Cytochalasin compound, and preparation method and application thereof

A technology of cytochalasin and compounds, applied in biochemical equipment and methods, organic chemical methods, microbial-based methods, etc., to achieve strong inhibitory activity

Active Publication Date: 2021-12-31
INST OF OCEANOLOGY - CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

But so far there is no report on the systematic research on the secondary metabolites of Curvularia verruculosa. The present invention isolates cytochalasin compounds with anti-tumor activity from this bacteria for the first time.

Method used

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  • Cytochalasin compound, and preparation method and application thereof
  • Cytochalasin compound, and preparation method and application thereof
  • Cytochalasin compound, and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] Embodiment 1. Compound structural formula

[0029] The structure of the cytochalasin compound isolated from the fermentation product of Curvularia verruculosa (Curvularia verruculosa) is shown in formula (I) (the Arabic numerals in the formula represent the carbon atom label in the chemical structure):

[0030]

Embodiment 2

[0031] The preparation method of compound shown in embodiment 2. formula I

[0032] 1) Fermentation culture

[0033] The Curvularia verruculosa (Curvularia verruculosa) takes an appropriate amount of strains and inoculates it on a PDA plate. On the PDA (potato sucrose agar) medium, the mycelium is white-gray, and produces white spores in the later stage. After cultivating for 7 days at 28° C. stand-by.

[0034] Inoculate the mycelium of the above-mentioned PDA plate in a sterile solid medium, and culture it statically at room temperature for 30 days. After the fermentation product is extracted with petroleum ether to remove small polar products, it is soaked and extracted 4 times with ethyl acetate, combined and concentrated After obtaining the fermented crude extract;

[0035] The formula of the solid medium is: every 100 milliliters of seawater contains 70 grams of rice, 0.1 grams of corn steep liquor and 0.3 grams of peptone.

[0036] 2) Separation and purification of th...

Embodiment 3

[0045] Embodiment 3. Antitumor activity experiment

[0046] Select the following 3 test cell lines: liver cancer cell line (HepG-2), colon cancer cell line (HCT-116), breast cancer cell line (MCF-7) for anti-tumor activity test.

[0047] 1) Tested cell lines and their culture

[0048] The test cell lines used in the present invention are liver cancer cell lines (HepG-2), colon cancer cell lines (HCT-116), breast cancer cell lines (MCF-7), and the cells are contained in 10% fetal calf serum, 100U / ml penicillin and 100 mg / ml streptomycin in RPMI-1640 medium. All experiments were performed with the same batch of cell lines between passage 2 and passage 5.

[0049] 2) Preparation of samples to be tested

[0050] The test sample is the pure compound obtained in the above examples, accurately weighs an appropriate amount of sample, and prepares a solution with a required concentration with dimethyl sulfoxide (DMSO) for activity testing. The preparation method of positive contro...

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Abstract

The invention relates to a microbial metabolite and an application technology thereof in the field of drug research, and concretely relates to a preparation method and application of a cytochalasin compound produced by microbial metabolism. The chemical structure of the cytochalasin compound is shown as a formula I, and the cytochalasin compound is prepared by carrying out fermentation culture on Curvularia verruculosa. Experiments show that the compound has anti-tumor activity and can be used as a cell proliferation inhibitor or an anti-tumor preparation. The prepared cytochalasin compound is produced by fermentation culture of microorganisms, and has the characteristics of simplicity in operation, short production period, low cost and the like.

Description

technical field [0001] The invention relates to microbial metabolites and their application technology in the field of pharmaceutical research, in particular to a cytochalasin compound obtained from a fermentation product of Curvularia verruculosa and its preparation method and application. Background technique [0002] Malignant tumors are important diseases that seriously threaten human health. China is a country with a large incidence of malignant tumors. According to the "2017 China Tumor Registration Annual Report" of the National Cancer Center, Chinese malignant tumor patients account for nearly 40% of the total number of cancer patients in the world. About 10,000 people are diagnosed with cancer every day, an average of 7 people are diagnosed every minute. Liver cancer, colon cancer, and female breast cancer are still the main malignant tumors in my country, and breast cancer is the first among females. [0003] Although researchers have been committed to the study ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D491/107C12P17/18A61K31/407A61P35/00C12R1/645
CPCC07D491/107C12P17/18A61P35/00C07B2200/07
Inventor 王斌贵胡雪怡李晓明孟令红李鑫
Owner INST OF OCEANOLOGY - CHINESE ACAD OF SCI
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