Fluorinated Derivatives of Digalloyl-Flavan-3-ol Induce Autophagic Cell Death by Forming Granular Aggregates Containing Mitochondria

Flavan-3-ol derivatives are polyphenolic compounds with multifunctional properties. One of the flavan-3-ol derivatives, green tea catechin epigallocatechin gallate, is known to have anticancer activity as one its We studied synthesis and conducted structure-activity relationship studies; we found that fluorinated exhibited high toxicity against HeLa A549 cells. It was confirmed cytotoxicity affected by conformation skeleton 2,3-cis form dominant. The addition increased amount intracellular mitochondrial superoxide, abolished membrane potential mitochondria, and, interestingly, formed granular aggregates containing mitochondria. When level LC3-II, a marker autophagy induction, confirmed, it suggested promoted autophagy. These results suggest novel highly cytotoxic compound synthesized in this study promotes induces cell death triggering dysfunction. believe these possibility conferring more functionality through structural transformations derivatives.