球毛壳菌素 F | 55945-75-0

• 分子结构分类: 有机化合物 - 生物碱及其衍生物 - 细胞松弛素类
• 中文名称: 球毛壳菌素 F
• 中文别名: 球毛壳菌素F
• 英文名称: chaetoglobosin F
• 英文别名: (1R,5S,7E,9S,11E,13R,14S,16R,17S,18R,19S)-5-hydroxy-19-(1H-indol-3-ylmethyl)-7,9,16,17-tetramethyl-15-oxa-20-azatetracyclo[11.8.0.01,18.014,16]henicosa-7,11-diene-2,6,21-trione
• CAS: 55945-75-0
• 化学式: C₃₂H₃₈N₂O₅
• 分子量: 530.664
• InChiKey: KTFGDHPTDQFFRL-USMZZGTESA-N

物化性质

• 熔点：
  173-175 °C
• 沸点：
  798.1±60.0 °C(Predicted)
• 密度：
  1.29±0.1 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  4
• 重原子数：
  39
• 可旋转键数：
  2
• 环数：
  6.0
• sp3杂化的碳原子比例：
  0.53
• 拓扑面积：
  112
• 氢给体数：
  3
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  球毛壳菌素 F 在 硫酸 、 bismuth(III) oxide 作用下， 以 溶剂黄146 为溶剂， 反应 0.75h， 生成 chaetoglobosin G monoacetate
  参考文献：
  名称：

  Chaetoglobosins, cytotoxic 10-(indol-3-yl)-(13)cytochalasans from Chaetomium spp. III. Structures of chaetoglobosins C, E, F, G, and J.

  摘要：

  根据物理数据，特别是1H-NMR和化学相关性，确定了chaetoglobosins C、E、F、G和J（10-(吲哚-3-基)-[13]细胞色素）的结构（图1）。本文讨论了chaetoglobosins的立体结构特征。

  DOI：

  10.1248/cpb.30.1629

文献信息

• Chaetoglobosins from<i>Chaetomium globosum</i>, an Endophytic Fungus in<i>Ginkgo biloba</i>, and Their Phytotoxic and Cytotoxic Activities
  作者：He Li、Jian Xiao、Yu-Qi Gao、Jiang−Jiang Tang、An-Ling Zhang、Jin-Ming Gao

  DOI：10.1021/jf500390h

  日期：2014.4.30

  In preceding studies, cultivation of Chaetomium globosum, an endophytic fungus in Ginkgo biloba, produced five cytochalasan mycotoxins, chaetoglobosins A, G, V, Vb, and C (1–5), in three media. In the present work, five known chaetoglobosins, C, E, F, Fex, and 20-dihydrochaetoglobosin A (5–9), together with the four known compounds (11–14), were isolated from the MeOH extracts of the solid culture

  在前述研究中，培养球毛壳菌，在一个内生真菌银杏，制作了五种cytochalasan真菌毒素，chaetoglobosins A，G，V，V b，和C（1 - 5），在三个介质。另外，在本工作中，5个已知chaetoglobosins，C，E，F，F EX和20-dihydrochaetoglobosin A（5 - 9），与四个已知化合物（一起11 - 14），从该固体的甲醇提取物中分离相同内生菌的培养。在光谱分析的基础上阐明了这些代谢物的结构。脂球蛋白F的治疗（7）与（二乙基氨基）三氟化硫（DAST）的二氯甲烷溶液混合后，得到了意想不到的氟化chaetoglobosin，称为chaetoglobosin F a（10），在C-20和C-23之间含有一个环氧丙烷环。化合物的植物毒性效果1，3 - 8，和10中测定的萝卜幼苗; 一些这些化合物（的1，3，和6 - 8）显著抑制萝卜的生长（萝卜）在浓度为50
• Intravascular stent with cytoskeletal inhibitors for the prevention of restenosis
  申请人：Boston Scientific Limited

  公开号：EP1512398A1

  公开（公告）日：2005-03-09

  Methods are provided for inhibiting stenosis or restenosis following vascular trauma in a mammalian host, comprising administering to the host a therapeutically effective dosage of a cytostatic agent and/or cytoskeletal inhibitor so as to biologically stent the traumatized vessel. Also provided is a method to inhibit or reduce vascular remodeling following vascular trauma, comprising administering an effective amount of a cytoskeletal inhibitor. Further provided are pharmaceutical compositions and kits comprising the therapeutic agents of the invention.

