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Carbazoles alkaloid, preparation and application thereof

A compound and crude product technology, used in carbazole alkaloids, the application of inhibiting cancer cell growth and anti-virus, the field of preparation of alkaloids

Inactive Publication Date: 2009-01-14
SOUTH CHINA SEA INST OF OCEANOLOGY - CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But at present, there is no research report on black coral coral (Antipathes subpinnata) at home and abroad, only two foreign research reports on the isolation of nine new polyhydric sterols from another species of black coral (Antipathes subpinnata) in this genus ( [1] Aiello A, Fattorusso E, Menna M. Steroids, 1991, 56(10): 513-517. [2] Aiello A, Fattorusso E, Menna M.J Nat Prod, 1992, 55(3): 321-325.)

Method used

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  • Carbazoles alkaloid, preparation and application thereof
  • Carbazoles alkaloid, preparation and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] Using antipathes dichotcma (Pallas) with a wet weight of 3Kg as raw material, freeze-dried and chopped, extracted 3 times with 15 L of ethanol-dichloromethane mixed organic solvent with a volume ratio of 2:1, and decompressed the extract Concentrated crude extract. The crude extract was suspended and dissolved in water, extracted three times with ethyl acetate (500 mL each time), and the ethyl acetate layer was taken and concentrated under reduced pressure to obtain 27 g. Use chloroform-methanol mixed solvent to dissolve the ethyl acetate layer and mix with silica gel, mix about 600mL petroleum ether with approximately 500g silica gel for wet packing, and change the volume ratio of petroleum ether-ethyl acetate solvent system from 10:0 to 0:10 Carry out gradient elution, thin-layer chromatography TLC (GF 254 ) to track and merge 8 components. These 8 components were tested in TLC (GF 254 ) was washed with chloroform-acetone solvent system from 10:1 to 9:1 by volume r...

Embodiment 2

[0023] The logarithmic growth phase SGC-7901 and Hep_G2 cell lines were collected and seeded in 96-well culture plates respectively, with the number of cells per well being 1.0×10 5 / 100μL in 5% CO 2 Cultivate in an incubator, remove the medium the next day, add 100 μL of drugs of different concentrations (the drug concentration is double-diluted), no drug is added to the negative control group, after 48 hours, add 10 μL of MTT to each well, continue to cultivate for 4 hours, and then add 100 μL of DMSO to each well Terminate the reaction, place it at room temperature for 1h, detect the absorbance A value of each well at 570nm with a microplate reader, and calculate the cell growth inhibition rate. The calculation formula is: growth inhibition rate (%)=[(A 阴性 -A 实验 ) / (A 阴性 -A 空白 )] × 100%. The half inhibitory rate IC50 of SGC-7901 and Hep_G2 cell growth were 67.38μg / mL and 73.65μg / mL respectively.

Embodiment 3

[0025] Collect vero cells in the logarithmic growth phase and inoculate them in 96-well culture plates, the number of cells per well is 1.0×10 5 / 100μL, placed in 5%, CO 2 Incubator cultivation. The next day, suck out the growth solution in the microwells, add 50 μL of the diluted solution of the compound of formula (1) in Example 1 to each well, immediately add 50 μL of HSV-1 virus use solution, and set normal cell control and virus control at the same time, 37 ° C , 5% CO 2 Incubator cultivation. Observe the cytopathic effect (CPE), observe the cell growth every day, and express the cytopathic condition by -, +, ++, +++, ++++. The results show that the compound of the present invention has a maximum nontoxic concentration of 25ug / ml to vero cells, and it inhibits the IC of herpes simplex virus type I lesions. 50 The value was 30.68ug / mL.

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Abstract

The invention relates to a new carbazole alkaloid represented by the formula (1), and also relates to a preparation method thereof and applications thereof. The alkaloid is characterized in that: crude extracts of an organic solvent of Antipathes dichotcma (Pallas) are extracted with ethyl acetate or chloroform after being suspended on water, an ethyl acetate layer or a chloroform layer is collected for carrying out the normal pressure silica gel column chromatography, the thin-layer chromatography is used for tracing and combination, and a chloroform-acetone solvent system in a volume ratio of 9:1 is used for elution, the collected Rf value is about 0.5 to 0.7, and compositions of ultraviolet absorption exist under the wavelength of 254nm of an ultraviolet lamp, a crude product is gained, and a pure product is obtained through the further purification. The carbazole alkaloid can be used for preparing medicines treating gastric cancers, liver cancers and anti-herpes simplex virus, and has the half inhibition concentration IC50 of 67.38mu g / mL and 73.65mu g / mL respectively to human gastric adenocarcinoma cell line SGC-7901 and human hepatoma cell Hep G2; and the IC50 value of the anti-herpes simplex HSV-I virus is 30.68mu g / mL.

Description

technical field [0001] The present invention relates to a new alkaloid, specifically to a new carbazole alkaloid represented by the following formula (1), in addition to the preparation method of this alkaloid and its role in inhibiting cancer cell growth and Antiviral applications. Background technique [0002] Antipathes dichotcma (Pallas) medicine name sea iron tree, iron tree, "Chinese Materia Medica" records that it has the effect of clearing away heat, reducing astringency, softening and softening, and mainly treating food mucosa damage, bloody dysentery, night sweats, scrofula, bone choking, etc. . But at present, there is no research report on black coral coral (Antipathes subpinnata) at home and abroad, only two foreign research reports on the isolation of nine new polyhydric sterols from another species of black coral (Antipathes subpinnata) in this genus ( [1] Aiello A, Fattorusso E, Menna M. Steroids, 1991, 56(10): 513-517. [2] Aiello A, Fattorusso E, Menna M.J...

Claims

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Application Information

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IPC IPC(8): C07D487/04A61K31/551A61K35/56A61P35/00A61P31/12A61K35/614
Inventor 漆淑华张偲
Owner SOUTH CHINA SEA INST OF OCEANOLOGY - CHINESE ACAD OF SCI
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