title: Unnatural enantiomer of chaetocin shows strong apoptosis-inducing activity through caspase-8/caspase-3 activation.
abstract: Chaetocin, a natural product isolated from Chaetomium species fungi, was reported to have various biological activities, including antitumor and antifungal activities. Recently, we reported the first total synthesis of chaetocin and its derivatives. Here, we examined the cell-death-inducing activity of these compounds in human leukemia HL-60 cells. The unnatural enantiomer of chaetocin (ent-chaetocin) was more potent than chaetocin, and was found to induce apoptosis through the caspase-8/caspase-3 activation pathway.
authors.affiliation: Sodeoka Live Cell Chemistry Project, ERATO, JST, Wako-shi, Saitama, Japan.
authors.forename: Yuou
authors.initials: Y
authors.lastname: Teng
authors.forename: Katsuya
authors.initials: K
authors.lastname: Iuchi
authors.forename: Eriko
authors.initials: E
authors.lastname: Iwasa
authors.forename: Shinya
authors.initials: S
authors.lastname: Fujishiro
authors.forename: Yoshitaka
authors.initials: Y
authors.lastname: Hamashima
authors.forename: Kosuke
authors.initials: K
authors.lastname: Dodo
authors.forename: Mikiko
authors.initials: M
authors.lastname: Sodeoka
mesh_terms: D017209:Apoptosis / Q000187:drug effects*; D015153:Blotting, Western; D053148:Caspase 3 / Q000378:metabolism*; D053181:Caspase 8 / Q000378:metabolism*; D004789:Enzyme Activation; D018922:HL-60 Cells; D006801:Humans; D010879:Piperazines / Q000737:chemistry / Q000494:pharmacology; D013237:Stereoisomerism
chemical_list: D010879:Piperazines; C002511:chaetocin; D053148:Caspase 3; D053181:Caspase 8