Compounds with tumor cell proliferation resistance, and preparation method and application thereof

A compound, separation and purification technology, applied in the field of medicine, can solve the problem of very little research on symbiotic bacteria and their metabolites

Inactive Publication Date: 2015-02-25
HUAZHONG UNIV OF SCI & TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, compared with the species diversity of insects, there

Method used

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  • Compounds with tumor cell proliferation resistance, and preparation method and application thereof
  • Compounds with tumor cell proliferation resistance, and preparation method and application thereof
  • Compounds with tumor cell proliferation resistance, and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] Example 1: Preparation and structure identification of the compounds chaetomin F and H.

[0030] (1) Preparation of Chaetomycin F and H as shown in formula (1)

[0031] 1. Fermentation conditions

[0032] Preparation of seed culture solution: Take 3.0g of yeast extract, 3.0g of malt extract, 5.0g of peptone, and 10.0g of glucose, dissolve them in an appropriate amount of water, then dilute to 1000mL with water, sterilize at 121°C for 30 minutes, and set aside. The insect symbiotic bacterium Chaetomium globosum TW1-1 was inoculated into the above-mentioned culture medium, and cultured on a shaker under the conditions of 25-28° C. and 100-120 rpm for 3-5 days to obtain a seed culture solution.

[0033] Fermentation: put 200g of rice into a 1000mL Erlenmeyer flask, add 200mL of water, sterilize at 121°C for 30min, and set aside. The above seed culture solution is inoculated into the rice culture medium, and cultured statically for 25-30 days under the condition of 25-28°...

Embodiment 2

[0039] Example 2: Inhibitory activity of compounds 2-9 on leukemia cells HL-60, human liver cancer cells SMMC-7721, human lung cancer cells A-549, human breast cancer cells MCF-7, and human colon cancer cells SW480 cells.

[0040] The antitumor activity of compound 2-9 was tested by MTS method against leukemia cell HL-60, human liver cancer cell SMMC-7721, human lung cancer cell A-549, human breast cancer cell MCF-7, and human colon cancer cell SW480 five human tumor cells Make an evaluation. The results are shown in Table 3:

[0041] Table 1. 1 H NMR data for compounds 1,6,and 8(400MHz,J in Hz)

[0042]

[0043]

[0044]

[0045] Experimental conclusion: Compound 4 selectively inhibits human liver cancer cells SMMC-7721, and can be used as a lead compound for the development of anti-hepatoma cell drugs. Compound 8 has significant inhibitory activity on five human tumor cells, among which it is superior to the positive control drug cisplatin on human lung cancer cell...

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Abstract

The invention belongs to the technical field of medicine, and provides activities and structure of new indole alkaloid compounds 1-10 derived from insect symbiotic bacterium Chaetomium globosum secondary metabolite and also provides a separation purification preparation method and related activities of compounds pillworm chaetoglobosins E and H with favorable antitumor activity. The structural formula is disclosed as (I). The invention provides an alternative compound for developing new antitumor drugs, and has very important meanings for development and utilization of medicinal insect symbiotic bacterium resources.

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to the separation and preparation method and application of compound 1-10. It specifically involves the separation and purification process, structure confirmation, anti-tumor cell proliferation, etc. Background technique [0002] Symbiotic bacteria are a large group of special microorganisms that live together with the host for a long time. According to different hosts, they can be divided into plant endophytes, insect symbiotic bacteria, sponge symbiotic bacteria and other symbiotic bacteria. Insect symbionts are an important source of active secondary metabolites, and they also play very important roles in insects. With the limitation of plant resources, the probability of discovering new active ingredients from plants and plant endophytes is getting smaller and smaller. The types of insects are very rich, and the number of insects that have been reported is close to 1 million, ...

Claims

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Application Information

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IPC IPC(8): C07D491/044C07D209/96C07D491/08C12P17/18C12P17/16A61P35/00A61P35/02C12R1/645
CPCC07D491/044C07D209/96C07D491/08C12P17/165C12P17/18
Inventor 张勇慧薛永波陈春梅朱虎成张锦文
Owner HUAZHONG UNIV OF SCI & TECH
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