  提供了抑制哺乳动物宿主血管创伤后狭窄或再狭窄的方法，包括向宿主施用治疗有效剂量的细胞抑制剂和/或细胞骨架抑制剂，以便对创伤血管进行生物支架治疗。还提供了一种抑制或减少血管创伤后血管重塑的方法，包括施用有效量的细胞骨架抑制剂。还提供了包含本发明治疗剂的药物组合物和试剂盒。
• Use of cytoskeletal inhibitors in crystalline form for the inhibition or prevention of restenosis
  申请人：BOSTON SCIENTIFIC SCIMED LIMITED

  公开号：EP2098230A1

  公开（公告）日：2009-09-09

  Methods are provided for inhibiting stenosis or restenosis following vascular trauma in a mammalian host, comprising administering to the host a therapeutically effective dosage of a cytostatic agent and/or cytoskeletal inhibitor so as to biologically stent the traumatized vessel. Also provided is a method to inhibit or reduce vascular remodeling following vascular trauma, comprising administering an effective amount of a cytoskeletal inhibitor. Further provided are pharmaceutical compositions and kits comprising the therapeutic agents of the invention.

  提供了抑制哺乳动物宿主血管创伤后狭窄或再狭窄的方法，包括向宿主施用治疗有效剂量的细胞抑制剂和/或细胞骨架抑制剂，以便对创伤血管进行生物支架治疗。还提供了一种抑制或减少血管创伤后血管重塑的方法，包括施用有效量的细胞骨架抑制剂。还提供了包含本发明治疗剂的药物组合物和试剂盒。
• Therapeutic inhibitors of vascular smooth muscle cells
  申请人：Boston Scientific Limited

  公开号：EP2298310A2

  公开（公告）日：2011-03-23

  Methods are provided for inhibiting stenosis following vascular trauma or disease in a mammalian host, comprising administering to the host a therapeutically effective dosage of a therapeutic conjugate containing a vascular smooth muscle binding protein that associates in a specific manner with a cell surface of the vascular smooth muscle cell coupled to a therapeutic agent dosage form that inhibits a cellular activity of the muscle cell. Methods are also provided for the direct and/or targeted delivery of therapeutic agents to vascular smooth muscle cells that cause a dilation and fixation of the vascular lumen by inhibiting smooth muscle cell contraction, thereby constituting a biological stent.

  本发明提供了抑制哺乳动物宿主血管创伤或疾病后狭窄的方法，包括向宿主施用治疗有效剂量的治疗共轭物，该共轭物含有血管平滑肌结合蛋白，该蛋白以特定方式与血管平滑肌细胞的细胞表面结合，并与抑制肌肉细胞的细胞活性的治疗剂剂型耦合。还提供了向血管平滑肌细胞直接和/或靶向输送治疗剂的方法，这种方法通过抑制平滑肌细胞收缩，使血管腔扩张和固定，从而构成生物支架。
• Dosage form comprising taxol in crystalline form
  申请人：BOSTON SCIENTIFIC SCIMED LIMITED

  公开号：EP2292225A1

  公开（公告）日：2011-03-09

  Methods are provided for inhibiting stenosis or restenosis following vascular trauma in a mammalian host, comprising administering to the host a therapeutically effective dosage of a cytostatic agent and/or cytoskeletal inhibitor so as to biologically stent the traumatized vessel. Also provided is a method to inhibit or reduce vascular remodeling following vascular trauma, comprising administering an effective amount of a cytoskeletal inhibitor. Further provided are pharmaceutical compositions and kits comprising the therapeutic agents of the invention.

  提供了抑制哺乳动物宿主血管创伤后狭窄或再狭窄的方法，包括向宿主施用治疗有效剂量的细胞抑制剂和/或细胞骨架抑制剂，以便对创伤血管进行生物支架治疗。还提供了一种抑制或减少血管创伤后血管重塑的方法，包括施用有效量的细胞骨架抑制剂。还提供了包含本发明治疗剂的药物组合物和试剂盒。