Abstract
Several Petasites hybridus eremophilanes have been tested for cytotoxicity in primary rat hepatocytes by means of the MTT assay [1, 2, 3]. (8S)-8-Hydroxyeremophil-7(11)-en-12,8-olide, (8R,9β)-2-[(Angeloyl)oxy]-9-hydroxyeremophil-7(11)-en-12,8-olide and (8S)-2-[Methacroyl)oxy]eremophil-7(11)-en-12,8-olide were not cytotoxic up to a concentration of 0.5mg/mL. No EC50 values were determinable for these less soluble compounds. (8S)-2-{[(Z)-3-(Methylsulfanyl)prop-2-enoyl]oxy}eremophil-7(11)-en-12,8-olide was not cytotoxic up to 1mg/mL. (8R)-2-[Methacroyl)oxy]eremophil-7(11)-en-12,8-olide was the most cytotoxic constituent (EC50 approx. 0.3mg/mL). The non-steroid-like 8α-conformers of both 8-H-isomeric couples of the 2-angeloyloxy and 2-methacroyloxy esters of eremophilanolide seemed to be more cytotoxic than the steroid-like 8β-H-conformers. The additionally measured cytotoxicity parameters mitochondrial dehydrogenase activity, ATP-content and LDH-leakage were considerably lower for the 8α-conformer of 2-[Methacroyl)oxy]eremophil-7(11)-en-12,8-olide than for the corresponding 8β-conformer [4]. This stereoselectivity points to a specific new cytotoxicity target.
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