Synthesis and anticonvulsant activity evaluation of 8-alkoxy-5-(4H-1,2,4-triazol-4-yl)quinoline derivatives

Shi-Ben Wang,Xian-Qing Deng,Yan Zheng,Hong-Jian Zhang,Zhe-Shan Quan 대한약학회 2013 Archives of Pharmacal Research Vol.36 No.1

Two series of 8-alkoxy-5-(4H-1,2,4-triazol-4-yl)quinolines and 8-alkoxy-5-(2H-1,2,4-triazol-3-one-4-yl)quinolineswere synthesized.The anticonvulsant activity ofthese compounds was evaluated with maximal electroshockseizure test and rotarod test. Among the synthesized compounds,8-octoxy-5-(4H-1,2,4-triazol-4-yl)quinoline (4g)was the most active compound with ED50 of 8.80 mg/kg,TD50 of 176.03 mg/kg and protective index of 20.0. Itsneurotoxicity was lower than all other synthesized compoundsand also markedly lower than that of the referencedrug carbamazepine. In addition, the potency of compound 4gagainst seizures induced by pentylenetetrazole, 3-mercaptopropionicacid, and bicuculline suggested its broad spectrumactivity, and the mechanisms of action including inhibition ofvoltage-gated ion channels and modulation of GABAergicactivity might involve in its anticonvulsant activity.

Sensitivity of Plasmodium falciparum to Antimalarial Drugs in Hainan Island, China

Shan-Qing Wang,Guang-Ze Wang,Yu-Chun Li,Feng Meng,Shi-Gan Lin,Zhen-Hu Zhu,Ding-Wei Sun,Chang-Hua He,Xi-Min Hu,Jian-Wei Du 대한기생충학열대의학회 2015 The Korean Journal of Parasitology Vol.53 No.1

miR-126 Suppresses the Proliferation of Cervical Cancer Cells and Alters Cell Sensitivity to the Chemotherapeutic Drug Bleomycin

Yu, Qing,Liu, Shan-Ling,Wang, He,Shi, Gang,Yang, Pei,Chen, Xin-Lian Asian Pacific Journal of Cancer Prevention 2013 Asian Pacific journal of cancer prevention Vol.14 No.11

In cervical cancer, one of the most common malignant tumors in women worldwide, miR-126 has been reported to exhibit decreased expression. However, its role in cervical cancer cell proliferation and drug sensitivity has remained relatively unexplored. Here, we compared the expression of miR-126 in cervical cancer tissues (n = 20) with that in normal cervical tissue (n = 20) using quantitative RT-PCR. The viability of Siha cervical cancer cells was further measured by MTT assay after transfection with miR-126 mimic (Siha-miR-126 mimic) or microRNA mimic negative control (Siha-miR mimic NC) and after treatment with various concentrations of bleomycin (BLM). IC50s were calculated, and the survival rates (SRs) of Siha cells were calculated. miR-126 expression in cervical cancer tissue was significantly decreased compared with that in normal cervical tissue (P < 0.01). The relative SRs of Siha-miR-126 mimic cells were also significantly decreased compared with those of Siha-miR mimic NC cells at 24-96 h after transfection. The IC50 of BLM in Siha-miR-126 mimic cells ($50.3{\pm}2.02{\mu}g/mL$) was decreased compared with that in Siha-miR mimic NC cells ($70.5{\pm}4.33{\mu}g/mL$) at 48 h after transfection (P < 0.05). Finally, the SRs of Siha-miR-126 mimic cells were significantly lower than those of SihamiR mimic NC cells after cultured in medium containing 40 ${\mu}g/mL$ BLM for 24-96 h (P < 0.05). These results suggest that miR-126 is expressed at low levels in cervical cancer. Upregulation of miR-126 inhibited cervical cancer cell proliferation and enhanced the sensitivity to BLM. Thus, miR-126 may represent a novel approach to cervical cancer treatment.

Diagnostic value of Thyroglobulin Measurement with Fine-needle Aspiration Biopsy for Lymph Node Metastases in Patients with a History of Differentiated Thyroid Cancer

Zhang, Hai-Shan,Wang, Ren-Jie,Fu, Qing-Feng,Gao, Shi,Sun, Bu-Tong,Sun, Hui,Ma, Qing-Jie Asian Pacific Journal of Cancer Prevention 2014 Asian Pacific journal of cancer prevention Vol.15 No.24

