BPIC: A novel anti-tumor lead capable of inhibiting inflammation and scavenging free radicals. Issue 5 (1st March 2015)

• Record Type: Journal Article
• Authors: Li, Shan; Wang, Yuji; Zhao, Ming; Wu, Jianhui; Peng, Shiqi
• Is Part Of: Bioorganic & medicinal chemistry letters. Volume 25:Issue 5(2015)
• Page Start: 1146
• Page End: 1150
• Publication Date: 2015-03-01
• Subjects: Docking -- Anti-tumor activity -- Anti-inflammation -- Free radical -- Lead; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1016/j.bmcl.2014.12.013
• Languages: English
• ISSNs: 0960-894X

Abstract

Graphical abstract: Abstract: Inflammation has a critical role in the tumor progression, free radical damage can worse the status of patients in cancer condition. The anti-cancer agents capable of inhibiting inflammation and scavenging free radicals attract a lot of our interest. Aimed at the discovery of such anti-tumor agent, a novel intercalator, benzyl 1-[4-hydroxy-3-(methoxycarbonyl)-phenyl-9 H -pyrido[3, 4- b ]indole-3-carboxylate (BPIC) was presented. The docking investigation of BPIC and doxorubicin towards the DNA (PDB ID:1NAB ) gave equal score and similar feature. The anti-proliferation assay of 8 cancer cells identified S180 cells had equal sensitivity to BPIC and doxorubicin. The anti-tumor assay defined the efficacy of BPIC been 2 folds higher than that of doxorubicin. At 1 μmol/kg of dose BPIC effectively inhibited xylene-induced ear edema and decreased the plasma TNF-α and IL-8 of the mice. BPIC scavenged OH, O2 − and NO free radicals in a concentration dependent manner and NO free radicals had the highest sensitivity. BPIC could be a novel anti-tumor lead capable of simultaneously inhibiting inflammation and scavenging free radicals.