CAS: 481-49-2; (15S,31R)-36,54-Dimethoxy-16,32-Dimethyl-15,16,17,18,31,32,33,34-Octahydro-2,6-Dioxa-1(4,5)-[1,3]Dioxolo[4,5-G]Isoquinolina-3(7,1)-Isoquinolina-5(1,3),7(1,4)-Dibenzenacyclooctaphane

该化合物是源自史蒂芬尼亚脑膜炎的天然二苯苯基碱性藻类,具有显著的药理特性,包括抗炎,免疫分子和抗病毒活动,其行动机制包括抑制NF-NB信号和调节细胞自发性,使其成为对炎症和传染病研究感兴趣的对象.Cepharanthine还展示了提高辐射敏感度和减轻氧化压力的潜力.其低毒性特征和跨细胞膜的能力有效地进一步支持其在临床前研究中的适用性.这种化合物通常用于生物化学研究,以研究其多种生物效应和精密的分子相互作用.

结构式图片

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cepharanthine-2′α-N-oxide(R)-6-methoxy-1-(4-methoxybenzyl)-2-methyl-1,2,3,4-tetrahydroisoquinolin-7-ol sec°Cepharanthine dihydrosec°Cepharanthine

合成工艺路线路线简述

    📜Cepharanthine-2-N-Oxide置于盐酸,锌体系中,用 水 作为反应溶剂,化学反应 2.0H,以4 Mg的收率获得产物千金藤素
    参考文献:Stephania Epigaea的细胞毒性双苄基异喹啉生物碱
    标题:Stephania Epigaea的细胞毒性双苄基异喹啉生物碱
    摘要:六个新bisbenzylisoquinoline生物碱(1-6)和七个已知化合物(8-14)获自的块茎中分离出千金藤epigaea,除了主要的生物碱,千金藤素(7).的结构1-6通过组合光谱数据分析和化学方法阐明,与它们的配置从它们的旋光值确定,并使用圆二色性的证实.化合物1-6属于oxyacanthine类型bisbenzylisoquinoline生物碱和具有罕见亚甲二氧基的取代基.化合物1中,苄基异的和开环aristolactam单元构成的二聚体,代表了一种新类型bisbenzylisoquinoline生物碱,而化合物3-6是bisbenzylisoquinoline ñ-Oxides.评估了这些化合物对六种人类癌细胞系(a-549,Eca109,Hl-60,Mcf-7,Smmc-7721和sw480)的体外细胞毒性.头孢葡萄球菌(s. Epigaea)的主
    DOI:10.1021/np400084T

    专利信息


    专利号:US-6193975-B1
    优先权日:1996-11-07
    标题:Use of potentilla erecta extract in the cosmetic and pharmaceutical field
    发明人:BONTE FREDERIC; DUMAS MARC; CHAUDAGNE CATHERINE; MEYBECK ALAIN
    权利人:LVMH RECH
    摘要:The invention relates to the use of an extract of the plant Potentilla erecta in the field of cosmetics and pharmacy, especially in dermatology. The invention more particularly relates to any application in which it is sought to reinforce the dermo-epidermal junction or to improve hair condition, by the improvement of the synthesis of collagen VII by keratinocytes and/or fibroblasts. In particular, these applications concern toning of the skin, diminishing of wrinkles or hair care. The invention also relates to a novel method of culture of cells, in particular of human fibroblasts or keratinocytes, for promoting the formation of collagen VII.

    专利号:WO-9421230-A1
    优先权日:1993-03-19
    标题 :Method and compositions for disrupting the epithelial barrier function
    发明人:ELIAS PETER M; THORNFELDT CARL R; GRAYSON STEPHEN
    权利人:CELLEGY PHARMA INC; UNIV CALIFORNIA; ELIAS PETER M; THORNFELDT CARL R; GRAYSON STEPHEN
    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:WO-9817253-A1
    优先权日:1996-10-23
    标 题 :Method and compositions for disrupting the epithelial barrier function
    发明人:ELIAS PETER M; FEINGOLD KENNETH R; HOLLERAN WALTER M; THORNFELDT CARL R
    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-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-7678380-B2
    优先权日:1996-11-07
    标 题 :Cosmetic treatment method for fighting against skin ageing effects
    发明人:BONTE FREDERIC; DUMAS MARC; HEUSELE CATHERINE; LE BLAY JACQUES
    权利人:LVMH RECH
    摘要:The present invention relates to a method of cosmetic treatment for combating the effects of skin ageing and to novel cosmetic compositions which are particularly suitable for carrying it out. According to the invention, at least one agent for promoting the adhesion of the keratinocytes of the epidermal basal layer to the dermo-epidermal junction, especially to the collagen IV of said junction, such as, in particular, a divalent metal salt or complex, preferably magnesium aspartate or magnesium chloride, is used, optionally in association with a stimulant of collagen IV synthesis and/or a stimulant of collagen VII synthesis.

    专利号:WO-9701346-A1
    优先权日:1995-06-27
    标题:Cosmetic or pharmaceutical composition containing an extract of plants of genus filicium, and use of said extract for stimulating glycosaminoglycan synthesis

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    📌 第三方产品分析报告

    ✅ COA系统入驻 | 共享模式

    主要参考文献


    1: Fang ZH, Li YJ, Chen Z, Wang JJ, Zhu LH. Inhibition of signal transducer and activator of transcription 3 and cyclooxygenase-2 is involved in radiosensitization of cepharanthine in HeLa cells. Int J Gynecol Cancer. 2013 May;23(4):608-14. doi: 10.1097/IGC.0b013e31828a05fd. doi: 10.3892/ijo.2012.1501. Epub 2012 May 31. doi: 10.1016/j.intimp.2012.04.015. Epub 2012 May 3. Review. doi: 10.1155/2011/281651. Epub 2011 Jun 30.
    6: Rogosnitzky M, Danks R. Therapeutic potential of the biscoclaurine alkaloid, cepharanthine, for a range of clinical conditions. Pharmacol Rep. 2011;63(2):337-47. Review. doi: 10.1111/j.1349-7006.2010.01572.x. Epub 2010 Mar 24. doi: 10.1002/ijc.24521.

    合成参考文献


    参考文献:10.1155/2011/281651
    摘要:Li H, Yan Z, Ning W, Xiao-Juan G, Cai-Hong Z, Jin-Hua J, Fang M, Qing-Duan W. Using Rhodamine 123 Accumulation in CD8+ Cells as a Surrogate Indicator to Study the P‐Glycoprotein Modulating Effect of Cepharanthine Hydrochloride In Vivo. BioMed Research International. 2011 Jan;2011(1). doi: 10.1155/2011/281651.
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