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Zhang L.,Chongqing Medical University | Li H.-Z.,Chongqing Medical University | Li H.-Z.,Chongqing Pharmaceutical Research Institute | Gong X.,Chongqing Medical University | And 6 more authors.
Phytomedicine | Year: 2010

Asiaticoside (AS), a triterpenoid product isolated from Centella asiatica, has been described to exhibit anti-inflammatory activities in several inflammatory models. However, the effects of AS on liver injury are poorly understood. The present study was undertaken to investigate whether AS is efficacious against Lipopolysaccharide (LPS)/D-galactosamine (D-GalN)-induced acute liver injury in mice and its potential mechanisms. AS (5,10 and 20 mg/kg/d) was pretreated orally once daily for 3 days before LPS/D-GalN injected in mice. The mortality, hepatic tissue histology, plasma levels of Tumor necrosis factor- alpha (TNF-α) and alanine aminotransferase (ALT) and aspartate aminotransferase (AST), hepatic tissue TNF-α and caspase-3 activity were measured. Besides, western blotting analysis of phospho-p38 mitogen-activated protein kinase (phospho-p38 MAPK), phospho-c-jun N-terminal kinase (phospho- JNK) and phospho-extracellular signal regulated kinase (phospho-ERK) were determined. As a result, AS showed significant protection as evidenced by the decrease of elevated aminotransferases, hepatocytes apoptosis and caspase-3, alleviation of mortality and improvement of liver pathological injury in a dose-dependent manner. Further, we found that AS dose-dependently reduced the elevation of phospho-p38 MAPK, phospho-JNK, phospho-ERK protein and TNF-α mRNA expression in liver tissues and plasma TNF-α. These results suggest that AS has remarkable hepatoprotective effects on LPS/D-GalN-induced liver injury and the possible mechanism is related to inhibition of TNF-α and MAPKs. © 2010 Elsevier GmbH. Source

Gong X.,Chongqing Medical University | Luo F.-l.,Chongqing Medical University | Zhang L.,Chongqing Medical University | Li H.-z.,Chongqing Medical University | And 8 more authors.
International Immunopharmacology | Year: 2010

Fulminant hepatic failure (FHF) remains an extremely poor prognosis and high mortality; better treatments are urgently needed. Tetrandrine (TET), a traditional anti-inflammatory drug, has been reported to exhibit hepatoprotective activities in several liver injury models. We now investigated the effects and underlying mechanisms of TET on lipopolysaccharide (LPS) and d-galactosamine (d-GalN)-induced FHF in mice. TET (50, 100, and 200 mg/kg) was given intraperitoneally 1 h before LPS/d-GalN injection in mice. The mortality and liver injury was evaluated subsequently. The results showed that administering TET to mice reduced mortality and improved liver injury induced by LPS/d-GalN in a dose-dependent manner. In addition, TET dose-dependently inhibited LPS/d-GalN-induced NF-κB activation, serum and hepatic tissues tumor necrosis factor-α (TNF-α) production, caspase-3 activation and hepatocellular apoptosis, myeloperoxidase (MPO) activity, intercellular adhesion molecule-1 (ICAM-1) and endothelial cell adhesion molecule-1 (ECAM-1) expression. Our experimental data indicated that TET might alleviate the FHF induced by LPS/d-GalN through inhibiting NF-κB activation to reduce TNF-α production. © 2009 Elsevier B.V. All rights reserved. Source

Jin N.-S.,Chongqing Medical University | Dong Z.,Chongqing Medical University | Fu J.-M.,Chongqing Pharmaceutical Research Institute | Zeng F.-X.,Chongqing Pharmaceutical Research Institute
World Chinese Journal of Digestology | Year: 2010

Inflammatory bowel disease (IBD) is a chronic, debilitating disease associated with severe damage to the intestinal mucosa whose etiology is still unknown. The two most common forms of IBD are ulcerative colitis (UC) and Crohn's disease (CD). DPP-4 inhibitors are a new class of agents developed for treatment of diabetes. However, recent studies have indicated that DPP-4 inhibitors have therapeutic effects against IBD in animal models. This may provide a new avenue to cure IBD. Source

Long B.,Chongqing Cancer Institute | Su Y.-Q.,Chongqing Medical and Pharmaceutical College | Xia Y.,Chongqing Medical and Pharmaceutical College | Zou Y.-Y.,Chongqing Pharmaceutical Research Institute | And 3 more authors.
International Journal of Clinical Pharmacology and Therapeutics | Year: 2016

Purpose: The aim of this study was to investigate the sex-dependent difference in P-glycoprotein activity as measured by the probe drug talinolol. Methods: A randomized, single-blind, parallel study was carried out in 20 healthy male and 20 healthy female volunteers. The pharmacokinetics of talinolol were measured after single oral dosing of 50-mg tablet and the pharmacokinetic parameters for male and female subjects were compared after excluding the potential influence of P-gp genetic polymorphisms. Results: Talinolol AUC0- 48h in the female subjects was 23.5% (p = 0.003) higher than that of male subjects. There was no significant sex difference in weight-corrected oral clearance, AUC, or other PK parameters. Conclusion: The AUC and other PK data of talinolol, corrected for body weight, did not differ between genders after oral administration. The observed sex difference in talinolol systemic exposure is of little clinical relevance. The overall activity of P-gp shows no sex-related difference. © 2016 Dustri-Verlag Dr. K. Feistle. Source

Lin Y.,Chongqing Pharmaceutical Research Institute | Zou Y.,Chongqing Pharmaceutical Research Institute | Lin J.,Chongqing Pharmaceutical Research Institute | Zhang T.,Chongqing Pharmaceutical Research Institute | Deng J.,Chongqing Pharmaceutical Research Institute
Xenobiotica | Year: 2013

1. A rasagiline transdermal patch was developed for the treatment of early and advanced Parkinson's disease. Relevant pharmacokinetic parameters of rasagiline obtained after transdermal administration to minipigs were compared with those of rasagiline after oral administration. 2. A total of 18 minipigs were randomly divided into three groups (six animals for each group). A single dose of 1mg rasagiline tablet was orally administrated to one group. Meanwhile, single dose of 1.25 and 2.5mg (2 and 4cm2) rasagiline patches were given (at the postauricular skin) to the other two groups, respectively. The pharmacokinetic parameters such as plasma half-life (t1/2), time to peak plasma-concentration (Tmax), mean residence time (MRT), area under the curve (AUC(0-t)) were significantly (p< 0.05) different between transdermal and oral administrations. 3. The plasma half-life (t 1/2) of rasagiline (1.25mg patch: 11.8± 6.5h, 2.5mg patch: 12.5 ± 4.7 h) in minipig following transdermal administration was significantly prolonged as compared with that following the oral administration (1 mg tablet: 4.7 ± 2.5 h). The dose-normalized relative bioavailability of rasagiline patch in minipig were 178.5% and 156.4%, respectively, for 1.25 and 2.5 mg patches compared with 1 mg rasagiline tablet. The prolonged t1/2 and increased bioavailability of rasagiline patch suggested a possible longer dosing interval compared with oral tablet. © 2013 Informa UK Ltd. All rights reserved. Source

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