DNA-Damaging, Mutagenic, and Clastogenic Activities of Gentiopicroside Isolated from Cephalaria kotschyi Roots

Gentiopicroside (1) is the major secoiridoid glucoside constituent of Cephalaria kotschyi roots. The mutagenicity, DNA-damaging capacities, and clastogenicity of this molecule were evaluated by the Salmonella typhimurium mutagenicity assay (Ames test) on tester strains TA97a, TA98, TA100, and TA102, the alkaline comet assay, and the micronucleus assay on CHO cells. All tests were performed with and without the metabolization mixture, S9 mix. In the Ames test, the mutagenicity of 1 was limited to TA102 without S9 mix (2.3 rev μg−1). The genotoxicity was more evident without S9 mix (0.78 OTMχ2 units μg−1 mL) than with the metabolic mixture (0.16 OTMχ2 units μg−1 mL) with the comet assay. Similarly, the clastogenicity without S9 mix was 0.99 MNC μg−1 mL and 0.38 MNC μg−1 mL with S9 mix in the micronucleus assay. The interaction of 1 with DNA is probably through the involvement of oxidative DNA lesions.