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Compound Blapsins A and B, pharmaceutical composition containing the same, and preparation method and application thereof

A compound and drug technology, applied in the field of natural compounds, can solve problems such as unseen compounds

Active Publication Date: 2012-06-20
KUNMING INST OF BOTANY - CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] No reports of compounds 1 and 2 of the present invention on the regulation of 14-3-3 in the prior art

Method used

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  • Compound Blapsins A and B, pharmaceutical composition containing the same, and preparation method and application thereof
  • Compound Blapsins A and B, pharmaceutical composition containing the same, and preparation method and application thereof
  • Compound Blapsins A and B, pharmaceutical composition containing the same, and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] Preparation and structure confirmation of compounds 1 and 2:

[0026] Take the dried Japanese pipa beetle body (5kg), stir and extract with 30%-95% ethanol or methanol at room temperature for 1-3 times, each time for 48 hours, and the amount of each solvent is 30L. The combined extracts were concentrated under reduced pressure to obtain 500 g of extract. After the extract was diluted with an appropriate amount of water, it was extracted three times with an equal volume of n-butanol, and the n-butanol extract was concentrated under reduced pressure to obtain 150 g. The n-butanol extract was chromatographically separated with a normal-phase silica gel (200-300 mesh) column, the ratio of the extract to the adsorbent was 1:20 (g / g), and the solvent elution system was a gradient chloroform-methanol, and the gradients were as follows: 99:1, 98:2, 96:4, 94:6, 90:10, 88:12, 85:15, the amount of each gradient solvent is 2 times the column bed volume. According to thin-layer ch...

Embodiment 2

[0039] According to the structural formula and / or molecular weight of compounds 1 and 2 given in Example 1, compounds 1 and 2 were prepared from insects of the genus Blaps by using LC-MS tracking method according to conventional chromatographic methods.

Embodiment 3

[0041] Compounds 1 and 2 were prepared according to the method of Example 1, which were respectively dissolved in sterile water for injection, filtered with a sterile funnel, subpackaged, freeze-dried at low temperature, and then aseptically melted and sealed to obtain a powder injection.

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PUM

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Abstract

The invention discloses compounds 1 and 2 of the following structural formula, pharmaceutical compositions containing the compounds as effective components, a preparation method of the two compounds, and application of the two compounds for preparing protein 14-3-3 small molecule chemical probes and preparing pharmaceuticals for treating cancers or nerve degenerative diseases relates to over-expression of protein 14-3-3. The compounds 1 and 2 have a significant inhibitory effect on protein 14-3-3.

Description

Technical field: [0001] The invention belongs to the field of pharmaceutical compounds, in particular, it relates to natural compounds Blapsins A and B isolated and extracted from Japanese lute beetles, and their application in the preparation of small molecule chemical probes or in the preparation of anti-cancer or anti-neurodegenerative disease drugs , a pharmaceutical composition containing the same and a preparation method thereof. Background technique: [0002] 14-3-3 is a family of acidic proteins widely expressed in eukaryotes. It was first discovered in 1967 from bovine brain extracts, and then aroused the interest of the scientific community. By the mid-1990s, a large number of scientific papers on 14-3-3 research began to appear. At present, the 14-3-3 protein field It has become an international research hotspot. Seven subtypes of 14-3-3 have been found in mammals so far, and the amino acid sequences of 14-3-3 or each subtype of different species are highly cons...

Claims

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Application Information

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IPC IPC(8): C07C69/732C07C67/48C07D311/76A61K31/216A61K31/353A61P35/00A61P25/00
Inventor 程永现晏永明吕青
Owner KUNMING INST OF BOTANY - CHINESE ACAD OF SCI
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