CAS: 16503-32-5; (3S,3Ar,4S,4Ar,7Ar,8R,9Ar)-3,4A,8-Trimethyl-2,5-Dioxo-2,3,3A,4,4A,5,7A,8,9,9A-Decahydroazuleno[6,5-B]Furan-4-Yl (Z)-2-Methylbut-2-Enoate

该化合物是来自Centipeda minima(一种传统用于草药的植物)的精液乳腺化合物,它具有显著的生物活动,包括抗炎,抗癌和免疫细胞性能.Brevilin A在结构上具有α-甲基-苯-γ-单体细胞性能的特点,它与NF-B和STAT3信号路径等细胞目标相互作用,使它成为研究肿瘤学和炎症的有希望的候选体.它在临床前研究中证明了它诱发流行性疾病和抑制肿瘤细胞扩散的能力.Brevilin A因其高度纯度和稳定性而受到重视,确保生物化学和药理学调查的可靠性能.

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    专利信息


    专利号:US-2024336679-A1
    优先权日:2021-08-06
    标题 :Methods for the treatment of cancer
    发明人:LINARES LÆTITIA; FIRMIN NELLY; MANTEAUX GABRIELLE
    权利人:INST REGIONAL CANCER MONTPELLIER; INST NAT SANTE RECH MED; UNIV MONTPELLIER
    摘要:The present disclosure relates to an Interleukin-6 (IL-6) signaling inhibitor selected from an IL-6 inhibitor, an IL-6 receptor inhibitor, an IL-6/IL-6 receptor complex inhibitor, a gp130 inhibitor and a STAT3 inhibitor or a pharmaceutical composition comprising such an IL-6 signaling inhibitor. for use in a method for treating and/or preventing cancer in a subject in need thereof. wherein the subject has been previously classified as being affected with a cancer exhibiting recruitment of MDM2 to chromatin. The inventors have observed that cancers exhibiting recruitment of MDM2 to chromatin have been shown to secrete IL-6 that in turn acts on myoblast cells to activate serine synthesis. Following these surprising and unexpected observations. the inventors set up methods of treatment that are able to induce cancer cells death in subjects that have been previously classified as being affected with a cancer exhibiting recruitment of MDM2 to chromatin.

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    主要参考文献


    1: Yen LJ, Yen CY, Li CL, Liao EC, Wang KC, Shih MC, Huang HS, Chen YC, Lu LY, Yu SJ. Brevilin A Ameliorates Imiquimod-Induced Psoriasis-like Dermatitis and Reduces Th17 Differentiation in Psoriasis Patients. J Pers Med. 2022 Nov 10;12(11):1888. doi: 10.3390/jpm12111888.
    2: Lee D, Kwak HJ, Kim BH, Kim DW, Kim HY, Kim SH, Kang KS. Brevilin A Isolated from Centipeda minima Induces Apoptosis in Human Gastric Cancer Cells via an Extrinsic Apoptotic Signaling Pathway. Plants (Basel). 2022 Jun 23;11(13):1658. doi: 10.3390/plants11131658.
    3: Zhu X, Liu F, Wu Q, Li S, Ruan G, Yang J, Yu C, Jiang N, Xiao Y, Liu Y. Brevilin A enhances innate immunity and the resistance of oxidative stress in Caenorhabditis elegans via p38 MAPK pathway. Int Immunopharmacol. 2022 Dec;113(Pt A):109385. doi: 10.1016/j.intimp.2022.109385. Epub 2022 Oct 30.

    合成参考文献


    参考文献:10.1124/mol.119.115964
    摘要:Lee TD, Lee OW, Brimacombe KR, Chen L, Guha R, Lusvarghi S, Tebase BG, Klumpp-Thomas C, Robey RW, Ambudkar SV, Shen M, Gottesman MM, Hall MD. A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. Molecular Pharmacology. 2019 Nov;96(5):629–40. doi: 10.1124/mol.119.115964.
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