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Novel triterpene compound of C3,4 split ring and preparation method thereof

A technology for triterpenoid compounds and compounds, which is applied in the field of medicine and achieves the effects of simple extraction and separation method, convenient pharmacological and clinical research, and small toxic and side effects

Inactive Publication Date: 2013-05-15
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The C3, 4-position ring-cleaved and C3-position carboxyl methyl esterified new triterpene compounds involved in the present invention have not been seen so far at home and abroad with similar compounds and activities related patents or literature reports

Method used

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  • Novel triterpene compound of C3,4 split ring and preparation method thereof
  • Novel triterpene compound of C3,4 split ring and preparation method thereof
  • Novel triterpene compound of C3,4 split ring and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0031] Embodiment 1: the preparation of formula I compound:

[0032] Using 10 kg of dried medicinal material from the root of Schisandra chinensis as raw material, it was heated and refluxed with 90% ethanol for 3 times, each time for 2 hours, and concentrated to obtain 1500 g of extract-like ethanol extract. The ethanol extract was suspended in water, and extracted 4 times with petroleum ether, 1000 mL each time. Part of the extract extracted from petroleum ether was separated by 200-300 mesh silica gel column chromatography, and gradient eluted with petroleum ether-ethyl acetate (100:1-1:1), wherein the volume ratio of petroleum ether-ethyl acetate was 100: The eluted fraction of 7 was separated by 200-300 mesh silica gel column chromatography, and eluted with petroleum ether-acetone with a volume ratio of 16:1 to obtain the compound of formula I (7 mg).

Embodiment 2

[0033] Embodiment 2: The growth inhibition test of the compound of formula I to human acute promyelocytic leukemia cell line HL-60 in vitro:

[0034] HL-60 cells were cultured in a medium containing 10% heat-inactivated fetal bovine serum, 100 IU / mL penicillin, 100 mg / mL streptomycin and 1 mmol / L L -Glutamine in RPMI1640 medium, 37 °C, 5% CO 2 Incubate in a saturated humidity incubator. Weigh trypan blue, add a small amount of distilled water to grind, add double distilled water to dilute to 4% storage concentration, filter with filter paper, and store at 4 °C. When used, this stock solution was diluted to a working concentration of 0.4% with PBS. Take the above cells (1'10 5 / mL) were inoculated in a 12-well plate, 2 mL per well. Add different concentrations of drugs to prepare a single cell suspension after incubation, take 50 mu L cell suspension added 50 mu 0.4% trypan blue solution in L, mix well, and observe under the microscope within 3 minutes, the dead cells are...

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Abstract

The invention relates to a novel triterpene compound extracted and separated from rosy south fructus schisandrae root and application of the compound to preparing of inhibitors of human promyelotic leukemia cell lines HL-60. The compound has a structure as shown in the formula I described in the specification. Experimental researches show that the compound has the growth inhibition action on the human promyelotic leukemia cell lines HL-60. Furthermore, a method for extracting and separating the compound is simple and easy; and the method is advantageous for carrying out further pharmacology and clinical research and developing the application of the compound to preparing of anti-tumour drugs.

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to a new triterpene compound with C3 and 4 split rings obtained by extracting and separating from the root of a medicinal plant of the genus Schisandra Schisandra in the family Schisandraceae and a preparation method thereof. Background technique [0002] Triterpenoids are one of the main chemical constituents of Schisandraceae. The reported triterpenoids isolated from the root of Schisandra chinensis are mostly lanolin-type and cycloaltin-type. According to the literature, many of these compounds have antitumor activity, for example, from Kadsura longipedunculata The pentalactone E, nanic acid and pentalactone F obtained from the medium showed growth inhibitory effect on leukemia P-388 cells; from Kadsuraheteroclita The 13 triterpenoids obtained in the study have cytotoxic effects on HL-60, Bel-7402, BGC-823 and MCF-7; Kadsura heteroclita The cytotoxicity of 13 triterpenes obta...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07C69/738C07C67/56A61K31/215A61P35/02
Inventor 华会明李占林王楠裴月湖白皎景永奎
Owner SHENYANG PHARMA UNIVERSITY
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