title: Anticancer, antiradical and antioxidative actions of novel Antoksyd S and its major components, baicalin and baicalein.
abstract: Here we show for the first time that the novel designed drug, Antoksyd S and its polyphenolic flavones (baicalin and baicalein), act as cell proliferation modifiers of mouse leukemia cells (L1210). The cytotoxicity of Antoksyd S and baicalein in vitro was expressed as ED50 and compared with those of the cytostatics doxorubicin, cisplatin and DACA, under the same experimental conditions. Cell viability was determined by modified tetrazolium dye assay, using as a model cells with neoblastic phenotype (L1210). The antiradical activity of Antoksyd S and baicalin were investigated using the DPPH test in order to obtain their antioxidant characteristics. Structure- and concentration-dependent one electron bioactivations (peroxidative oxidation) of Antoksyd S and baicalin were performed in the absence or in the presence of GSH or SOD. It appears that Antoksyd S is a low toxic novel drug which could be effective in providing concentration-dependent antioxidative activity, acting as a cell proliferation modifier and, probably, as an apoptosis inducer in vitro, though this remains to be explored. These findings are discussed from a mechanistic standpoint as well as in terms of potential pharmacological applications under acute oxidative stress and apoptotic events. This work provides the basis for further investigations of Antoksyd S action in vitro and in vivo, since the presented results are indicative of its intracellular metabolic activation, which can only be partially associated with its observed action towards model cancer cells (mouse leukemia L1210).
authors.affiliation: Department of Medicinal Chemistry, Institute of Physiology and Biochemistry, Medical University of Lodz, Lindleya 6, 90-131 Lodz, Poland.
authors.forename: Ewa
authors.initials: E
authors.lastname: Ciesielska
authors.forename: Antoni
authors.initials: A
authors.lastname: Gwardys
authors.forename: Diana
authors.initials: D
authors.lastname: Metodiewa
mesh_terms: D000609:Aminoacridines / Q000494:pharmacology; D000818:Animals; D000972:Antineoplastic Agents, Phytogenic / Q000494:pharmacology*; D002455:Cell Division / Q000187:drug effects; D002470:Cell Survival / Q000187:drug effects; D002945:Cisplatin / Q000494:pharmacology; D004317:Doxorubicin / Q000494:pharmacology; D004338:Drug Combinations; D044950:Flavanones; D005419:Flavonoids / Q000378:metabolism / Q000494:pharmacology*; D007939:Leukemia L1210 / Q000188:drug therapy / Q000473:pathology; D051379:Mice; D010084:Oxidation-Reduction; D031364:Scutellaria baicalensis / Q000737:chemistry
chemical_list: D000609:Aminoacridines; D000972:Antineoplastic Agents, Phytogenic; D004338:Drug Combinations; D044950:Flavanones; D005419:Flavonoids; C471185:antoksyd S; C038044:baicalin; C006680:baicalein; D004317:Doxorubicin; C062948:N-((2-dimethylamino)ethyl)-9-aminoacridine-4-carboxamide; D002945:Cisplatin