Steroid saponin compound and use in preparation antineoplastic

A technology of steroidal saponins and compounds, which is applied in the field of steroidal saponins and their new applications in the preparation of antitumor drugs, and can solve the problems of compound biological activity reports and other issues

Inactive Publication Date: 2009-07-08
FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In recent years, the research on Xiaobaibu has only focused on the separation and structural identification of chemical components, and some steroidal saponins have been isolated from it, but so far there have been no reports on the biological activities of these compounds

Method used

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  • Steroid saponin compound and use in preparation antineoplastic
  • Steroid saponin compound and use in preparation antineoplastic
  • Steroid saponin compound and use in preparation antineoplastic

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] Example 1 Preparation of total saponins

[0024] Take 6 kg of rhizome powder of Lily chinensis, soak in ethanol at room temperature (20L×3 times), combine the extracts and concentrate until there is no alcohol smell, add water to dilute the extracts to 2L, extract with n-butanol (2L×3 times), combine and normal The butanol extract was concentrated to dryness to obtain 170 g of total saponins. Take 150g of total saponins and apply dry method to carry out silica gel column chromatography, and use chloroform, chloroform-methanol, methanol gradient elution, the specific steps are as follows:

[0025] 1. The obtained fractions were eluted with chloroform-methanol (7:3), repeated silica gel column chromatography with chloroform-methanol-water (4:1:0.2), and then passed through RP-18 column (60-90% methanol) to obtain white Amorphous powder 20mg, that is, paretia saponin A (1). Using spectroscopy and chemical analysis, its structure was determined to be smilagenin-3-O-[β-D-x...

Embodiment 2

[0028] Embodiment 2 in vitro antitumor test (SRB method)

[0029] Two kinds of tumor cell strains of A549 and MCF-7 are contained in the T-25 flask of the 10% calf serum RPMI1640 culture fluid 4ml of 25mM HEPES, 0.2% (w / v) sodium bicarbonate and 100 μ g / ml kanamycin, 37°C, 5% CO 2 cultivated under conditions. The cell suspension digested by trypsin was added to a 96-well plate, and the cell concentration was 0.25-1×10 4 / hole. Tumor cells were added different concentrations of components to be tested and cultured at 37°C for 72 hours, fixed with ice-cold 50% trichloroacetic acid and stained with 0.4% (SRB). After the dye was dissolved, the absorbance was measured at 562 nm. The drug concentration EC at the time of half cell growth inhibition 50 Conversion was performed according to dose-effect data. Each experiment was repeated three times, and the difference in absorbance value was less than 5%, EC 50 The difference is less than 30%.

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Abstract

The invention belongs to the field of traditional Chinese medicine pharmacy, and relates to a steroidal saponin compound of formula 1 and its new application in the preparation of antitumor drugs. The invention extracts active substance steroidal saponins from the total saponin part of Asparagus filicinus Buch.-Ham in Liliaceae, and proves that it has significant antitumor activity through in vitro antitumor activity screening test. The EC50 values ​​of the compound against two tumor cell lines of human lung cancer (A549) and breast cancer (MCF-7) are 2.3 and 3.6 μg / ml, respectively.

Description

technical field [0001] The invention belongs to the field of traditional Chinese medicine pharmacy, and relates to a steroidal saponin in Radix chinensis and its new application in the preparation of antitumor drugs. Background technique [0002] The study of anticancer drugs has been the focus and focus of the world's pharmaceutical research for many years. The clinical application of anti-tumor chemical drugs is greatly limited due to their high toxicity and side effects. Therefore, people have paid more and more attention to finding new anti-tumor active drugs from natural sources in recent years. Scholars at home and abroad have isolated a large number of monomeric compounds with biological activity from natural products including marine organisms, which provides broad prospects for the research and development of antitumor drugs. Liliaceae (Liliaceae) Asparagus L. has a long history as a medicinal plant. "Shen Nong's Materia Medica" listed Asparagus L. as a top-grade h...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07J71/00A61K31/58A61P35/00A61K36/8965
Inventor 陈道峰周丽波李国雄
Owner FUDAN UNIV
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