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Sesquiterpene compound and its preparation method and application in the preparation of antitumor drugs

An anti-tumor drug, a technology of sesquiterpenoids, applied in the field of medicine and biology

Active Publication Date: 2021-12-31
GUANGDONG INST OF MICROBIOLOGY GUANGDONG DETECTION CENT OF MICROBIOLOGY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

So far, there is no report on the secondary metabolites of this model strain, and it is urgent to do in-depth research on it

Method used

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  • Sesquiterpene compound and its preparation method and application in the preparation of antitumor drugs
  • Sesquiterpene compound and its preparation method and application in the preparation of antitumor drugs
  • Sesquiterpene compound and its preparation method and application in the preparation of antitumor drugs

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Experimental program
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Embodiment 1

[0028] 1. The present invention Aspergillus saureoterrus GDMCC 3.619 is deposited in Guangdong Microbial Culture Collection Center (GDMCC).

[0029] 2, Aspergillus saureoterrus Solid Fermentation of GDMCC 3.619

[0030] Aspergillus Aspergillus saureoterrus The mycelium of GDMCC 3.619 was inoculated in potato dextrose agar medium, cultured statically at 28°C for 5 days, and then about 1×1 cm 2 The agar block with hyphae was inoculated in potato dextrose broth (PDB) liquid medium, and cultured at 28°C and 160 rpm / min for 16 days to obtain a liquid fermentation culture. Potato dextrose agar medium, passed per liter The following method is prepared: 200 g potato flour, 20 g glucose and 20 g agar are added to 1000 mL distilled water, heated to dissolve, and sterilized; Mix with 1000 mL of water for sterilization.

[0031] 3. Compound preparation

[0032] (1) Extraction with ethyl acetate Aspergillus saureoterrus The liquid fermentation culture of GDMCC 3.619 was extracte...

Embodiment 2

[0049] The in vitro antitumor activity of compound 1 was tested.

[0050] The human cells detected in this experiment are as follows: human promyelocytic leukemia cell HL-60, human ovarian adenocarcinoma cell SKOV-3, and human liver cancer cell HepG-2.

[0051] 1. The principle of MTS method for detecting cell activity: MTS is a brand new MTT analogue, its full name is 3-(4,5-dimethylthiazol-2-yl)-5(3-carboxymethoxyphenyl)-2-(4-sulfopheny)- 2H-tetrazolium, is a yellow dye. Succinate dehydrogenase in the mitochondria of living cells can metabolize and reduce MTS to generate soluble formazan (Formazan) compounds. The content of formazan can be measured at 490 nm with a microplate reader. Under normal circumstances, the amount of formazan produced is directly proportional to the number of living cells, so the number of living cells can be inferred from the optical density OD value.

[0052] 2. Experimental method

[0053] (1) Cell inoculation: Prepare a single cell suspension ...

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Abstract

The invention discloses a sesquiterpene compound, a preparation method thereof and an application in preparation of antitumor drugs. The sesquiterpenoid compound described in the present invention is from Aspergillus fungus Aspergillus saureoterrus It is isolated and prepared from the fermentation culture of GDMCC 3.619. Tests have proved that the compound has strong inhibitory activity on human promyelocytic leukemia cells (HL‑60), liver cancer cells (HepG‑2) and ovarian adenocarcinoma cells (SKOV‑3), and can be used to prepare anti-acute promyelocytic leukemia cells Drugs for myeloid leukemia, liver cancer, or ovarian adenocarcinoma.

Description

technical field [0001] The invention belongs to the technical field of medicine and biology, and in particular relates to a sesquiterpene compound, a preparation method thereof and an application in preparation of antitumor drugs. Background technique [0002] Fungi are widely present in nature, and their main sources are soil, ocean, plants, animals, etc., which can produce a large number of structurally diverse and biologically active secondary metabolites, including aromatic polyketides, terpenes, alkaloids, etc. type of complex structure. Aspergillus saureoterrus GDMCC3.619 is a soil-derived Aspergillus fungus. So far, there is no report on the secondary metabolites of this model strain, and further research is urgently needed. Contents of the invention [0003] The first object of the present invention is to provide sesquiterpenoids having tumor inhibitory activity. [0004] The compound of the present invention has a structure as shown in formula (І): [0005] ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07C69/587A61K31/232A61P35/02A61P35/00C12P7/64C12N1/14C12R1/66
CPCC07C69/587A61P35/02A61P35/00C12P7/6436C12N1/14C07C2602/28
Inventor 臧毅朱红惠邓名荣周北平
Owner GUANGDONG INST OF MICROBIOLOGY GUANGDONG DETECTION CENT OF MICROBIOLOGY
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