Purpose: The aim of this study was to evaluate the diagnostic value of FNA-Tg for detecting lymph node metastases in patients with a history of differentiated thyroid cancer (DTC). Materials and Methods: A total of 58 patients with DTC diagnosis and evidence of single or multiple suspicious cervical lymph nodes were assessed. All underwent total or near-total thyroidectomy with (35 cases) or without (23 cases) radioiodine (RAI) ablation, followed by thyroid stimulating hormone (TSH) suppression therapy. A total of 68 lymph nodes were examined by ultrasound-guided fine needle aspiration (US-FNA) for both cytological examination and FNA-Tg measurement. Serum Tg and anti-thyroglobulin antibody (TgAb) levels were also measured. Diagnostic performance including sensitivity, specificity, accuracy, positive (PPV) and negative predictive value (NPV) of FNAC and FNA-Tg were calculated and compared. The Spearman's rank correlation coefficient was used to estimate the relationship between FNA-Tg and serum TgAb. Results: The FNA-Tg levels were significantly higher with DTC metastatic lymph nodes (median 927.7 ng/mL, interquartile range 602.9 ng/mL) than non-metastatic lymph nodes (median 0.1 ng/mL, interquartile range 0.4 ng/mL) (p<0.01). Considering 1.0 ng/mL as a threshold value for FNA-Tg, the sensitivity, specificity, accuracy, PPV and NPV of FNA-Tg were 95.7%, 95.5%, 95.6%, 97.8% and 91.3%, respectively. The sensitivity and accuracy of the combination of FNAC and FNA-Tg were significantly higher than that of FNAC alone (p<0.05). The diagnostic performance of FNA-Tg was not significantly different between cases with or without RAI ablation, and the serum TgAb levels did not interfere with FNA-Tg measurements. Conclusions: Measurement of FNA-Tg is useful. The combination of FNAC and FNA-Tg is more sensitive and accurate for detecting lymph node metastases in patients with a history of DTC than FNAC alone. Serum TgAbs appear to be irrelevant for measurement of FNA-Tg.

Prevalence and Subtypes of Blastocystis in Alpacas, Vicugna pacos in Shanxi Province, China

Ye-Ting Ma,Qing Liu,Shi-Chen Xie,Xiao-Dong Li,Yuan-Yuan Ma,Tao-Shan Li,Wen-Wei Gao,Xing-Quan Zhu 대한기생충학ㆍ열대의학회 2020 The Korean Journal of Parasitology Vol.58 No.2

Blastocystis, an enteric protist, has been reported to be an important cause of protozoal gastrointestinal manifestations in humans and animals worldwide. Animals harboring certain Blastocystis subtypes (STs) may serve as a potential source of human infection. However, information about the prevalence and genetic diversity of Blastocystis in alpacas is limited. In the present study, a total of 366 fecal samples from alpacas in Shanxi Province, northern China, were examined for Blastocystis by PCR amplification of the small subunit rRNA gene, followed by sequencing and phylogenetic analysis. The prevalence of Blastocystis in alpacas was 23.8%, and gender difference in the prevalence of Blastocystis was observed. The most predominant Blastocystis ST was ST10, followed by ST14 and ST5. The detection of ST5, a potentially zoonotic genotype, indicates that alpacas harboring ST5 could be a potential source of human infection with Blastocystis. These data provide new insight into the prevalence and genetic diversity of Blastocystis in alpacas.

Analysis on Response Prediction of a Single Pile and Pile Groups Based on the Runge-Kutta Method

Dong-dong Pan,Qian-qing Zhang,Shan-wei Liu,Shi-min Zhang 대한토목학회 2018 KSCE JOURNAL OF CIVIL ENGINEERING Vol.22 No.1

The conventional load-transfer approach can not consider the interaction of piles, and can not be directly used in the analysis of the response of pile groups. The interactive effects among piles can be taken into account in the shear displacement method based on the principle of superposition. In the present analysis, the shaft displacement of a single pile at a given depth is assumed to be composed of the pile-soil relative displacement developed at the disturbed soil around pile and the elastic vertical soil displacement developed in the soil mass. A new load-transfer function which is very similar to a hyperbolic model is then established to describe the relationship between unit skin friction and shaft displacement at a given depth. Furthermore, a hyperbolic model is used to simulate the relationship between unit end resistance and pile end displacement. As to the analysis of the response of pile groups, the interactive effects among piles are considered by using the shear displacement method. For an individual pile in pile groups, new load-transfer functions are established to capture the relationship between unit skin friction and shaft displacement and the relationship between end resistance and pile end displacement. Based on the fourth order Runge-Kutta method, a modified loadtransfer method is proposed to analyze the response of pile groups considering the interactive effects among piles. The reliability of the present method is checked by using comparisons of the present calculated results, the measured results and the computed values derived from other methods.

