Use of polygonum hydropiper aldehyde compounds as acid sphingomyelinase inhibitor

A sphingomyelin and inhibitor technology, applied in the development of acid sphingomyelinase inhibitors, can solve problems such as lack of ASM inhibitors

Inactive Publication Date: 2018-10-16
赵熙
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, highly effective ASM inhibitors are currently lacking

Method used

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  • Use of polygonum hydropiper aldehyde compounds as acid sphingomyelinase inhibitor
  • Use of polygonum hydropiper aldehyde compounds as acid sphingomyelinase inhibitor

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Experimental program
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Embodiment Construction

[0024] The substantive content of the present invention will be described below in conjunction with the accompanying drawings and embodiments, but the protection scope of the present invention is not limited thereto.

[0025] 1. Experimental materials

[0026] Nardon guaiacol C (CAS accession number: 309966-66-3), nard pine guaiacone D (CAS accession number: 309966-67-4), nard pine guaiacone G (CAS accession number: 309966-57-2) , deacylated cynarin (CAS accession number: 31565-50-1), Pasche's vantacyanin B (CAS accession number: 23554-79-2), hydroglycidic acid (CAS accession number: 98204-84 -3), Polygonum water hemiacetal (CAS registration number: 72581-69-2), 14-deacetyl colsparagine (CAS registration number: 147742-07-2) self-made or purchased, with a purity of not less than 98% . chemical structure such as figure 1 shown.

[0027] ASM enzyme was purchased from Nanjing Jiancheng Biology, and PBS buffer was purchased from Sigma Company. 3 H-labeled sphingomyelin was pu...

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Abstract

The invention discloses use of polygonum hydropiper aldehyde compounds as an acid sphingomyelinase inhibitor. Spikenard guaiacum ketone C, spikenard guaiacum ketone D, deacetylated anthraquinone cynaropicrin, parishin B, polygonic acid, polygonum hydropiper hemiacetal and 14-deacetylated farfaratin are found to have excellent inhibitory activity on acid sphingomyelinase, thus being developed intothe acid sphingomyelinase inhibitor for treating diseases caused by the rise of the acid sphingomyelinase.

Description

technical field [0001] The invention belongs to the field of biomedicine and relates to the development of acid sphingomyelinase inhibitors. Background technique [0002] Sphingomyelinase (SMase) is a hydrolase that acts on sphingomyelin (SM) and can hydrolyze the phosphodiester bond of sphingomyelin on the plasma membrane surface to produce ceramide and phosphorylcholine. As an important second messenger, ceramide can play a role in various signal transduction processes and participate in various cellular functions, such as regulating cell growth, proliferation and variation, causing apoptosis, regulating protein secretion, and participating in immune processes and inflammatory responses. Generally, SMase can be divided into six subtypes, among which acid sphingomyelinase (ASM) is the most important subtype, and its biological activity accounts for 90% of the total activity of SMase. Studies have shown that ASM can be highly expressed and highly active to participate in t...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/19A61K31/357A61K31/365A61K31/343A61K31/22A61P17/00A61P11/00A61P9/00A61P1/16
CPCA61K31/19A61K31/22A61K31/343A61K31/357A61K31/365A61P1/16A61P9/00A61P11/00A61P17/00
Inventor 赵熙
Owner 赵熙
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