title: A Supramolecular Substance, [2] Rotaxane, Induces Apoptosis in Human Molt-3 Acute Lymphoblastic Leukemia Cells.
abstract: The antitumor effects of a supramolecular substance, the [2] rotaxane (TRO-A0001), and its molecular mechanisms were investigated. TRO-A0001 suppressed the proliferation of cultured human Molt-3 acute lymphoblastic leukemia cells for 12-72 h in a dose-dependent manner. Based on flow cytometry, TRO-A0001 clearly induced apoptosis after 24 h. The mitochondrial membrane potential disappeared after treatment with 1.0 µM of TRO-A0001. Expression of the cleaved forms of capase-9 and caspase-3 was significantly increased in cells exposed to TRO-A0001, whereas the expression of XIAP, a type of inhibitor of apoptosis family, was decreased. These results suggest that [2] rotaxane TRO-A0001 may be a highly promising new antitumor medicine.
authors.affiliation: Medicinal-Informatics and Research Unit, Faculty of Pharmaceutical Sciences, Fukuoka University, Fukuoka, Japan.
authors.forename: M
authors.initials: M
authors.lastname: Kimura
authors.affiliation: Medicinal-Informatics and Research Unit, Faculty of Pharmaceutical Sciences, Fukuoka University, Fukuoka, Japan.
authors.forename: K
authors.initials: K
authors.lastname: Makio
authors.affiliation: Medicinal-Informatics and Research Unit, Faculty of Pharmaceutical Sciences, Fukuoka University, Fukuoka, Japan.
authors.forename: K
authors.initials: K
authors.lastname: Hara
authors.affiliation: Medicinal-Informatics and Research Unit, Faculty of Pharmaceutical Sciences, Fukuoka University, Fukuoka, Japan.
authors.forename: W
authors.initials: W
authors.lastname: Hiruma
authors.affiliation: Department of Genome Biology, Kinki University School of Medicine, Osaka, Japan.
authors.forename: Y
authors.initials: Y
authors.lastname: Fujita
authors.affiliation: Department of Organic and Polymeric Materials, Tokyo Institute of Technology, Tokyo, Japan.
authors.forename: T
authors.initials: T
authors.lastname: Takata
authors.affiliation: Department of Genome Biology, Kinki University School of Medicine, Osaka, Japan.
authors.forename: K
authors.initials: K
authors.lastname: Nishio
authors.affiliation: Medicinal-Informatics and Research Unit, Faculty of Pharmaceutical Sciences, Fukuoka University, Fukuoka, Japan.
authors.forename: N
authors.initials: N
authors.lastname: Ono
mesh_terms: D000970:Antineoplastic Agents / Q000008:administration & dosage / Q000494:pharmacology*; D017209:Apoptosis / Q000187:drug effects*; D053148:Caspase 3 / Q000235:genetics; D053453:Caspase 9 / Q000235:genetics; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D005434:Flow Cytometry; D006801:Humans; D053078:Membrane Potential, Mitochondrial / Q000187:drug effects; D054198:Precursor Cell Lymphoblastic Leukemia-Lymphoma / Q000188:drug therapy* / Q000473:pathology; D043862:Rotaxanes / Q000008:administration & dosage / Q000494:pharmacology*; D013997:Time Factors; D051636:X-Linked Inhibitor of Apoptosis Protein / Q000235:genetics
chemical_list: D000970:Antineoplastic Agents; D043862:Rotaxanes; D051636:X-Linked Inhibitor of Apoptosis Protein; C496866:XIAP protein, human; D053148:Caspase 3; D053453:Caspase 9