CAS: 34157-83-0; (2R,4As,6As,12Br,14As,14Br)-10-Hydroxy-2,4A,6A,9,12B,14A-Hexamethyl-11-Oxo-1,2,3,4,4A,5,6,6A,11,12B,13,14,14A,14B-Tetradecahydropicene-2-Carboxylic Acid

该化合物是一种天然的三叶细胞类动物,它从威尔福迪河的根部提取. 它的主要优势在于其强大的抗炎和抗氧化性特性,这使得它成为研究应用的宝贵化合物. 研究表明它有能力抑制NF-B活化并减少氧化性压力.

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CAS号1258-84-0 扁塑藤素

合成工艺路线路线简述

    Celastrogenic Acid置于氧气体系中,用 甲醇 用作溶剂,化学反应生成雷公藤红素
    参考文献:抗肥胖剂雷公藤红素的生物合成及生物技术生产
    标题:抗肥胖剂雷公藤红素的生物合成及生物技术生产
    摘要:肥胖是一个主要的健康风险,目前仍缺乏有效的药物治疗.在雷公藤的根中发现了一种有效的抗肥胖剂雷公藤红素.然而,需要一种有效的合成方法来更好地探索其生物学效用.在这里,我们阐明了雷公藤红素生物合成路线中缺失的 11 个步骤,以使其能够在酵母中从头生物合成.首先,我们揭示了细胞色素 P450 酶,该酶催化产生关键中间体 Celastrogenic 酸的四个氧化步骤.随后,我们表明,非酶脱羧触发的雷公藤红素酸活化导致串联儿茶酚氧化驱动的双键延伸事件级联,从而产生雷公藤红素的特征醌甲基化物部分.利用所获得的知识,我们开发了一种从食糖生产雷公藤红素的方法.这项工作强调了将植物生物化学与代谢工程和化学相结合对于复杂的专门代谢物的可扩展合成的有效性.
    Doi:10.1038/s41557-023-01245-7

    海关参考信息

    专利信息


    专利号:US-2024209029-A1
    优先权日:2021-04-21
    标题:Adiponectin glycopeptides and compositions and methods of use thereof
    发明人:WANG YU; LI XUECHEN; XU AIMIN; WU HONGXIANG; ZHANG YIWEI; LI YUANXIN
    权利人:UNIV HONG KONG
    摘要:An improved method for the chemical synthesis of glycosylated peptides has been developed. The method uses stereoselective glycan synthesis and chemical peptide ligation to produce glycopeptides at lower-cost and with higher efficiency/yield compared to conventional methods. In particular, a method for the large-scale, chemical synthesis of hydroxylated amino acid building blocks and glycosylated amino acids suitable for solid phase peptide synthesis (SPPS) are disclosed. SPPS-based methods using the glycosylated amino acids to chemically synthesize adiponectin-like peptides are also described. In vivo studies show that the adiponectin mimicking glycopeptides exhibit significant anticancer, anti-obesity and insulin sensitizing effects. Pharmaceutical compositions of the synthetic glycopeptides and methods of use thereof in treating diseases associated with deficient adiponectin are also described.

    专利号:US-2025263763-A1
    优先权日:2020-08-27
    标 题 :Production of oxygenated diterpenoid compounds
    发明人:ANDERSEN-RANBERG JOHAN; HANSEN NIKOLAJ; FORMAN VICTOR
    权利人:UNIV COPENHAGEN
    摘要:Disclosed is a method for production of oxygenated diterpenoid compounds, such as triptophenolide, triptonide and triptolide, by inserting genes encoding particular cytochrome P450 enzymes and expressing the genes in selected host cells for synthesis of the compounds. Further disclosed are particular cytochrome P450 enzymes suitable for this synthesis.

    专利号:WO-2022043461-A1
    优先权日:2020-08-27
    标 题 :Production of oxygenated diterpenoid compounds
    发明人:ANDERSEN-RANBERG JOHAN; HANSEN NIKOLAJ; FORMAN VICTOR
    权利人:UNIV COPENHAGEN
    摘要:Disclosed is a method for production of oxygenated diterpenoid compounds, such as triptophenolide, triptonide and triptolide, by inserting genes encoding particular cytochrome P450 enzymes and expressing the genes in selected host cells for synthesis of the compounds. Further disclosed are particular cytochrome P450 enzymes suitable for this synthesis.

    专利号:WO-2014018862-A1
    优先权日:2012-07-27
    标 题 :Pharmaceutical compositions comprising a heat shock protein inhibitor and a; purine de novo synthesis inhibitor for treating rheumatoid arthritis or cancer
    发明人:FANG YE
    权利人:CORNING INC; FANG YE
    摘要:A pharmaceutical composition including an effective amount of the combination of: an heat shock protein (HSP) inhibitor, and a purine de novo biosynthesis inhibitor, or a pharmaceutically acceptable salt thereof. Also disclosed is a method of treating rheumatoid arthritis or cancer including administering an effective amount of the above mentioned pharmaceutical composition to a patient in need of such treatment, as defined herein.

