Biologically active indolizidine alkaloids.

Indolizidine alkaloids are chemical constituents isolated from various marine and terrestrial plants and animals, including but not limited to trees, fungi, ants, and frogs, with a myriad of important biological activities. In this review, we discuss the biological activity and pharmacological effects of indolizidine alkaloids and offer new avenues toward the discovery of new and better drugs based on these naturally occurring compounds.

A value-added application of eugenol as acaricidal agent: The mechanism of action and the safety evaluation.

Introduction: Eugenol is a major component of essential oils of several plants, it exhibits significant antiparasitic and acaricidal activities, yet its molecular targets remain unknown. Objectives: We aimed to systematically investigate the mechanism of action and the potential targets of eugenol against P. cuniculi, and evaluate the safety for laying the theoretical foundation for clinical application as an acaricide. Methods: Using RNA-Seq analysis, surface plasmon resonance analysis and RNA interference assay, the mode of action of eugenol against Psoroptes cuniculi was investigated. The effect on the mitochondrial membrane potential and complex I of PC12 cells and C6/36 cells was assayed to investigate the species specificity of eugenol in insects and mammals. Finally, a safety evaluation of eugenol in vivo was performed. Results: Eugenol inhibited complex I activity of the mitochondrial respiratory chain in the oxidative phosphorylation pathway by binding to NADH dehydrogenase chain 2 and resulted in the death of mites. The inhibition rates were 37.89% for 50 µg/mL and 60.26% for 100 µg/mL, respectively. Further experiments indicated that the difference in the complex I sequence between insects and mammals led to the different affinity of eugenol to specific peptide, resulting in species specificity. Eugenol exhibited significant inhibitory effects against the mitochondrial membrane potential and complex I in Aedes albopictus C6/36 cells but was not active in rat PC12 cells. Insect cells were particularly sensitive to eugenol. In contrast to the known inhibitor rotenone, eugenol had better safety and did not result in Parkinson's disease or other diseases in rats. Conclusion: This is the first report on acaricidal eugenol targeting complex I of the mitochondrial respiratory chain. This work lays the foundation for the development of eugenol as an environmentally alternative acaricidal agent.

Design and synthesis of novel 7-[(N-substituted-thioureidopiperazinyl)-methyl]-camptothecin derivatives as potential cytotoxic agents.

As part of continuing our research on diverse C-7 derivatives of camptothecin (CPT), 16 CPT derivatives bearing piperazinyl-thiourea chemical scaffold and different substituent groups have been designed, synthesized and evaluated in vitro for cytotoxicity against five tumor cell lines (A-549, MDA-MB-231, MCF-7, KB and KBvin). As a result, all the synthesized compounds showed promising in vitro cytotoxic activity against the five tumor cell lines tested, and were more potent than irinotecan. Importantly, compounds 13 g (IC50 = 0.514 µM) and 13o (IC50 = 0.275 µM) possessed similar or better antiproliferative activity against the multidrug-resistant (MDR) KBvin subline than that of topotecan (IC50 = 0.511 µM) and merit further development as anticancer candidates for clinical trail. With these results in hand, we have a reason to conclude that incorporating piperazinyl-thiourea motifs into position-7 of camptothecin confers well cytotoxic activity against cancer cell lines, probably resulting in new anticancer drugs.

Impact of rapid maxillary expansion in unilateral cleft lip and palate patients after secondary alveolar bone grafting: review and case report.

The purpose of this article was to analyze the effects and short-term stability of rapid maxillary expansion performed after secondary alveolar bone grafting in unilateral cleft lip and palate (UCLP) patients. Two UCLP patients with severe maxillary constriction who had previous bone grafting were involved in this study. A hyrax rapid expansion appliance was placed on 4 abutment teeth and activated twice daily. An opening of the midpalatal suture was found on the posttreatment occlusal radiographs, which was clinically confirmed by the diastema. Posteroanterior cephalometric tracing analysis demonstrated significant increases in maxillary and dental arch width. No obvious radiographic alteration was observed in the grafted areas.

[Bolton tooth-size discrepancy among different skeletal malocclusion groups].

PURPOSE: To evaluate the differences in tooth size ratios and distributions of Bolton anterior and overall ratios among different skeletal malocclusions. METHODS: 180 subjects were involved in this study, each malocclusion group consisted of 60 subjects(30 males and 30 females). The mesio-distal width from left first molar to right first molar was measured, Bolton anterior and overall ratios were calculated. Student's t test, ANOVA, LSD and chi2 test were performed for statistical analysis with SPSS15.0 software package. RESULTS: No statistically significant sex difference was found in anterior or overall ratio in any malocclusion. Significant difference was found for all ratios between skeletal Class III and skeletal Class I, so with skeletal Class II. No significant differences in all ratios between skeletal Class I and Class II were noted. Significant difference was found in the distribution of subjects with anterior and overall ratio discrepancies between skeletal Class III and skeletal Class II. CONCLUSIONS: The mean anterior and overall ratios for skeletal Class III malocclusions are significantly greater than those for skeletal Class I and Class II. The number of subjects with anterior ratio discrepancies for skeletal Class III malocclusions are larger than that for skeletal Class I and Class II malocclusion.

[Evaluations of self-perceived orthodontic treatment need using 2 different scales in adolescents].

PURPOSE: To evaluate the self-perceived dental aesthetics through visualized analogue scale (VAS) and aesthetic component (AC) of index of orthodontic treatment (IOTN) among adolescents in Shanghai area. METHODS: The investigation was carried out among 302 students (148 boys and 144 girls) aged 11-13 years. Self-perception of the dental aesthetic appearance was evaluated through VAS and AC. Additionally, the objective dental aesthetics were scored by orthodontists using AC and the actual dental attractiveness satisfaction was determined by a simple question. The data was analyzed using SPSS11.0 software package for Spearman correlation analysis. RESULTS: Generally, no statistically significant sex differences were found in relation to the VAS score and SAC degree (P > 0.05). No correlation was found between actual dental attractiveness satisfaction and self-perceived AC grade (r = 0.04. P = 0.441). However, statistically significant, positive, strong correlations were found between the actual dental attractiveness satisfaction and VAS score (r = 0.80, P = 0.000). And meaningful relation between the AC and VAS score was found. CONCLUSIONS: VAS showed high ability to predict the self-perceived dental aesthetics and act as a simple and useful tool, which can be used in further investigations.