Cytotoxic Activity Evaluation on Breast Cells of Guest-host Complexes Containing Artemisinin

Abstract

Artemisinin is a sesquiterpene lactone with vastly proved anti-cancer effects and a low toxicity profile. However, the compound has poor water solubility, bioavailability and a short half-life. As such, the present paper aims to evaluate the cytotoxic effect on breast cells of three guest-host inclusion complexes containing artemisinin as the active compound and different cyclodextrins as hosts. These were tested using two different concentrations (i.e. 12.5 mM and 25 mM) and three cell lines, namely two human breast adenocarcinoma cell lines (MCF7 and MDA-MB-231) and one human non-tumorigenic breast epithelial cell line (MCF10A) employing the colorimetric microculture tetrazolium assay. After a 72h stimulation period, the most promising results were obtained for the complex containing artemisinin and Heptakis(2,3,6-tri-O-methyl)-b-cyclodextrin, the cell viability decrease being significant for the estrogen positive MCF7 cell line (80.0 � 2.3 %), making the complex a potential candidate for further in vivo testing.

Applications of Sesquiterpene Lactones: A Review of Some Potential Success Cases

“…Natural sesquiterpene lactones exhibit poor pharmacokinetic properties due mainly to their low bioavailability, deriving from low solubility in water. As a result, in order to overcome these limitations, research interest in the synthesis of their derivatives has increased [21,22]. In addition, structural modification and synthesis has also allowed for an in-depth knowledge of their chemical properties, as well as the establishment of structure-activity relationships.…”