title: A novel therapy for ovarian cancer using real‑time imaging.
abstract: The present study was designed to develop an activable, dual‑targeted theranostic platform combining fluorescent and cytotoxic templates to provide a novel strategy for specific drug delivery and cellular imaging in ovarian cancer cells. Two compounds of a folic acid‑prodrug‑doxorubicin (Dox) scaffold were synthesized, and their antiproliferative activities were evaluated using 3‑(4,5‑dimethylthiazol‑2‑yl)‑2,5‑diphenyltetrazolium bromide and flow cytometric analysis. The process of drug release was investigated using fluorescence emission spectra assay and confocal laser scanning microscopy. The results showed that the synthesized compounds exhibited potent antitumor activities against ovarian cell lines. Among them, compound 1e exhibited the most potent activity demonstrating half maximal inhibitory concentration values of 0.85±0.10, 8.64±0.37 and 0.81±0.03 µM against A2780, A2780/Dox and A2780/cisplatin cell lines. The fluorescence imaging of live cell lines also provided an easy and reliable method to monitor site‑specific drug activities through turn‑on systems induced by drug release. The results of the present study may assist in the treatment of ovarian cancer cells with strengthened efficiency and real‑time imaging, which may be used as a multifunctional system for the optimization of anticancer drugs.
authors.affiliation: Department of Gynaecology, Linyi People's Hospital, Linyi, Shandong 276003, P.R. China.
authors.forename: Zhen
authors.initials: Z
authors.lastname: Zhang
authors.affiliation: Department of Gynaecology, Linyi People's Hospital, Linyi, Shandong 276003, P.R. China.
authors.forename: Zhaojie
authors.initials: Z
authors.lastname: Chen
authors.affiliation: Department of Gynaecology, Linyi People's Hospital, Linyi, Shandong 276003, P.R. China.
authors.forename: Beibei
authors.initials: B
authors.lastname: Xie
authors.affiliation: Department of Gynaecology, Linyi People's Hospital, Linyi, Shandong 276003, P.R. China.
authors.forename: Haiyan
authors.initials: H
authors.lastname: Zhang
mesh_terms: D000970:Antineoplastic Agents / Q000737:chemistry / Q000494:pharmacology*; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D004396:Coloring Agents / Q000737:chemistry; D004317:Doxorubicin / Q000031:analogs & derivatives / Q000494:pharmacology*; D005260:Female; D005434:Flow Cytometry; D005492:Folic Acid / Q000031:analogs & derivatives / Q000494:pharmacology*; D006801:Humans; D018613:Microscopy, Confocal; D061848:Optical Imaging; D010051:Ovarian Neoplasms / Q000000981:diagnostic imaging / Q000188:drug therapy*; D010053:Ovary / Q000000981:diagnostic imaging / Q000187:drug effects*; D011355:Prodrugs / Q000737:chemistry / Q000494:pharmacology*; D013778:Tetrazolium Salts / Q000737:chemistry; D013844:Thiazoles / Q000737:chemistry
chemical_list: D000970:Antineoplastic Agents; D004396:Coloring Agents; D011355:Prodrugs; D013778:Tetrazolium Salts; D013844:Thiazoles; D004317:Doxorubicin; D005492:Folic Acid; C022616:thiazolyl blue