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Cyclic tetrapeptide compounds with anti-tumor activity as well as preparation method and application thereof

A compound, the technology of cyclic tetrapeptide, applied in the field of cyclic tetrapeptide compound cyclo- and cyclo- and its preparation

Inactive Publication Date: 2014-09-03
GUANGXI ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

So far, there is no report on the acquisition of cyclotetrapeptide compounds cyclo-(Ile-Pro-Leu-Pro) and cyclo-(Tyr-Pro-Phe-Gly) with antitumor activity from the marine bacterium Bacillus amyloliquefaciens

Method used

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  • Cyclic tetrapeptide compounds with anti-tumor activity as well as preparation method and application thereof
  • Cyclic tetrapeptide compounds with anti-tumor activity as well as preparation method and application thereof
  • Cyclic tetrapeptide compounds with anti-tumor activity as well as preparation method and application thereof

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Experimental program
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Embodiment 1

[0013] (1) prepare diterpenoid cyclo-(Ile-Pro-Leu-Pro) and cyclo-(Tyr-Pro-Phe-Gly) of the present invention

[0014] Prepare 720mL liquid seed medium and distribute it into six 250mL Erlenmeyer flasks, each bottle is about 120mL. Sterilize at 121°C for 15 minutes, cool to room temperature, and insert marine bacteria Bacillus amyloliquefaciens into it. In a constant temperature shaker, culture at 150r / min and 28°C for about 3 days. Obtain 720mL seed culture solution.

[0015] Prepare 100L of liquid medium: 1000g of peptone, 500g of yeast extract, 500g of sodium chloride, 100L of aged seawater, and adjust the pH value to about 7.4 with sodium hydroxide. Divide into 320 Erlenmeyer flasks of 250 mL (approximately 150 mL), add silica gel stoppers, sterilize at 121°C for 20 minutes, cool to room temperature naturally, and receive 2 mL of seed culture solution in each bottle. 150r / min and 28°C were shaken for 6 days to obtain 100L of fermentation broth.

[0016] The fermentation ...

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Abstract

The invention discloses a preparation method and application for cyclic tetrapeptide compounds with anti-tumor activity. The invention provides two novel cyclic tetrapeptide compounds which are obtained by extracting and separating from marine bacteria bacillus amyloliquefaciens, have structural formulas as shown in formula (I), are respectively named as cyclo-(Ile-Pro-Leu-Pro) (1) and cyclo-(Tyr-Pro-Phe-Gly) (2). Activity test results of the compounds 1-2 indicate that the compounds 1 and 2 can be used as an inhibitor of NFKB, have effects for inducing apoptosis of tumor cells, and can be used for preparing anti-tumor drugs. The invention provides a novel pilot compound for researching the anti-tumor drugs, and provides scientific basis for developing and utilizing natural active substances of a marine microorganism source.

Description

technical field [0001] The invention relates to the technical field of marine natural medicines, and relates to cyclotetrapeptide compounds cyclo-(Ile-Pro-Leu-Pro) and cyclo-(Tyr-Pro) isolated from marine bacteria Bacillus amyloliquefaciens and having antitumor activity. -Phe-Gly) and its preparation method and use. Background technique [0002] Malignant tumor, often called cancer, is a major disease that threatens human health, and its incidence rate ranks second among major diseases. And with the aging of the population, the increase in the number of smokers, the reduction in physical activity, and the lack of vegetables and fruits in the diet and other bad habits may further lead to a sharp increase in the number of cancers worldwide. At present, 20% of new cancer patients in the world are in China, and 24% of cancer deaths are in China. Therefore, antineoplastic drugs are currently the key areas of new drug development in the world. [0003] Marine microbial secondar...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K5/12C12P21/06A61K38/12A61P35/00C12R1/07
Inventor 高程海潘丽霞张荣灿陈波珂珂庄军莲
Owner GUANGXI ACAD OF SCI
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