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

Autoren

Victor Kuete
Bathelemy Ngameni
Benjamin Wiench
Benjamin Krusche
Cindy Horwedel
Bonaventure Ngadjui
Thomas Efferth

DOI

10.1055/s-0031-1280023

eISSN

1439-0221

ISSN

0032-0943

Ausgabe der Veröffentlichung

18

Zeitschrift

Planta Medica

Sprache

en

Online publication date

2011

Paginierung

1984 - 1989

Datum der Veröffentlichung

2011

Status

Published

Herausgeber

Georg Thieme Verlag KG

Herausgeber URL

http://dx.doi.org/10.1055/s-0031-1280023

Datum der Datenerfassung

2017

Titel

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

Ausgabe der Zeitschrift

77

Data source: Crossref

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 IC (50) values below 20 µg/mL. Compounds 2, 4, and 3 showed selective activity, with IC (50) 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. IC (50) 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.

Addresses

Department of Biochemistry, Faculty of Science, University of Dschang, Cameroon.

Autoren

Victor Kuete
Bathelemy Ngameni
Benjamin Wiench
Benjamin Krusche
Cindy Horwedel
Bonaventure T Ngadjui
Thomas Efferth
Thomas Efferth

DOI

10.1055/s-0031-1280023

eISSN

1439-0221

Externe Identifier

PubMed Identifier: 21800276

Open access

false

ISSN

0032-0943

Ausgabe der Veröffentlichung

18

Zeitschrift

Planta medica

Schlüsselwörter

Zygote
Chorioallantoic Membrane
Hela Cells
Hepatocytes
Chick Embryo
Animals
Quail
Humans
Moraceae
Neovascularization, Pathologic
Oxazines
Flavonoids
Flavones
Xanthenes
Doxorubicin
Angiogenesis Inhibitors
Plant Extracts
Antineoplastic Agents, Phytogenic
Inhibitory Concentration 50
Cell Cycle
Cell Survival
Enzyme Activation
Structure-Activity Relationship
Time Factors
Caspase 3
Caspase 7

Sprache

eng

Medium

Print-Electronic

Online publication date

2011

Paginierung

1984 - 1989

Datum der Veröffentlichung

2011

Status

Published

Datum der Datenerfassung

2011

Titel

Cytotoxicity and mode of action of four naturally occuring flavonoids from the genus Dorstenia: gancaonin Q, 4-hydroxylonchocarpin, 6-prenylapigenin, and 6,8-diprenyleriodictyol.

Sub types

Research Support, Non-U.S. Gov't
Journal Article

Ausgabe der Zeitschrift

77

Data source: Europe PubMed Central

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 IC (50) values below 20 µg/mL. Compounds 2, 4, and 3 showed selective activity, with IC (50) 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. IC (50) 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.

Autoren

Victor Kuete
Bathelemy Ngameni
Benjamin Wiench
Benjamin Krusche
Cindy Horwedel
Bonaventure T Ngadjui
Thomas Efferth

Autoren-URL

https://www.ncbi.nlm.nih.gov/pubmed/21800276

DOI

10.1055/s-0031-1280023

eISSN

1439-0221

Ausgabe der Veröffentlichung

18

Zeitschrift

Planta Med

Schlüsselwörter

Angiogenesis Inhibitors
Animals
Antineoplastic Agents, Phytogenic
Caspase 3
Caspase 7
Cell Cycle
Cell Survival
Chick Embryo
Chorioallantoic Membrane
Doxorubicin
Enzyme Activation
Flavones
Flavonoids
HeLa Cells
Hepatocytes
Humans
Inhibitory Concentration 50
Moraceae
Neovascularization, Pathologic
Oxazines
Plant Extracts
Quail
Structure-Activity Relationship
Time Factors
Xanthenes
Zygote

Sprache

eng

Country

Germany

Paginierung

1984 - 1989

Datum der Veröffentlichung

2011

Status

Published

Datum, an dem der Datensatz öffentlich gemacht wurde

2012

Titel

Cytotoxicity and mode of action of four naturally occuring flavonoids from the genus Dorstenia: gancaonin Q, 4-hydroxylonchocarpin, 6-prenylapigenin, and 6,8-diprenyleriodictyol.

Sub types

Journal Article
Research Support, Non-U.S. Gov't

Ausgabe der Zeitschrift

77

Data source: PubMed

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

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