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Applications of xanthone compounds and derivatives thereof in preparing medicines for lowering blood lipid

A technology of compounds and derivatives is applied in the application field of xanone compounds and their derivatives in the preparation of hypolipidemic drugs, and can solve the problems of liver injury, high recurrence rate, organic lesions and the like

Inactive Publication Date: 2017-11-21
SHANGHAI JIAOTONG UNIV SCHOOL OF MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although the above-mentioned lipid-lowering drugs have definite curative effects, most of them have a single effect, and have disadvantages such as easy to cause liver damage, organic disease, easy rebound, high recurrence rate, and need for long-term medication, which has brought great limitations to clinical medication.

Method used

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  • Applications of xanthone compounds and derivatives thereof in preparing medicines for lowering blood lipid
  • Applications of xanthone compounds and derivatives thereof in preparing medicines for lowering blood lipid
  • Applications of xanthone compounds and derivatives thereof in preparing medicines for lowering blood lipid

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0095] Example 1. The effect of ketone compounds on the protein expression of proprotein convertase subtilisin 9 (PCSK9)

[0096] Using liver HepG2 cells, planted in 6-well plates, the number of cells per well is about 60,000, divided into solvent group, α-mangostin group, 13179-11-8, 76996-27-5, β-mangostin , Γ-Mangostin, CAS number 127716-76-1, 84955-04-4, 21044-78-0, 105742-86-7, 21044-85-9, 19274-65-8, 130774-33- 3. Groups 20245-38-9, 112649-21-5 and 3542-72-1. The dosage of the drug is 1000ng / mL. After 24 hours of action, the culture medium is discarded, and 100μL of cell lysate is added for WesternBlot experiment. The primary antibody dilution concentration is PCSK9 (Origin Rabbit) 1:1000. After incubating overnight at 4℃, wash with TBST For 3 times, the secondary antibody is Donkey anti-Rabbit 1:3000 and incubated for 2 hours at room temperature. After washing 3 times with TBST, the color develops. The experimental results show that α-mangostin, 13179-11-8 and 76996-27-5...

Embodiment 2

[0097] Example 2. The effect of ketone compounds on plasma triglyceride levels

[0098] The 7-month-old SAMP8 mice were divided into a physiological saline group and a α-M nanoparticle-loaded group, with 9 mice in each group. SAMR mice served as normal controls and were given saline. Mice were administered by tail vein injection at a dose of 1 mg / kg α-M, 0.2 mL for each injection for 4 weeks. Blood was taken before and after administration, and the plasma triglyceride level was detected by lipidomics method. Animals given normal saline, as the month age increases from 7 months to 8 months, the plasma triglyceride level increases, and the plasma triglyceride ratio after administration / pre-administration is about 1.5, an increase of 50%; and In the α-M nanoparticle-loaded group, as the month age increased from 7 months to 8 months, plasma triglyceride levels did not increase significantly, and some types even declined, such as Figure 4 As shown, the ratio of plasma triglycerides...

Embodiment 3

[0099] Example 3. The effect of ketone compounds on plasma triglyceride levels

[0100] Kunming mice were orally administered at a dose of 20 mg / kg α-M for 2 weeks. Fasting plasma samples were taken before administration and after continuous administration for 2 weeks, and the level of triglycerides in plasma was determined by lipidomics method. Such as Figure 5 As shown, plasma triglyceride levels with different numbers of double bonds and fat chain length decreased significantly after 2 weeks of administration. β-Mangostin, γ-Mangostin, CAS No. 13179-11-8, 76996-27-5, 127716-76-1, 84955-04-4, 21044-78-0, 105742-86-7 The compounds of, 21044-85-9, 19274-65-8, and 130774-33-3 are similar to α-mangostin, and mouse plasma triglycerides also showed a downward trend after 2 weeks of administration.

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Abstract

The invention relates to novel applications of xanthone compounds (as shown in the general formula I), derivatives, enantiomers, diastereoisomers and racemes of the xanthone compound, mixtures of the xanthone compounds, the derivatives, the enantiomers, the diastereoisomers and the racemes of the xanthone compounds, pharmaceutically acceptable salts of the xanthone compounds, and compositions of the pharmaceutically acceptable salts in preparing products for preventing and / or treating hyperlipidemia or preparing products for inhibiting pro-protein convertase subtilisin / kexin 9 (PCSK9).

Description

Technical field [0001] The invention relates to a new application of ketone compounds and their derivatives in the preparation of products for reducing blood lipids. Background technique [0002] In modern society, health problems such as obesity, high blood pressure, and hyperlipidemia have become increasingly serious. Hyperlipidemia is a common multiple metabolic disease, often manifested as high serum total cholesterol (TC) or triglyceride (TAG) levels, which are common in middle-aged and elderly people, but with changes in diet and increased alcohol consumption , The prevalence of youth is also increasing year by year. Atherosclerosis caused by hyperlipidemia is the main cause of coronary heart disease, hypertension, and cardiovascular and cerebrovascular diseases, and is closely related to diabetes. Intervention of dyslipidemia is the basis for primary and secondary prevention of cardiovascular disease. Therefore, research and development of new blood lipid-lowering drugs ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/352A61P3/06A23L33/105
CPCA23V2002/00A61K31/352A23V2200/3262A23V2250/21
Inventor 高小玲胡朦王小林陈红专
Owner SHANGHAI JIAOTONG UNIV SCHOOL OF MEDICINE
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