Koizumi Fumito, Agatsuma Tsutomu, Ando Katsuhiko, Kondo Hidemasa, Saitoh Yutaka, Matsuda Yuzuru, Nakanishi Satoshi
Tokyo Research Laboratories, Kyowa Hakko Kogyo Co., Ltd., 3-6-6 Asahimachi, Machida-shi, Tokyo 194-8533, Japan.
J Antibiot (Tokyo). 2003 Nov;56(11):891-8. doi: 10.7164/antibiotics.56.891.
EI-2128-1, a novel interleukin-1beta converting enzyme (ICE) inhibitor, was isolated from the culture broths of Penicillium sp. E-2128. EI-2128-1 selectively inhibited human recombinant ICE activity with IC50 value of 0.59 microM, without inhibiting elastase and cathepsin B. EI-2128-1 also inhibited mature interleukin-1beta secretion from THP-1 cells induced by LPS with IC50 value of 0.28 microM.
EI-2128-1是一种新型白细胞介素-1β转化酶(ICE)抑制剂,从青霉菌E-2128的培养液中分离得到。EI-2128-1选择性抑制人重组ICE活性,IC50值为0.59微摩尔,而不抑制弹性蛋白酶和组织蛋白酶B。EI-2128-1还抑制脂多糖诱导的THP-1细胞分泌成熟白细胞介素-1β,IC50值为0.28微摩尔。