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.
