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Application of Xyloketal B in preparing antiatherosclerotic medicaments

A technology for atherosclerosis and atherosclerosis, which is applied in drug combinations, anti-toxins, and pharmaceutical formulas to achieve good medicinal prospects, strong pharmacological effects, and the effect of reducing macrophage deposition

Active Publication Date: 2011-04-20
SUN YAT SEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The application of xyloketal B in anti-atherosclerosis has not been reported

Method used

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  • Application of Xyloketal B in preparing antiatherosclerotic medicaments
  • Application of Xyloketal B in preparing antiatherosclerotic medicaments
  • Application of Xyloketal B in preparing antiatherosclerotic medicaments

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0018] Example 1 Effect of Xyloketal B on Plaque Area in Atherosclerotic Mice

[0019] (1) Materials and methods

[0020] 1. Drugs:

[0021] Xyloketal B, white powder. It was dissolved in DMSO first, the storage concentration was 80mmol / L, and it was stored at 4°C for later use. It was diluted with 10% propylene glycol saline, and administered by intraperitoneal injection (the final concentration of Xyloketal B was 14mg / kg·d). Simvastatin was purchased from Hangzhou Merck Pharmaceutical Co., Ltd. (40 mg tablet, batch number 07279), and it was ground into powder during administration, dissolved in deionized water and administered intragastrically (the final concentration of simvastatin was 10 mg / kg·d) .

[0022] 2. Grouping, feeding and administration of experimental animals

[0023] In this experiment, apoE knockout mice (strain C57BL / 6J, male, clean grade, 5 weeks old) and wild-type male C57BL / 6J mice were selected. All animals were adaptively fed for 1 week, and wer...

Embodiment 2

[0045] Example 2 Effect of Xyloketal B on Blood Lipid Level and Anti-Ox-LDL Antibody in Atherosclerotic Mice

[0046] (1) Materials and methods

[0047] 1. Drug preparation, animal model grouping, administration see Example 1

[0048] 2. Plasma and reagents Fresh plasma from healthy people was purchased from the Department of Hematology, The First Affiliated Hospital of Sun Yat-sen University, Ethylene glycol-bis(2-aminoethylether) -N,N,N', N'-tetraacetic acid (EGTA), polyethylene glycol (PEG 6000), agarose (agarose), and Coomassie Brilliant Blue G-250 were all purchased from Sigma. Enzymatic detection of blood lipid analysis direct high-density lipoprotein cholesterol (HDL-C) kit, direct low-density lipoprotein cholesterol (LDL-C) kit. Purchased from Zhongsheng Beikong Biotechnology Co., Ltd. Serum anti-Ox-LDL antibody assay kit (Protein Detector TM ELISA Kit) was purchased from Kirkegaard Perry Labs.

[0049] 3. Separation, purification and oxidation of low density...

Embodiment 3

[0069] Example 3 Effects of Xyloketal B on plaque components and arterial endothelial injury in atherosclerotic mice

[0070] (1) Materials and methods

[0071] 1. See Example 1 for drug preparation, animal model grouping, and administration methods

[0072] 2. Other experimental materials: Mac-3 (BD ​​Biosciences), CD31 ([PECAM-1]) (BD Pharmingen). Anti-shedding glass slide, microscope cover glass, mouse two-step detection kit, rabbit two-step detection kit, DAB chromogenic kit, immunofluorescent secondary antibody (all purchased from Beijing Zhongshan Jinqiao Biological Company), neutral Resin glue (Beijing Chemical Reagent No. 4 Factory), acetone (Guangzhou Chemical Reagent Co., Ltd.).

[0073] 3. Immunohistochemistry and immunofluorescence detection methods

[0074] Immunohistochemical experimental steps: (1) Frozen sections were fixed with acetone at -20°C for 10 minutes and washed with PBS for 5 minutes. (2) 0.3% H 2 o 2 Methanol solution (to block endogenou...

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Abstract

The invention discloses application of Xyloketal B in preparing antiatherosclerotic medicaments. Experiments prove that: Xyloketal B has the effects of reducing the plaque area and regulating blood fat on atherosclerotic lesions, and can prevent and treat atherosclerosis by protecting vascular endothelium, regulating the blood fat level such as reducing low-density lipoprotein cholesterol (LDL-C) and raising the LDL-C, resisting oxidative stress in vivo and other action mechanisms. A novel application field of the Xyloketal B is developed when the Xyloketal B is applied to preparing the antiatherosclerotic medicaments, and the Xyloketal B is safe and non-toxic and has strong pharmacological action and good medicinal prospect.

Description

technical field [0001] The present invention relates to the application of Xyloketal B in the pharmaceutical field, in particular to the application of Xyloketal B in the preparation of anti-atherosclerotic drugs. Background technique [0002] Xyloketal compounds are endophytic fungi from South China Sea mangroves Xyloraria A series of new compounds isolated from sp. 2508 have more than 10 rare structures, and Xyloketal B is one of them. "Research progress on the synthesis of secondary metabolites of three types of marine fungi from the South China Sea", Organic Chemistry, Vol. 29, No. 3, 2009, pages 341-349, discloses the structure and preparation method of this compound. That is, it is synthesized by using phloroglucinol as a raw material through a one-pot method and a domino reaction. Chinese patent application 200910042204.0 discloses the application of Xyloketal B in the preparation of drugs for the treatment of free radical damage diseases, and points out that it has...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/352A61P9/10A61P9/14A61P3/06A61P39/06
Inventor 王冠蕾庞冀燕林永成刘捷解煜刘灿昭
Owner SUN YAT SEN UNIV
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