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Compound with LSD1 inhibitory activity, preparation method and application

A technology for inhibiting activity and compounds, applied in the preparation of sugar derivatives, chemical instruments and methods, organic chemistry, etc., can solve the problems of less research on chemical components

Active Publication Date: 2021-02-26
XUCHANG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, there are few studies on the chemical components of the n-butanol extraction part of the star anise extract

Method used

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  • Compound with LSD1 inhibitory activity, preparation method and application
  • Compound with LSD1 inhibitory activity, preparation method and application
  • Compound with LSD1 inhibitory activity, preparation method and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] 1. Extraction, separation and purification of compounds 1-7:

[0040] Collect large star anise stems and leaves, dry in the shade, its scientific name is identified as Illicium majus, and crush. Take 10 kg dried and pulverized large star anise stems and leaves, reflux extraction with 95% ethanol for 3 times, 40 L each time, 3 hours each time, concentrate the filtrate to a small volume, add 3 L of water to suspend, and use chloroform (3 L × 3) and normal Extracted with butanol (3L×4), and distilled under reduced pressure to obtain chloroform fraction (300g) and n-butanol fraction (150g). The n-butanol fraction (150g) was eluted with ethanol / water gradient (0:100, 20:80, 40:60, 60:40, 80:20, 100:0) with macroporous resin (D101, 120×12cm) to obtain 6 Fractions (Frs.1–6). Fraction 5 (20g) passed through a silica gel column (9×40cm, 1000g, 200-300 mesh) with CH 2 Cl 2 / MeOH gradient elution (100:0,90:10,80:20,70:30v / v) to obtain 7 fractions (Frs.5.1–5.7).

[0041] Fract...

Embodiment 2

[0052]Example 2: Determination of the inhibitory activity of compounds 1-7 on LSD1

[0053] (1) Experimental method: the sample is the natural product (7R,8S)-4,3′,9-trihydroxyl-3-methoxyl-7,8-dihydro-benzofuran-1′- propylneolignan-9′-O-β-D-glucopyranoside(1), (7R,8S)-4,3′,9′-trihy-droxyl-3-methoxyl-7,8-dihydrobenzofuran-1′-propylneolignan-9 -O-α-L-rhamnopyranosyl-(1→2)-β-D-glucopyranoside(2),(7R,8S)-4,3′,9′-trihydroxyl-3-methoxyl-7,8-dihydrobenzofuran- 1′-propylneolignan-9-O-α-L-rhamnopyranosyl-(1→2)-β-D-xylopyran oside(3), (7R,8S)-4,3′-dihydroxyl-3-methoxyl-9′ -acetyl-7,8-dihydrobenzofuran-1′-propylneol ignan-9-O-α-(4’-acetyl)-L-rhamnopyran-osyl-(1→2)-β-D-xylopyranoside(4), xanthiumnolic C(5), 1-O-caffeoyl-β-D-glucopyranose(6), soulieana acid 1(7); sample stock solution: Weigh 3-5mg samples respectively into 1.5mL EP tubes, then prepare with DMSO Make a solution with a concentration of 20mM, store it at 4 degrees Celsius, and dilute it with DMSO according to the required ...

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Abstract

The invention discloses a compound which is extracted and separated from star anise and has LSD1 inhibitory activity, a preparation method and application. The compound is shown as a formula (I). Thecompounds of the invention may be used in combination or alone as novel histone lysine specific demethylase 1(LSD1) inhibitors. The compound is used as an LSD1 inhibitor for preventing and treating diseases and symptoms related to the activity of histone demethylase LSD1, especially diseases related to abnormal gene transcription, cell differentiation and proliferation, such as tumors and the like.

Description

technical field [0001] The invention belongs to the technical field of LSD1 inhibitors, and specifically relates to a compound with LSD1 inhibitory activity, a preparation method and an application. Background technique [0002] Illicium majus Hook et Thomas is a plant of the genus Illicium, a tree, mainly distributed in Hunan, Guangdong, Guangxi and Guizhou provinces, and generally grows in mixed forests, dense forests, shrubs or forested stone slopes and along streams. It is also distributed in northern Vietnam and southern Myanmar. Its roots and leaves are used in the folk to treat epigastric pain and vomiting, while the bark can dispel wind and dampness, activate blood and relieve pain, and can be used to treat joint swelling and pain. At present, there are few studies on the chemical components of the n-butanol extraction part of the star anise extract. [0003] Malignant tumors seriously affect people's health. According to the statistics of the World Health Organiza...

Claims

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Application Information

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IPC IPC(8): C07D307/80C07H13/04C07H15/203C07H1/08A61P35/00A61P31/12A61P29/00A61P3/00
CPCC07D307/80C07H13/04C07H15/203C07H1/08A61P35/00A61P31/12A61P29/00A61P3/00
Inventor 王磊柳继锋李芳温婷羽付莹莹
Owner XUCHANG UNIV
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