Iwasaki Arihiro, Ohno Osamu, Katsuyama Shun, Morita Maho, Sasazawa Yukiko, Dan Shingo, Simizu Siro, Yamori Takao, Suenaga Kiyotake
Department of Chemistry, Keio University, 3-14-1 Hiyoshi, Yokohama, Kanagawa 223-8522, Japan.
School of Advanced Engineering, Kogakuin University, 2665-1 Nakanocho, Hachioji, Tokyo 192-0015, Japan.
Bioorg Med Chem Lett. 2015 Nov 15;25(22):5295-8. doi: 10.1016/j.bmcl.2015.09.044. Epub 2015 Sep 21.
In 2014, we isolated kurahyne, an acetylene-containing lipopeptide, from a marine cyanobacterial assemblage of Lyngbya sp. Kurahyne exhibited growth-inhibitory activity against human cancer cells, and induced apoptosis in HeLa cells. However, its mode of action is not yet clear. To elucidate its mode of action, we carried out several cell-based assays, and identified the intracellular target molecule of kurahyne as sarco/endoplasmic reticulum Ca(2+) ATPase (SERCA). In addition, we found that kurahyne inhibited the differentiation of macrophages into osteoclasts.
2014年，我们从林氏藻属的海洋蓝藻菌群中分离出了kurahyne，一种含乙炔的脂肽。Kurahyne对人类癌细胞表现出生长抑制活性，并诱导HeLa细胞凋亡。然而，其作用方式尚不清楚。为了阐明其作用方式，我们进行了几种基于细胞的试验，并确定kurahyne的细胞内靶分子为肌浆网/内质网Ca(2+)ATP酶（SERCA）。此外，我们发现kurahyne抑制巨噬细胞向破骨细胞的分化。
