Antitumor agent-214

Antitumor agent-214 is a chalcone analogue with anticancer properties. It induces cell cycle arrest and apoptosis (apoptosis) in tumor cells, disrupts mitochondrial metabolic homeostasis, upregulates caspase-3, caspase-7, and caspase-9, and downregulates PARP1. Antitumor agent-214 is applicable in antitumor research related to colorectal cancer, breast cancer, lung cancer, and cervical cancer.

Antitumor agent-214 (Compound 3f) exhibits cytotoxicity against various cancer cell lines, with IC 50 values: HCT-116 cells (3.56 μM), MCF-7 cells (4.08 μM), A549 cells (12.70 μM), HeLa cells (8.37 μM), HT-29 cells (6.18 μM), and MD-MBA-231 cells (10.62 μM). It shows significantly lower cytotoxicity towards non-cancerous MCF-10A cells (IC 50 = 9.81 μM). Treatment with Antitumor agent-214 (1.78-7.12 μM; 24 h) results in dose-dependent accumulation of HCT-116 cells in the sub-G1 phase, indicating apoptosis induction. This apoptosis is confirmed using Annexin V-FITC/PI dual staining, with similar apoptosis rates to Staurosporine at 7.12 μM, and a weaker effect on MCF-10A cells. Further confirmation via AO-EB dual staining shows an increase in orange fluorescent apoptotic cells in a dose-dependent manner. Using MitoSOX Red staining, Antitumor agent-214 (3.56 μM, 7.12 μM; 24 h) is found to increase mitochondrial superoxide generation in HCT-116 cells, while JC-1 staining shows mitochondrial membrane potential depolarization at 7.12 μM. Moreover, Antitumor agent-214 (7.12 μM; 4-12 h) promotes cleavage of PARP1, caspase 3, caspase 7, and caspase 9 in HCT-116 cells, with significant accumulation of cleaved proteins at 12 h.