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Monogalactosyl diacyl glyceride, and preparation method and application thereof

A technology of lactosyl diacylglycerol and acyl, applied in the field of preparation of monogalactosyl diacylglyceride

Active Publication Date: 2017-07-28
OCEAN UNIV OF CHINA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, there is no literature report on the use of MGDG as a PPARα agonist, especially a dual agonist of PPARα / γ

Method used

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  • Monogalactosyl diacyl glyceride, and preparation method and application thereof
  • Monogalactosyl diacyl glyceride, and preparation method and application thereof
  • Monogalactosyl diacyl glyceride, and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033] Example 1: Extraction preparation and structural identification of monogalactosyldiacylglyceride

[0034] Take 2000g of Hijiki, extract with 10 times the volume of 75% ethanol under reflux for 2h, repeat 3 times. Combine the extracts, filter and concentrate until there is no alcohol smell, extract 3 times with an equal volume of ethyl acetate, combine the extracts, concentrate to obtain 33.26 g of extract. The extract was dissolved in ethyl acetate, mixed with 41g 200-300 mesh silica gel H, and subjected to silica gel column chromatography, using dichloromethane-methanol as a solvent for gradient elution, wherein dichloromethane-methanol (v / v 95:5 ) to elute the resulting components, and then through Sephadex LH-20 gel column chromatography (dichloromethane-methanol 1:1) and silica gel column chromatography to obtain a mixture of monogalactosyl diacylglycerides (MGDG) , measure its 1 H-NMR spectrum and 13 C-NMR spectrum (such as figure 1 and 2 shown).

[0035] accor...

Embodiment 2

[0039] Example 2: Activation of PPARα and PPARγ by MGDG

[0040] Transcriptional activation of PPARα and PPARγ was detected using a dual-luciferase reporter gene assay. 293T cells were inoculated in 96-well plates with DMEM medium (10% FBS, without antibiotics). After 8-12 hours, the cells grew to about 60%. The medium was not changed, and the plasmid was directly transfected according to the instructions of lipo2000. The total amount of plasmid was 0.075 g / well (0.05 μg PPRE, 0.005 μg internal control pRL-TK and 0.02 μg PPARα / γ). The amount of lipo2000 used was 2.5 times the mass of the transfected plasmid (2.5*0.075L=0.1875 μL / well). The plasmid and lipo2000 were mixed in 25 μL / well optim medium in advance. After 12 hours of transfection, the positive drug (the positive drug for PPARγ is rosiglitazone at a concentration of 1 μM, and the positive drug for PPARα is WY14643 at a concentration of 10 μM) and the MGDG obtained in Example 1 were added. 24 hours after adding the ...

Embodiment 3

[0041] Example 3: Activation of MD1-MD6 on PPARα and PPARγ

[0042] The transcriptional activation of PPARα and PPARγ was detected by dual-luciferase reporter gene analysis technology, and the specific method was the same as that in Example 2. The drugs added are MD1-MD6 prepared in Example 1. The results are shown in Table 2.

[0043] Table 2 Activation of PPARα / γ by MD1~MD6

[0044]

[0045]

[0046] Note: Compared with the blank group, "*"P<0.05; "**"P<0.01; "***"P<0.001.

[0047] The results showed that the above compounds could activate PPARα and / or PPARγ to varying degrees. In particular, MD5 (compound of formula (II)) exhibited significant PPARα / γ dual agonism.

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Abstract

The invention discloses monogalactosyl diacyl glyceride, and a preparation method and an application thereof for preparing a PPAR (alpha) agonist and a PPAR (alpha / gamma) double agonist. R1 and R2 represent acyl fragments which are straight chain or branch chain fatty acids with 1-30 carbon atoms; and the acyl fragments contain 0-15 cis- or trans- double bonds. According to the invention, the agonistic effect of monogalactosyl diacyl glyceride on PPAR (alpha) and the double agonistic effect of the monogalactosyl diacyl glyceride on PPAR(alpha / gamma) are found for the first time. The application value of the compounds in preventing and treating PPARs related diseases is disclosed. In addition, active ingredients which are beneficial for cardiovascular health, of seaweed, are found and separated, and material basis for efficacy and functional factors for developing seaweed drugs, health-care food and food are provided.

Description

technical field [0001] The present invention relates to a preparation method and application of monogalactosyl diacylglyceride, in particular to a preparation method of monogalactosyl diacylglyceride and its use as a PPARα agonist and a PPARα / γ double agonist the use of. Background technique [0002] Peroxisome proliferator-activated receptors (PPARs for short) is a member of the nuclear receptor superfamily, including three subtypes of PPARα, PPARβ (or PPARδ) and PPARγ. After being activated by ligand, PPARs first form a heterodimer with retinoid X receptor (RXR), and then with the peroxisome proliferator response element (PPRE) upstream of the target gene promoter. Combined with transcriptional regulation of target genes to regulate important biochemical processes such as lipid metabolism, lipogenesis, insulin sensitivity, inflammatory response, cell growth and differentiation. A series of metabolic syndromes are associated with PPARs, including insulin resistance, impai...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/7032C07H15/06C07H1/08A61P3/06A61P3/04A61P9/12A61P1/16A61P9/10A61P13/12A61P3/10A61P9/00A61P37/06
CPCA61K31/7032A61K36/02C07H1/08C07H15/06
Inventor 刘红兵王梦雪蒋盈
Owner OCEAN UNIV OF CHINA
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