Synthesis of 8-Alkoxy-4,5-dihydro-[1,2,4]triazole[4,3-a]quinoline-1-ones and Evaluation of their Anticonvulsant Properties

Sun, Xian-Yu,Jin, Yun-Zhe,Li, Fu-Nan,Li, Gao,Chai, Kyu-Yun,Quan, Zhe-Shan The Pharmaceutical Society of Korea 2006 Archives of Pharmacal Research Vol.29 No.12

A series of 8-alkoxy-4,5-dihydro-[1,2,4]triazole[4,3-a]quinoline-1-one derivatives were synthesized using 7-hydroxy-3,4-dihydro-2(1H)-quinolone as the starting material. Their anticonvulsant activities were evaluated by the maximal electroshock test (MES) and the subcutaneous pentylenetetrazole test (sc-PTZ), and their neurotoxicities were measured by the rotarod neurotoxicity test (Tox). The tests demonstrated that 8-hexyloxy-4,5-dihydro-[1.2.4]triazole[4.3-a]quinoline-1-one (4e) and 8-heptyloxy-4,5-dihydro-[1,2,4]triazole[4, 3-a]quinoline-1-one (4f) were the most potent anticonvulsants, with 4e having $ED_{50}$ values of 17.17 mg/kg and 24.55 mg/kg and protective index ($PI=TD_{50}/ED_{50}$) values of 41.9 and 29.3 in the MES and sc-PTZ tests, respectively, and 4f having $ED_{50}$ values of 19.7 mg/kg and 21.2 mg/kg and PI values of 36.5 and 33.9 in the MES and sc-PTZ tests, respectively. The PI values of 4e and 4f were many fold better than that of the marketed drugs phenytoin, carbamazepine, phenobarbital and valproate, which have PI values in the range of 1.6-8.1 in the MES test and <0.22-5.2 in the sc-PTZ test. Structure-activity relationships were also discussed.

Synthesis of 8-Alkoxy-4,5-dihydro-[1,2,4]triazole[4,3-a]quinoline-1-ones and Evaluation of their Anticonvulsant Properties

Xian-Yu Sun,Yun-Zhe Jin,Fu-Nan Li,Gao Li,Kyu-Yun Chai,Zhe-Shan Quan 대한약학회 2006 Archives of Pharmacal Research Vol.29 No.12

A series of 8-alkoxy-4,5-dihydro-[1,2,4]triazole[4,3-a]quinoline-1-one derivatives were synthesized using 7-hydroxy-3,4-dihydro-2(1H)-quinolone as the starting material. Their anticonvulsant activities were evaluated by the maximal electroshock test (MES) and the subcutaneous pentylenetetrazole test (sc-PTZ), and their neurotoxicities were measured by the rotarod neurotoxicity test (Tox). The tests demonstrated that 8-hexyloxy-4,5-dihydro-[1.2.4]triazole[4.3- a]quinoline-1-one (4e) and 8-heptyloxy-4,5-dihydro-[1,2,4] triazole[4,3-a]quinoline-1-one (4f) were the most potent anticonvulsants, with 4e having ED50 values of 17.17 mg/kg and 24.55 mg/kg and protective index (PI = TD50/ED50) values of 41.9 and 29.3 in the MES and sc-PTZ tests, respectively, and 4f having ED50 values of 19.7 mg/kg and 21.2 mg/kg and PI values of 36.5 and 33.9 in the MES and sc-PTZ tests, respectively. The PI values of 4e and 4f were many fold better than that of the marketed drugs phenytoin, carbamazepine, phenobarbital and valproate, which have PI values in the range of 1.6-8.1 in the MES test and <0.22-5.2 in the sc-PTZ test. Structure-activity relationships were also discussed.

Investigation into performance enhancements of Li–S batteries via oxygen-containing functional groups on activated multi-walled carbon nanotubes using Fourier transform infrared spectroscopy

Yu Hai Wang,Zhe Dai,Chao Yue Zhang,Guo Wen Sun,Zhong Wei Lu,Xiu Ping Gao,Geng Zhi Sun,Wei Lan,Zhen Xing Zhang,Xiao Jun Pan,Jin Yuan Zhou 한국물리학회 2020 Current Applied Physics Vol.20 No.9

