Document Type

Journal Article

Department/Unit

School of Chinese Medicine

Title

Isolation of anticancer constituents from flos genkwa (Daphne genkwa Sieb.et Zucc.) through bioassay-guided procedures

Language

English

Abstract

Background: Flos Genkwa (yuanhua in Chinese), the dried flower buds of Daphne genkwa Sieb.et Zucc. (Thymelaeaceae), is a traditional Chinese medicinal herb mainly used for diuretic, antitussive, expectorant, and anticancer effects. However, systematic and comprehensive studies on Flos Genkwa and its bioactivity are limited.Results: After confirmation of the anti-tumor activity, the 95% ethanolic extract was subjected to successive solvent partitioning to petroleum ether, dichloromethane, n-butanol, and water soluble fractions. Each fraction was tested using the same biological activity model, and the dichloromethane fraction had the highest activity. The dichloromethane fraction was subjected to further chromatographic separation for the isolation of compounds 1-13. Among the 13 compounds, the diterpene esters (compounds 10-13) showed anticancer activity, whereas the flavonoids, lignanoids, and peptides showed moderate activity. Compound 13 was a new daphnane diterpenoid, which was named genkwanin VIII.The preliminary antitumor mechanism of yuanhuacine was studied by protein expression and cell cycle analysis in MCF-7 cancer cells.Conclusion: The present investigation tends to support the traditional use of Flos Genkwa for treating cancer. Through bioassay-guided fractionation and isolation techniques, the CH2Cl2 fraction was determined as the active fraction of the flower buds of D. genkwa, and the anti-tumor activity was ascribable to the compounds 10-13. © 2013 Li et al.; licensee Chemistry Central Ltd.

Keywords

Antitumor, Daphne genkwa, Flow cytometric, MTT, Western blot

Publication Date

2013

Source Publication Title

Chemistry Central Journal

Volume

7

Issue

159

Start Page

1

End Page

9

Publisher

Chemistry Central

DOI

10.1186/1752-153X-7-159

Link to Publisher's Edition

http://dx.doi.org/10.1186/1752-153X-7-159

ISSN (print)

1752153X

ISSN (electronic)

1752153X

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