CAS |
113558-15-9 |
Chinese Name |
宝藿苷Ⅰ |
English Name |
Baohuoside I |
Synonyms |
宝藿苷I;淫羊藿次苷II;宝藿苷Ⅰ; |
Molecular Formula |
C27H30O10 |
Molecular Weight |
514.52 |
Solubility |
Soluble in DMSO |
Purity |
HPLC≥98% |
Appearance |
Light yellow to yellow Solid |
Storage |
Powder:2-8℃,2 years;Insolvent(Mother Liquid):-20℃,6 months;-80℃,1 year |
MDL |
MFCD15071140 |
InChIKey |
NGMYNFJANBHLKA-LVKFHIPRSA-N |
InChI |
InChI=1S/C27H30O10/c1-12(2)5-10-16-17(28)11-18(29)19-21(31)26(37-27-23(33)22(32)20(30)13(3)35-27)24(36-25(16)19)14-6-8-15(34-4)9-7-14/h5-9,11,13,20,22-23,27-30,32-33H,10H2,1-4H3/t13-,20-,22+,23+,27-/m0/s1 |
PubChem CID |
5488822 |
Target Point |
CXCR |
Passage |
Immunology & Inflammation;GPCR & G Protein |
Background |
Baohuoside I, a flavonoid, is an inhibitor of CXCR4. |
Biological Activity |
Baohuoside I 是从朝鲜淫羊藿中得到的黄酮类化合物,作为 CXCR4 的抑制剂,能够抑制 CXCR4 的表达,诱导凋亡,具有抗肿瘤活性。[1-3] |
In Vitro |
宝霍赛德I是CXCR4的抑制剂,并在12-25μM下调CXCR4表达。宝霍赛德I(0-25μM)以剂量依赖性方式抑制NF-κB活化,抑制CXCL12诱导宫颈癌细胞的侵袭。宝霍赛德我也抑制乳腺癌细胞的侵袭[1]。宝霍赛德I抑制A549细胞活力,24小时,11.5μM和9.6μM的48小时和72小时的IC50分别为25.1μM。宝霍赛德I((25μM)抑制A549细胞中的caspase级联,提高ROS水平并激活JNK和p38MAPK信号级联反应[2]。宝霍赛德I(3.125,6.25,12.5,25.0和50.0μg/ mL)显著且剂量依赖性阻断食管鳞状细胞癌Eca109细胞的生长,48小时IC50为4.8μg/ mL [3]。 |
In Vivo |
宝霍赛德I(25 mg/kg)可降低裸鼠体内β-catenin蛋白水平,cyclin D1和survivin的表达[3]。 |
Cell Experiment |
通过MTT测定法测定了宝霍赛德I对A549细胞的细胞毒作用。将细胞(1×10 4个细胞/孔)接种在96孔板中,并用宝华苷I(6.25,12.5和25μM)或1mM NAC处理24,48或72小时。除去含MTT的培养基后,通过向每个孔中加入DMSO溶解已形成的晶体。混合后,使用Multiskan Spectrum Microplate Reader [2]在540 nm处测量细胞的吸光度。 |
Animal Experiment |
小鼠[3]雌性Balb/c裸鼠(4-6周龄)用于测定。收获亚汇合的Eca109-Luc细胞并重悬于PBS中至最终密度为2×10 7个细胞/ mL。在注射之前,将细胞重悬于PBS中并通过0.4%台盼蓝排除测定法(活细胞> 90%)进行分析。对于皮下注射,使用27G针将200μLPBS中的1×107个Eca109-Luc细胞注射到每只小鼠的左侧腹中。在肿瘤细胞注射后1周,每天一次在病灶内注射宝霍赛德I(每只小鼠25mg/kg),而用于载体治疗的10只小鼠给予等体积的PBS [3]。 |
Data Literature Source |
[1]. Kim B,et al. Baohuoside I suppresses invasion of cervical and breast cancer cells through the downregulation of CXCR4 chemokine receptor expression. Biochemistry. 2014 Dec 9;53(48):7562-9. [2]. Song J,et al. Reactive oxygen species-mediated mitochondrial pathway is involved in Baohuoside I-induced apoptosis in human non-small cell lung cancer. Chem Biol Interact. 2012 Jul 30;199(1):9-17. [3]. Wang L,et al. The flavonoid Baohuoside-I inhibits cell growth and downregulates survivin and cyclin D1 expression in esophageal carcinoma via β-catenin-dependent signaling. Oncol Rep. 2011 Nov;26(5):1149-56. |
Unit |
Bottle |
Specification |
5mg 10mM*1mL in DMSO 10mg |