Unnatural enantiomer of chaetocin shows strong apoptosis-inducing activity through caspase-8/caspase-3 activation.
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.
Teng
Yuou
Y
Sodeoka Live Cell Chemistry Project, ERATO, JST, Wako-shi, Saitama, Japan.
Iuchi
Katsuya
K
Iwasa
Eriko
E
Fujishiro
Shinya
S
Hamashima
Yoshitaka
Y
Dodo
Kosuke
K
Sodeoka
Mikiko
M
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
D010879:Piperazines; C002511:chaetocin; D053148:Caspase 3; D053181:Caspase 8