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Antineoplastic alkaloid compound, and its medicine composition, preparation method and application

A technology of anti-tumor drugs and compounds, applied in the field of medicine, can solve the problems of no reports of dimeric monoterpene indole alkaloids, reports of no activity, etc.

Inactive Publication Date: 2012-07-25
KUNMING INST OF BOTANY - CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0002] Bermudagrass ( Ervatamia ) There are 15 species and 5 varieties in my country, which are mainly distributed in Southwest China to South China. At present, there is no report of the dimeric monoterpene indole alkaloid Ervachinines A-D in the prior art, let alone its activity.

Method used

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  • Antineoplastic alkaloid compound, and its medicine composition, preparation method and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0018] Chinese dog tooth flower ( Ervatamia.chinensis ) 7.5 kg of the whole plant, heated and refluxed with 95% ethanol for three times (3′4 h), combined the extracts, recovered the ethanol under reduced pressure, kneaded the concentrated extract with 3% tartaric acid aqueous solution and adjusted the pH value to 2~ 3. Extract three times with petroleum ether and ethyl acetate respectively, and then use saturated Na 2 CO 3 The solution was adjusted to pH 9-10 with CHCl 3 The extraction obtained 40 g of the total alkali fraction. The total alkali part was obtained by silica gel column chromatography (petroleum ether-acetone gradient elution) to obtain four parts (F 1 –F 4 ), F 3 (1.2 g) was separated from the compound ervachinine A ( 1 , 17.0 mg), ervachinine C ( 3 , 25.0 mg); F 4 (1.5 g) three fractions (P 1 –P 3 ), P 2 Part (600 mg) was subjected to silica gel column chromatography (petroleum ether / ethyl acetate, 10:1? 3:1) and Sephadex LH-20 (methanol) to obta...

Embodiment 2

[0024] Ervachinines A-D ( 1 - 4 ) Experimental results of anti-tumor pharmacological effects:

[0025] 1. Determination of Drugs and Compounds

[0026]Samples to be tested ervachinines A-D ( 1 - 4 ) is prepared by Example 1 of the present invention. The sample to be tested was dissolved in DMSO, stored at 4°C, and the storage concentration was 40 μM;

[0027] 2. Test method

[0028] 1. Inoculate cells: Use culture medium (DMEM or RMPI1640) containing 10% fetal bovine serum to prepare a single cell suspension, inoculate 5000-10000 cells per well into a 96-well plate with a volume of 100 μl per well, and adherent cells in advance 12 hour inoculation.

[0029] 2. Add the compound solution to be tested (fixed concentration of 40 μM for primary screening, at which concentration the compound that inhibits tumor cell growth at around 50% is set for gradient re-screening), the final volume of each well is 200 μl, and each treatment is set at 3 multiple holes.

[0030] 3. Colo...

Embodiment 3

[0038] Dimeric indole alkaloid ervachinines A-D (shown in structures 1-4) were first prepared according to the method of Example 1, and water for injection was added respectively according to the routine, finely filtered, potted and sterilized to make an injection.

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Abstract

The invention provides vobasine-iboga type alkaloid compound ervachinines A-D (1-4) with antineoplastic activities, its preparation method, a medicine composition containing the alkaloid compound, and an application of the alkaloid compound and the medicine composition in preparation of antineoplastic drugs, wherein structural formulas of the vobasine-iboga type alkaloid compound ervachinines A-Dare shown as the formulas of 1 to 4.

Description

technical field [0001] The invention belongs to the technical field of medicines, in particular, it relates to Ervachinines A-D, which are dimeric monoterpene indole alkaloids of formula (1-4) with antitumor activity, which are pharmaceutical compositions of active ingredients of medicines. application in antineoplastic drugs. Background technique [0002] Bermudagrass ( Ervatamia ) There are 15 species and 5 varieties in my country, which are mainly distributed in Southwest my country to South China. At present, there is no report on the dimeric monoterpene indole alkaloid Ervachinines A-D in the prior art, and there is no report on its activity. Contents of the invention [0003] The object of the present invention is to provide dimeric monoterpene indole alkaloid ervachinines A-D and pharmaceutically acceptable salts (organic acid or inorganic acid) of formula (1-4), such compounds are active ingredients of antitumor drugs The pharmaceutical composition, its preparati...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D471/22A61K31/55A61P35/00
Inventor 郝小江张于何红平李艳郭伶俐邸迎彤
Owner KUNMING INST OF BOTANY - CHINESE ACAD OF SCI
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