📜在 盐酸,Palladium Hydroxide On Carbon,氢气体系中,用 四氢呋喃,水,叔丁醇 用作溶剂,化学反应 18.0H,以45%的收率获得伏马毒素b1 参考文献:Pereira,Claney L.; Chen,Yi-Hung; Mcdonald,Frank E.,Journal Of The American Chemical Society,2009,Vol. 131,P. 6066-6067 标题:Pereira,Claney L.; Chen,Yi-Hung; Mcdonald,Frank E.,Journal Of The American Chemical Society,2009,Vol. 131,P. 6066-6067
专利号:US-2004110228-A1 优先权日:2002-04-01 标 题:Combinatorial organic synthesis of unique biologically active compounds 发明人:MCALPINE SHELLI R; TAYLOR RACHEL E; BOLLA MEGAN L; SEGALL ANCA M 摘要:The invention provides a method for making a combinatorial library of cyclic compounds, such as Holliday junction-trapping compounds, comprising the steps of (a) obtaining a plurality of trimers according to the generic structure X 1- X 2- X 3 , wherein X 1 , X 2 and X 3 can be independently any naturally or nonnaturally occurring amino acids or peptidomimetics thereof; (b) optionally coupling a spacer S to the trimer at either end; (c) cyclizing two trimers or trimer-spacer conjugates in a head-to-tail orientation; thereby obtaining a combinatorial library of compounds, wherein the library does not include an unmodifed or naturally occurring Holliday Junction-trapping compounds. The invention additionally provides methods macrocyclic compounds that are synergimycin derivatives.
专利号:US-2013131146-A1 优先权日:2010-04-30 标题:Compositions and Methods for Treating Pulmonary Conditions 发明人:VIJ NEERAJ; BODAS MANISH 权利人:VIJ NEERAJ; BODAS MANISH; UNIV JOHNS HOPKINS 摘要:The present invention relates to the role of cystic fibrosis transmembrane conductance regulator (CFTR) in pulmonary conditions. In one embodiment, a method for assessing the severity of lung damage from a pulmonary condition in a subject comprises the steps of (a) measuring the level and/or functional activity of membrane/lipid-raft cystic fibrosis transmembrane conductance regulator (CFTR)in a sample from the subject; (b) measuring the level of ceramide or its species in a sample from the subject; and (c) comparing the membrane/lipid- raft CFTR level and/or functional activity and ceramide level to a control sample, wherein a difference in membrane/lipid-raft CFTR level and/or functional activity and ceramide level is indicative of the severity of lung damage. The method can further comprise treating the subject based on the severity of lung damage. In particular embodiments, the treatment comprises administering a CFTR agonist and/or an agent that inhibits the synthesis of ccramide or its species.
专利号:US-6562606-B1 优先权日:1993-03-19 标 题:Methods and compositions for disrupting the epithelial barrier function 发明人:ELIAS PETER M; FEINGOLD KENNETH R; HOLLERAN WALTER M 权利人:UNIV CALIFORNIA; CELLEGY PHARMA INC 摘要:A method for disrupting epithelial barrier function in a host in need of the topical administration of a physiologically active substance which comprises applying to the epithelium of the host, barrier-disrupting amount of at least one agent selected from the group consisting of an inhibitor of ceramide synthesis, inhibitor of acylceramide synthesis, inhibitor of glucosylceramide synthesis, and inhibitor of sphingomyelin synthesis, an inhibitor of fatty acid synthesis, an inhibitor of cholesterol synthesis, a degradation enzyme of ceramides, acylceramide, glucosylceramides, sphingomyelin, an inhibitor of phospholipid, glycosphingolipid, including glucosylceramide, acylceramide or sphingomyelin degradation, and both inhibitors and stimulators of metabolic enzymes of free fatty acids, ceramide, and cholesterol, as well as a topical composition useful therefor are disclosed.
专利号:US-9925160-B1 优先权日:2017-01-16 标 题:Methods for treating cardiac reperfusion injury 发明人:GHIDONI RICCARDO; SIGNORELLI PAOLA; ANASTASIA LUIGI 权利人:UNIV DEGLI STUDI MILANO; Policlinico Sandonato; POLICLINICO SAN DONATO S P A 摘要:The inventors have made the surprising discovery that when ceramide production is upregulated in the infarct and at-risk areas upon reperfusion injury in the heart, such upregulation is effected through the de novo ceramide synthesis pathway. Upon treatment of cardiac tissues subject to reperfusion injury with a specific inhibitor of the novo ceramide synthesis pathway (myriocin), the inventors have determined that the inhibition of such pathway not only reduces the inflammation of the interested area, but most surprisingly reduces infarct size, ameliorates cardiac contractility and activates cell detoxification and survival programs. There is thus provided an inhibitor of de novo ceramide synthesis pathway, particularly myriocin, for the treatment of cardiac reperfusion injury.
