7380-40-7
基本信息
香柠檬素
佛手柑亭
佛手柑素
佛手柑素对照品
佛手柑素标准品
佛手柑素,佛手柑亭
佛手柑亭、香柠檬素、香柠檬亭
RHO GTP酶激活蛋白5抗体
佛手柑亭、香柑素、香柠檬素、香柠檬亭、5-牻牛儿醇基补骨脂素
p190-B
ARHGAP5
RhoGAP5
BERGAPTIN
BERGAMOTIN
Bergaptine
BERGAMOTINE
BERGAMOTTIN
AKOS 214-13
物理化学性质
常见问题列表
CYP1A1 10.703 nM (Ki) |
CYP1A1 0.192 μM (IC 50 ) |
CYP1A2 5.077 μM (IC 50 ) |
CYP2B2 4.535 μM (IC 50 ) |
CYP2B1 9.495 μM (IC 50 ) |
Bergamottin is a competitive inhibitor of CYP1A1. Bergamottin inhibits CYP1A1, CYP1A2, CYP2B1, and CYP2B2 with IC 50 s of 0.192±0.029 μM, 5.077±0.31 μM, 9.495±0.979 μM, 4.535±0.092 μM, respectively. Bergamottin has potent antiproliferative effects on the A549 cells. Bergamottin shows both concentration-dependent as well as time‑dependent growth inhibitory effects against these cells. Bergamottin also inhibits the clonogenic activity of the A549 cancer cells by reducing the number of cancer colony forming cells. A reduction in clonogenicity also follows the concentration dependence on Bergamottin.
The anticancer efficacy of Bergamottin under in vivo conditions using female BALB/c nude mice (a total of 20 mice are used) is determined. Tumors are induced in the mice by injecting non-small cell lung cancer A549 cells (1×10 6 cells/mouse). After tumor formation, the mice are sacrificed and tumors are removed and their weights and volumes are calculated. The results show that 25, 50 and 100 mg/kg Bergamottin injection reduce the tumor weight from 1.61 g in the PBS-treated group (control) to 1.21, 0.42 and 0.15 g, respectively. Tumor weight in the nude mice is reduced much more significantly in the highest-concentration Bergamottin group (100 mg/kg body weight) compared with the vehicle group (P<0.05). Likewise, 25, 50 and 100 mg/kg Bergamottin injection reduces the tumor volume from 2.2 cm 3 in the PBS-treated group (control) to 1.71, 1.1 and 0.51 cm3, respectively. The periodic measurement of the tumor xenograft volume indicates that the tumor volume in the nude mice is reduced considerably in the highest-concentration Bergamottin group (100 mg/kg body weight) compared with the vehicle group (P<0.05).