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Synthesis and biological evaluation of glucagon-like peptide-1 receptor agonists
Yu-Juan Zhang,Liu-Lan Shen,천혜경,Yongnan Xu,정진현 대한약학회 2014 Archives of Pharmacal Research Vol.37 No.5
In this study, a series of fused-heterocyclicderivatives were systematically designed and synthesizedusing an efficient route, and evaluated in terms of GLP-1Ragonist activity. We employed short synthetic steps andreactions that are tolerant of the presence of variousfunctional groups and suitable for parallel operations toenable the rapid generation of libraries of diverse andstructurally complex small molecules. Of the compoundssynthesized, 3-(8-chloro-6-(trifluoromethyl)imidazo[1,2-a]pyridin-2-yl)phenyl methanesulfonate (8e) was the mostpotent agonist with an EC50 of 7.89 lM, and thus is thecompound with the greatest potential for application. Thesefindings represent a valuable starting point for the designand discovery of small-molecule GLP-1R agonists that canbe administered orally.
Gadolinium- and lead-containing functional terpolymers for low energy X-ray protection
Yu-Juan Zhang,Xin-Tao Guo,Chun-Hong Wang,Xiang An Lu,De-Feng Wu,Ming Zhang 한국원자력학회 2021 Nuclear Engineering and Technology Vol.53 No.12
By polymerization of gadolinium methacrylate (Gd (MAA)3), lead methacrylate (Pb(MAA)2) and methylmethacrylate (MMA), Gd and Pb were chemically bonded into polymers. The X-ray shielding performance was evaluated by Monte Carlo simulation method, and the results showed that the more metalfunctional organic monomer, the better the shielding performance of terpolymers. When the X-rayenergy is 65 keV, Gd (MAA)3-containing polymers have better shielding performance than Pb(MAA)2-containing polymers. Gd could compensate for the weak absorption region of Pb. Therefore, polymerscontaining both Gd and Pb enhanced shielding efficiency against X-ray in various low-energy ranges. Forobtaining terpolymers with uniform monomer compositions, the relationship between the monomercomposition of the terpolymers and the conversion level was optimized by calculating the reactivityratios. The value of reactivity ratios of r (Gd (MAA)3/Pb(MAA)2), r (Pb(MAA)2/Gd (MAA)3), r (Gd (MAA)3/MMA), r (MMA/Gd (MAA)3), r (Pb(MAA)2/MMA) and r (MMA/Pb(MAA)2) was 0.483, 0.004, 0.338, 2.508,0.255, 0.029. The terpolymers with uniform monomer composition could be obtained by controlling themonomer compositions or conversion levels. The results can provide new radiation protection materialsand contribute to the improvement in nuclear safety.
Synthesis and biological evaluation of glucagon-like peptide-1 receptor agonists
Zhang, Yu-Juan,Shen, Liu-Lan,Cheon, Hyae-Gyeong,Xu, Yong-Nan,Jeong, Jin-Hyun 대한약학회 2014 Archives of Pharmacal Research Vol.37 No.5
In this study, a series of fused-heterocyclic derivatives were systematically designed and synthesized using an efficient route, and evaluated in terms of GLP-1R agonist activity. We employed short synthetic steps and reactions that are tolerant of the presence of various functional groups and suitable for parallel operations to enable the rapid generation of libraries of diverse and structurally complex small molecules. Of the compounds synthesized, 3-(8-chloro-6-(trifluoromethyl)imidazo[1,2-a] pyridin-2-yl)phenyl methanesulfonate (8e) was the most potent agonist with an $EC_{50}$ of $7.89{\mu}M$, and thus is the compound with the greatest potential for application. These findings represent a valuable starting point for the design and discovery of small-molecule GLP-1R agonists that can be administered orally.
( Jian Zhang ),( Xue Zhang ),( Li Zhang ),( Yu Juan Zhao ),( Chun Hua Niu ),( Zhen Nai Yang ),( Sheng Yu Li ) 한국미생물 · 생명공학회 2014 Journal of microbiology and biotechnology Vol.24 No.2
Total 121 lactic acid bacteria were isolated from homemade Inner Mongolia extra hard Hurood cheese. Seven of these strains, identified as Lactobacillus plantarum, were studied for probiotic characteristics. All seven strains survived at pH 3.0 for 3 h, or in the presence of oxgall at 0.3% or 0.6% for 4 h, but their viabilities were affected to different extents at pH 2.0 for 3 h. Strains C37 and C51 showed better adherence to Caco-2 cells, and higher hydrophobicity. The seven L. plantarum strains were different in in vitro free radical scavenging activities and cholesterolreducing ability. In vivo evaluation of the influence of L. plantarum C37 on the intestinal flora in a mouse model showed strain C37 could increase the viable counts of lactobacilli in feces of mice and decrease the viable counts of enterococci. When L. plantarum C37 was used to prepare probiotic Hurood cheese, it was able to maintain high viable counts (>7.8 log CFU/g) during the whole storage period, but the composition of the cheese was not changed. These results indicate that L. plantarum C37 could be considered as a promising probiotic strain.
