Planta Med 2011; 77(18): 1984-1989
DOI: 10.1055/s-0031-1280023
Biological and Pharmacological Activity
Original Papers
© Georg Thieme Verlag KG Stuttgart · New York

Cytotoxicity and Mode of Action of Four Naturally Occuring Flavonoids from the Genus Dorstenia: Gancaonin Q, 4-Hydroxylonchocarpin, 6-Prenylapigenin, and 6,8-Diprenyleriodictyol

Victor Kuete1 , 3 , Bathelemy Ngameni2 , Benjamin Wiench3 , Benjamin Krusche3 , Cindy Horwedel3 , Bonaventure T. Ngadjui2 , 4 , Thomas Efferth3
  • 1Department of Biochemistry, Faculty of Science, University of Dschang, Cameroon
  • 2Department of Pharmacy and Traditional Pharmacopoeia, Faculty of Medicine and Biomedical Science, University of Yaoundé I, Yaoundé, Cameroon
  • 3Department of Pharmaceutical Biology, Institute of Pharmacy and Biochemistry, University of Mainz, Mainz, Germany
  • 4Department of Organic Chemistry, Faculty of Science, University of Yaoundé I, Cameroon
Further Information

Publication History

received March 22, 2011 revised May 26, 2011

accepted June 1, 2011

Publication Date:
28 July 2011 (online)

Abstract

Several flavonoid-like compounds were found to possess good antiproliferative properties. Herein, we examined the ability of four naturally occuring and biologically active flavonoids from the genus Dorstenia, gancaonin Q (1), 6-prenylapigenin (2), 6,8-diprenyleriodictyol (3), and 4-hydroxylonchocarpin (4), to inhibit the proliferation of a panel of fourteen cancer cell lines including leukemia and solid cancer cells, as well as AML12 normal hepatocytes. The study was extended to the analysis of cell cycle distribution, apoptosis induction, and caspase 3/7 activity and the antiangiogenic properties of the four compounds. The results of the cytotoxicity assays showed that more than 50 % inhibition of proliferation was obtained with compound 1 on all the fourteen studied cancer cell lines, with IC50 values below 20 µg/mL. Compounds 2, 4, and 3 showed selective activity, with IC50 values below 20 µg/mL being noted on 57.15 %, 71.42 %, and 85.71 % of the fourteen cancer cell lines, respectively. None of the compounds exhibited more than 50 % inhibition against AML12 normal hepatocytes cells at 20 µg/mL. IC50 values below or around 4 µg/mL were recorded on 28.57 % of the tested cell lines for both compound 1 and 4 and 21.43 % for compound 3, which appeared to be the best cytotoxic compounds. This study indicates that caspase 3/7 activation is one of the modes of induction of apoptosis for compounds 1, 3, and 4 in CCRF-CEM cells. The results of the antiangiogenic assay indicated that compounds 1, 3, and 4 were also able to inhibit the growth of blood capillaries on the chorioallantoic membrane of quail eggs, the best effect being noted for compound 4 (54.1 % inhibition).

The results of the present work provide evidence of the cytotoxic potential of the four studied flavonoids and supportive data for further investigations.

Supporting Information

References

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Prof. Dr. Thomas Efferth

Department of Pharmaceutical Biology
Institute of Pharmacy and Biochemistry
University of Mainz

Staudinger Weg 5

55128 Mainz

Germany

Phone: +49 6 13 13 92 57 51

Fax: +49 6 13 13 92 37 52

Email: efferth@uni-mainz.de