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Cyclic-ahltin type triterpenoid saponin compound and preparation method and application thereof

A technology of triterpene saponins and cycloaltin type, which is applied in the field of medicine, can solve the problems of limited application, achieve strong anti-tumor activity, simple and reliable preparation method, and high purity

Inactive Publication Date: 2010-09-08
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In short, there are more researches on the activity of total plant extracts rich in cycloaltin triterpenoids, but less research on monomeric compounds, which limits the application of such ingredients in the development of new drugs

Method used

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  • Cyclic-ahltin type triterpenoid saponin compound and preparation method and application thereof
  • Cyclic-ahltin type triterpenoid saponin compound and preparation method and application thereof
  • Cyclic-ahltin type triterpenoid saponin compound and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] Example 1 Preparation of Cycloaltin-type triterpenoids from Pteridocarpus persicae

[0029] (1) by LC-MS technology, select the plant fern of the genus Pteridophyllaceae as the plant raw material;

[0030] (2) Utilize solvent extraction method after the plant raw material is pulverized, adopt 70% ethanol reflux to extract three times, reclaim extract under reduced pressure until alcohol concentration is lower than 2%, extract with chloroform, ethyl acetate, n-butanol extraction respectively, recover Dissolve and collect to obtain chloroform, ethyl acetate, n-butanol extract;

[0031] (3) The n-butanol extract was processed by non-polar macroporous resin (HPD-100) column chromatography, followed by water and 30%, 60%, 90% ethanol gradient elution, and each elution site was screened by LC-MS technology Determining the effective part of the 60% ethanol gradient elution part to enrich the cycloaltin-type triterpene saponins to obtain crude total saponins;

[0032] (4) The...

Embodiment 2

[0039] Embodiment 2 prepares cycloaltin-type triterpenoids from bitter horse bean

[0040] (1) Selecting the leguminous horse bean as a plant raw material by LC-MS technology;

[0041](2) After the plant raw material is pulverized, the solvent extraction method is used, and 90% ethanol is used for reflux extraction twice, and the extract is recovered under reduced pressure until the alcohol concentration is lower than 5%. After centrifugation, it is left to stand for 24 hours, and the supernatant is taken;

[0042] (3) The supernatant was processed by non-polar macroporous resin (D101) column chromatography, followed by water and 40%, 70%, 90% ethanol gradient elution, and each elution site was screened by LC-MS technology to determine 70% ethanol The gradient elution site enriches the active site of ring Altin-type triterpene saponins to obtain crude total saponins;

[0043] (4) The crude total saponins obtained in operation (3) were subjected to rapid treatment by silica ge...

Embodiment 3

[0046] The determination of the in vitro antitumor activity of embodiment 3 ring Altin type triterpenoids

[0047] The in vitro antitumor activity of the isolated part of cycloaltin-type triterpenoids (1-10) was determined by high-throughput screening in vitro by MTT method. The experimental results are shown in Table 1.

[0048] experimental method:

[0049] 1. Cell Culture

[0050] The culture conditions of HL-60 cell line, Du145 cell line and Colon205 cell line are all RMPI 1640 culture medium, 10% fetal bovine serum, and the culture conditions of MCF-7 cell line are low-sugar DMEM medium 10% fetal bovine serum, HepG2 cells The culture condition of the strain is high-glucose DMEM culture medium with 10% fetal bovine serum, and the culture condition of A549 cell line is RMPI 1640 culture medium with 10% calf serum. All the above cell lines were cultured in 5% CO 2 , in a 37 °C incubator.

[0051] 2. Drug preparation

[0052] The determined cycloaltin-type triterpenoids...

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Abstract

The invention belongs to the technical field of medicines and provides a cyclic-ahltin type triterpenoid saponin compound and a preparation method and application thereof. The cyclic-ahltin type triterpenoid saponin compound is prepared by the steps of: obtaining an extracting solution or extract liquor by using a flash extraction technology or a solvent extraction method; processing the extracting solution or the extract liquor by using a non-polar resin column to obtain crude saponin; quickly processing the crude saponin by using a silica gel flash column chromatography, and then carrying out solvent gradient elution, and further separating and purifying by using a medium-low pressure column chromatography or open ODS (Oxide Dispersion Strengthened) column chromatography and an HPLC (High Performance Liquid Chromatography) technology. An LC-MS technology is used for detecting the components of the cyclic-ahltin type triterpenoid saponin compound in the preparation process. The prepared cyclic-ahltin type triterpenoid saponin compound has better anti-tumor activity.

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to saponins and their preparation, in particular to cycloaltin-type triterpene saponins, their preparation methods and their application. Background technique [0002] Cycloartane (9,19-cycloartane) compounds are lanosterane-type tetracyclic triterpenes. In recent decades, a large number of cycloaltin glycosides have been discovered. The cycloaltin compounds that have been isolated mainly come from the plant kingdom, such as Astragalus in the leguminous family, Cimicifugae and Thalictrum in the Ranunculaceae family. [0003] Cycloaltin compounds are the main components of Cimicifuga and Astragalus. Studies in recent years have shown that it has various pharmacological activities. It has been reported in the literature that Astragalus oleifolius has antiperspirant and diuretic effects, and has curative effects on nephritis, diabetes, leukemia, and uterine cancer. Its main component...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07J63/00C07J53/00A61P35/00A61K31/58
Inventor 李宁李铣孟大利肖皖
Owner SHENYANG PHARMA UNIVERSITY
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