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Unnatural enantiomer of chaetocin shows strong apoptosis-inducing activity through caspase-8/caspase-3 activation

✍ Scribed by Yuou Teng; Katsuya Iuchi; Eriko Iwasa; Shinya Fujishiro; Yoshitaka Hamashima; Kosuke Dodo; Mikiko Sodeoka

Publisher: Elsevier Science
Year: 2010
Tongue: English
Weight: 646 KB
Volume: 20
Category: Article
ISSN: 0960-894X
DOI: 10.1016/j.bmcl.2010.07.032

No coin nor oath required. For personal study only.

✦ Synopsis

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.

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