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Application of saringosterol

A technology of sargassum sterol and application, applied in the field of sargassum sterol as LXR agonist

Active Publication Date: 2014-02-12
OCEAN UNIV OF CHINA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0008] Studies on sargassum sterols have shown that it has anti-tuberculosis activity, especially the 24R isomer against Mycobacterium tuberculosis H 37 The MIC value of Rv is 8 times that of the 24S isomer (see Gerald A.Wachter et al., "Inhibition of Mycobacterium tuberculosis Growth by Saringosterol from Lessonia nigrescens" J.Nat.Prod.2001, 64, pages 1463-1464), but There is no literature report on the use of sargastric sterol, especially 24(S)-sargastric sterol as an LXR agonist

Method used

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Examples

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Embodiment 1

[0026] Example 1: Extraction and Separation and Purification of 24(S)-Sargasso Sterol

[0027] Take 500 g of Sargassum sargassum, and use 10 times the volume of dichloromethane-methanol with a volume fraction ratio of 2:1 to reflux for 2 hours, and repeat 3 times. The extracts were combined, filtered, and concentrated to dry solvent to obtain 31.5 g of extract.

[0028]After the extract (31.5g) was dissolved in dichloromethane, mix the sample with 41g 200-300 mesh silica gel H (product of Qingdao Ocean Chemical Group Co., Ltd.), remove the solvent under reduced pressure, use silica gel column chromatography, and use cyclohexane-dichloro Methane and dichloromethane-methanol were used as solvents for gradient elution, and the eluate of dichloromethane-methanol (v / v 99:1) was subjected to Sephadex LH-20 gel column chromatography (dichloromethane-methanol 1 : 1 elution), the resulting fraction was recrystallized from dichloromethane-methanol to obtain sargassum sterol. Sargasso ...

Embodiment 2

[0032] Example 2: Testing of LXRβ Activation

[0033] Transcriptional activation of LXRβ was detected using a dual-luciferase reporter gene assay. 293T cells were inoculated in 48-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 plasmids was 0.075 μg / well (0.05 μg TK-luc containing UAS element, 0.005 μg internal control pRL-TK and 0.02 μg Gal4 fusion protein expression plasmid GAL4-LXRα / β containing LXRα / β LBD domain). The amount of lipo2000 used was 2.5 times the mass of the transfected plasmid (2.5*0.075 μl=0.1875ul / well). Plasmid and lipo2000 were mixed in 25μl / well optim medium in advance. Add phytosterol samples 12 hours after transfection, and detect Luciferase activity 24 hours later. The results showed that at the concentration of 100 μM, the activation folds of sargassum sterol...

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Abstract

The invention discloses an application of saringosterol to preparation of an LXR (liver X receptor) excitant, and particularly discloses an application of 24(S)-saringosterol as an LXR beta excitant.

Description

technical field [0001] The present invention relates to a use of sargastric sterol, in particular to the use of sargastric sterol as an LXR agonist. Background technique [0002] Saringosterol, namely 24ζ-hydroxyl-24-vinylcholesterol, is extracted from Phaeophyta Sargassum family Sargassum (Sagarssum), and its structural formula is shown in Formula I, which is a pair of 24R and 24S isomer. [0003] [0004] Wang Wei et al. used normal phase preparative liquid chromatography to separate the 24S and 24R isomers of sargassum sterols from Hijiki for the first time (Chinese Herbal Medicine, 2008, Vol. 39, No. 5, pp. 657-661) , its structural formula is shown in formula II and formula III: [0005] [0006] Liver X receptors (liver X receptors, referred to as LXRs) are members of the nuclear receptor superfamily, including two homologous subtypes LXRα (NR1H3) and LXRβ (NR1H2). After LXRs are activated by endogenous ligand oxysterols or synthetic ligands, they first form h...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/575A61P9/10A61P3/10A61P25/28A61P35/00C07J9/00
Inventor 刘红兵应浩陈震管华诗
Owner OCEAN UNIV OF CHINA
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