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Polyketone compound, and preparation method and application of polyketone compound

A technology of polyketone compounds and crude extracts, applied in organic chemistry, drug combination, cardiovascular system diseases, etc., to achieve a significant effect of blocking activity

Active Publication Date: 2018-01-19
ZHEJIANG SCI-TECH UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there has been no report on the isolation of related compounds with blocking activity on KV1.5 ion channels from this genus of cyanobacteria.

Method used

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  • Polyketone compound, and preparation method and application of polyketone compound
  • Polyketone compound, and preparation method and application of polyketone compound
  • Polyketone compound, and preparation method and application of polyketone compound

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Experimental program
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Embodiment 1

[0034] Embodiment 1 prepares the compound of the present invention

[0035] 1. Prepare dichloromethane crude extract

[0036] Cut 150g (dry weight) of cyanobacteria Lyngbya majuscula through freeze-drying into pieces, use 1L dichloromethane:methanol (2:1, V / V) percolation extraction for 5 times, combine the extracts, and concentrate the extracts under reduced pressure to obtain leaching paste, the extract was suspended in 60%, V / V methanol water, extracted 3 times with dichloromethane, and the extract was concentrated to obtain 20 g of dichloromethane crude extract;

[0037] 2. Separation and purification

[0038] 1) Separation and purification: the dichloromethane crude extract was subjected to forward vacuum silica gel (200-300 mesh) column chromatography VLC, first using petroleum ether: ethyl acetate system = 5:1, 2:1, 1:1, 1:2, 1:5, 0:1, V / V elution, and finally use pure methanol as solvent to carry out gradient elution, according to TLC thin-layer chromatography with s...

Embodiment 2

[0045] Example 2 The in vitro ion channel impact experiment of the compound of the present invention:

[0046]The compound of formula (I) of the present invention is subjected to an experiment on the influence of ion channels in vitro, and the materials used are: HEK293 cells with steady-state expression of hERG ion channels, HEK293 cells with steady-state expression of Kir2.1 ion channels, and HEK293 cells with steady-state expression of Nav1.5 ion channels. In HEK293 cells, Nav1.8 ion channel is stably expressed in HEK293 cells, KV1.5 ion channel is stably expressed in CHO cells, and Nav1.7 ion channel is stably expressed in CHO cells. These materials were purchased from Sigma (St.Louis, MO) company.

[0047] 1. Experimental principle

[0048] hERG, Kir2.1, Nav1.5, Nav1.8 ion channels were stably expressed in HEK293 cells. KV1.5 and Nav1.7 ion channels are stably expressed on CHO cells. After the current is stable, compare the magnitude of the current before and after the ...

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Abstract

The invention discloses a polyketone compound, a preparation method of the polyketone compound and an application of the polyketone compound in the preparation of a potassium-ion KV1.5 channel inhibitor. The polyketone compound is obtained by the steps of performing extraction on marine blue-green algae Lyngbya majusca which is located in a sea area near the Lingshui port, Sanya, Hainan, and performing separation purification. The structure is represented as a formula (1), and the compound has a blocking effect on an ion channel KV1.5.

Description

technical field [0001] The invention relates to the technical fields of marine biology and medicine, in particular to a polyketide compound, its preparation method and its application in the preparation of potassium ion channel KV1.5 inhibitors. Background technique [0002] Marine cyanobacteria are a kind of microbial group, which are widely distributed and can produce many natural toxins. Among them, marine cyanotoxins and anti-tumor active substances have become the focus of research on marine biological active substances. [0003] The cyanobacteria Lyngbya majuscula produced in the waters near Lingshui Port, Sanya, Hainan contains a variety of polyketide compounds. Some polyketide compounds have been isolated from this genus of cyanobacteria, and these compounds have shown good biological activity. For example, Debromoaplysiatoxin isolated from Lyngbya majuscula showed strong antiproliferative activity on mouse leukemia P388 lymphocytes (see literature: Mynderse J-S, Moo...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D493/08A61P9/00A61P9/06
Inventor 韩兵男梁婷婷郑玲辉
Owner ZHEJIANG SCI-TECH UNIV