专利号:CN-114452278-B 优先权日:2022-03-21 标 题 :Application of Inhibitors in Ceramide Synthesis and Decomposition Pathways in Preparation of Ebola Virus Disease Drugs
专利号:CN-114452278-A 优先权日:2022-03-21 标 题:Application of inhibitors in the synthesis and decomposition pathway of ceramide in the preparation of Ebola virus disease drugs
1: Jebali A, Yasini Ardakani SA, Shahdadi H, Balal Zadeh MH, Hekmatimoghaddam S. Modification of nanocellulose by poly-lysine can inhibit the effect of fumonisin B1 on mouse liver cells. Colloids Surf B Biointerfaces. 2015 Feb 1;126:437-43. doi: 10.1016/j.colsurfb.2014.12.047. Epub 2015 Jan 3. doi: 10.1016/j.fct.2014.09.008. Epub 2014 Sep 30. doi: 10.1002/mnfr.201300481. Epub 2013 Dec 23. doi: 10.3109/09637486.2014.979316. Epub 2014 Dec 4. doi: 10.1016/j.ntt.2015.08.007. Epub 2015 Sep 2. doi: 10.1016/j.theriogenology.2014.01.027. Epub 2014 Jan 30. doi: 10.1002/mnfr.201200465. Epub 2012 Dec 23. doi: 10.1080/19393210.2013.841294. Epub 2013 Oct 25. doi: 10.1016/j.toxicon.2015.10.014. Epub 2015 Oct 23. doi: 10.1016/j.toxicon.2014.07.019. Epub 2014 Aug 7. doi: 10.1016/j.tiv.2015.07.019. Epub 2015 Jul 21. doi: 10.3390/toxins7020560. 13: Gui H, Jin Q, Zhang Y, Wang X, Yang Y, Shao C, Cheng C, Wei F, Yang Y, Yang M, Song H. [Development of an aptamer/fluorescence dye PicoGreen-based method for detection of fumonisin B1]. Sheng Wu Gong Cheng Xue Bao. 2015 Sep;31(9):1393-400. Chinese. doi: 10.1016/j.fct.2015.01.024. Epub 2015 Feb 4. doi: 10.1007/s00216-015-8896-7. Epub 2015 Aug 22. Chinese. doi: 10.1007/s00204-014-1323-6. Epub 2014 Aug 26. doi: 10.1016/j.tox.2013.11.004. Epub 2013 Nov 23. doi: 10.1111/tpj.12778. doi: 10.1007/s00244-014-0004-z. Epub 2014 Feb 19.
合成参考文献
参考文献:10.1194/jlr.m017582 摘要:Kavishwar A, Medarova Z, Moore A. Unique sphingomyelin patches are targets of a beta-cell-specific antibody. Journal of Lipid Research. 2011 Sep;52(9):1660–71. doi: 10.1194/jlr.m017582. 参考文献:10.1007/s00216-011-5237-3 摘要:Krska R, Becalski A, Braekevelt E, Koerner T, Cao X, Dabeka R, Godefroy S, Lau B, Moisey J, Rawn DFK, Scott PM, Wang Z, Forsyth D. Challenges and trends in the determination of selected chemical contaminants and allergens in food. Analytical and Bioanalytical Chemistry. 2011 Jul 20;402(1):139–62. doi: 10.1007/s00216-011-5237-3. 参考文献:10.1007/s12032-011-0023-9 摘要:Zhang S, Zhou J, Zhang C, Wu H, Wang Y, Bian J, Guo J, Wu X. Arsenic trioxide inhibits HCCLM3 cells invasion through de novo ceramide synthesis and sphingomyelinase-induced ceramide production. Med Oncol. 2012 Sep;29(3):2251–60. doi: 10.1007/s12032-011-0023-9. 参考文献:10.1007/s11033-011-1207-2 摘要:Jang YS, Kang YJ, Kim TJ, Bae K. Temporal expression profiles of ceramide and ceramide-related genes in wild-type and mPer1/mPer2 double knockout mice. Mol Biol Rep. 2012 Apr;39(4):4215–21. doi: 10.1007/s11033-011-1207-2. 参考文献:10.1007/s12094-011-0689-7 摘要:Xiaoxia Z, Weihua N, Qingyong Z, Fengli W, Yingying L, Xiaxia S, Zhonghui L, Guixiang T. Maltose-binding protein isolated from Escherichia coli induces Toll-like receptor 2-mediated viability in U937 cells. Clinical and Translational Oncology. 2011 Jul 31;13(7):509. doi: 10.1007/s12094-011-0689-7.