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Pimarane diterpene compounds containing four-membered rings and antitumor application thereof

A kind of technology of pimamarane diterpenes and compounds, which is applied in the preparation of antitumor drugs, the field of pimamarane diterpenoids

Active Publication Date: 2018-07-10
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

[0006] But so far there is no report on the isolation of four-membered ring-containing pirimane diterpenoids with antitumor activity from this genus of fungi

Method used

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  • Pimarane diterpene compounds containing four-membered rings and antitumor application thereof
  • Pimarane diterpene compounds containing four-membered rings and antitumor application thereof
  • Pimarane diterpene compounds containing four-membered rings and antitumor application thereof

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Embodiment 1

[0037] Embodiment 1. Preparation of compounds of the present invention

[0038] The strain used in the present invention is isolated from Arctic Curvularia sp.D-1 (Eutypella sp.D-1) from the soil sample of London Island (100 meters above sea level) in Kongsfjorden, was preserved in the China Center for Type Culture Collection (CCTCC) on April 12, 2013. The deposit number is CCTCC NO: M 2013144.

[0039] 1. Prepare the total crude extract

[0040] 1) pick a small amount of mycelium of the 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 is equipped with 100mL of seed culture 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, 180r / min on ...

Embodiment 2

[0059] Embodiment 2 The in vitro antitumor activity experiment of the compound of the present invention:

[0060] Method: CCK8 method (references: Tominaga H, Ishiyama M, Ohseto F, et al.A water-soluble tetrazolium salt useful for colorimetric cell viability assay[J].Analytical Communications,1999,36(2):47-50. )

[0061] Human cervical cancer cells Hela, human breast cancer cells MCF-7, human colon cancer cells HCT-116, human chronic leukemia cells K562, and human pancreatic cancer cells SW1990 in the logarithmic growth phase were respectively taken at a cell density of 5000 cells / well. Inoculated in 96-well plates, placed at 37 °C 5% CO 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...

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Abstract

The invention relates to the technical field of medicine, in particular to a series of rare diterpene compounds which contain four-membered rings merged with pimarane mother nucleuses and are obtainedby conducting extraction, separation and purification on Eutypella sp. D-1 in Arctic soil. The chemical structures of the compounds are shown in the description. It is proved through in-vitro activity tests that the compounds have certain inhibitory activity on various different tumor cells such as human cervical cancer cells Hela, human breast cancer 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 drugs.

Description

technical field [0001] The invention relates to the technical fields of marine biology and medicine, in particular, it is a kind of quaternary-containing Cyclic piparane diterpenoids and their application in the preparation of antineoplastic 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. Eutypella sp.D-1 is isolated from the root soil of the high arctic latitude (78°55’N) of the nymphaeum, and belongs to the phylum Asco...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C69/30C07D305/14C12P7/62C12P17/02A61P35/00A61P35/02C12R1/645
CPCC07C69/30C07D305/14C12P7/62C12P17/02
Inventor 于豪冰张艺馨刘小宇卢小玲王晓丽焦炳华
Owner SECOND MILITARY MEDICAL UNIV OF THE PEOPLES LIBERATION ARMY
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