基于半花菁结构的线粒体靶向抗肿瘤药物的合成及性能研究OA

Objective To first synthesize a mitochondria-targeting hemicyanine derivative with antitumor activity.Methods The com-pound PNIN((E)-2-(4-(bis(4-(pyridin-4-yl)phenyl)amino)styryl)-1-ethyl-3,3-dimethyl-3H-indole-1-iodide)was designed and synthe-sized by using the indole cation in the hemicarbocyanine structure and 4-(bis(4-(pyridin-4-yl)phenyl)amino)benzaldehyde as substrate.The structural characterization of the compound was identified through nuclear magnetic resonance(NMR)and high-resolution mass spec-trometry,while the photophysical and chemical properties were investigated by means of fluorescence and UV-visible absorption spectrosco-py.The electronic structure parameters,including the electron spin-up(ESP),the electron hole(HOMO),the electron spin-down(LU-MO),and the energy gap(Eg),were derived through theoretical calculations.The toxicity of the compound was detected by using MTT as-say and live/dead double staining of cells.Mitochondrial fluorescence co-localization imaging was photographed by laser confocal microsco-py.Results The synthesized hemicyanine derivatives exhibited anticancer toxicity,red-light imaging ability,and excellent mitochondrial tar-geting.Conclusion PNIN has the capacity to mitochondrial-target red-light imaging and exhibits cytotoxicity,makeing it a potential mitochon-dria-targeting antitumor drug.