Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

Polyketone compounds with antitumor activity, preparation method therefor and application of polyketone compounds

A compound and anti-tumor technology, which are applied in the field of polyketone compounds and their preparation, can solve the problems of unreported anti-tumor activity and anti-tumor application, and achieve the effect of simple separation and purification

Active Publication Date: 2018-02-16
WUHAN UNIV
View PDF0 Cites 3 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The polyketide compound with antitumor activity and its antitumor application isolated therefrom by the present invention have not been reported

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Polyketone compounds with antitumor activity, preparation method therefor and application of polyketone compounds
  • Polyketone compounds with antitumor activity, preparation method therefor and application of polyketone compounds
  • Polyketone compounds with antitumor activity, preparation method therefor and application of polyketone compounds

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0037] The features and advantages of the present invention can be further understood through the following detailed description in conjunction with the accompanying drawings. The examples provided are only illustrative of the method of the present invention and do not limit the rest of the present disclosure in any way. [Example 1] Construction of enterocin biosynthetic gene cluster deletion mutant strain Δenc

[0038] Using the genomic DNA of wild-type 172205 as a template, primers enc-L1 (5'-CCTAGGCAGTTCCATCACCCCGTTCG-3', SEQ NO.1) and enc-L2 (5'-AAGCTTGTCGTCGCAGCAGCAGTTCG-3', SEQ NO.2) were designed for amplification To increase the upstream fragment enc-L of the enterocin synthetic gene cluster, design primers enc-R1 (5'-CATATGAGAGGGCGGACGGGAACTGC-3', SEQ NO.3) and enc-R2 (5'-CCTAGGGCGCCATCCCAACGGGCTAC-3', SEQ NO.4) for Amplify the downstream fragment enc-R of enterocin synthesis gene cluster. 20 μL PCR reaction system using Taq Mix enzyme: 8 μL Mix enzyme, 1 μL each pr...

Embodiment 2

[0042] [Example 2] Large-scale fermentation of the mutant strain 172205Δenc and its pretreatment method for fermented product samples

[0043] The mutant strain 172205Δenc obtained in Example 1 was inoculated in ISP2 liquid medium, shaken at 28°C and 200r / min for 3 days, transferred to a shaker flask of 60L fermentation medium with 5% inoculum, and incubated at 28°C at 200r / min Min shaking culture for 7 days to obtain fermentation broth. The supernatant of the fermentation broth was extracted 3 times with an equal volume of ethyl acetate, and the ethyl acetate layer was combined; the mycelium was ultrasonically broken by adding 3 times the volume of 80% acetone aqueous solution for 1 hour, repeated 3 times, centrifuged to take the supernatant, and after removing the acetone , the aqueous solution was extracted three times with 2 times the volume of ethyl acetate; all the ethyl acetate layers were combined and concentrated under reduced pressure to obtain a crude extract. The ...

Embodiment 3

[0044] [Example 3] Isolation and structure confirmation of compounds

[0045] (1) Compound separation

[0046] About 80 g of the crude extract obtained in Example 2 was mixed with 100-200 mesh silica gel, and the silica gel column was filled with 200-300 mesh silica gel. Eluent petroleum ether / dichloromethane (v / v, 1:0, 1:1, 0:1) and dichloromethane / methanol (v / v, 100:1, 50:1, 5:1, 2 :1, 0:1) for gradient elution, each gradient elution volume is 3L, a total of 24 components are obtained after each liter of separate concentration, after HPLC liquid phase detection, the samples of the same components are mixed and divided into It is 7 major components Fr1~Fr7.

[0047] After the final elution of methanol, take the loading silica gel retained on the silica gel column and dissolve it with an appropriate amount of DMSO, centrifuge to take the supernatant, then add an equal volume of saturated NaCl brine, and extract the mixed solution with an equal volume of ethyl acetate (EA). ...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

No PUM Login to View More

Abstract

The invention discloses polyketone compounds with antitumor activity, a preparation method therefor and an application of the polyketone compounds. The polyketone compounds (1 to 4) with structures represented by a formula (I) shown in the description are prepared through subjecting an enterocin gene cluster deficient mutant of Steptomyces qinglanensis 1772205 to fermentation and carrying out separation. Proven by in-vitro cytotoxin activity tests, the compounds (1 to 4) disclosed by the invention show inhibition activity of different degrees to tumor cells (HeLa and MCF-7), and particularly,the compound 1 shows a remarkable inhibiting effect on the tumor cells. Ideal candidate compounds are provided for the development of efficient antitumor drugs.

Description

technical field [0001] The invention belongs to the field of microbial medicines, and in particular relates to various polyketide compounds with antitumor activity and their preparation methods and applications. Background technique [0002] Cancer is a leading cause of morbidity and mortality worldwide, accounting for 8.2 million deaths in 2012 alone. However, the morbidity and mortality in our country are still rising gradually, and the trend of younger onset is obvious. Although some anti-tumor drugs have been developed, the high price of anti-tumor drugs, clinical drug resistance, and the side effects of therapeutic drugs have put forward a continuous demand for human discovery of new anti-cancer drugs with high efficiency and low toxicity. [0003] Microbial natural products are an important source of drug lead compounds, and a large number of antitumor compounds have been found in microbial fermentation products. The over-exploitation of terrestrial microorganisms ha...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
Patent Type & Authority Applications(China)
IPC IPC(8): C07D491/16C07D307/33C07C49/203A61P35/00C12P17/04C12P17/18C12P7/26C12R1/465
CPCC07C49/203C07D307/33C07D491/16C12P7/26C12P17/04C12P17/18
Inventor 洪葵徐东波田二丽邓子新
Owner WUHAN UNIV
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com