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Previously, a growth inhibiting effect of PC-Spes on head and neck carcinomacell lines had been demonstrated. In order to determine the toxic impact of particularherbs in the mixture, we exposed the head and neck cancer cell lines FADU, HLaC79and its Paclitaxel-resistant subline HLaC79-Clone1 as well as primary mucosalkeratinocytes to increasing concentrations of the herbal mixture Prostaprotect,which has a similar formulation as PC-Spes, as well as its single herbal componentsDendranthema morifolium, Ganoderma lucidium, Glycyrrhiza glabra, Isatis indigotica,Panax pseudo-ginseng, Rabdosia rubescens, Scutellaria baicalensis and Pygeum africanum.Growth inhibition was measured using the MTT assay. Expression of P-glycoprotein(P-GP), multidrug resistance protein-1 (MRP-1), multidrug resistance protein-2(MRP-2), breast cancer resistance protein (BCRP) and androgen receptor (AR) wereexamined by western blot analysis. Pygeum africanum extract clearly turned outas the main cytotoxic component of the Prostaprotect prescription mixture, andinitated apoptosis in sensitive cell lines. All other extracts had only minortoxic effects. Western blot analysis revealed increased expression of P-GP inHLaC79-Clone1 cells, while HLaC79 and FADU cells were negative. All three celllines were negative for MRP-1 and BCRP but positive for MRP-2. HLaC79 and itsdescendant HLaC79-Clone1 both expressed AR, as verified by western blotting andimmunofluorescence staining. Primary mucosal keratinocytes were negative for allmultidrug resistance markers as well as for AR. Growth inhibition rates of thesingle herbal extracts were compared with previously published results in prostatecarcinoma cell lines. The relationship between expression levels of AR and multidrugresistance markers in relation to the measured toxicity of herbal extracts inour head and neck cancer cell system is critically discussed.

Cytotoxicity of herbal extracts used for treatment of prostatic disease on head and neck carcinoma cell lines and non-malignant primary mucosal cells