Correlation between Intravoxel Incoherent Motion Magnetic Resonance Imaging Derived Metrics and Serum Soluble CD40 Ligand Level in an Embolic Canine Stroke Model

Xiao-Quan Xu,Chen-Jiang Wu,Shan-Shan Lu,Qian-Qian Gao,Qing-Quan Zu,Xing-Long Liu,Hai-Bin Shi,Sheng Liu 대한영상의학회 2017 Korean Journal of Radiology Vol.18 No.5

Objective: To determine the relationship between intravoxel incoherent motion (IVIM) imaging derived quantitative metrics and serum soluble CD40 ligand (sCD40L) level in an embolic canine stroke model. Materials and Methods: A middle cerebral artery occlusion model was established in 24 beagle dogs. Experimental dogs were divided into low- and high-sCD40L group according to serum sCD40L level at 4.5 hours after establishing the model. IVIM imaging was scanned at 4.5 hours after model establishment using 10 b values ranging from 0 to 900 s/mm2. Quantitative metrics diffusion coefficient (D), pseudodiffusion coefficient (D*), and perfusion fraction (f) of ischemic lesions were calculated. Quantitative metrics of ischemic lesions were normalized by contralateral hemisphere using the following formula: normalized D = Dstroke / Dcontralateral. Differences in IVIM metrics between the low- and high-sCD40L groups were compared using t test. Pearson’s correlation analyses were performed to determine the relationship between IVIM metrics and serum sCD40L level. Results: The high-sCD40L group showed significantly lower f and normalized f values than the low-sCD40L group (f, p < 0.001; normalized f, p < 0.001). There was no significant difference in D*, normalized D*, D, or normalized D value between the two groups (All p > 0.05). Both f and normalized f values were negatively correlated with serum sCD40L level (f, r = -0.789, p < 0.001; normalized f, r = -0.823, p < 0.001). However, serum sCD40L level had no significant correlation with D*, normalized D*, D, or normalized D (All p > 0.05). Conclusion: The f value derived from IVIM imaging was negatively correlated with serum sCD40L level. f value might serve as a potential imaging biomarker to assess the formation of microvascular thrombosis in hyperacute period of ischemic stroke.

Dynamic behavior analysis of push-the-bit rotary steerable bottom hole assembly

Zhi-chuan Guan,Heng Wang,Yu-cai Shi,Wei-qing Chen,Guo-shan Zhao,Jian-yun Wang,Guang-qiang Cao 대한기계학회 2019 JOURNAL OF MECHANICAL SCIENCE AND TECHNOLOGY Vol.33 No.4

Rotary steerable drilling technology is currently an advanced technology in the field of drilling engineering. A good understanding of dynamic behavior of rotary steerable system will benefit the drilling progress. Aimed at push-the-bit type of rotary steerable tool, finite element method was employed to model the rotary steerable bottom hole assembly (RSBHA) and establish the motion equation. Contact interaction between drill string and wellbore wall was analyzed and taken as the constraint condition in solving RSBHA motion equation. Force applied by steering pads was as the external force acting at the pads node. Then RSBHA motion state and bit lateral force were obtained by using Newmark method to solve the motion equation. A case was given and effects of influencing factors were analyzed. The results show that stick-slip phenomenon occurs under 60 r/min rotary speed condition and disappears when rotary speed rises to 90 r/min. Fully developed backward whirl comes into being at the near-bit stabilizer when rotary speed increases to 120 r/min. High weight on bit intensifies bit torsional vibration while larger pads’ steering force decreases the bit torsional vibration. Upper stabilizer plays a part in weakening RSBHA backward whirl under high rotary speed condition but reduces the inclination force. Time average of bit lateral force is mainly determined by pads’ steering force. Based on the results, corresponding suggestions were proposed to make the RSBHA be better used in the field applications.

Effects of Nutritional and Environmental Conditions on Planktonic Growth and Biofilm Formation of Citrobacter werkmanii BF-6

( Gang Zhou ),( Long Jie Li ),( Qing Shan Shi ),( You Sheng Ouyang ),( Yi Ben Chen ),( Wen Feng Hu ) 한국미생물 · 생명공학회 2013 Journal of microbiology and biotechnology Vol.23 No.12

Citrobacter sp. is a cause of significant opportunistic nosocomial infection and is frequently found in human and animal feces, soil, and sewage water, and even in industrial waste or putrefaction. Biofilm formation is an important virulence trait of Citrobacter sp. pathogens but the process and characteristics of this formation are unclear. Therefore, we employed in vitro assays to study the nutritional and environmental parameters that might influence biofilm formation of C. werkmanii BF-6 using 96-well microtiter plates. In addition, we detected the relative transcript levels of biofilm formation genes by RT-PCR. Our results indicated that the capacity of C. werkmanii BF-6 to form biofilms was affected by culture temperature, media, time, pH, and the osmotic agents glucose, sucrose, NaCl, and KCl. Confocal laser scanning microscopy results illustrated that the structure of biofilms and extracellular polysaccharide was influenced by 100 mM NaCl or 100 mM KCl. In addition, nine biofilm formation genes (bsmA, bssR, bssS, csgD, csgE, csgF, mrkA, mrkB, and mrkE) were found to contribute to planktonic and biofilm growth. Our data suggest that biofilm formation by C. werkmanii BF-6 is affected by nutritional and environmental factors, which could pave the way to the prevention and elimination of biofilm formation using proper strategies.