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Bisindole compound as well as preparation method and application thereof

A bisindole compound and compound technology, applied in the field of bisindole compound and its preparation, achieves the effects of low IC50 concentration, low cost and high yield

Inactive Publication Date: 2015-12-16
SHANGHAI OCEAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

There is no report of a pharmaceutical composition using it as an active ingredient, nor is it used for inhibiting the activity of 3-hydroxy-3-methylglutaryl coenzyme A reductase (HMG-CoA reductase) or reducing blood lipids , or contain therapeutically effective amount of claim 1 compound and / or pharmaceutically acceptable carrier, the report of treatment arteriosclerosis drug

Method used

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  • Bisindole compound as well as preparation method and application thereof
  • Bisindole compound as well as preparation method and application thereof
  • Bisindole compound as well as preparation method and application thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0032] The strain FG216 was inoculated into a 500 mL Erlenmeyer flask containing 100 mL of seed medium, and the flask was shaken for 3 days at 25°C and 180 r / min. The seed culture liquid was inoculated into the fermentation medium at 1% (v / v), and the flask was shaken for 7 days under the culture conditions of 25°C and 180 r / min. The mycelium of the fermentation broth was separated and extracted with methanol. The methanol extract was used as the fermentation product of FG216. The elution peak at the retention time of 15.6 minutes in high performance liquid chromatography was the bisindole compound (I).

[0033] The structural formula of the bisindole compound (I) is:

[0034]

[0035] The physical and chemical properties of compound (I) are that the appearance is brown powder, and the molecular formula is C. 51 H 68 N 2 O 10 、FAB-MS:869.3867(M+1) + 、ESI-MS:869.3659(M+1) + , ExactMS: 868.4874, melting point 203-205℃, IR: 3397Cm -1 , 2073Cm -1 , 1670Cm -1 , 1465Cm ...

Embodiment 2

[0039] The strain FG216 was inoculated in a 1000 mL Erlenmeyer flask containing 150 mL of seed medium, and the flask was shaken for 3 days under the culture conditions of 20°C and 160 r / min. The seed culture solution was inoculated into the fermentation medium in an amount of 3% (v / v), and the flask was shaken for 10 days under the culture conditions of 25° C. and 180 r / min. The mycelium of the fermentation culture liquid was separated and extracted with ethyl acetate. The ethyl acetate extract was used as the fermentation product of FG216, and the elution peak at the high performance liquid chromatography retention time of 15.6 minutes was the bisindole compound (I).

[0040] Test Data:

[0041] 3.0mmol / L HMG-CoA, 5U / mgHMG-CoA reductase, 15mmol / LNADPH and the sample to be tested (the bisindole compound prepared in Example 2) were injected into the wells of the 96-well round-bottom plate to form a 100 μL reaction system. The change of NADPH absorbance was continuously measure...

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Abstract

The invention relates to the technical field of biological medicine, in particular to a bisindole compound as well as a preparation method and an application thereof. The preparation method comprises the following steps: an FG216 strain is inoculated to a seed medium and cultured on a shaking table for 1-3 days under the conditions of 22-28 DEG C and 160-220 r*min<-1>; then a seed culture solution is inoculated to a fermentation medium and cultured on the shaking table for 5-10 days under the conditions of 22-28 DEG C and 160-220 r*min<-1>; mycelia of a fermentation solution are separated and extracted with methanol or ethyl acetate, a methanol extracting solution or an ethyl acetate extracting solution is taken as a fermentation product of the FG216 strain, and an elution peak reserved for 15.6 min in HPLC (high performance liquid chromatography) is the bisindole compound. The preparation method has the advantages of high yield and low cost. The prepared bisindole compound can inhibit HMG-CoA (3-hydroxy-3-methylglutaryl-coenzyme A) reductase effectively, has low IC50 (half maximal inhibitory concentration) and can be used for preparing drugs for treating arteriosclerosis diseases.

Description

technical field [0001] The invention belongs to the technical field of biomedicine, and particularly relates to a bisindole compound and a preparation method and application thereof. Background technique [0002] Atheroclerosis (AS) is the main pathological basis of cardiovascular and cerebrovascular diseases, which mainly occurs in large and medium arteries, especially coronary arteries, cerebral arteries and aorta. Chinese health big data shows that the proportion of dyslipidemia among adults of different ages in my country is 15.9%-23.4%, and the population with hyperlipidemia such as hypercholesterolemia, hypertriglyceridemia, and low-density lipoproteinemia Over 100 million, hyperlipidemia is closely related to the morbidity and mortality of cardiovascular and cerebrovascular diseases. Blood lipid-lowering drugs can delay or reduce the development of AS lesions and promote their regression. At the same time, blood lipid-lowering drugs can reduce heart disease mortality b...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D519/00A61K31/407A61P9/10C12P17/18C12R1/645
CPCC07D519/00C12P17/18
Inventor 吴文惠包斌郭锐华孟晓琴傅诗情张朝燕
Owner SHANGHAI OCEAN UNIV
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