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A pimarane type diterpenoid compound having an oxygen-containing five-membered ring, a preparation method and application thereof

A technique for a diterpenoid and a five-membered ring, which is used in the preparation of antitumor drugs, in the field of diterpenoids, and achieves the effect of strong inhibitory activity.

Active Publication Date: 2018-09-25
SECOND MILITARY MEDICAL UNIV OF THE PEOPLES LIBERATION ARMY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] So far, there is no report on the isolation of pimarane diterpenoids with anti-tumor activity from this genus of fungi

Method used

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  • A pimarane type diterpenoid compound having an oxygen-containing five-membered ring, a preparation method and application thereof
  • A pimarane type diterpenoid compound having an oxygen-containing five-membered ring, a preparation method and application thereof
  • A pimarane type diterpenoid compound having an oxygen-containing five-membered ring, a preparation method and application thereof

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Experimental program
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Effect test

Embodiment 1

[0036] Embodiment 1. Preparation of compounds of the present invention

[0037] 1. Prepare the total crude extract

[0038]1) Pick a small amount of mycelium of the bacterial strain of Eutypella sp.D-1 whose preservation number is CCTCC NO: M 2013144 from the plate, inoculate it into a 250mL Erlenmeyer flask for seed culture, and each Erlenmeyer flask contains 100mL of seed medium, Cultivate at a constant temperature on a shaker at 28°C with a rotation speed of 180r / min, and cultivate for 3.5 days to obtain a first-class seed liquid, insert the same seed medium according to the inoculation amount of 5% (v / v), and cultivate at 28°C and 180r / min on a shaker for 3.5d , to obtain fresh secondary seed liquid for fermentation and cultivation. Then the seed culture liquid is inoculated into the Erlenmeyer flask of 2000mL and carries out expanded cultivation, and the fermentation medium of 400mL of each Erlenmeyer flask, inserts fresh secondary seed liquid according to the inoculum s...

Embodiment 2

[0052] Embodiment 2 The in vitro antitumor activity experiment of the compound of the present invention:

[0053] Method: CCK8 method (Tominaga H, Ishiyama M, Ohseto F, et al.A water-solubleetrazolium salt useful for colorimetric cell viability assay[J].Analytical Communications,1999,36(2):47-50.)

[0054] Human pancreatic cancer cells PANC-1, human breast cancer cells MCF-7, human colon cancer cells HCT-116, human chronic leukemia cells K562, and human pancreatic cancer cells SW1990 in logarithmic growth phase were respectively taken at 5000 cells / well. The cell density was seeded in a 96-well plate and placed in 5% CO at 37°C. 2 cultured in a constant temperature incubator. After 24 hours, add 10 μL of samples of different concentrations to the 96-well plate, so that the final volume of the solution in the plate is 100 μL. After continuing to cultivate in the incubator for 48 hours, add 10 μL of CCK-8 solution and continue to incubate for about 1 hour. Take it out, and use ...

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Abstract

A pimarane type diterpenoid compound having an oxygen-containing five-membered ring is disclosed. The chemical structure of the compound is shown as a formula (I) in the description. In-vitro activitytests prove that the compound has high inhibitory activity for a plurality of human tumor cells such as human pancreatic cancer cells PANC-1, human breast carcinoma cells MCF-7, human colon cancer cells HCT-116, human chronic leukemia cells K562 and human pancreatic cancer cells SW1990, and can be used for preparing antitumor medicines.

Description

technical field [0001] The present invention relates to the technical fields of marine biology and medicine, in particular to a kind of oxygen-containing pentaphyllum obtained through extraction, separation and purification from arctic soil Curvularia sp.D-1. Pirimane diterpenoids with member rings, preparation method and application thereof in the preparation of antitumor drugs. Background technique [0002] Due to the special environment of low temperature, repeated freezing and thawing and strong radiation in the polar regions, in order to adapt to the extreme living environment, polar microorganisms may have different molecular biological mechanisms and physiological and biochemical characteristics from temperate and tropical microorganisms, and produce many novel structures and activities. Unique secondary metabolites. Therefore, the research on the secondary metabolites of polar microorganisms has attracted more and more attention from domestic and foreign research. ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D307/77A61P35/00A61P35/02C12P17/04C12R1/645
CPCA61P35/00A61P35/02C07D307/77C12P17/04
Inventor 于豪冰刘小宇张艺馨王晓丽许维恒卢小玲焦炳华
Owner SECOND MILITARY MEDICAL UNIV OF THE PEOPLES LIBERATION ARMY
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