TY - JOUR AU - Fang Fang AU - Wang Ai-ping AU - Yang Shi-fang PY - 2016 TI - Antitumor activity of a novel recombinant mutant human tumor necrosis factor-related apoptosis-inducing ligand JF - Acta Pharmacologica Sinica; Vol 26, No 11 (November 2005): Acta Pharmacologica Sinica Y2 - 2016 KW - N2 - Aim: To investigate the antitumor activity and safety of a novel recombinant mutant human tumor necrosis factor-related apoptosis-inducing ligand (rmh TRAIL). Methods: Antitumor activity of rmh TRAIL was evaluated by using several tumor cell lines by MTT assay in vitro , and by using a mouse xenograft model in vivo . rmh TRAIL-induced apoptosis in tumor cells was detected by cell death enzyme-linked immunosorbent assay (ELISA), TdT-mediated dUTP nick-end labeling (TUNEL) assay and flow cytometry. The safety of rmh TRAIL was also evaluated in several normal human cell lines. Results: At the concentration of 0.32–1000 ng/mL, rmh TRAIL remarkably inhibited the proliferation of 5 tumor cell lines from lung, colon, and breast cancer compared with wild type (wt TRAIL) in vitro , whereas at the concentration of 1 ng/mL-10 mug/mL, rmh TRAIL showed no or mild cytotoxicity in the normal cell lines. rmh TRAIL (3,15 mg/kg, ip, once daily for 10 d) exerted a significant inhibition on the growth of xenograft tumor NCI-H460 in nude mice compared with the saline group ( P Conclusion: rmh TRAIL provided potent antitumor activity in vivo and in vitro , whereas most normal human cells were resisitant to rmh TRAIL. The results suggested that rmh TRAIL might be a useful anticancer agent in future. UR - http://www.chinaphar.com/article/view/3935