It was demonstrated that the electrochemical performance enhancements in KOH-activated carbon materials should be mainly due to the created polar oxygen-containing functional groups (OFGs, such as such as C–O, C–– O, –OH, and O–C–– O), while the role of each OFGs on the electrochemical enhancements is still unclear. In this work, KOH activation treatments were systematically conducted on carbon nanotubes (CNTs) to explore the role of each OFG on the performance enhancements of Li–S batteries (LSBs). Results showed that the capacity of activated-CNT-sulfur (a-CNT-S) cathodes is 33% higher than that of the pristine CNT-S cathodes, and their rate capability and cycling stability are also enhanced. And the electrochemical analysis combining with Fourier transform infrared spectroscopy indicated that the formed C–O bonds are the real factor for the enhanced electrochemical performances of a-CNT-S cathodes. Furthermore, the optimal activation conditions on CNTbased cathodes for LSBs were optimized to be 10 min at 700 ℃.

Sentiment analysis and product personalization - An emotional design approach to AI technology

Yu-Zhe Qi,Kie-Su Kim,Hong-Yan Ren,Xu Sun,Jiang-Yue Han,Xiang Zhang 한국콘텐츠학회 2023 한국콘텐츠학회 ICCC 논문집 Vol.2023 No.12

Comparison Different Methods of Intraoperative and Intraperitoneal Chemotherapy for Patients with Gastric Cancer: A Meta-analysis

Huang, Jin-Yu,Xu, Ying-Ying,Sun, Zhe,Zhu, Zhi,Song, Yong-Xi,Guo, Peng-Tao,You, Yi,Xu, Hui-Mian Asian Pacific Journal of Cancer Prevention 2012 Asian Pacific journal of cancer prevention Vol.13 No.9

Purpose: To investigate the efficacy and safety of intraperitoneal chemotherapy (IPC) for patients with gastric cancer and to compare effects between different regimens of IPC. Method: Randomized controlled trials comparing the effects of surgery plus intraperitoneal chemotherapy with surgery alone or comparing the efficacy between different regimens of intraperitoneal chemotherapy were searched for in Medline, Embase, Pubmed, the Cochrane Library and the Chinese BioMedical Disc and so on by two independent reviewers. After quality assessment and data extraction, data were pooled for meta-analysis using RevMan5.16 software. Tests of interaction were used to test for differences of effects among subgroups grouped according to different IPC regimens. Results: Fifteen RCTs with a total of 1713 patients with gastric cancer were included for quality assessment and data extraction. Ten studies were judged to be of fair quality and entered into meta-analysis. Hyperthermic intraoperative intraperitoneal chemotherapy (HR=0.60, P<0.01), hyperthermic intraoperative intraperitoneal chemotherapy plus postoperative intraperitoneal chemotherapy (HR=0.47, P<0.01) and normothermic intraoperative intraperitoneal chemotherapy (HR=0.70, P=0.01) were associated with a significant improvement in overall survival. Tests of interaction showed that hyperthermia and additional postoperative intraperitoneal chemotherapy did not impact on its effect. Further analysis revealed that intraperitoneal chemotherapy remarkably decrease the rate of postoperative hepatic metastasis by 73% (OR=0.27, 95% CI=0.12 to 0.67, P<0.01). However, intraperitoneal chemotherapy increased risks of marrow depression (OR=5.74, P<0.01), fever (OR=3.67, P=0.02) and intra-abdominal abscess (OR=3.57, P<0.01). Conclusion: The present meta-analysis demonstrates that hyperthermic intraoperative intraperitoneal chemotherapy and normothermic intraoperative intraperitoneal chemotherapy should be recommended to treat patients with gastric cancer because of improvement in overall survival. However, it is noteworthy that intraperitoneal chemotherapy can increase the risks of marrow depression, intra-abdominal abscesses, and fever.

Selection signature reveals genes associated with susceptibility loci affecting respiratory disease due to pleiotropic and hitchhiking effect in Chinese indigenous pigs

Xu, Zhong,Sun, Hao,Zhang, Zhe,Zhang, Cheng-Yue,Zhao, Qing-bo,Xiao, Qian,Olasege, Babatunde Shittu,Ma, Pei-Pei,Zhang, Xiang-Zhe,Wang, Qi-Shan,Pan, Yu-Chun Asian Australasian Association of Animal Productio 2020 Animal Bioscience Vol.33 No.2

