Tumor necrosis factor-alpha production-inhibiting activity of phthalimide analogues on human leukemia THP-1 cells and a structure-activity relationship study
1997; Elsevier BV; Volume: 5; Issue: 11 Linguagem: Inglês
10.1016/s0968-0896(97)00148-x
ISSN1464-3391
AutoresHiroyuki Miyachi, Asuka Ogasawara, Arata Azuma, Yuichi Hashimoto,
Tópico(s)Immune Response and Inflammation
ResumoN-Substituted phthalimides (2-substituted 1H-isoindole-1,3-diones) were prepared and their inhibitory effects on tumor necrosis factor-alpha (TNF-α) production by human leukemia cell line THP-1 stimulated with 12-O-tetradecanoylphorbol 13-acetate (TPA) or okadaic acid (OA) were examined. A structure-activity relationship study of these phthalimide analogues revealed that their inhibitory effects on TPA- and OA-induced TNF-α production by THP-1 cells are well correlated to each other, i.e. they may involve the same target molecule(s). An analysis by the use of phthalimide analogue-immobilized affinity gels indicated the existence of several phthalimide-binding proteins in THP-1 cell extract.
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