TY - JOUR AU - Salucci, Sara AU - Burattini, Sabrina AU - Buontempo, Francesca AU - Orsini, Ester AU - Furiassi, Lucia AU - Mari, Michele AU - Lucarini, Simone AU - Martelli, Alberto M. AU - Falcieri, Elisabetta PY - 2018/04/10 Y2 - 2024/03/29 TI - Marine bisindole alkaloid: A potential apoptotic inducer in human cancer cells JF - European Journal of Histochemistry JA - Eur J Histochem VL - 62 IS - 2 SE - Original Papers DO - 10.4081/ejh.2018.2881 UR - https://www.ejh.it/ejh/article/view/2881 SP - AB - <p>Marine organisms such as corals, sponges and tunicates produce active molecules which could represent a valid starting point for new drug development processes. Among the various structural classes, the attention has been focused on 2,2-bis(6-bromo-3-indolyl) ethylamine, a marine alkaloid which showed a good anticancer activity against several tumor cell lines. Here, for the first time, the mechanisms of action of 2,2-bis(6-bromo-3-indolyl) ethylamine have been evaluated in a U937 tumor cell model. Morpho-functional and molecular analyses, highlighting its preferred signaling pathway, demonstrated that apoptosis is the major death response induced by this marine compund. Chromatin condensation, micronuclei formation, blebbing and <em>in situ</em> DNA fragmentation, occurring through caspase activation (extrinsic and intrinsic pathways), were observed. In particular, the bisindole alkaloid induces a mitochondrial involvement in apoptosis machinery activation with Blc-2/Bcl-x down-regulation and Bax up-regulation. These findings demonstrated that 2,2-bis(6-bromo-3-indolyl) ethylamine alkaloid-induced apoptosis is regulated by the Bcl-2 protein family upstream of caspase activation.</p> ER -