Kondeva-Burdina, MagdalenaSimeonova, RumyanaVitcheva, VesselaLazarova, IrinaGevrenova, RenetaZheleva-Dimitrova, DimitrinaZengin, Gökhan2020-03-262020-03-2620181570-18081875-628Xhttps://dx.doi.org/10.2174/1570180814666170306122707https://hdl.handle.net/20.500.12395/36557Background: In the current study, we evaluate the possible in vitro hepatoprotective and antioxidant activity of Asphodeline lutea (L.) Rchb. dry root extract (ALE), and isolated from the same extract 2-acetyl-1,8-dimethoxy-3-methylnaphthalene (1). The potential of the main root compounds, chrysophanol (2) and caffeic acid (3), was studied as well. A model of non-enzyme lipid peroxidation (LPO) in isolated liver microsomes was induced by iron-ascorbic acid (Fe2+/AA) mixture and assessed by the quantity of malondialdehyde (MDA) -an LPO product. The incubation of the microsomes with ALE (1 mg/ml) and 1-3 (100 mu g/ml) resulted in a significant decrease in MDA production, compared to the Fe2+/AA incubated samples with 23% (ALE), 61 % (1), 62% (3), while classical hepatoprotector silymarin decreased the parameter with 64 %. Methods: Studied compounds showed some toxicity in isolated rat hepatocytes discerned by increased LDH leakage and MDA quantity, decreased cell viability and reduced glutathione (GSH) levels compared to the control (non-treated hepatocytes). Results: The antioxidant and hepatoprotective potential of 1-3 was observed in vitro against carbon tetrachloride (CCl4)-induced toxicity, where they normalize all the examined parameters pertur-bated by CCl4 administration. The effects of 1 are lower than 3 and silymarin, but were better than those of 2. Conclusion: On the basis of these results, we discuss a bidirectional potential of the assayed parameters that might be explained with naphthalene transformation in cytochrom P450-dependent oxidation by CYP3A. The lack of metabolism and bioactivation of CCl4 could explain the cytoprotective effects of 1-3. The pro-oxidant effects of 1 and 2, in in vitro models, could be due to naphthalene and anthraquinone bioactivation pathways involving toxic metabolites.en10.2174/1570180814666170306122707info:eu-repo/semantics/closedAccessMicrosomeshepatocytesmalondialdehydeAsphodeline lutea (L.) Rchb.anthraquinonesnaphthalenesArticle153251255Q3WOS:000423791700006Q4