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Benzodifuranone compound with antitumor activity, preparation method and use thereof

A technology for benzodifuranone and anti-tumor activity, which is applied in the field of compounds and can solve the problems of low bioavailability, complex structure and little research.

Active Publication Date: 2021-04-09
THIRD INST OF OCEANOGRAPHY MINIST OF NATURAL RESOURCES +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

STAT3 inhibitors include natural products, peptides and peptidomimetics, and small molecule inhibitors; natural product STAT3 inhibitors have complex structures and few studies; peptides and peptidomimetics have good activity, but due to low bioavailability in vivo, It is still very difficult to develop into clinical drugs; therefore, small molecule inhibitors with good activity, physical and chemical properties, and ideal pharmacokinetic properties are hot spots in the research of STAT3 inhibitors

Method used

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  • Benzodifuranone compound with antitumor activity, preparation method and use thereof
  • Benzodifuranone compound with antitumor activity, preparation method and use thereof
  • Benzodifuranone compound with antitumor activity, preparation method and use thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] Example 1: Extraction and separation of benzodifuranone compounds

[0032] Preparation of strains: use seawater PDA medium, sterilize at high temperature, make a plate, place it at room temperature, inoculate the activated Aspergillus terreus CC-S06-18 as a strain; the seawater PDA medium The ingredients are 200g of potatoes, 20g of glucose, 15-20g of agar, and 1L of seawater;

[0033] The deposit information of Aspergillus terreus CC-S06-18 is as follows:

[0034] Preserved strains: Aspergillus terreus CC-S06-18,

[0035] Deposit unit: China Center for Type Culture Collection,

[0036] Deposit address: Wuhan University, Wuhan, China,

[0037] Deposit number: CCTCC No.M2019793,

[0038] Deposit date: October 10, 2019.

[0039] Preparation of fermented seed liquid: put seawater PDA liquid culture medium (200g of potatoes, 20g of glucose, 1L of seawater) into several Erlenmeyer flasks respectively, after high-temperature sterilization, inoculate the above-mentioned s...

Embodiment 2

[0043] Example 2: Structural Analysis of Benzodifuranone Compounds

[0044] The structures of benzodifuranones were determined based on their mass spectrometry and nuclear magnetic resonance data analysis.

[0045] Irregular dark red powder; NMR data are shown in the table (measured at 600MHz); molecular formula C 20 h 18 o 4 , high resolution mass spectrum HRESIMS(positive)m / z 345.1106[M+Na] + (theoretical molecular formula is C 20 h 18 o 4 Na, the theoretical molecular weight is 345.1103).

[0046] The structure is:

[0047]

[0048] NMR data are shown in Table 1.

[0049] Table 1 NMR data sheet

[0050] position δ C ,Type

Embodiment 3

[0051] Embodiment 3: Function test of benzodifuranone compound AtrA

[0052] 1. AtrA cytotoxicity test

[0053] CCK8 assay was used to determine the effect of compound AtrA on the viability of gastric cancer cell lines HGC27, MGC803, BGC823, AGS and normal gastric epithelial cell line GES-1.

[0054] Culture of human gastric cancer cell lines:

[0055] Human gastric cancer cell lines MGC803, BGC823, AGS, HGC27 and human normal gastric epithelial cell line GES-1 were obtained from the Institute of Cells, Chinese Academy of Sciences (Shanghai, China). These cells are commercially available and can also be purchased from the ATCC. All cell lines were cultured in RPMI1640 containing 10% fetal bovine serum and 1% penicillin / streptomycin at 37 °C, 5% CO 2 cultured in an incubator.

[0056] Cell viability assay: Gastric cancer cell lines MGC803, BGC823, AGS and HGC27 and normal gastric epithelial cell line GES-1 were cultured overnight in 96-well plates, and then treated with dif...

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Abstract

The invention discloses a benzodifuranone compound with antitumor activity, a preparation method and an application thereof. The benzodifuranone compounds have obvious cytotoxicity to gastric cancer cell lines.

Description

technical field [0001] The invention relates to the field of compounds, in particular to a benzodifuranone compound with antitumor activity, a preparation method and use thereof. Background technique [0002] Cancer is a general term for a large class of malignant tumors. Cancer cells are characterized by unlimited and endless proliferation, which consumes a large amount of nutrients in the patient's body; cancer cells release a variety of toxins, causing a series of symptoms in the human body; cancer cells can also be transferred to grow and multiply throughout the body, Lead to body weight loss, weakness, anemia, loss of appetite, fever, and severe damage to organ function. [0003] Due to their special living environment, marine microorganisms have formed unique genetic metabolic mechanisms and chemical defense mechanisms during the evolution process of adapting to the environment, and are currently the main source of new structures or new active natural products. Marin...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D493/04A61P35/00A61K31/365C12P17/18C12N1/14C12R1/66
CPCA61P35/00C07D493/04C12N1/14C12P17/181
Inventor 王伟毅覃江江邵宗泽杨静
Owner THIRD INST OF OCEANOGRAPHY MINIST OF NATURAL RESOURCES
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