Sakurai Masaaki, Kohno Jun, Yamamoto Kouzou, Okuda Toru, Nishio Maki, Kawano Kimio, Ohnuki Tetsuo
Discovery Research Laboratory, Tanabe Seiyaku Co., Ltd., Toda-shi, Saitama, Japan.
J Antibiot (Tokyo). 2002 Aug;55(8):685-92. doi: 10.7164/antibiotics.55.685.
New inhibitors of IL-4 signal transduction, designated as TMC-256A1 and C1, were discovered together with TMC-256B1, a previously known dihydronaphthopyrone, from the fermentation broth of Aspergillus niger var niger TC 1629 by using an IL-4 driven reporter gene assay. Based on spectroscopic analyses, TMC-256A1 and C1 were found to be new members of the naphthopyrone antibiotics. TMC-256A1, B1 and C1 inhibited the IL-4 driven luciferase activity with IC50 values of 25 microM, 30 microM and 1.7 microM, respectively in this assay system. Furthermore, these compounds inhibited the expression of germline C epsilon mRNA with IC50 values of 6.6 microM , 34 microM and 0.31 microM, respectively.
