Cytotoxicity and p-glycoprotein modulating effects of quinolones and indoloquinazolines from the Chinese herb Evodia rutaecarpa

Autoren

Michael Adams
Anne Mahringer
Olaf Kunert
Gert Fricker
Thomas Efferth
Rudolf Bauer

DOI

10.1055/s-2007-993743

eISSN

1439-0221

ISSN

0032-0943

Ausgabe der Veröffentlichung

15

Zeitschrift

Planta Medica

Sprache

en

Paginierung

1554 - 1557

Datum der Veröffentlichung

2007

Status

Published

Herausgeber

Georg Thieme Verlag KG

Herausgeber URL

http://dx.doi.org/10.1055/s-2007-993743

Datum der Datenerfassung

2017

Titel

Cytotoxicity and P-Glycoprotein Modulating Effects of Quinolones and Indoloquinazolines from the Chinese Herb <i>Evodia rutaecarpa</i>

Ausgabe der Zeitschrift

73

Data source: Crossref

Abstract

The antimycobacterial quinolones 1-methyl-2-undecyl-4-quinolone, dihydroevocarpine and evocarpine as well as the indoloquinazoline alkaloids rutaecarpine and evodiamine - all from the Chinese medicinal herb Evodia rutaecarpa - were tested in two in vitro assays, for cytotoxicity and interaction with p-glycoprotein (p-gp). Cytotoxicity was measured in a cell proliferation assay against CCRF-CEM leukemia cells and their p-gp over-expressing subline CEM/ADR5000. An assay monitoring the p-gp-dependent accumulation of the dye calcein in porcine brain capillary endothelial cells (PBCECs) was used to study interactions of the test substances with this efflux pump. Rutaecarpine and evodiamine showed quite high toxicity with IC (50) values from 2.64 to 4.53 microM and were weak modulators of p-gp activity. The degrees of resistance in CEM/ADR5000 towards the saturated quinolones 1-methyl-2-undecyl-4-quinolone and dihydroevocarpine were between 3 and 4. In the calcein assay, these two quinolones were shown to be moderate modulators of p-gp activity. Evocarpine, on the other side, is not transported by p-gp, and showed only slight toxicity at the highest test concentration of 30 microM.

Addresses

Institute of Pharmaceutical Sciences, University of Graz, Graz, Austria.

Autoren

Michael Adams
Anne Mahringer
Olaf Kunert
Gert Fricker
Thomas Efferth
Thomas Efferth
Rudolf Bauer

DOI

10.1055/s-2007-993743

eISSN

1439-0221

Externe Identifier

PubMed Identifier: 18058680

Open access

false

ISSN

0032-0943

Ausgabe der Veröffentlichung

15

Zeitschrift

Planta medica

Schlüsselwörter

Blood-Brain Barrier
Endothelium, Vascular
Cell Line, Tumor
Animals
Swine
Humans
Evodia
Indolequinones
Quinolones
Plant Extracts
Antineoplastic Agents, Phytogenic
Medicine, Chinese Traditional
Phytotherapy
Drug Resistance, Multiple
Cell Proliferation
ATP Binding Cassette Transporter, Subfamily B, Member 1

Sprache

eng

Medium

Print-Electronic

Online publication date

2007

Paginierung

1554 - 1557

Datum der Veröffentlichung

2007

Status

Published

Datum der Datenerfassung

2007

Titel

Cytotoxicity and p-glycoprotein modulating effects of quinolones and indoloquinazolines from the Chinese herb Evodia rutaecarpa.

Sub types

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

Ausgabe der Zeitschrift

73

Data source: Europe PubMed Central

Abstract

The antimycobacterial quinolones 1-methyl-2-undecyl-4-quinolone, dihydroevocarpine and evocarpine as well as the indoloquinazoline alkaloids rutaecarpine and evodiamine - all from the Chinese medicinal herb Evodia rutaecarpa - were tested in two in vitro assays, for cytotoxicity and interaction with p-glycoprotein (p-gp). Cytotoxicity was measured in a cell proliferation assay against CCRF-CEM leukemia cells and their p-gp over-expressing subline CEM/ADR5000. An assay monitoring the p-gp-dependent accumulation of the dye calcein in porcine brain capillary endothelial cells (PBCECs) was used to study interactions of the test substances with this efflux pump. Rutaecarpine and evodiamine showed quite high toxicity with IC (50) values from 2.64 to 4.53 microM and were weak modulators of p-gp activity. The degrees of resistance in CEM/ADR5000 towards the saturated quinolones 1-methyl-2-undecyl-4-quinolone and dihydroevocarpine were between 3 and 4. In the calcein assay, these two quinolones were shown to be moderate modulators of p-gp activity. Evocarpine, on the other side, is not transported by p-gp, and showed only slight toxicity at the highest test concentration of 30 microM.

Autoren

Michael Adams
Anne Mahringer
Olaf Kunert
Gert Fricker
Thomas Efferth
Rudolf Bauer

Autoren-URL

https://www.ncbi.nlm.nih.gov/pubmed/18058680

DOI

10.1055/s-2007-993743

ISSN

0032-0943

Ausgabe der Veröffentlichung

15

Zeitschrift

Planta Med

Schlüsselwörter

ATP Binding Cassette Transporter, Subfamily B, Member 1
Animals
Antineoplastic Agents, Phytogenic
Blood-Brain Barrier
Cell Line, Tumor
Cell Proliferation
Drug Resistance, Multiple
Endothelium, Vascular
Evodia
Humans
Indolequinones
Medicine, Chinese Traditional
Phytotherapy
Plant Extracts
Quinolones
Swine

Sprache

eng

Country

Germany

Paginierung

1554 - 1557

Datum der Veröffentlichung

2007

Status

Published

Datum, an dem der Datensatz öffentlich gemacht wurde

2008

Titel

Cytotoxicity and p-glycoprotein modulating effects of quinolones and indoloquinazolines from the Chinese herb Evodia rutaecarpa.

Sub types

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

Ausgabe der Zeitschrift

73

Data source: PubMed

Cytotoxicity and p-glycoprotein modulating effects of quinolones and indoloquinazolines from the Chinese herb Evodia rutaecarpa

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