Kuramochi Kouji, Yukizawa Shunsuke, Ikeda Seiki, Sunoki Takashi, Arai Satoshi, Matsui Rie, Morita Akinori, Mizushina Yoshiyuki, Sakaguchi Kengo, Sugawara Fumio, Ikekita Masahiko, Kobayashi Susumu
Department of Applied Biological Science, Tokyo University of Science, 2641 Yamazaki, Noda, Chiba 278-8510, Japan.
Bioorg Med Chem. 2008 May 1;16(9):5039-49. doi: 10.1016/j.bmc.2008.03.029. Epub 2008 Mar 14.
Epolactaene, isolated from cultured Penicillium sp. BM 1689-P mycelium, induces neurite outgrowth and arrests the cell cycle of the human neuroblastoma cell line, SH-SY5Y, at the G1 phase. We have found that epolactaene and its derivatives induce apoptosis in the human leukemia B-cell line, BALL-1. In this study, we prepared fluorescent and biotinylated epolactaene derivatives. We characterized the cellular location and the identification of BALL-1 proteins that reacted with these compounds. The results obtained from the reaction of epolactaene or its derivative with N-acetylcysteine methyl ester indicate that these compounds induce the disulfide formation and the alpha-position of the epoxylactam core is the reactive site.
从培养的青霉属菌株BM 1689-P菌丝体中分离得到的表乳糖烯可诱导神经突生长，并使人类神经母细胞瘤细胞系SH-SY5Y的细胞周期停滞在G1期。我们发现表乳糖烯及其衍生物可诱导人类白血病B细胞系BALL-1发生凋亡。在本研究中，我们制备了荧光和生物素化的表乳糖烯衍生物。我们对这些化合物反应的BALL-1蛋白的细胞定位和鉴定进行了表征。表乳糖烯或其衍生物与N-乙酰半胱氨酸甲酯反应得到的结果表明，这些化合物可诱导二硫键形成，且环氧内酰胺核心的α位是反应位点。
