title: Influence of novel supramolecular substance, [2] rotaxane, on the caspase signaling pathway in melanoma and colon cancer cells in vitro.
abstract: We studied the influence of novel supramolecular substance, [2] rotaxane (TRO-A0001), on caspase signaling and cell viability in cancer cell lines. TRO-A0001 suppressed concentration-dependently cell proliferation. Expression of the cleaved-form caspase-3 and PARP was significantly increased in cells exposed to TRO-A0001. The expression of Bax was increased by TRO-A0001. Furthermore, the down-regulation of Bax by siRNA resulted in growth activation significantly. The morphological analysis demonstrated that TRO-A0001 increased the levels of apoptotic cells in human cancer cell lines. These results suggest that TRO-A0001 induces apoptosis in cancer cells and holds potential as a new anti-tumor medicine.
authors.affiliation: Medicinal Informatics and Research Unit, Faculty of Pharmaceutical Sciences, Fukuoka University, Fukuoka, Japan.
authors.forename: Kazuki
authors.initials: K
authors.lastname: Hara
authors.forename: Tatsuya
authors.initials: T
authors.lastname: Beppu
authors.forename: Masahiko
authors.initials: M
authors.lastname: Kimura
authors.forename: Yoshihiko
authors.initials: Y
authors.lastname: Fujita
authors.forename: Toshikazu
authors.initials: T
authors.lastname: Takata
authors.forename: Kazuto
authors.initials: K
authors.lastname: Nishio
authors.forename: Nobufumi
authors.initials: N
authors.lastname: Ono
mesh_terms: D000230:Adenocarcinoma / Q000473:pathology*; D017209:Apoptosis / Q000187:drug effects* / Q000235:genetics*; D020169:Caspases / Q000378:metabolism* / Q000502:physiology*; D003110:Colonic Neoplasms / Q000473:pathology*; D006801:Humans; D046911:Macromolecular Substances; D008545:Melanoma / Q000473:pathology*; D058990:Molecular Targeted Therapy; D043862:Rotaxanes / Q000494:pharmacology*; D015398:Signal Transduction / Q000187:drug effects* / Q000235:genetics* / Q000502:physiology; D014407:Tumor Cells, Cultured; D051028:bcl-2-Associated X Protein / Q000378:metabolism
chemical_list: C494826:BAX protein, human; D046911:Macromolecular Substances; D043862:Rotaxanes; D051028:bcl-2-Associated X Protein; D020169:Caspases