Plant extracts with antitumor activity and active ingredients thereof

A technology for extracting and compounding, which is applied in the field of medical technology and achieves the effects of novel structure, simple extraction and separation method, and significant anti-tumor activity.

Inactive Publication Date: 2016-01-27
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The present invention relates to the 5 new Buxus alkaloids isolated from the total alkaloids in the leaves of Buxus japonica, and so far there are no related patents or literature reports on similar compounds and anti-tumor activities at home and abroad.

Method used

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  • Plant extracts with antitumor activity and active ingredients thereof
  • Plant extracts with antitumor activity and active ingredients thereof
  • Plant extracts with antitumor activity and active ingredients thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0019] Embodiment 1: Preparation of total alkaloids in the leaves of Populus korean:

[0020] Korean poplar leaves (1600g) were cut into pieces, soaked in 0.2% HCl aqueous solution (5L) for 12h, then percolated and extracted with 0.2% HCl aqueous solution to obtain a total of 29L acidic water extract, which was alkalized to pH with 5% NaOH aqueous solution =11, get about 30L of alkaline water, use HPD-100 type macroporous adsorption resin 1.5kg to dynamically absorb the alkaline water, and elute with 95% ethanol after eluting with NaOH aqueous solution with pH=11 for 4 retention volumes 5 retention volumes, 95% ethanol elution partially recovered the solvent to obtain the total alkaloids (18g).

Embodiment 2

[0021] Example 2: In Vitro Antitumor Activity of Total Alkaloids in the Leaves of Populus Koreana (Example 1)

[0022] Take the test cells in the logarithmic growth phase, and use (2-3)×10 4 The density of cells / mL was inoculated in a 96-well culture plate, 100 μL in each well, and after 24 hours of making it adhere to the wall, 100 μL of the compound to be tested diluted to different concentrations with the culture medium was added, and the culture was continued at 37°C for 96 hours. Then add 50 μL MTT solution to each well and incubate at 37°C for 4 h, discard the supernatant, add 200 μL DDMSO to each well, shake at room temperature for 10 min, measure the absorbance value of each well at 570 nm on a microplate reader, set A1 (containing 200 μD DMSO) as For blank control wells, cisplatin (CP) was used as positive control. The tumor cell growth inhibition rate was obtained by using the following formula: 1-(absorbance value of drug-dosed well / absorbance value of control well...

Embodiment 3

[0026] Example 3: The preparation method of five monomer compounds such as formulas I to V in the total alkaloids of leaves of Populus korean (Example 1)

[0027]Using 18g of total alkaloid extract from the leaves of Populus korean as raw material, it was separated by 200-300 mesh silica gel column chromatography, and mixed solvent gradients of petroleum ether-acetone with a volume ratio of 3:1, 1:1 and 0:1 respectively For elution, the eluted part with a volume ratio of petroleum ether-acetone of 3:1 is separated by 200-300 mesh alumina column chromatography, and eluted with a mixed solvent of petroleum ether-acetone with a volume ratio of 100:2 The compound of formula IV (6.0 mg) was obtained, and the compound of formula III (5.2 mg) was obtained by elution with a mixed solvent of petroleum ether-acetone with a volume ratio of 100:10, wherein the volume ratio of petroleum ether-acetone was 1: The eluted part of 1 was then separated by open ODS column chromatography, and elut...

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Abstract

The invention belongs to the field of medical technology and relates to total alkaloids which are extracted and separated from leaves of Buxusmicrophyllavar.koreanaNakai and have in-vitro antitumor activity, and a preparation method of the total alkaloids, as well as five buxus alkaloid compounds separated from the leaves of Buxusmicrophyllavar.koreanaNakai, and a preparation method of the five buxus alkaloid compounds. raw materials of the extract are easily and massively obtained, the obtained monomeric compounds are novel in structure and has in-vitro antitumor activity, the method for extracting and separating the total alkaloids and active monomeric compounds in the total alkaloids is simple, pharmacological and clinical research on the total alkaloids and active monomeric compounds are facilitated and conditions for developing novel antitumor drug with good curative effect and fewer toxic and side effects are created.

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to extracting and separating total alkaloids with in vitro anti-tumor activity from the leaves of Buxus microphyllavar. Antitumor active boxwood alkaloid compound and its preparation method. Background technique [0002] Buxus alkaloids are a series of alkaloid compounds with the basic skeleton of Altin-type triterpenoids distributed only in Buxus plants of the family Buxaceae. More than 220 such compounds have been reported [Yu-xinYan, Current Bioactive Compound, 2011, 47-64], and most of them have the activities of treating myocardial ischemia, anti-senile dementia and antibacterial. Among them, cyclovirobuxin D (cyclovirobuxin D) was included in the "Chinese Pharmacopoeia" in 2010, and it is used for the treatment of coronary heart disease and arrhythmia. The clinical preparations include Huangyangning Tablets. [0003] There are more than 70 species of Buxus in the world. Dist...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07J53/00C07J75/00A61K36/185A61K31/57A61K31/56A61P35/00A61P35/02
Inventor 李占林华会明王丽伟李丹毅
Owner SHENYANG PHARMA UNIVERSITY
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