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Aim To study the analgesic effect of geraniol on neuropathic pain and to explore the possible mechanism.Method A neuropathic pain rat model of Spared Nerve Injury(SNI) was established to measure changes in the threshold of paw withdrawal before and after i.p.administration of geraniol.Patch clamp whole-cell recording was performed to measure activity of sodium channels using ipsilateral L3/L4/L5 dorsal root ganglion(DRG) cells isolated from the SNI rats.In addition, HEK 293 cells expressing hNav1.7 and hTRPA1 channels were used for measuring the changes in channel activities with or without geraniol by whole-cell patch clamp.Results Geraniol had a fast analgesic effect on hypersensitivity of mechanical pain in the SNI model.It significantly inhibited sodium channels on DRGs isolated from SNI rats and hNav1.7 but not hTRPA1 channels expressed by HEK293 cells.However, high concentrations of geraniol facilitated the activation of HTRPA1 channel stimulated by AITC.Conclusion Geraniol may abirritate hypersensitivity of mechanical pain in the SNI model by specifically inhibiting Nav1.7 channel activity on the DRG cells.
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Objective To study the relationship between expression of cyclooxygenase-2 (COX-2) and vas-culax endothelial growth factor (VEGF) with liver sinusnidal capillarization (LSC) of chronic hepatitis B (CHB). Methods We studied liver biopsies from 200 patients with CHB COX-2 ,VEGF immunohistochemical stain were ob-served to accomplish relationship between expression of COX-2,VEGF and LSC. Results LSC occupy above 80% in the group. There were manifestation in mild-LSC (focal) , middle-LSC (sheet-shape) and severe-LSC (widespread). Electron microscope shown the laceration in the endothelium of sinuses and formation of basal lamina and budding for-mation lumen of blood vessel and fat-storing cell convert myofibroblast. Expression of COX-2, VEGF, Co-Ⅳ and retic-ulum, collagen and elastic fibers with mild or severe in LSC is manifest locking relate. Conclusion Increased ex-pression of COX-2 ,VEGF in liver tissue of CHB may facilitate LSC and hepatic fibrosis.
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Objective To observe the correlation of histologicalactivity(HAI) of chronic hepatitis B (CHB) with CCL20 expression, and to investigate the impact of CCL20 expression in CHB infection. Methods On the basis of established competitive quantitative RT-PCR with an internal standard, the expression of the CCL20 in the hepatocytes in different infected patterns of HBV infected cells and liver biopsies were quantified and at the same time its correlation to HAI were explored. Results In the cell levels, the expression quantity of CCL20 in control cells (HepG2), persistent HBV infected hepatocytes( HepG2. 2. 15) are (2. 65 ± 0. 02) pg/106 cells, ( 1.22± 0. 04) pg/106 cells, respectively. There were significantly differences between them ( t = 39. 66, P < 0. 01 ). The expression of CCL20 was enhanced in hepatocytes stimulated by PMA but their expression pauern was not changed. Moreover, CCL20 expression in liver biopsies with CHB was (3.54 ± 0. 65 ) pg/20 mg and CCL20 expression in control groups was ( 8. 74±0. 56) pg/20 mg. The expression of CCL20 between two groups was different (t =30. 09,P <0. 01 ) and correlation lied in between HAI and CCL20 expression in liver biopsies of CHB patients ( r = 0. 675, P =0. 023 ). Conclusion CCL20 expression was down-regulated and it was correlated to HAI of liver biopsies in CHB patients.
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AIM To study the pharmacokinetics and bioavailability of clinafloxacin in rats. METHODS The drug concentration was determined by HPLC. The main pharmacokinetic parameters were obtained by 3P87 program. An RP-C18 was used as the stationary phase. The mobile phase was a mixture of acetonitrile-0.05 mol*L-1 citric acid triethylamine (pH 2.5) (20∶80). The flow rate was 1.0 mL*min-1. The UV absorbance detector was set at 300 nm. RESULTS A good linearity was obtained from 0.03-20 μg*mL-1 of clinafloxacin in rat plasma with γ=0.9998. The plasma concentration-time curve of clinafloxacin conformed to one compartment open model. After ig administration of 50 mg*kg-1 and 100 mg*kg-1 dose of clinafloxacin in six rats, mean Cmax and AUC values increased in proportion to dose. Mean T1/2 appeared to be independent of dose. Mean AUC was 65±6 and 27±4 μg*h*mL-1 respectively after iv and ig adminostration of 100 mg*kg-1 dose. The extent of bioavailability (F) of clinafloxacin was 42%. CONCLUSION The results of the pharmacokinetic study of clinafloxacin showed that it exhibited first order kinetic characteristics and the bioavailability is low.