Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 25, Issue 5, Pages 1146-1150Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2014.12.013
Keywords
Docking; Anti-tumor activity; Anti-inflammation; Free radical; Lead
Categories
Funding
- Beijing Municipal Science & Technology Commission [Z141100002114049]
- Project of Construction of Innovative Teams and Teacher Career Development for Universities and Colleges Under Beijing Municipality
- NSFC [81172930, 81270046, 81373265]
- Beijing Natural Science Foundation [7132032]
Ask authors/readers for more resources
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. (C) 2015 Elsevier Ltd. All rights reserved.
Authors
I am an author on this paper
Click your name to claim this paper and add it to your profile.
Reviews
Recommended
No Data Available