EI-1511-3, -5 and EI-1625-2, novel interleukin-1 beta converting enzyme inhibitors produced by Streptomyces sp. E-1511 and E-1625. III. Biochemical properties of EI-1511-3, -5 and EI-1625-2.
EI-1511-3, -5 and EI-1625-2, novel interleukin-1 beta converting enzyme (ICE) inhibitors from the culture broths of Streptomyces sp. selectively inhibited the recombinant human ICE activity with IC50 values of 0.09, 0.38 and 0.2 microM, respectively, without inhibiting elastase and cathepsin B. Manumycin G, ent-alisamycin, U-56,407, and manumycin A and B isolated simultaneously from the same strains also inhibited ICE. EI-1511-3, -5 and EI-1625-2 also inhibited mature interleukin-1 beta secretion from THP-1 cells with IC50 values of 5.4, 3.6 and 2.2 microM, respectively. In this article, biological properties of EI-1511-3, -5 and EI-1625-2 and, in addition, properties of manumycin-related compound are described.
Tanaka
T
T
Tokyo Research Laboratories, Kyowa Hakko Kogyo Co., Ltd., Japan.
Tsukuda
E
E
Uosaki
Y
Y
Matsuda
Y
Y
D000577:Amides / Q000494:pharmacology*; D002478:Cells, Cultured; D003512:Cyclohexanones / Q000494:pharmacology*; D004791:Enzyme Inhibitors / Q000494:pharmacology*; D006801:Humans; D008826:Microbial Sensitivity Tests; D013302:Streptomyces; D013329:Structure-Activity Relationship
D000577:Amides; D003512:Cyclohexanones; C103155:EI 1511-3; C103156:EI 1511-5; C103157:EI 1625-2; D004791:Enzyme Inhibitors