic structure of the compound represents a new group substituting hydroxyl, comprising -H. -C1, -PO3H3, -NO3, SO4H, -SH, -COOH, -COH, -CH3, -C2H5 and any other groups capable of substituting hydroxyl. In The invention, the compound substituting 3-hydroxyl in a cholesterol structure is used to demonstrate that the new mechanism has a competitive antagonistic effect at the first time in the world; and the action mechanism is to substitute cholesterol 3-hydroxyl, which can competitively interfere absorption of cholesterol in intestinal canal, synthesis in liver and utilization in an issue, thus lowering the low-concentration lipoprotein and the total cholesterol concentration in blood, and having the function of resisting fatty liver and atherosclerosis.

Description

Technical field [0001] The present invention involves a compound of compounds, which especially refers to a type of compound that blocks cholesterol and reduce cholesterol. Background technique [0002] Human atherosclerosis and coronary heart disease are diseases that affect people's health and even life.Medical research shows that the occurrence of such diseases is closely related to the increased cholesterol concentration in the body; cholesterol is a type of compound necessary for human metabolism. The main role is to participate in the maintenance of cell membranes, hormone synthesis, and bile formation.The concentration of cholesterol in the human body is affected by various ways such as food absorption and liver synthesis, cholesterol metabolism.Once the cholesterol concentration in the body increases, it may cause atherosclerosis and the occurrence of coronary heart disease.Therefore, treatment and prevention of such diseases must effectively reduce the cholesterol concen...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07J9/00A61K31/575A61K31/662A61P3/06A61P1/16A61P9/10
Inventor 张佳周艳萍殷宇芳李凯廖端芳向定元
Owner 向定元
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