Objective: Porcine respiratory disease is one of the most important health problems causing significant economic losses. To understand the genetic basis for susceptibility to swine enzootic pneumonia (EP) in pigs, we detected 102,809 single nucleotide polymorphisms in a total of 249 individuals based on genome-wide sequencing data. Methods: Genome comparison of susceptibility to swine EP in three pig breeds (Jinhua, Erhualian, and Meishan) with two western lines that are considered more resistant (Duroc and Landrace) using cross-population extended haplotype homozygosity and F-statistic (F_ST) statistical approaches identified 691 positively selected genes. Based on quantitative trait loci, gene ontology terms and literature search, we selected 14 candidate genes that have convincible biological functions associated with swine EP or human asthma. Results: Most of these genes were tested by several methods including transcription analysis and candidate genes association study. Among these genes: cytochrome P450 1A1 and catenin beta 1 (CTNNB1) are involved in fertility; transforming growth factor beta receptor 3 plays a role in meat quality traits; Wnt family member 2, CTNNB1 and transcription factor 7 take part in adipogenesis and fat deposition simultaneously; plasminogen activator, urokinase receptor (completely linked to AXL receptor tyrosine kinase, r² = 1) plays an essential role in the successful ovulation of matured oocytes in pigs; colipase like 2 (strongly linked to SAM pointed domain containing ETS transcription factor, r² = 0.848) is involved in male fertility. Conclusion: These adverse genes susceptible to swine EP may be selected while selecting for economic traits (especially reproduction traits) due to pleiotropic and hitchhiking effect of linked genes. Our study provided a completely new point of view to understand the genetic basis for susceptibility or resistance to swine EP in pigs thereby, provides insight for designing sustainable breed selection programs. Finally, the candidate genes are crucial due to their potential roles in respiratory diseases in a large number of species, including human.

A quick, accurate and general ultra performance liquid chromatography method for evaluating the quality of enological tannins

Wei Chao Yu,Zhe Li,Bao Shan Sun,Yan Cui 한국식품과학회 2020 Food Science and Biotechnology Vol.29 No.8

Commercial enological tannins from variousorigins have been widely used in modern wine making. Inorder to investigate the diverse quality of tannin products, aquick, accurate and simple UPLC method was developed,which could simultaneously determine 11 principle characteristiccomponents of hydrolysable tannins and condensedtannins. The optimum resolution of the tannins wasachieved on a Waters Acquity UPLC-BEH C18 column(2.1 mm 9 50 mm, 1.7 lm) at 280 nm with gradient elution. The method was validated to achieve desired specificity,linearity, precision, accuracy and stability. Thedeveloped method was successfully applied to 30 commercialenological tannins from different origins for theirquality evaluation. The 30 tannin samples were qualitativelydistinguished into hydrolysable, condensed or mixturetannins, and quantificationally classified into fourlevels of excellent, good, fair and poor products. Themethod could be used for quick evaluating the quality ofenological tannins in practical use.

Influence of Transformation-induced Plasticity on Formability of TRIP Steels

Hai Yan Yu,Shi Jin Yuan,Zhe Sun 한국소성가공학회 2011 기타자료 Vol.2011 No.8

A micromechanical flow stress model for the transformation-induced plasticity (TRIP) steel is proposed on the basis of continuum mechanics. In the model, TRIP effect and degradation of elastic modulus are considered. TRIP effect is introduced by regarding the volume fraction of retained austenites as varying with plastic strain. Degradation of elastic modulus is evaluated by an empirical expression. Both the contribution of individual phases and that of interaction between constituent phases to the overall stress are taken into account. The proposed model is introduced into LSDYNA software to simulate the cup forming and U-channel springback. Cup drawing and U-channel bending experiments are provided. Comparison shows that formability results simulated with TRIP effect are closer to the experimental ones.

태권도 수련생의 참여동기가 운동지속에 미치는 영향에서 만족도의 매개효과

유원등(Won-Deung Yu),추취센(Zhe-Sen Chu),장선미(Sun-Mi Jang),정영주(Young-Joo Jung),김용재(Yong-Jae Kim) 한국자료분석학회 2018 Journal of the Korean Data Analysis Society Vol.20 No.1

