肉盘菌内酯
- CAS号:133613-71-5
- 英文名:galiellalactone
- 中文名:肉盘菌内酯
- CBNumber:CB21397587
- 分子式:C11H14O3
- 分子量:194.23
- MOL File:133613-71-5.mol
- 沸点 :400.7±38.0 °C(Predicted)
- 密度 :1.29±0.1 g/cm3(Predicted)
- 储存条件 :Store at -20°C
- 溶解度 :DMSO:0.97(Max Conc. mg/mL);4.99(Max Conc. mM)
Ethanol:0.97(Max Conc. mg/mL);4.99(Max Conc. mM) - 形态 :White to light tan solid.
- 酸度系数(pKa) :12.48±0.40(Predicted)
肉盘菌内酯性质、用途与生产工艺
- 生物活性 Galiellalactone 是一种小的无毒且无致突变性的真菌代谢产物，是一种选择性的 STAT3 信号抑制剂，IC50 值为 250-500 nM。Galiellalactone 可用于研究去势抵抗性前列腺癌。
-
靶点
STAT3
250-500 nM (IC 50 )
-
体外研究
Galiellalactone (2.5-25 μM; 24-72 hour) induces apoptosis of prostate cancer (PCa) cell lines expressingp-Stat3.
Galiellalactone (2.5-25 μM; 24-72 hour) decreases viability of DU145 cells.
Galiellalactone (10 μM) inhibits STAT3 signaling activity as assessed by luciferase reporter gene assay in IL-6-stimulated LNCaP cells.
Galiellalactone (10-100 μM; 1 hour) binds directly to STAT3 in DU145 cells .
Galiellalactone (5-50 μM; 1 hour) interferes with STAT3 DNA binding without inhibiting phosphorylation in DU145 cells .Apoptosis Analysis
Cell Line: DU145, PC-3, and LNCaP cells Concentration: 0, 2.5, 5, 10, 25 μM Incubation Time: 24, 48, 72 hours Result: Induced an apoptotic response in PC-3 and DU145 cells. Cell Viability Assay
Cell Line: DU145 cells Concentration: 0, 2.5, 5, 10, 17.5, 25 μM Incubation Time: 24, 48, 72 hours Result: Decreased DU145 cells viability in a dose- and time-dependent manner. Western Blot Analysis
Cell Line: DU145 cells Concentration: 0, 10, 25 μM Incubation Time: 48 hours Result: Induced expression of the apoptotic marker cleaved caspase-3 and increased expression of cleaved PARP. Western Blot Analysis
Cell Line: DU145 cells Concentration: 0, 10, 25, 50, 100 μM Incubation Time: 1 hour Result: Prevented the binding of the biotinylated analogue of galiellalactone (GL-biot) to STAT3 in a dose-dependent manner demonstrating competitive binding. Western Blot Analysis
Cell Line: DU145 cells Concentration: 0, 5, 10, 25, 50 μM Incubation Time: 1 hour Result: Inhibited STAT3 binding to DNA in a dose-dependent manner.
Did not affect phosphorylation of STAT3 Tyr-705 and Ser-727 or the expression of total STAT3. -
体内研究
Galiellalactone (1, 3 mg/kg; daily i.p. for 3 weeks) inhibits PCa tumor growth in vivo.
Animal Model: Male nude NMR1 mice are injected PCa cell Dosage: 0, 1, 3 mg/kg Administration: Daily i.p. injections for 3 weeks Result: Reduced the tumor growth rate in DU145 xenografts by 41-42% and was well tolerated.
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