GUO Kai, WANG Yilian, ZHOU Hongzi, CHEN Quan, CHEN Kai, LI Jishun, HU Jindong, YANG Hetong
The objective was to investigate the antitumor effect of F3-PE39KDEL in vitro and in vivo. MTT method was employed to determine the inhibiting effect of F3-PE39KDEL on MCF-7, A549, SKOV3 and HepG2 cell lines. Its toxicity in mice was observed using the median lethal dose method. Its antitumor effect was determined based on the transplanted A549 cell line in nude mice. The results showed that when the culture times were 72 h and 120 h, the F3-PE39KDEL showed significant inhibitory effect on A549 and MCF-7 cell lines, with IC50 values of 0.41 and 0.42 μg/mL, and 4.95 and 2.53 μg/mL, respectively. The toxicity test showed that the median lethal dose was 1.1782 mg/kg. The animals' spontaneous movement was decreased after administration, and animals died mainly within 1d after administration. All the animals including the dead and alive showed no abnormalities after sectional examination. The F3-PE39KDEL showed a potential antitumor effect in vivo. At the doses of 0.1, 0.2 and 0.4 mg/kg, its inhibitory rates were 37.0%, 43.2% and 53.1%, respectively, and the dose-activity relationship was also observed. These results suggest that the F3-PE39KDEL has good prospects in terms of targeted cancer therapy.