CAS: 27215-14-1; 3-(2-((1R,4As,5R,8As)-5,8A-Dimethyl-2-Methylene-5-((((2R,3R,4S,5S,6R)-3,4,5-Trihydroxy-6-(Hydroxymethyl)Tetrahydro-2H-Pyran-2-yl)Oxy)Methyl)Decahydronaphthalen-1-yl)Ethyl)Furan-2(5H)-One

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CAS号82209-74-3 新穿心莲内酯苷元

尿苷(5')二氢二磷酰(1)-Alpha-D-葡萄糖,新穿心莲内酯苷元置于glucosyltransferase From Andrographis Paniculata体系中,用 Aq. Buffer 用作溶剂,化学反应 12.0H,反应生成新穿心莲内酯
参考文献:Glucosyltransferase Capable Of Catalyzing The Last Step In Neoandrographolide Biosynthesis
标题:Glucosyltransferase Capable Of Catalyzing The Last Step In Neoandrographolide Biosynthesis
摘要:Apugt,A Diterpene Glycosyltransferase From Andrographis Paniculata,Could Transfer A Glucose To The C-19 Hydroxyl Moiety Of Andrograpanin To Form Neoandrographolide. This Glycosyltransferase Has A Broad Substrate Scope,And It Can Glycosylate 26 Natural And Unnatural Compounds Of Different Structural Types. This Study Provides A Basis For Exploring The Glycosylation Mechanism Of Ent-Labdane-Type Diterpenes And Plays An Important Role In Diversifying The Structures Used In Drug Discovery.
Doi:10.1021/acs.Orglett.8B02146

专利信息

专利号:US-2013144035-A1
优先权日:2010-04-21
标 题:Compositions and methods for leukocyte-targeting multi-valent imaging probes
发明人：PAN DONGFENG; BERR STUART S; ZHANG YI
权利人:PAN DONGFENG; BERR STUART S; ZHANG YI
摘要:The present application discloses a new multivalent peptide ligand specifically targeting polymorphonuclear leukocytes (PMNs) with favorable pharmacological parameters to monitor sites of inflammation for imaging. The detailed synthesis, characterization, and pharmacological evaluation of the ligands are reported here. Two separate peptide binding ligands for formyl peptide and tuftsin receptors were chosen to link together based on the high expression levels of the two receptors on activated PMNs The heterobivalency and pegylated links were incorporated in the structural design to improve the sensitivity of the detection and to improve the bioavailability along with blood clearance profile, respectively. Two chemical constructs: cFLFLF-(PEG) n -TKPPR- 99m Tc (n=4, 12) were evaluated in vitro with human PMNs for binding affinity and bioavailability. As a result, FLFLF-(PEG) 12 -TKPPR 99m Tc was found to have more favorable pharmacological properties and was therefore used for further in vivo studies. Preliminary in vivo assessment of the agent was performed using Single Gamma Emission Computed Tomography (SPECT) imaging of a mouse model of ear inflammation. The results of these studies indicate cFLFLF-(PEG) 12 -TKPPR- 99m Tc may be a desirable imaging agent for binding to PMNs to identify sites of inflammation by SPECT.