Benzophenanthridine Alkaloids of Chelidonium majus; II. Potent Inhibitory Action Against the Growth of Human Keratinocytes

Abstract

The benzophenanthridine alkaloids sanguinarine and chelerythrine of Chelidonium majus, L. (Papaveraceae), were tested for their action against the growth of human keratinocytes. Cell proliferation was independently determined by directly counting the cells and in the colorimetric MTT assay. Sanguinarine potently inhibited cell growth with an IC₅₀ of 0.2 µM. Chelidonine, the main alkaloid of Ch. majus, was much less efficient. The extract of the herb of Ch. majus was also effective with an IC₅₀ of 1.9 µM, calculated on the basis of its alkaloid content in terms of chelidonine. Keratinocytes were further tested for their susceptibility for the action of sanguinarine and chelerythrine on plasma membrane integrity, which resulted in a twofold increase in lactate dehydrogenase (LDH) activity as compared to controls. On the other hand, the activity of the extract of the herb of Ch. majus was due to cytostatic rather than cytotoxic effects, as LDH release was unchanged as compared to controls.

Key words

Antiproliferative activity - chelerythrine - chelidonine - Chelidonium majus L. - Papaveraceae - HaCaT keratinocytes - sanguinarine