    专利号:US-2008281105-A1
    优先权日:2005-01-18
    标题:Novel Quinolinium Salts and Derivatives
    发明人:MACDONALD JAMES E; HYSELL MICHELLE K; YU DEHUA; LI HENRY; WONG-STAAL FLOSSIE
    权利人:IMMUSOL INC
    摘要:The present invention relates generally to the synthesis of novel quinolinium salts and derivative compounds. Such salts and compounds are useful for inhibiting the growth of cancer cells.

    专利号:US-8257754-B2
    优先权日:2002-10-21
    标 题:Synergistic compositions that treat or inhibit pathological conditions associated with inflammatory response
    发明人:TRIPP MATTHEW L; BABISH JOHN G; BLAND JEFFREY S; DARLAND GARY K; LERMAN ROBERT; LUKACZER DANIEL O; LISKA DEANN J; HOWELL TERRENCE M
    权利人:TRIPP MATTHEW L; BABISH JOHN G; BLAND JEFFREY S; DARLAND GARY K; LERMAN ROBERT; LUKACZER DANIEL O; LISKA DEANN J; HOWELL TERRENCE M; METAPROTEOMICS LLC
    摘要:A natural formulation of compounds that would to modulate inflammation is disclosed. The formulation would also inhibit expression of COX-2, inhibit synthesis of prostaglandins selectively in target cells, and inhibit inflammatory response selectively in target cells. The compositions containing at least one fraction isolated or derived from hops. Other embodiments relate to combinations of components, including at least one fraction isolated or derived from hops, tryptanthrin and conjugates thereof, rosemary, an extract or compound derived from rosemary, a triterpene species, or a diterpene lactone or derivatives or conjugates thereof.
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    主要参考文献


    1: Deane CA, Brown IR. Induction of heat shock proteins in differentiated human neuronal cells following co-application of celastrol and arimoclomol. Cell Stress Chaperones. 2016 Jun 8. [Epub ahead of print] doi: 10.1016/j.yexmp.2016.05.013. [Epub ahead of print] doi: 10.1016/S2095-4964(16)60257-1. doi: 10.1016/j.ejphar.2016.04.045. [Epub ahead of print] doi: 10.1016/j.actbio.2016.05.012. Epub 2016 May 6. doi: 10.1159/000445554. Epub 2016 May 9. Molecules. 2016 Apr 30;21(5). pii: E574. doi: 10.3390/molecules21050574. doi: 10.1016/j.metabol.2016.01.009. Epub 2016 Jan 25. doi: 10.4103/0973-1482.150407. doi: 10.1155/2016/2641248. Epub 2016 Jan 19.
    13: Guan Y, Cui ZJ, Sun B, Han LP, Li CJ, Chen LM. Celastrol attenuates oxidative stress in the skeletal muscle of diabetic rats by regulating the AMPK-PGC1α-SIRT3 signaling pathway. Int J Mol Med. 2016 May;37(5):1229-38. doi: 10.3892/ijmm.2016.2549. Epub 2016 Apr 5.
    14: Zou YC, Yang XW, Yuan SG, Zhang P, Li YK. Celastrol inhibits prostaglandin E2-induced proliferation and osteogenic differentiation of fibroblasts isolated from ankylosing spondylitis hip tissues in vitro. Drug Des Devel Ther. 2016 Mar 7;10:933-48. doi: 10.2147/DDDT.S97463. eCollection 2016.

    合成参考文献


    参考文献:10.1074/jbc.m109.090209
    摘要:Sung B, Park B, Yadav VR, Aggarwal BB. Celastrol, a Triterpene, Enhances TRAIL-induced Apoptosis through the Down-regulation of Cell Survival Proteins and Up-regulation of Death Receptors. Journal of Biological Chemistry. 2010 Apr;285(15):11498–11507a. doi: 10.1074/jbc.m109.090209.
    参考文献:10.2174/157016310791162785
    摘要:Yang H, Liu J, Dou QP. Targeting tumor proteasome with traditional Chinese medicine. Curr Drug Discov Technol. 2010 Mar;7(1):46–53.
    参考文献:10.1016/j.jmb.2011.04.013
    摘要:Narayan V, Ravindra KC, Chiaro C, Cary D, Aggarwal BB, Henderson AJ, Prabhu KS. Celastrol Inhibits Tat-Mediated Human Immunodeficiency Virus (HIV) Transcription and Replication. Journal of Molecular Biology. 2011 Jul;410(5):972–83. doi: 10.1016/j.jmb.2011.04.013.
    参考文献:10.1186/1749-8546-6-27
    摘要:Tan W, Lu J, Huang M, Li Y, Chen M, Wu G, Gong J, Zhong Z, Xu Z, Dang Y, Guo J, Chen X, Wang Y. Anti-cancer natural products isolated from chinese medicinal herbs. Chinese Medicine. 2011 Jul 22;6(1):27. doi: 10.1186/1749-8546-6-27.
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