Bioactivity and structure-activity relationship of cinnamic acid derivatives and its heteroaromatic ring analogues as potential high-efficient acaricides against Psoroptes cuniculi.

A series of cinnamic acid derivatives and its heteroaromatic ring analogues were synthesized and evaluated for acaricidal activity in vitro against Psoroptes cuniculi, a mange mite. Among them, eight compounds showed the higher activity with median lethal concentrations (LC50) of 0.36-1.07mM (60.4-192.1µg/mL) and great potential for the development of novel acaricidal agent. Compound 40 showed both the lowest LC50 value of 0.36mM (60.4µg/mL) and the smallest median lethal time (LT50) of 2.6h at 4.5mM, comparable with ivermectin [LC50=0.28mM (247.4µg/mL), LT50=8.9h], an acaricidal drug standard. SAR analysis showed that the carbonyl group is crucial for the activity. The type and chain length of the alkoxy in the ester moiety and the steric hindrance near the ester group significantly influence the activity. The esters were more active than the corresponding thiol esters, amides, ketones or acids. Replacement of the phenyl group of cinnamic esters with α-pyridyl or α-furanyl significantly increase the activity. Thus, a series of cinnamic esters and its heteroaromatic ring analogues with excellent acaricidal activity emerged.

Cytotoxic activity, apoptosis induction and structure-activity relationship of 8-OR-2-aryl-3,4-dihydroisoquinolin-2-ium salts as promising anticancer agents.

As our continuing research, a series of 2-aryl-8-OR-3,4-dihydroisoquinolin-2-ium bromides were evaluated for cytotoxic activity on cancer cells and apoptosis induction in the present study. SAR was derived also. Among them, 23 compounds showed the higher cytotoxicity on MKN-45 cells with IC50 values of 1.99-11.3µM than a standard anticancer drug cis-platinum (IC50=11.4µM) or their natural model compound chelerythrine (IC50=12.7µM); 16 compounds possessed the medium to high activity on NB4 cells with IC50 values of 1.67-4.62µM. SAR analysis showed that both substitution patterns of the N-aromatic ring and the type of 8-OR significantly impact the activity. AO/EB staining and flow cytometry analysis with Annexin V/PI double staining showed that the compounds were able to induce apoptosis in a concentration-dependent manner. The results above suggested that the title compounds are a class of promising compounds for the development of new anti-cancer drugs.

A Laser-Based Measuring System for Online Quality Control of Car Engine Block.

For online quality control of car engine production, pneumatic measurement instrument plays an unshakeable role in measuring diameters inside engine block because of its portability and high-accuracy. To the limitation of its measuring principle, however, the working space between the pneumatic device and measured surface is too small to require manual operation. This lowers the measuring efficiency and becomes an obstacle to perform automatic measurement. In this article, a high-speed, automatic measuring system is proposed to take the place of pneumatic devices by using a laser-based measuring unit. The measuring unit is considered as a set of several measuring modules, where each of them acts like a single bore gauge and is made of four laser triangulation sensors (LTSs), which are installed on different positions and in opposite directions. The spatial relationship among these LTSs was calibrated before measurements. Sampling points from measured shaft holes can be collected by the measuring unit. A unified mathematical model was established for both calibration and measurement. Based on the established model, the relative pose between the measuring unit and measured workpiece does not impact the measuring accuracy. This frees the measuring unit from accurate positioning or adjustment, and makes it possible to realize fast and automatic measurement. The proposed system and method were finally validated by experiments.

A Fast and in-Situ Measuring Method Using Laser Triangulation Sensors for the Parameters of the Connecting Rod.

The connecting rod is a critical part inside the marine engine. The inspection of its important parameters is directly related to the assembly and quality of the marine engine. A coordinate measuring machine (CMM) is a conventional choice to measure the parameters of a connecting rod. However, CMM requires significant resources in time and cost, which leads researchers into in-situ measurement. This article presents a fast and in-situ measuring method by using a laser-based measuring head. Two measuring strategies are adopted in the inspection process. For positional measurements (such as the hole-center distance), whose accuracy requirement is generally low, the coordinate system of the numerical control (NC) machine is combined with the measuring head to acquire the positional parameters. For dimensional measurements (such as inner diameters), whose accuracy requirement is rather high, the NC machine is used just as transportation. Note that the measuring head has the ability to perform the dimension inspection independently. The accuracy of the measuring head is high enough to meet the dimensional accuracy requirements. Experiments are performed to validate the proposed method. The measuring error of the inner diameters is from 5 µm to 7 µm. The measuring error of hole-center distance is within 15 µm. The measurement of all these parameters can be done within 1 min.

[Clinical utilization of veiled incision and sternocleidomastoid flap in parotidectomy of parotid benign tumors].

PURPOSE: To describe a modified technique of parotidectomy using face-lift approach and sternocleidomastoid flap. METHODS: Forty-six patients were divided into two groups; group 1 (23 cases) using veiled incision and sternocleidomastoid flap, group 2 (23 cases) using traditional incision (Blair's approach) without sternocleidomastoid flap. Postoperative complications included temporary facial paralysis and salivary fistula. The follow-up period was 2 years, oncological recurrence was compared between the two groups. The incidence of Frey's syndrome and the feeling of the region around the auricular lobule were evaluated. The data was analyzed using SPSS10.0 software package with Student's t test and Chi-square test. RESULTS: During the follow up period, the patients in the group 1 showed better aesthetic results than those in the group 2 and without obvious scar and deformity. There was no significant difference between these two groups in temporary facial paralysis, salivary fistula, tumor recurrence, Frey's syndrome, the feeling of the region around the auricular lobule. CONCLUSION: The modified technique of parotidectomy using veiled incision and sternocleidomastoid flap greatly reduces the disadvantages of traditional parotidectomy and provides better aesthetic results.

[A clinical retrospective study on modified parotidectomy in benign tumors of parotid gland].

PURPOSE: A clinical perspective study was designed for patients undergoing a modified parotidectomy to reduce complications of parotidectomy. METHODS: 110 patients were divided randomly into two groups; Group 1 (55 cases) was operated via routine surgical modality. Group 2(55 cases) was treated with preserving the fascia parotideomasseterica and great auricular nerve and partial parotidectomy. Tumor size, blood loss, operating time, temporary facial paralysis, tumour recurrence were compared between the two groups. The follow-up period was 2 years. The incidence of Frey's syndrome was clinically evaluated by Minor test (starch-iodine test). The feeling of the region around the auricular lobule was also evaluated. The data were analyzed using SPSS10.0 software package for Student's t test and Chi-square test. RESULTS: There was no significant difference between the two groups in tumor size, temporary facial paralysis and tumor recurrence. Group 1 was significantly lower than that in Group 2 in the bleeding volume and operating time. The incidence rate of Frey's syndrome in Group 1 was significantly lower than that in Group 2 by objective observation and Minor test. There was significant difference between the feeling of pro- operation and pre-operation in the auricular lobule. CONCLUSIONS: The modified parotidectomy is a function-preserving surgery for benign parotid tumours, which improves the cosmetics, the feeling around ear, reduces the duration of surgery, and the incidence rate of Frey's syndrome. Supported by Research Fund of Science and Technology Bureau of Shanxi Province [Grant No.2005K14-G8(2)] and Science and Technology Project of Xi'an City [Grant No.SF08008-(4)].