Synthesis and biological evaluation of hydantoin derivatives as potent antiplasmodial agents.

Malaria, a devastating disease, has claimed numerous lives and caused considerable suffering, with young children and pregnant women being the most severely affected group. However, the emergence of multidrug-resistant strains of Plasmodium and the adverse side effects associated with existing antimalarial drugs underscore the urgent need for the development of novel, well-tolerated, and more efficient drugs to combat this global health threat. To address these challenges, six new hydantoins derivatives were synthesized and evaluated for their in vitro antiplasmodial activity. Notably, compound 2c exhibited excellent inhibitory activity against the tested Pf3D7 strain, with an IC50 value of 3.97 ± 0.01 nM, three-fold better than chloroquine. Following closely, compound 3b demonstrated an IC50 value of 27.52 ± 3.37 µM against the Pf3D7 strain in vitro. Additionally, all the hydantoins derivatives tested showed inactive against human MCR-5 cells, with an IC50 value exceeding 100 µM. In summary, the hydantoin derivative 2c emerges as a promising candidate for further exploration as an antiplasmodial compound.

Effect of simvastatin on bone morphogenetic protein-2 expression in the periodontal tissue after rat tooth movement / 中华口腔医学杂志

<p><b>OBJECTIVE</b>To investigate the effect of systematic administration of simvastatin on the bone morphogenetic protein-2 (BMP-2) expression in the periodontal tissue after rat tooth movement and on the relapse of tooth movement.</p><p><b>METHODS</b>Orthodontic tooth movement of upper first molar was performed in 32 rats with coil spring for 21 days. The 32 rats were randomly allocated into 4 groups: negative control group (isotonic saline) and three experimental groups (2.5 mg x kg(-1), 5.0 mg x kg(-1) and 10.0 mg x kg(-1)). The simvastatin started to be administered to the experimental groups 1 day before appliances were removed, and once a day there after for 4 weeks. The negative control group received the isotonic saline only. The interdental distance between the first and second maxillary molars were measured, when appliances were removed, and 1 week and 4 weeks after that. After the rats were sacrificed, sections of first maxillary molar and periodontal tissue were studied by immunohistochemistry.</p><p><b>RESULTS</b>The number and percentage of relapse was lower in the three experimental groups than in the negative control group (P < 0.05, P < 0.01). The lower dose was given, the less relapse there was, with the lowerest dose resulting in lowest percentage of relapse (26.81% and 53.38%). BMP-2 expression in experimental groups was higher than in the negative control group, with the lowerest dose group showing the highest expression (P < 0.001). The BMP-2 expression on the tension side was slightly stronger than that on the compression side (P > 0.05).</p><p><b>CONCLUSIONS</b>Systemic administration of simvastatin could decrease the extent of relapse of the orthodontic-moved tooth in rat, and the lower-dose of simvastatin seemed more effective. The possible mechanism for this may be that simvastatin functions by increasing the expression of BMP-2 in the periodontal tissue, accelerating the osteoblast activity and promoting bone formation.</p>

Research of cranio-occlusional change of skeletal class III malocclusion in permanent dentition treated by the multiloop edgewise arch wire technique / 华西口腔医学杂志

<p><b>OBJECTIVE</b>To analyze the mechanics in correction of skeletal class III malocclusion with Multiloop Edgewise Arch Wire (MEAW).</p><p><b>METHODS</b>15 patients with skeletal class III malocclusion were treated with MEAW technique. Cephalometric analysis was performed with pre-treatment and post-treatment cephalograms. Paired t-test was conducted to assess the treatment effects.</p><p><b>RESULTS</b>L6-XI decreased by 2.87 mm, L6/MP increased by 8.60 degrees, L1-XI decreased by 2.60 mm, OP/MP increased by 2.33 degrees. Skeleton changed a little. There was no significant change in the soft tissue.</p><p><b>CONCLUSION</b>(1) Dento-alveolar compensation is the main change after the treatment by MEAW technique; (2) The improvement in molar relationship and overjet is achieved with upright and distal movement of the lower posterior teeth; (3) The lower anterior teeth moved lingually and protracted. Occlusal plane is flattened.</p>