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Briarane type diterpenoid compounds with anti-tumor and antibacterial activities and application thereof

A technology for anti-tumor drugs and compounds, which can be used in anti-tumor drugs, organic active ingredients, medical preparations containing active ingredients, etc., and can solve problems such as no anti-tumor or antibacterial activity.

Active Publication Date: 2011-11-02
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

In addition to the report that compound dichotellide C has weak inhibitory activity on pancreatic cancer cells SW1990 (Sun, J.F., Huang, X.Y. Yang, X.W., Meng, L., Huang, C.G., Zhou, X.F., Yang, B., Hu, J. , Chen, X.Q., Wang, L.S.and Liu, Y.H.Dichotellides A-E, five new iodine-containing briarane type diterpenoids from.Dichotella gemmacea.Tetrahedron, 2011, 67, 1245-1250.), no information about the isolation from this species of gorgonian Reports of antitumor or antibacterial activity of Briarane-type diterpenoids

Method used

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  • Briarane type diterpenoid compounds with anti-tumor and antibacterial activities and application thereof
  • Briarane type diterpenoid compounds with anti-tumor and antibacterial activities and application thereof
  • Briarane type diterpenoid compounds with anti-tumor and antibacterial activities and application thereof

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] Embodiment 1. preparation compound gemmacolides G~Z, gemmacolides ZI~gemmacolide ZXXXIII, Juncin O and Junceellolide C

[0024] 1. Preparation: crush the gorgonian coral (Dichotella gemmacea) with a wet weight of 3.5Kg, and extract it with 2L acetone ultrasonically as usual, and concentrate the extract under reduced pressure to obtain a total crude extract of 29.6g, then suspend and disperse with water, and separate Extracted 5 times with ethyl acetate and n-butanol, and concentrated under reduced pressure to obtain 16.1 g of ethyl acetate extract and 3.6 g of n-butanol extract, respectively. Then the ethyl acetate extraction extract was suspended and dispersed in 1.5L methanol, extracted 4 times with n-hexane, and the n-hexane extract and the methanol layer were concentrated under reduced pressure respectively to obtain 3.7 g of n-hexane extract extract and 3.7 g of methanol layer extract. Cream 11.2g. Then 11.2g of the methanol layer extract was separated by normal p...

Embodiment 2

[0163] Example 2. Antitumor experiments of diterpenoids 1 to 55 (Gemmacolides G to Z, Juncin O, Junceellolide C, gemmacolides ZI to gemmacolide ZXXXIII) of the present invention

[0164] 1. Experimental method

[0165] The compound of the present invention was tested for inhibition of tumor cell proliferation by conventional MTT method (Mosmann, T. Rapid colorimetric assay for cellular growth and survival: application to proliferation and cytotoxicity assays. J. Immunol. Methods 1983, 65, 55-63).

[0166] 1. Cell lines used in the experiment: A549 (human lung cancer cells), U251 (human glioma cells) and MG63 (human osteosarcoma cells). The cell lines used in the experiments were from the Institute of Cells, Chinese Academy of Sciences.

[0167] 2. Experimental reagents, consumables and instruments:

[0168]DMEM medium (Invitrigen); 1640 medium (Invitrigen); McCoy's 5a (Invitrigen); serum (Invitrigen); trypsin (Invitrigen); DMSO (sigma); dish (Corning); pipette (Corning); 96...

Embodiment 3

[0185] Embodiment 3. the antibacterial experiment of diterpenoids 1~55 (Gemmacolides G~Z, Juncin O, Junceellolide C, gemmacolides ZI~gemmacolide ZXXXIII) of the present invention

[0186] 1. Experimental method

[0187] The compound of the present invention is carried out in vitro antibacterial test by agar diffusion method

[0188] 1. Experimental bacteria (provided by the Marine Drug Research Center of the Second Military Medical University)

[0189] Fungi: Microbotryum violaceum, Septoria tritici;

[0190] Bacteria: Escherichia coli, Bacillus megaterium.

[0191] 2. Experimental drugs

[0192] 1) Positive control drugs: penicillin (purchased from Harbin Pharmaceutical Group General Pharmaceutical Factory), streptomycin (purchased from North China Pharmaceutical Co., Ltd.), ketoconazole (purchased from North China Pharmaceutical Co., Ltd. company);

[0193] 2) Negative reference substance: acetone (Acetone) (purchased from Sinopharm Chemical Reagent Co., Ltd.);

[0194...

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Abstract

The invention relates to the technical field of medicines, discloses 53 novel Briarane type diterpenoid compounds with anti-tumor and antibacterial activities, i.e. gemmacolides G-Z and gemmacolides ZI-ZXXXIII, which are obtained through the separation of marine animal gorgonian Dichotella gemmacea, and also discloses two known compounds, i.e., Juncin O and Junceellolide C. Experiments of anti-tumor and antibacterial activities in vitro show that the compounds disclosed by the invention have obvious inhibiting effects on multiple tumor cells such as A549 (human lung cancer cells), U251 ( human brain glioma cells) and MG63 (human bone sarcoma cells) and the like and has obvious bacteriostatic activity on anther smut fungus, septoria musiva septoria tritici, escherichia coli and enormous bacillus and the like; and therefore, the compounds can be used for preparing anti-tumor or antibacterial medicines. The invention has the advantages of providing a leading compound for the research of new anti-tumor or antibacterial medicines and being beneficial to the development and utilization of ocean medicinal resources.

Description

technical field [0001] The present invention relates to the technical field of medicine, in particular to 53 new Briarane-type diterpenoids gemmacolides G-Z, gemmacolides ZI-gemmacolide ZXXXIII and 2 species isolated from the marine animal Dichotella gemmacea with anti-tumor and antibacterial activities Known Briarane-type diterpenoids Juncin O and Junceellolide C with antitumor and antibacterial activities and their applications. Background technique [0002] Dichotellagemmacea belongs to the class Anthozoa, Octocorallia, Gorgonacea, and Ellisellidae. About 20 diterpenoids have been isolated from this species of gorgonian, such as compounds gemmacolides A-F, dichotellides A-E, praelolide, juncin P, juncin ZI, junceellin A and several unnamed compounds (see Bowden, B.F., Coll , J.C., Konig, G.M.Studies of Australian Soft Corals.XLVIII.New Briaran Diterpenoids From the Gorgonian Coral Junceela gemmacea.Aust.J.Chem,1990,43,151-159;He,H.Y.and Faulkner,D.J.new cholrinated diter...

Claims

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Application Information

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IPC IPC(8): C07D307/93A61K31/365A61P35/00A61P31/04A61P31/10
CPCY02A50/30
Inventor 张文易杨华李翠李玲孙鹏刘宝姝汤华
Owner SECOND MILITARY MEDICAL UNIV OF THE PEOPLES LIBERATION ARMY
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