Evaluation of the in vitro Cytotoxicity of some Sesquiterpene Lactones on a Human Lung Carcinoma Cell Line Using the Fast Green Dye Exclusion Assay

H. J. Woerdenbag; C. Meijer; N. H. Mulder; E. G. E. de Vries; H. Hendriks; Th. M. Malingré

doi:10.1055/s-2007-969093

Planta Medica, Table of Contents

Planta Med 1986; 52(2): 112-114
DOI: 10.1055/s-2007-969093

Full Papers

Evaluation of the in vitro Cytotoxicity of some Sesquiterpene Lactones on a Human Lung Carcinoma Cell Line Using the Fast Green Dye Exclusion Assay

H. J. Woerdenbag¹ , C. Meijer² , N. H. Mulder² , E. G. E. de Vries² , H. Hendriks¹ , Th. M. Malingré¹

¹Laboratory of Pharmacognosy, State University of Groningen, Ant. Deusinglaan 2, 9713 AW Groningen, The Netherlands.
²Division of Medical Oncology, Department of Internal Medicine, University Hospital, P.O. Box 30001, 9700 RB Groningen, The Netherlands.

Abstract

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Abstract

Amongst the properties associated with the sesquiterpene lactones, their cytotoxicity is probably the most valuable. In this in vitro study cytotoxicity of some sesquiterpene lactones from Eupatorium cannabinum L. and related compounds have been tested on a human small cell lung carcinoma cell line, using the Fast Green dye exclusion assay (FGA). From the results certain conclusions could be drawn about structure activity relationship.

Eupatoriopicrin, eupatoriopicrin acetonide, “substance 1” and hiyodorilactone E showed highest cytotoxicity (ID50 1-2 µg/ml) following 1 h incubation. Moieties of the sesquiterpene lactones (α-methylene γ-butyrolactone, eupatolide, angelic and tiglic acid) and related compounds (alantolactone and isoalantolactone) were less or not active at these concentrations.

From the results of the experiments it can be concluded that the entire molecule (germacranolide ester) is necessary for optimal cytotoxicity in vitro and that cytotoxicity increases with decreasing hydrophilicity.

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