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Azotone alkaloid with antitumor activity, preparation method and use thereof

A technology of anti-tumor activity and azotrope, which is applied in the field of compounds, can solve the problems of low selectivity, toxic and side effects, etc.

Active Publication Date: 2021-04-27
THIRD INST OF OCEANOGRAPHY MINIST OF NATURAL RESOURCES +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

This patented chemicals are able to kill both types of cells in mice that have been exposed during oral chemotherapy treatment (MCG). They also work with other tumor-associated genes like KRAS genetically linked to certain forms of lung carcinoma called EMLA) which may help explain why these treatments reduce their effectiveness against this type of disease.

Problems solved by technology

The technical problem addressed in this patented text relates to finding effective treatments against advanced forms of breast carcinoma (BCC) without causing harmful side effects on other tissues such as bone marrow stroma and blood vessels.

Method used

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  • Azotone alkaloid with antitumor activity, preparation method and use thereof
  • Azotone alkaloid with antitumor activity, preparation method and use thereof
  • Azotone alkaloid with antitumor activity, preparation method and use thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] Example 1: Fermentation of bacteria Chaetomium MP4-S01-7

[0039] (1) Preparation of bacterial species: use seawater PDA medium, sterilize at high temperature, make a flat plate, place it in a normal temperature state, inoculate activated Chaetomium globosum MP4-S01-7, as bacterial species; the seawater PDA medium The ingredients are 200g potato, 20g glucose, 15-20g agar, 1L seawater;

[0040] The deposit information for Chaetomium globosum MP4-S01-7 is as follows:

[0041] Preserved strain: Chaetomium globosum MP4-S01-7,

[0042] Depository: China Type Culture Collection Center,

[0043] Deposit address: Wuhan University, Wuhan, China,

[0044] Deposit number: CCTCC No.M2019509,

[0045] Deposit date: July 3, 2019.

[0046](2) Preparation of fermented seed liquid: respectively pack seawater PDA liquid culture medium in a plurality of Erlenmeyer flasks, after high-temperature sterilization, inoculate the above-mentioned strains for cultivation, and use the culture ...

Embodiment 2

[0048] Embodiment 2: Extraction and separation of azone alkaloids

[0049] (1) Extraction: After standing at room temperature for 25 days, add 500 mL / bottle of methanol solution to soak the fermentation product, dissolve the fermentation product in the methanol solution, soak overnight, pour out the upper methanol solution to obtain the extract, and extract 3 Once, the resulting extract was filtered with filter paper, concentrated under reduced pressure to a solid state to obtain methanol extraction extract; after methanol extraction extract was dispersed with 1L of distilled water, liquid-liquid extraction was carried out with ethyl acetate, and the ethyl acetate part was taken under reduced pressure. Concentrate to dryness to obtain ethyl acetate extract.

[0050] (2) Separation: extract the extract with ethyl acetate, and perform gradient elution from volume ratio 95:5 to 80:20 with silica gel column chromatography using petroleum ether-ethyl acetate as the eluent to obtain...

Embodiment 3

[0051] Example 3: Structural analysis of azone alkaloids

[0052] The structures of the azone alkaloids were determined based on their mass spectrometry, NMR data analysis.

[0053] Compound 1

[0054] Irregular dark red powder; NMR data see figure 1 ( a Measured at 600 MHz. b measured at 850 MHz); Molecular formula C 33 h 42 ClNO 5 , high resolution mass spectrum HRESIMS(positive)m / z 568.2835[M+H] + (calcd forC 33 h 43 35 ClNO 5 , 568.2830). The structure is:

[0055]

[0056] Compound 2

[0057] Irregular dark red powder; NMR data see figure 1 ;Molecular formula C 33 h 42 ClNO 5 , high resolution mass spectrum HRESIMS(positive)m / z 568.2851[M+H] + (calcd for C 33 h 43 35 ClNO 5 , 568.2830). The structure is:

[0058]

[0059] Compound 3

[0060] Irregular dark red powder; NMR data see figure 1 ;Molecular formula C 28 h 34 ClNO 5 , high resolution mass spectrum HRESIMS(positive)m / z 500.2199[M+H] + (calcd for C 28 h 35 35 ClNO 5 , 500.220...

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Abstract

The invention discloses an azone alkaloid with antitumor activity, a preparation method and an application thereof. The azotone alkaloid has obvious cytotoxicity to gastric cancer cell lines.

Description

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Claims

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Application Information

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Owner THIRD INST OF OCEANOGRAPHY MINIST OF NATURAL RESOURCES
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