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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.
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.
( 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).
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.
An Effective Framework for Contented-Based Image Retrieval with Multi-Instance Learning Techniques
Yu Peng,Kun-Juan Wei,Da-Li Zhang 대한전자공학회 2007 JUCT : Journal of Ubiquitous Convergence Technolog Vol.1 No.1
Multi-Instance Learning(MIL) performs well to deal with inherently ambiguity of images in multimedia retrieval. In this paper, an effective framework for Contented-Based Image Retrieval(CBIR) with MIL techniques is proposed, the effective mechanism is based on the image segmentation employing improved Mean Shift algorithm, and processes the segmentation results utilizing mathematical morphology, where the goal is to detect the semantic concepts contained in the query. Every sub-image detected is represented as a multiple features vector which is regarded as an instance. Each image is produced to a bag comprised of a flexible number of instances. And we apply a few number of MIL algorithms in this framework to perform the retrieval. Extensive experimental results illustrate the excellent performance in comparison with the existing methods of CBIR with MIL.
Yu, Xizhong,Ye, Lifang,Zhang, Hao,Zhao, Juan,Wang, Guoqiang,Guo, Chao,Shang, Wenbin The Korean Society of Ginseng 2015 Journal of Ginseng Research Vol.39 No.3
Background: Ginsenoside Rb1 (G-Rb1), the major active constituent of ginseng, improves insulin sensitivity and exerts antidiabetic effects. We tested whether the insulin-sensitizing and antidiabetic effects of G-Rb1 results from a reduction in ectopic fat accumulation, mediated by inhibition of lipolysis in adipocytes. Methods: Obese and diabetic db/db mice were treated with daily doses of 20 mg/kg G-Rb1 for 14 days. Hepatic fat accumulation was evaluated by measuring liver weight and triglyceride content. Levels of blood glucose and serum insulin were used to evaluate insulin sensitivity in db/db mice. Lipolysis in adipocytes was evaluated by measuring plasma-free fatty acids and glycerol release from 3T3-L1 adipocytes treated with G-Rb1. The expression of relevant genes was analyzed by western blotting, quantitative real-time polymerase chain reaction, and enzyme-linked immunosorbent assay kit. Results: G-Rb1 increased insulin sensitivity and alleviated hepatic fat accumulation in obese diabetic db/db mice, and these effects were accompanied by reduced liver weight and hepatic triglyceride content. Furthermore, G-Rb1 lowered the levels of free fatty acids in obese mice, which may contribute to a decline in hepatic lipid accumulation. Corresponding to these results, G-Rb1 significantly suppressed lipolysis in 3T3-L1 adipocytes and upregulated the perilipin expression in both 3T3-L1 adipocytes and mouse epididymal fat pads. Moreover, G-Rb1 increased the level of adiponectin and reduced that of tumor necrosis factor-${\alpha}$ in obese mice, and these effects were confirmed in 3T3-L1 adipocytes. Conclusion: G-Rb1 may improve insulin sensitivity in obese and diabetic db/db mice by reducing hepatic fat accumulation and suppressing adipocyte lipolysis; these effects may be mediated via the upregulation of perilipin expression in adipocytes.