ABSTRACT
Objective To screen 8 series of LY compounds, c-Met tyrosine kinase inhibitors, and evaluate their anti-tumor effects in vitro and in vivo. Methods Preliminary screening was carried out by detecting the c-Met kinase phosphor?ylation inhibition activity of the compounds. CCK-8 assay was adopted for secondary anti-tumor screen of the selected com?pounds using MKN-45, U87MG, Caki-1 and PC-3 cell lines in vitro. The transplanted tumor model of U87MG cells in nude mice was established to evaluate the antitumor activity in vivo. Results Four compounds (LY22, LY25, LY28 and LY32) with better activities were selected by HTRF method, in which LY28 had better inhibitory effect on c-Met than that of Crizo?tinib. The above active compounds showed different degrees of inhibition on the four kinds of target cells (MKN-45, U87MG, Caki-1 and PC-3) detected by CCK-8 method, and the inhibitory effect of LY28 showed the most obvious. Antitumor activi?ty in vivo showed that LY28 can significantly inhibited tumor growth in a dose-dependent manner. The tumor inhibitory rate in high-dose of LY28 was 78.13%. Conclusion The compound LY28 has good antitumor activity in vitro and in vivo, which will be a new tyrosine kinase inhibitor.
ABSTRACT
Objective To test the Footscan system for guiding the postoperative rehabilitation of calcaneus fractures.Methods Sixty patients with unilateral calcaneus fracture were divided randomly into a rehabilitation group and a control group.Patients in both groups began a routine of functional rehabilitation training 24 h after a reduction and fixation operation.The patients in the rehabilitation group received individualized rehabilitation protocols based on regular dynamic evaluation of their plantar pressure using the Footscan system.Those in the control group were administered routine rehabilitation training without the personal modifications.At the 2nd and 7th month postoperation,the dynamic plantar pressure of both groups was evaluated and the functioning of their feet Was scored.Results At the 2nd month post-operation,there was no significant difference between the two groups in terms of subtalar ioint range of motion,the lateral deviation of pressure center,the time of heel touch with the ground,the maximum pressure at the lateral aspect of the calcaneus and impulsive force during walking.The functional evaluation scores were also not significantly different.At the 7th month post-operation,all the indices in both groups had improved significantly over the 2nd month,bulthe improvement in the rehabilitation group Was greater(except the time of heel touch with the ground).Conclusion The Footscan system can be a valuable tool for evaluating patients with calcaneus fracture and serve as a reference for planning rehabilitation interventions for such patients.
ABSTRACT
Objective To evaluate the effects of post-operation rehabilitation treatment of patients with calcaneus fracture by dynamic plantar pressure analysis,and assess the value of the Footscan system.Methods Sixty-two patients with unilateral calcaneus fracture were randomly divided into a rehabilitation group and a control group.The patients in the rehabilitation group were given early,systemic standard rehabilitation treatment,while those in the control group took functional exercise following the doctors'advice.At 3 months and 6 months after operation,the plantar pressure distribution of the patients in both groups was analyzed with the Footscan system,respectively.Results After 3 months of treatment.there was statistically significant difference between the injured and the uninjured sides in both groups,with regard to the contact time,average plantar pressure and pressure-time integrals at different phases of gait.However,there was no significant difference between the injured and the uninjured sides after 6 months in rehabilitation group.But in control group,there was still statistically significant difference between the two sides with regard to the above parameters.Conclusion Early rehabilitation treatment could significantly improve the function outcome of patients with calcaneus fracture.Footscan System can objectively evaluate the recovery of the calcaneous fracture.