Bioorganic & Medicinal Chemistry Letters 2010-09-01

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

Yuou Teng, Katsuya Iuchi, Eriko Iwasa, Shinya Fujishiro, Yoshitaka Hamashima, Kosuke Dodo, Mikiko Sodeoka

Index: Bioorg. Med. Chem. Lett. 20(17) , 5085-8, (2010)

Full Text: HTML

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.Copyright 2010 Elsevier Ltd. All rights reserved.