Objective To study the effect of SYUIQ-5,a novel antitumor agent,on gene expression of hepatic cytochrome P450 in rats.Methods Male Sprague-Dawley rats were administered daily intraperitoneal dose of SYUIQ-5(0.1mg/kg,5mg/kg and 10mg/kg body weight) for 5 consecutive days.The levels of CYP 3A1,2B1/2,1A1,1A2 and 2E1 mRNA in rat liver were analyzed by reverse transcription-polymerase chain reaction(RT-PCR).Results The level of gene expression of CYP 1A1 was increased significantly compared with the control.The levels of CYP 3A1,2B1/2,1A2 and 2E1 mRNA were not changed by SYUIQ-5 treatment compared with the control.Conclusion A significant increase in the CYP 1A1 rather than CYP3A1,2B1/2,1A2 and 2E1 gene expression by SYUIQ-5 treatment is observed.

0.05). The generation of ROS increased obviously after the cells were incubated with them for 12 h, and the increase of ROS reached the peak treated for 24 h. The levels of ?? m were time-dependently decreased after treating with four compounds for 12, 24, and 48 h. Conclusion The grouth of both MDR KBv200 cells and parental drug-sensitive KB cells were inhibited to the treatment of four anthraquinone derivative in vitro. The mechanism of their effects is associated with the increase of the cellular ROS level and the decrease of ?? m.

OBJECTIVETo study the anti-cataract effect of gigantol combined with syringic acid and their action mechanism.

METHODH202-induced lens oxidative injury in vitro rat model was establish to observe the impact of gigantol combined with syringic acid on lens transparency under a dissecting microscope. D-galactose-induced cataract rat model was established to observe the impact of gigantol combined with syringic acid on lens transparency under a slit-lamp. UV spectrophotometry was adopted to detect the inhibitory activity of gigantol combined with syringic acid against AR. Molecular docking method was used to detect binding sites, binding types and pharmacophores of gigantol combined with syringic acid in prohibiting aldose reductase.

RESULTBoth in vitro and in vivo experiments showed a good anti-sugar cataract activity in the combination of gigantol and syringic acid and a better collaborative effect than single component-gigantol and syringic acid and positive control drug Catalin. Molecular docking and dynamic simulation showed their collaborative AR-inhibiting amino acid residue was Asn160 and the major acting force was Van der Waals' force, which formed common pharmacophores.

CONCLUSIONGigantol combined with syringic acid shows good anti-cataract, their action mechanism is reflected in their good collaborative inhibitory effect on AR.

Aldehyde Reductase ; antagonists & inhibitors ; Animals ; Bibenzyls ; Cataract ; drug therapy ; enzymology ; Drug Synergism ; Female ; Gallic Acid ; analogs & derivatives ; pharmacology ; Guaiacol ; analogs & derivatives ; pharmacology ; Humans ; In Vitro Techniques ; Lens, Crystalline ; drug effects ; enzymology ; Male ; Rats ; Rats, Wistar