이 연구의 목적은 태권도 수련생의 참여동기가 운동지속에 미치는 영향에서 만족도의 매개효과를 규명하여 이를 통해 태권도 활성화 방안을 위한 기초 자료를 제공하는데 있다. 이러한 목적을 달성하기 위하여 2017년 11월부터 2017년 12월까지 태권도 수련생 373명 대상으로 실시한 설문조사를 통해 매개효과 검증을 위하여 3단계 회귀분석을 사용하였으며, Sobel의 검증 공식을 사용하여 통계적 유의성 검증 분석하여 다음과 같은 결론을 얻었다. 태권도 수련생의 참여동기가 만족도에 미치는 영향에서 참여동기 하위요인은 사교로 나타났다. 태권도 수련생의 참여동기가 운동지속에 미치는 영향에서 운동능력은 즐거움, 성취감, 외적과시, 운동습관은 사교, 건강체력, 외적과시, 운동환경은 기술발달, 외적과시로 나타났으며, 운동관심은 성취감, 사교, 외적과시로 나타났으며, 운동친구는 성취감, 컨디션, 사교로 나타났다. 태권도 수련생의 참여동기와 만족도가 운동지속에 미치는 영향에서 운동능력은 즐거움, 성취감, 외적과시, 만족도, 운동습관, 운동환경은 외적과시, 만족도로 나타났으며, 운동관심은 성취감, 만족도, 운동친구는 성취감, 컨디션, 사교, 만족도로 나타났다. 참여동기 중 사교가 운동친구에서 미치는 영향에서 만족도는 부분매개 역할을 통계적으로 유의하게 하는 것으로 나타났다. The purpose of this study is to clearly identify the mediating effect of satisfaction on the participation motivation of Taekwondo practitioners in terms of the duration and persistence of exercise and to provide basic data about practical and effective ways of utilizing Taekwondo. In order to achieve this goal, a three-step regression analysis was used to verify the mediating effects through a survey of the 373 Taekwondo practitioners from November 2017 to December 2017. Using Sobel s verification formula, the mediating effects were found to be statistically significant, resulting in the following conclusion. In terms of the influence of the motivation to participate on the continuity of practice among Taekwondo practioners, socialization was found to have a statistically significant influence as a mediating effect on satisfaction among the different motivations to participate.

Ginsengenin derivatives synthesized from 20(R)-panaxotriol: Synthesis, characterization, and antitumor activity targeting HIF-1 pathway

Guo, Hong-Yan,Xing, Yue,Sun, Yu-Qiao,Liu, Can,Xu, Qian,Shang, Fan-Fan,Zhang, Run-Hui,Jin, Xue-Jun,Chen, Fener,Lee, Jung Joon,Kang, Dongzhou,Shen, Qing-Kun,Quan, Zhe-Shan The Korean Society of Ginseng 2022 Journal of Ginseng Research Vol.46 No.6

Background: Ginseng possesses antitumor effects, and ginsenosides are considered to be one of its main active chemical components. Ginsenosides can further be hydrolyzed to generate secondary saponins, and 20(R)-panaxotriol is an important sapogenin of ginsenosides. We aimed to synthesize a new ginsengenin derivative from 20(R)-panaxotriol and investigate its antitumor activity in vivo and in vitro. Methods: Here, 20(R)-panaxotriol was selected as a precursor and was modified into its derivatives. The new products were characterized by ¹H-NMR, ¹³C-NMR and HR-MS and evaluated by molecular docking, MTT, luciferase reporter assay, western blotting, immunofluorescent staining, colony formation assay, EdU labeling and immunofluorescence, apoptosis assay, cells migration assay, transwell assay and in vivo antitumor activity assay. Results: The derivative with the best antitumor activity was identified as 6,12-dihydroxy-4,4,8,10,14-pentamethyl-17-(2,6,6-trimethyltetrahydro-2H-pyran-2-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl(tert-butoxycarbonyl)glycinate (A11). The focus of this research was on the antitumor activity of the derivatives. The efficacy of the derivative A11 (IC₅₀ < 0.3 µM) was more than 100 times higher than that of 20(R)- panaxotriol (IC₅₀ > 30 µM). In addition, A11 inhibited the protein expression and nuclear accumulation of the hypoxia-inducible factor HIF-1α in HeLa cells under hypoxic conditions in a dose-dependent manner. Moreover, A11 dose-dependently inhibited the proliferation, migration, and invasion of HeLa cells, while promoting their apoptosis. Notably, the inhibition by A11 was more significant than that by 20(R)-panaxotriol (p < 0.01) in vivo. Conclusion: To our knowledge, this is the first study to report the production of derivative A11 from 20(R)-panaxotriol and its superior antitumor activity compared to its precursor. Moreover, derivative A11 can be used to further study and develop novel antitumor drugs.