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

作者：Teng Yuou; Iuchi Katsuya; Iwasa Eriko; Fujishiro Shinya; Hamashima Yoshitaka; Dodo Kosuke; Sodeoka Mikiko^*

来源：Bioorganic & Medicinal Chemistry Letters, 2010, 20(17): 5085-5088.

DOI：10.1016/j.bmcl.2010.07.032

• Apoptosis
• Caspase
• Dithiodiketopiperazine

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.

• 出版日期2010-9-1