Electrophysiological effects of anthopleurin-Q on rat hepatocytes

• Published in: World journal of gastroenterology : WJG Vol. 10; no. 1; pp. 96 - 99
• Main Authors: Zhou, Hong-Yi, Wang, Fang, Zhang, Ke-Qiang, Cheng, Lan, Zhou, Ji, Fu, Li-Ying, Yao, Wei-Xing
• Format: Journal Article
• Language: English
• Published: United States Department of Pharmacology, Tongji Medical College of Huazhong University of Science and Technology, Wuhan 430030, Hubei Province, China%Department of Infectious Diseases, Jianghan Oil Field Central Hospital, Qianjiang 433124, Hubei Province, China 2004; Baishideng Publishing Group Inc
• Subjects: Alanine Transaminase - blood; Animals; Aspartate Aminotransferases - blood; Basic Research; Calcium - metabolism; Calcium Channels - metabolism; Carbon Tetrachloride; Chemical and Drug Induced Liver Injury; Female; Hepatocytes - drug effects; Hepatocytes - physiology; Liver Diseases - drug therapy; Liver Diseases - physiopathology; Male; Membrane Potentials - drug effects; Mice; Mice, Inbred Strains; Patch-Clamp Techniques; Peptides - pharmacology; Potassium - metabolism; Potassium Channels, Inwardly Rectifying - metabolism; Rats; Rats, Wistar; 动物实验; 海葵素-Q; 生物化学; 电生理学; 肝功能; 肝实质细胞
• ISSN: 1007-9327; 2219-2840
• DOI: 10.3748/wjg.v10.i1.96

AIM: To study the effects of AP-Q on CCl4-induced acute liver injury, delayed outward potassium current (Iκ), inward rectifier potassium current (Iκ1) and calcium release-activated calcium current (ICRAC) in isolated rat hepatocytes. METHODS: A single dose of CCl4 (10 μg/mL, ip) was injected to induce acute liver injury in rats. Serum aminotransferase activities were determined. Whole cell patch-clamp techniques were used to investigate the effects of AP-Q on delayed outward potassium current (Iκ), inward rectifier potassium current (IKI) and calcium release-activated calcium current (ICRAC). RESULTS: AP-Q (3.5 and 7 μg/kg) pretreatment significantly reduced ALT and AST activities. AP-Q 0.1-100 nM produced a concentration-dependent increase of Iκ with EC50 value of 5.55±1.8 nM (n=6). AP-Q 30 nM shifted the I-V curve of Iκ leftward and upward. CCl4 4 mM decreased Iκ current 28.6±0.5% at 140 mV. After exposure to CCl4 for 5 rain, AP-Q 30 nM attenuated the decrease of Iκ induced by CCl4 close to normal amplitude. AP-Q 0.01-100 nM had no significant effect on either inward or outward components of Iκ1 at any membrane potential examined. AP-Q 0.1-100 nM had no significant influence on the peak amplitude of ICRAC, either,and did not affect the shape of its current voltage curve. CONCLUSION: AP-Q has a protective effect on CCl4-induced liver injury, probably through selectively increased Iκ in hepatocytes.