1.Effects of a novel thiazolidinedione ANY_2 on glycometabolism in HepG_2 cells
Haiqi QIAO ; Guanzhong WU ; Hongxia YANG
Chinese Journal of Clinical Pharmacology and Therapeutics 1999;0(04):-
AIM:To investigate the effects of a novel thiazolidinedione ANY2 on glycometabolism in HepG2 cells.METHODS:HepG2 cells are exposed to high concentrations of insulin for 24 h to build the model of insulin-resistance(IR-HepG2).The effects of ANY2,including glucose consumption(GC),gluconeogenesis and glucolysis were tested in this model.RESULTS:ANY2 could dose-dependently enhance GC in IR-HepG2 cells at high,medium and low levels of glucose.Compared with Modle Group,ANY2 increased IR-HepG2 cells glycogen synthesis significantly only in high dose group.It inhibited gluconeogenesis from lactic acid,but increased the production of lactic acid and the activity of pyruvate kinase(PK)in glucolysis.CONCLUSION:Compound ANY2 has remarkable effects on improving glycometabolism in IR-HepG2 cells.
2.Study on Vasodilatory Effect of Oxysophocarpine on Isolated Thoracic Aortic Rings of Rats and Its Mechanism
Haiqi QIAO ; Lin YAN ; Yang YU ; Zhi CHANG ; Jialing WANG ; Yanmin PEI ; Ru ZHOU
China Pharmacy 2019;30(22):3057-3061
OBJECTIVE: To study the vasodilatory effect of oxysophocarpine (OSC) on isolated thoracic aortic rings of rats and its possible mechanism. METHODS: Thoracic aortic rings of rats were collected (called “vascular ring” for short). Using K-H nutrient solution as blank control and the diastolic rate as index, the effects of different concentrations (0.2-1.0 mg/mL) of OSC on normal vascular rings in basal state, normal or endothelium-free vascular rings pre-contracted by norepinephrine (PE, 1×10-6 mol/L) were investigated. After pre-culturing normal thoracic aortic rings by nitric oxide synthase inhibitor L-nitro-arginine methyl ester(L-NAME)and cyclooxygenase inhibitor indomethacin(INDO),as well as pre-culturing endothelium-free vascular rings by potassium ion channel blocker BaCl2,tetraethylammonium(TEA)and 4-aminopyridine(4-AP), the diastolic effects of OSC of different concentrations (0.2-1.0 mg/mL) on the above vascular rings were investigated by using the same method. RESULTS: Compared with blank control, there was no significant effects of different concentrations of OSC on the diastolic rate of normal vascular rings in basal state (P>0.05), but 0.4-1.0 mg/mL OSC could significantly improve the diastolic rate of normal or endothelium-free vascular rings pre-contracted by PE (P<0.01), in concentration-dependent manner. After preculturing with L-NAME, INDO, 4-AP and BaCl2, different concentrations of OSC had no significant effect on the diastolic rate of normal or endothelium-free vascular rings pre-contracted by PE (P>0.05). After pre-culturing with TEA and Gli, 0.4-1.0 mg/mL OSC could significantly reduce the diastolic rate of endothelium-free vas- cular rings pre-contracted by PE (P<0.01). CONCLUSIONS: OSC did not significantly dilate the thoracic aortic rings of rats in the basal state within the dose range (0.2-1.0 mg/mL), but OSC of 0.4-1.0 mg/mL have significant diastolic effects on the normal or endothelium-free thoracic aortic rings of rats pre-contracted with PE. The mechanism of thoracic aortic rings dilation is endothelium-independent, which may be associated with receptor operational calcium channel,Ca2+-activated potassium channels and ATP-sensitive potassium channels.