2-(2,4-Dihydroxyphenyl)-3-(3-methyl-2-butenyl)-5-hydroxy-8,8-dimethyl-4H,8H-benzo[1,2-b:5,4-b']dipyran-4-one

• 常用名: 2-(2,4-Dihydroxyphenyl)-3-(3-methyl-2-butenyl)-5-hydroxy-8,8-dimethyl-4H,8H-benzo[1,2-b:5,4-b']dipyran-4-one
• 英文名: 2-(2,4-Dihydroxyphenyl)-3-(3-methyl-2-butenyl)-5-hydroxy-8,8-dimethyl-4H,8H-benzo[1,2-b:5,4-b']dipyran-4-one
• CAS号: 19275-49-1
• 分子量: 420.45
• 密度: N/A
• 沸点: N/A
• 分子式: C₂₅H₂₄O₆
• 熔点: N/A
• 闪点: N/A

用途

铜黄酮B是一种具有抗炎和抗肿瘤特性的异戊二烯基黄酮类化合物。铜黄酮B也是COX-1和COX-2的双重抑制剂。铜黄酮B阻断核因子κB(NF-κB)在巨噬细胞中从细胞质向细胞核的移位。因此,铜黄酮B抑制肿瘤坏死因子α(TNFα)基因的表达和分泌。铜黄酮B还触发线粒体凋亡途径,激活NF-κB、MAPK p38和ERK,并诱导SIRT1的表达。因此,铜黄酮B抑制人口腔鳞状细胞癌细胞的生长[1][2]。

名称

• 英文名: cudraflavone B

生物活性

• 描述: 铜黄酮B是一种具有抗炎和抗肿瘤特性的异戊二烯基黄酮类化合物。铜黄酮B也是COX-1和COX-2的双重抑制剂。铜黄酮B阻断核因子κB(NF-κB)在巨噬细胞中从细胞质向细胞核的移位。因此,铜黄酮B抑制肿瘤坏死因子α(TNFα)基因的表达和分泌。铜黄酮B还触发线粒体凋亡途径,激活NF-κB、MAPK p38和ERK,并诱导SIRT1的表达。因此,铜黄酮B抑制人口腔鳞状细胞癌细胞的生长[1][2]。
• 相关类别:
  信号通路 >> 表观遗传学 >> 抗衰老酶
  信号通路 >> 细胞周期/DNA损伤 >> 抗衰老酶
  信号通路 >> MAPK/ERK信号通路 >> p38 MAPK
  研究领域 >> 炎症/免疫
  信号通路 >> 免疫及炎症 >> COX
  信号通路 >> MAPK/ERK信号通路 >> ERK
  信号通路 >> 干细胞及 Wnt 通路 >> ERK
• 靶点实验:

  NF-κB

  COX-2

  COX-1

  TNFRSF1A

  p38 MAP kinase

  ERK

  SIRT1

• 参考文献:

  [1]. Hošek J, et al. Natural compound cudraflavone B shows promising anti-inflammatory properties in vitro. J Nat Prod. 2011 Apr 25;74(4):614-9.

  [2]. Lee HJ, et al. Growth inhibition and apoptosis-inducing effects of cudraflavone B in human oral cancer cells via MAPK, NF-κB, and SIRT1 signaling pathway. Planta Med. 2013 Sep;79(14):1298-306.

物理化学性质

• 分子式: C₂₅H₂₄O₆
• 分子量: 420.45
• 精确质量: 420.15700
• PSA: 100.13000
• LogP: 5.26970
• InChIKey: XIWCDUHPYMOFIL-UHFFFAOYSA-N
• SMILES: CC(C)=CCc1c(-c2ccc(O)cc2O)oc2cc3c(c(O)c2c1=O)C=CC(C)(C)O3

靶点实验

查看更多实验

实验名称：Primary cell-based high-throughput screening assay for identification of compounds th... 来源：Johns Hopkins Ion Channel Center 靶标：regulator of G-protein signaling 4 isoform 2 [Homo sapiens] External Id：JHICC_RGS_Act_HTS

实验名称：uHTS identification of small molecule activators of the adaptive arm of the Unfolded ... 来源：Burnham Center for Chemical Genomics 靶标：N/A External Id：BCCG-A405-UPR-XBP1-PrimaryAgonist-Assay

实验名称：Inhibition of Clostridium welchii neuraminidase 来源：ChEMBL 靶标：N/A External Id：CHEMBL1048098

实验名称：qHTS for Inhibitors of human tyrosyl-DNA phosphodiesterase 1 (TDP1): qHTS in cells in... 来源：NCGC 靶标：TDP1 protein [Homo sapiens] External Id：TDP1100

实验名称：Noncompetitive inhibition of Clostridium welchii neuraminidase by Dixon plot 来源：ChEMBL 靶标：N/A External Id：CHEMBL1048099

实验名称：qHTS for Inhibitors of human tyrosyl-DNA phosphodiesterase 1 (TDP1): qHTS in cells in... 来源：NCGC 靶标：TDP1 protein [Homo sapiens] External Id：TDP1101

实验名称：Primary cell-based high-throughput screening for identification of compounds that all... 来源：Johns Hopkins Ion Channel Center 靶标：MAS-related GPR member X1 [Homo sapiens] External Id：JHICC_MrgX1_AlloAgonist_Primary

实验名称：Primary cell-based high-throughput screening for identification of compounds that ant... 来源：Johns Hopkins Ion Channel Center 靶标：MAS-related GPR member X1 [Homo sapiens] External Id：JHICC_MrgX1_Antagonist_Primary

实验名称：qHTS for Inhibitors of AMA1-RON; Towards Development of Antimalarial Drug Lead: Prima... 来源：NCGC 靶标：apical membrane antigen 1, AMA1 [Plasmodium falciparum 3D7] External Id：AMA1100

实验名称：Inhibition of recombinant PTP1B catalytic domain (unknown origin) assessed as reducti... 来源：ChEMBL 靶标：Tyrosine-protein phosphatase non-receptor type 1 External Id：CHEMBL4832443

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英文别名

• Mulberrochromen
• mulberrochromene
• 2-(2,4-dihydroxy-phenyl)-5-hydroxy-8,8-dimethyl-3-(3-methyl-but-2-enyl)-8H-pyrano[3,2-g]chromen-4-one
• 2-(2,4-Dihydroxy-phenyl)-5-hydroxy-8,8-dimethyl-3-(3-methyl-but-2-enyl)-8H-pyrano[3,2-g]chromen-4-one