Department of Hepatobiliary Surgery, Affiliated Hospital of Logistics University of PAPF, Tianjin, P. R. China.
Arch Pharm (Weinheim). 2016 Jan;349(1):63-70. doi: 10.1002/ardp.201500349. Epub 2015 Dec 10.
Concerning the role of antioxidant and anti-inflammatory agents for hepatic fibrosis patients, the current study deals with the development of novel chalcone derivatives 5a-i via efficient synthetic methodology in a two-step reaction involving Claisen-Schmidt condensation. The obtained target analogs were screened for in vitro antioxidant activity by various methods (H2 O2 , DPPH, ferrous reducing power, and nitric oxide), where they exhibit considerable radical scavenging activity. These compounds were also evaluated for inhibitory potency against NF-κB activation induced by LPS for the determination of their anti-inflammatory activity. The inhibition values indicate that the entire set of compounds efficiently inhibits the NF-κB activation provoked by LPS. Among the series, compound 5i was identified as the most potent inhibitor of NF-κB, with a relative NF-κB activity of 1.12 ± 0.53. It also inhibits various inflammatory mediators, such as TNF-α, IL-1β, IL-6, and PGE2 .
关于抗氧化剂和抗炎剂在肝纤维化患者中的作用，本研究通过两步反应中的高效合成方法开发了新型查尔酮衍生物 5a-i，该两步反应包括 Claisen-Schmidt 缩合。通过各种方法（H2O2、DPPH、亚铁还原力和一氧化氮）对获得的目标类似物进行体外抗氧化活性筛选，结果表明它们具有相当强的自由基清除活性。还评估了这些化合物抑制 LPS 诱导的 NF-κB 激活的抑制能力，以确定其抗炎活性。抑制值表明，整个化合物系列有效地抑制了 LPS 引起的 NF-κB 激活。在该系列中，化合物 5i 被鉴定为 NF-κB 最强的抑制剂，相对 NF-κB 活性为 1.12±0.53。它还抑制各种炎症介质，如 TNF-α、IL-1β、IL-6 和 PGE2。