Edaphovirga cremea gen. nov., sp. nov., isolated from the rhizospheric soil of Codonopsis clematidea
Jin-Yan Xue,Meng-Yue Zhang,Yu Zhang,Juan Cheng,Li-Cheng Liu,Ying-Ying Wu,Tian-Yuan Zhang,Yi-xuan Zhang 한국미생물학회 2019 The journal of microbiology Vol.57 No.5
A Gram-negative, facultatively anaerobic, non-motile, nonspore- forming, coccoid or rod-shaped and creamy-pigmented bacterium, designated SYP-B2100T, was isolated from the rhizospheric soil of Codonopsis clematidea in the Xinjiang Uygur Autonomous Region, China. The optimal growth occurred at 28°C, pH 5.0, in the absence of NaCl. The cells tested positive in catalase and methyl red tests but negative in oxidase, urease, gelatinase, milk coagulation, and peptonisation, H2S production, nitrate reduction, and Voges-Proskauer tests. The major isoprenoid quinone was ubiquinone-8 (Q-8). The major cellular fatty acids were C16:0 and summed feature 8. The polar lipids consisted of diphosphatidylglycerol, phosphatidylethanolamine, and phosphatidylglycerol. The 16S rRNA gene sequence of strain SYP-B2100T was the most similar to that of Rahnella inusitata DSM 30078T (96.9%) within the family Enterobacteriaceae. The genomic DNA G+C content of strain SYP-B2100T was 50.3 mol%. The combined data from the phylogenetic, morphological, physiological, biochemical, and chemotaxonomic analyses presented in this study support the conclusion that strain SYP-B2100T represents a novel species of a new genus, for which the name Edaphovirga cremea gen. nov., sp. nov. is proposed; the type strain is SYPB2100T (= CGMCC 1.5857T = DSM 105170T = KCTC 62024T).
Zhang Ji,Ding Juan,Yu Ming,Li Fang,Zhou Xue,Shuai Hongxia 한국유전학회 2021 Genes & Genomics Vol.43 No.12
Background Diabetic nephropathy (DN) is the leading cause of end-stage renal disease (ESRD) worldwide. Emerging evidence suggests that long non-coding RNAs (lncRNAs) play crucial roles in DN pathogenesis. Objective The purpose of the present study was to explore the role and mechanism of lncRNA tetratricopeptide repeat domain 2B antisense RNA 1 (TTC28-AS1) in DN. Methods Cell viability and apoptosis were assessed by the Cell Counting-8 Kit (CCK-8) assay and fow cytometry, respectively. The levels of TTC28-AS1, miR-320a and CD2-associated protein (CD2AP) were determined by quantitative real-time polymerase chain reaction (qRT-PCR) or western blot. The levels of interleukin-6 (IL-6), tumor necrosis factor-α (TNFα), and IL-8 were gauged by enzyme-linked immunosorbent assay (ELISA). Targeted relationship between miR-320a and TTC28-AS1 or CD2AP was evaluated by dual-luciferase reporter and RNA immunoprecipitation (RIP) assays. Results Our data indicated that high glucose (HG) induced HK-2 cell damage by the repression of cell viability and autophagy and the enhancement of cell apoptosis, fbrosis and pro-infammatory cytokines production. TTC28-AS1 was down-regulated and miR-320a was up-regulated in HG-induced HK-2 cells. TTC28-AS1 overexpression or miR-320a knockdown alleviated HG-induced damage in HK-2 cells. MiR-320 was a molecular mediator of TTC28-AS1 in regulating HG-induced HK-2 cell damage. Moreover, TTC28-AS1 functioned as a post-transcriptional regulator of CD2AP expression by miR-320a. MiR-320a knockdown relieved HG-induced damage in HK-2 cells by up-regulating CD2AP. Conclusions Our fndings suggest that TTC28-AS1 attenuates HG-induced damage in HK-2 cells at least partially by targeting the miR-320a/CD2AP axis, highlighting its role as a promising therapeutic approach for DN treatment.
Juan Du,Lei Liu,Yifeng Yu,Yue Zhang,Aibing Chen 한국공업화학회 2019 Journal of Industrial and Engineering Chemistry Vol.76 No.-
A self-assembly method using ionic liquids as soft-template and nitrogen precursor, resin as carbonprecursor, silica as assistant agent, mesoporous resin spheres as additive, is employed to prepare Ndopedcore–shell mesoporous sphere and carbon sheet composite (N-CMCS/CS). The obtained N-CMCS/CS possesses thin sheet, core–shell spheres, dual-mesoporous structure, large specific area and a certainof N-doping, which endows it with superior electrochemical performance as electrode material insupercapacitor.
Juan Deng,Lei Chen,Aisong Zhang,Meng Wang,Ling Gong,Wenjie Wang,Kun Yu,Bisheng Huang 한국식물학회 2023 Journal of Plant Biology Vol.66 No.2
Plant microRNAs (miRNAs) are short, non-coding RNA molecules. They mediate RNA silencing and regulate a series of target mRNAs involved in plant development, metabolism, and responses to different ecological environments. As one of important medicinal plants, Atractylodes lancea has a high medicinal significance and commercial value. Mao and Dabie are two ecotypes of A. lancea which mainly distributes in Mao Mountain and Dabie Mountain, respectively. To better understand the genomic information and germplasm resource characteristics, miRNA profiling analysis by high-throughput sequencing was performed to identify rhizome miRNAs of two A. lancea ecotypes. A transcriptomic database was established to identify miRNAs precursors and their target transcripts. By comparing small RNAs and the transcriptomic database, 270 known miRNAs of 46 miRNA families and 91 novel miRNAs were identified, plus hundreds of putative targets. Using Mireap software, 5 and 12 of 22 significant differentially expressed miRNAs were involved in ecotype formation and terpenoid metabolism, respectively, which was verified by qRT-PCR tests. These results are an important resource to better understand the biological mechanism of terpene formation and A. lancea adaptation to different ecological environment.