osthole | 625817-49-4

• 分子结构分类: 有机化合物 - 苯丙烷和聚酮 - 3,4-二氢香豆素
• 英文名称: osthole
• 英文别名: 7-Methoxy-8-(3-methylbut-2-enyl)-3,4-dihydrochromen-2-one
• CAS: 625817-49-4
• 化学式: C₁₅H₁₈O₃
• 分子量: 246.306
• InChiKey: HDCUYVWVMGOCTK-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.5
• 重原子数：
  18
• 可旋转键数：
  3
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.4
• 拓扑面积：
  35.5
• 氢给体数：
  0
• 氢受体数：
  3

反应信息

• 作为产物：
  描述：

  3-[2-hydroxy-4-methoxy-3-(3-methyl-but-2-enyl)-phenyl]-propionic acid 在 1-羟基苯并三唑 、 盐酸-N-乙基-Nˊ-(3-二甲氨基丙基)碳二亚胺 作用下， 以 二氯甲烷 为溶剂， 生成 osthole
  参考文献：
  名称：

  Prenylcoumarin with Rev-export inhibitory activity from Cnidii Monnieris Fructus

  摘要：

  By use of the fission yeast expressing the model fusion protein comprised of GST, SV40 T antigen NLS, GFP, and Rev-NES in the bioassay, the prenylcoumarin osthol (1) was disclosed as the new Rev-export inhibitor from the MeOH extract of Cnidii Monnieris Fructus. Furthermore, 1 was also found to inhibit export the genuine Rev in HeLa cells by indirect fluorescent antibody technique. By the competitive experiment using the biotinylated probe 3, osthol (1) was revealed to inhibit nuclear export of Rev through a NES non-antagonistic mode. Structure-activity relationship analysis of several analogs of 1 clarified that both prenyl side chain and double bond adjacent to the lactone carbonyl residue play an important role in the Rev-export inhibitory potency of 1. (C) 2010 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2010.04.081

文献信息

• SGLT2 AS BIOMARKER FOR DIAGNOSING CHRONIC KIDNEY DISEASE AND MONITORING THE DISEASE STATUS AFTER TREATMENT
  申请人：National Defense Medical Center

  公开号：US20150104881A1

  公开（公告）日：2015-04-16

  The present invention relates to a method for diagnosis of a chronic kidney disease in a subject by detecting the expression level of a sodium-glucose linked transporter 2 (SGLT2) protein in urine samples. A method for monitoring progression of a chronic kidney disease in a patient is also provided.
• USE OF OSTHOLE FOR TREATING FOCAL SEGMENTAL GLOMERULOSCLEROSIS
  申请人：National Defense Medical Center

  公开号：US20150297560A1

  公开（公告）日：2015-10-22

  The present invention relates to use of osthole for manufacturing a composition for treating focal segmental glomerulosclerosis (FSGS). Particularly, the present invention discloses that osthole is effective in treating focal segmental glomerulosclerosis (FSGS), which can alleviate various symptoms and signs of FSGS, including proteinuria, renal fibrosis, glomerular epithelial hyperplasia lesion (EPHL), and macrophage/lymphocyte infiltration in the kidney, etc.
• US9393226B2
  申请人：——

  公开号：US9393226B2

  公开（公告）日：2016-07-19
• Prenylcoumarin with Rev-export inhibitory activity from Cnidii Monnieris Fructus
  作者：Satoru Tamura、Toshiaki Fujitani、Masafumi Kaneko、Nobutoshi Murakami

  DOI：10.1016/j.bmcl.2010.04.081

  日期：2010.6

  By use of the fission yeast expressing the model fusion protein comprised of GST, SV40 T antigen NLS, GFP, and Rev-NES in the bioassay, the prenylcoumarin osthol (1) was disclosed as the new Rev-export inhibitor from the MeOH extract of Cnidii Monnieris Fructus. Furthermore, 1 was also found to inhibit export the genuine Rev in HeLa cells by indirect fluorescent antibody technique. By the competitive experiment using the biotinylated probe 3, osthol (1) was revealed to inhibit nuclear export of Rev through a NES non-antagonistic mode. Structure-activity relationship analysis of several analogs of 1 clarified that both prenyl side chain and double bond adjacent to the lactone carbonyl residue play an important role in the Rev-export inhibitory potency of 1. (C) 2010 Elsevier Ltd. All rights reserved.