Isopentenyl flavonoid compound in Daphne giraldii Nitsche. and application thereof

High-purity isopentenyl flavonoids are isolated from Daphne chinensis through multi-step chromatography and semi-preparative HPLC technology, which solves the problem in the existing technology that the active ingredients of Daphne chinensis cannot be effectively used in the preparation of anti-tumor drugs, and achieves Effective inhibitory effect on human liver cancer cells and FGFR1.

CN111423403AActive Publication Date: 2020-07-17SHENYANG PHARMA UNIV
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Patent Information

Application Number
CN202010353026.X
Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
Filing Date
2020-04-29
Publication Date
2020-07-17
Estimated Expiration
2040-04-29

AI Technical Summary

Technical Problem

In the existing technology, the active ingredients of Daphne fragrans cannot be effectively used in the preparation of anti-tumor drugs, and the existing separation methods are inefficient and difficult to obtain high-purity prenyl flavonoids.

Method used

By using an ethanol cold-leaching extraction method from dried rhizome bark of Daphne chinensis, combined with multi-step chromatography methods such as silica gel column, polyamide column, MCI column and ODS column, and semi-preparative HPLC technology, six types of isopentenes were successfully separated and identified. based flavonoids and obtain optically pure compounds through chiral resolution.

Benefits of technology

Achieved the efficient isolation of six prenyl flavonoids from Daphne fragrans, especially compounds 2 and 5a, 5b, which have significant cytotoxic activity against human hepatoma cells and show activity against fibroblast growth factor receptor 1 (FGFR1) inhibition improves the efficiency of obtaining active ingredients of anti-tumor drugs.

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Abstract

The invention belongs to the technical field of medicines, and relates to an isopentenyl flavonoid compound and an application thereof, in particular to eight isopentenyl flavonoid compounds extractedand separated from rhizome and bark of daphne daphne plant Daphne giraldii Nitsche. The method comprises the following steps: extracting dried root bark of Daphne giraldii Nitsche. with ethanol, andseparating the crude extract by silica gel column chromatography, polyamide column chromatography, MCI column chromatography, ODS column chromatography, gel column chromatography and HPLC separation in sequence. The structure of the compound is identified through a nuclear magnetic technology, chiral resolution is carried out on the compound 4 and the compound 5 through chiral HPLC, and finally two pairs of enantiomers (4a, 4b and 5a, 5b) are obtained. The compound disclosed by the invention has a cytotoxic effect and an apoptosis promoting effect on a Hep3B cell line. The compounds of the present invention have inhibitory activity against Fibroblast Growth Factor Receptor 1 (FGFR1).
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