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ABPP-based antitumor drug ginsenoside Rg3 active molecular probe, synthesis and applications thereof

A technology of ginsenosides and active molecules, which is applied in the field of chemical biology and can solve problems such as research work that has not been reported yet

Inactive Publication Date: 2019-06-21
DALIAN INST OF CHEM PHYSICS CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

This patented technology allows for creation of small chemical compounds that are able to attach themselves specifically to certain types of cancer cell membranes called AMPA binding protein (AMPB) on their surface. These tiny substances have been shown to prevent neoplastic growth by blocking specific enzyme pathways involved in DNA damage caused during radiation therapy treatments. They may help identify new targets like those associated with inflammatory processes within tissues affected by these treatment methods.

Problems solved by technology

This patented technical problem addressed in this patents relates to studying how different types of compounds called Ginsenosides RhGa1 , Rehmannia root extractive agent 3, Radix etsinus Linnis Cathayanus dendriticum, Helicosanaxadioli radiciestricans, Poria planariae variegate seeds contain various structural motifs related to their medicinal properties like antioxic effects against brain cancer and blood vessel disease. Therefore, there may exist potential therapeutic agents containing specific structures found within them.

Method used

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  • ABPP-based antitumor drug ginsenoside Rg3 active molecular probe, synthesis and applications thereof
  • ABPP-based antitumor drug ginsenoside Rg3 active molecular probe, synthesis and applications thereof
  • ABPP-based antitumor drug ginsenoside Rg3 active molecular probe, synthesis and applications thereof

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Experimental program
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Embodiment Construction

[0020] The structure of the active molecular probe of ginsenoside Rg3 based on ABPP is:

[0021]

[0022] Wherein, the group connected to the rightmost end is an alkynyl group, which is used as a reporter group in the active molecular probe. The specific synthetic route is

[0023]

[0024] The reaction conditions are:

[0025] 20(R)-ginsenoside Rg3 (1g) was dissolved in 100ml of anhydrous pyridine, stirred to obtain 20(R)-ginsenoside Rg3 solution, and the acylating reagent acetyl chloride (2ml) was added dropwise for esterification reaction. The temperature was 80°C, the reaction time was 2h, then anhydrous methanol (5ml) was added to quench the esterification reaction, the pH value of the mixed solution was adjusted to 7.2, filtered, recrystallized; then dissolved in 100ml dichloromethane and acetic acid solution (two The volume ratio of the two reagents is 1:1), and O is introduced at -78°C 3 , until the reaction turns blue, then pass through O 2 remove excess O ...

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Abstract

The invention discloses an ABPP-based antitumor drug ginsenoside Rg3 active molecular probe, synthesis and applications thereof, and belongs to the field of chemical biology. According to the presentinvention, the active molecular probe is designed and synthesized through structure modification based on the parent compound Rg3, can achieve the recognition and labeling of the drug action target inliving cells, has antitumor activity similar to Rg3, and provides the advantageous tool in the research on the antitumor action target and the action mechanisms of Rg3.

Description

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Claims

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Application Information

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Owner DALIAN INST OF CHEM PHYSICS CHINESE ACAD OF SCI
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