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Application of alpha-, beta- and gamma- mangostin as lysine specific demethylase 1 (LSD1) inhibitor

A technology of mangostin and inhibitor, applied in the field of medicinal chemistry

Inactive Publication Date: 2019-03-12
ZHENGZHOU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

There are no reports about α-, β- and γ-mangostin as LSD1 inhibitors

Method used

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  • Application of alpha-, beta- and gamma- mangostin as lysine specific demethylase 1 (LSD1) inhibitor
  • Application of alpha-, beta- and gamma- mangostin as lysine specific demethylase 1 (LSD1) inhibitor
  • Application of alpha-, beta- and gamma- mangostin as lysine specific demethylase 1 (LSD1) inhibitor

Examples

Experimental program
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Embodiment 1

[0015] Example 1: α-, β- and γ-mangostin (mangostin) LSD1 inhibitory activity assay 1. Experimental method: the sample is the natural product α-, β- and γ-mangostin ( mangostin) (see SakagamiY.etal, Phytomedicine, 2005, 12(3):203-208 for the separation method); sample stock solution: weigh 3-5mg sample and place it in a 1.5mL EP tube, then prepare it with DMSO to a concentration of 20mM The solution, stored at 4 degrees Celsius, was diluted with DMSO according to the required concentration during the experiment. After incubating the sample to be tested with the LSD1 protein at room temperature, add the LSD1 reaction substrate H3K4me2 and incubate the reaction, and finally add the fluorescent dye Amplex and horseradish peroxidase HRP to incubate at room temperature, and detect on a microplate reader with an excitation light of 530nm and an emission light of 590nm Fluorescence value:

[0016]

[0017] Experimental results using SPSS software to calculate IC 50 value.

[00...

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Abstract

The invention belongs to the field of medicinal chemistry, and particularly relates to application of alpha-, beta- and gamma- mangostin as a novel histone lysine specific demethylase 1 (LSD1) inhibitor. As the LSD1 inhibitor, the alpha-, beta- and gamma- mangostin can be used for preventing and treating diseases and symptoms associated with the activity of the histone demethylase LSD1, particularly diseases associated with abnormal gene transcription, cell differentiation and proliferation, such as tumors. The structural formula of the alpha-, beta- and gamma- mangostin is as shown in the specification.

Description

technical field [0001] The invention relates to the field of medicinal chemistry, in particular to the application of α-, β- and γ-mangostin as novel histone lysine-specific demethylase 1 (LSD1) inhibitors. Background technique [0002] The husk of Garcinia mangostana L. is a traditional folk medicine in Southeast Asia, and it is often used to treat dysentery, sprains, typhoid, ulcers, skin infections and other diseases. Xanthone components such as α-, β- and γ-mangostin can be isolated therefrom by appropriate methods known to those skilled in the art. At present, it is mainly used for antifungal, antibacterial, antitumor, malaria, sialidase inhibitor and aromatase inhibitor. So far, there are no reports about α-, β- and γ-mangostin as LSD1 inhibitors. [0003] Malignant tumors seriously affect people's health. According to the statistics of the World Health Organization, there are more than 10 million newly diagnosed tumor patients in the world every year, which imposes ...

Claims

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Application Information

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IPC IPC(8): A61K31/352A61P35/00A61P31/12A61P29/00A61P3/00
CPCA61K31/352A61P3/00A61P29/00A61P31/12A61P35/00
Inventor 柳继锋郑一超马天放李芳温婷羽
Owner ZHENGZHOU UNIV
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