Newly synthesized phenanthroimidazole derivatives L082 as a safe anti-tumor and anti-injury inflammation bifunctional compound

• Published in: European journal of pharmacology 2020-12, Vol.889, p.173571-173571, Article 173571
• Main Authors: Lai, Shi-Feng, Liu, Ruo-Tong, Peng, Wen-Hui, Huang, Xiao-Ting, Wang, Xi-Cheng, Qian, Jia-Yi, Mei, Wen-Jie, Cheng, Meng-Ya, Wang, Teng, Wang, Bao-Guo
• Format: Article
• Language: English
• Subjects: A549 Cells; Animals; Animals, Genetically Modified; Anti-Inflammatory Agents - chemical synthesis; Anti-Inflammatory Agents - pharmacology; Anti-Inflammatory Agents - therapeutic use; Anti-post-injury inflammatory complication; Anti-tumor; Antineoplastic Agents - chemical synthesis; Antineoplastic Agents - pharmacology; Antineoplastic Agents - therapeutic use; Dose-Response Relationship, Drug; HeLa Cells; Hep G2 Cells; Humans; Inflammation - drug therapy; Inflammation - metabolism; Inflammation - pathology; Liver Neoplasms, Experimental - drug therapy; Liver Neoplasms, Experimental - metabolism; Liver Neoplasms, Experimental - pathology; Oxidative Stress - drug effects; Oxidative Stress - physiology; Phenanthrenes - chemical synthesis; Phenanthrenes - pharmacology; Phenanthrenes - therapeutic use; Phenanthroimidazole derivatives; Zebrafish
• ISSN: 0014-2999; 1879-0712
• DOI: 10.1016/j.ejphar.2020.173571

Chemotherapy drugs exerts beneficial antitumor activity before and after cancer surgery. Post-injury complications are a potential hazard after surgical tumor resection. Inflammation caused by surgical stress is known to promote the progression of post-injury complications. Recent studies have found that chemotherapy drugs can promote post-injury inflammatory response, leading to increased post-injury complications. Imidazole derivatives have effective anticancer activity. However, the impact of post-operative inflammation caused by imidazole derivatives is unclear. In this study, two novel phenanthroimidazole derivatives (L082 and L142) were synthesized and characterized. These compounds showed significant inhibitory effects on different tumor cells. The compound L082 also inhibited liver cancer in vivo. In addition, L082 played a significant role in inhibiting the accumulation of inflammatory cells and promoting the elimination of inflammatory cells at the incision, which may be related to inhibiting the production of ROS and NO in oxidative and nitric stress. These results suggest that L082 can be used as a bifunctional drug to suppress tumors and reduce post-injury inflammation complications.