BPIC: A novel anti-tumor lead capable of inhibiting inflammation and scavenging free radicals

作者：Li Shan; Wang Yuji; Zhao Ming^*; Wu Jianhui; Peng Shiqi

来源：Bioorganic & Medicinal Chemistry Letters, 2015, 25(5): 1146-1150.

DOI：10.1016/j.bmcl.2014.12.013

• Docking
• Anti-tumor activity
• Anti-inflammation
• Free radical
• Lead

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-9H-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 mu mol/kg of dose BPIC effectively inhibited xylene-induced ear edema and decreased the plasma TNF-alpha and IL-8 of the mice. BPIC scavenged (OH)-O-center dot, O-center dot(2) and NO center dot 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.

• 出版日期2015-3-1
• 单位首都医科大学