biostudies-otherUnknown5Cho HToxicology reports647-653https://www.ebi.ac.uk/biostudies/studies/S-EPMC6046687Kobophenol A (KPA) is a biologically active natural compound isolated from the roots of Caragana sinica (Buc'hoz) Rehder (C. sinica). However, the anti-inflammatory effects of KPA have not been reported. This study aims to find out whether KPA isolated from roots of C. sinica can act as a potential substance on inflammation and analyze the molecular mechanism using the lipopolysaccharide (LPS)-stimulated J774?A.1 macrophage cell line. We showed that KPA treatment significantly suppressed the production of nitric oxide (NO) by inhibiting inducible nitric oxide synthase (iNOS) expression in a dose-dependent manner without cytotoxicity. In the KPA also inhibited pro-inflammatory cytokine gene expression and production, such as interleukin-1? (IL-1?) and interleukin-6 (IL-6) in LPS-stimulated J774?A.1 cells. As continuing study on the mechanisms involved, we confirmed that these effects of KPA were related to the inhibition of nuclear factor-?B (NF-?B) pathway including the suppression of I?B kinase ?/? (IKK?/?) phosphorylation and translocation of NF-?B into the nucleus. Taken together, the present study is the first to demonstrate that KPA isolated from C. sinica suppresses the expression of inflammatory mediators and cytokines by inhibiting NF-?B nuclear translocation in LPS-stimulated J774?A.1 macrophages. KPA may be a potential candidate for the treatment of inflammatory diseases in the future.biostudies-otherPMC6046687Europe PMCCho HPark JHAhn EKOh JSfalseKobophenol A Isolated from Roots of Caragana sinica (Buc'hoz) Rehder Exhibits Anti-inflammatory Activity by Regulating NF-?B Nuclear Translocation in J774A.1 Cells.Kobophenol A (KPA) is a biologically active natural compound isolated from the roots of Caragana sinica (Buc'hoz) Rehder (C. sinica). However, the anti-inflammatory effects of KPA have not been reported. This study aims to find out whether KPA isolated from roots of C. sinica can act as a potential substance on inflammation and analyze the molecular mechanism using the lipopolysaccharide (LPS)-stimulated J774?A.1 macrophage cell line. We showed that KPA treatment significantly suppressed the production of nitric oxide (NO) by inhibiting inducible nitric oxide synthase (iNOS) expression in a dose-dependent manner without cytotoxicity. In the KPA also inhibited pro-inflammatory cytokine gene expression and production, such as interleukin-1? (IL-1?) and interleukin-6 (IL-6) in LPS-stimulated J774?A.1 cells. As continuing study on the mechanisms involved, we confirmed that these effects of KPA were related to the inhibition of nuclear factor-?B (NF-?B) pathway including the suppression of I?B kinase ?/? (IKK?/?) phosphorylation and translocation of NF-?B into the nucleus. Taken together, the present study is the first to demonstrate that KPA isolated from C. sinica suppresses the expression of inflammatory mediators and cytokines by inhibiting NF-?B nuclear translocation in LPS-stimulated J774?A.1 macrophages. KPA may be a potential candidate for the treatment of inflammatory diseases in the future.2018-01-01T00:00:00Z2018 2019-03-26T23:47:04Z2019-03-26T23:47:04ZS-EPMC60466873002331110.1016/j.toxrep.2018.05.011