5-7-dihydroxy-6-methoxy-2-phenylchromen-4-one and Carcinoma--Squamous-Cell

Squamous cell carcinoma (SCC) is a usually responds poorly to treatment suffers from poor therapeutic benefits while oroxylin A (OA) is a promising flavonoid with high anticancer efficacy against various cancer types. Here in our study, in order to reveal the potential of OA based drug delivery systems (DDSs) in the treatment of SCC, we firstly revealed that OA had a certain pharmacodynamic effect on skin SCC (A431 cells). Afterwards, OA was loaded into a newly synthesized aggregation-induced emission (AIE)-active polymer to construct OA-loaded PDots for the first time. Our results revealed that OA-loaded PDots showed preferable drug loading and enhanced stability. Moreover, the DDS was also capable of self-illumination in the aggregate state to reveal the uptake profile. Most importantly, the DDS showed much more elevated anticancer benefits than free OA in vitro and advanced tumor targetability in vivo, suggesting that it might be a promising system against SCC.

Topics: Animals; Antineoplastic Agents; Carcinoma, Squamous Cell; Cell Proliferation; Cell Survival; Dose-Response Relationship, Drug; Drug Delivery Systems; Drug Liberation; Drug Screening Assays, Antitumor; Flavonoids; Humans; Male; Mice; Mice, Inbred BALB C; Mice, Nude; Molecular Structure; Neoplasms, Experimental; Particle Size; Polymers; Structure-Activity Relationship; Surface Properties; Tumor Cells, Cultured

To evaluate the radiosensitization of Oroxylin A on esophageal carcinoma cell as well as the optimal scheduling of Oroxylin A and radiotherapy (RT). Cell proliferation was estimated by a CCK8 assay. Radiosensitization was evaluated by a clonogenic survival assay. The progressions of Cell apoptosis and Cell cycle were investigated by flow cytometry. Expressions of survivin and cell cycle regulators were evaluated by Western blot analysis. A dose-dependent cell survival reduction was found in response to radiation with or without Oroxylin A. The apoptosis rates were remarkably dose-dependent higher in combination groups than in either Oroxylin A or radiation alone group. Besides, Oroxylin A could obviously radiosensitize ESCC cells by arresting tumor cells in G2/M phase and regulating cyclin B1 and Cdc 2 protein expression. Oroxylin A could be a promising radiosensitizer for esophageal squamous cell carcinoma by inducing G2/M phase blocking and activating cell apoptosis.

Topics: Apoptosis; Carcinoma, Squamous Cell; Cell Cycle Checkpoints; Cell Line, Tumor; Cell Proliferation; Cyclin B1; Esophageal Neoplasms; Esophageal Squamous Cell Carcinoma; Flavonoids; G2 Phase Cell Cycle Checkpoints; Humans; Radiation-Sensitizing Agents