Metabolic pathways of dipfluzine in rats / 药学学报

<p><b>AIM</b>To investigate the metabolic pathways of dipfluzine in rats.</p><p><b>METHODS</b>After an oral dose of dipfluzine (80 mg x kg(-1)) to rats, urine was collected for 12 h. The metabolites of dipfluzine in urine were chromatographed and identified by LC/DAD/MS methods.</p><p><b>RESULTS</b>In the rat urine, there were 1-(4-fluorophenyl)-4-piperazinylbutanone and its glucuronide, 4-hydroxybenzophenone and its glucuronide, 4-fluoro-gamma-hydroxybenzenebutanoic acid and its glucuronide and sulfate, diphenylmethanol and its glucuronide, dipfluzine, and benzophenone.</p><p><b>CONCLUSION</b>In rats, dipfluzine was mainly metabolized in the pathways of N-desalkylation at 1- and 4-positions of piperazine ring. Some of metabolites were further conjugated with glucuronic acid and/or sulfuric acid.</p>

Effect of intra-articular carboxymethylated chitosan injection on nitric oxide synthase expression in cartilage of osteoarthritis in a rabbit model / 中华风湿病学杂志

Objective To investigate the effect of intra-articular carboxymethylated ehitosan(CM- CTS)injection on inducible nitric oxide synthase(iNOS)expression in cartilage at the early stage of os- teoarthfitis(OA).Methods Thirty-two white rabbits were underwent unilateral anterior cruciate ligament transection(ACLT)and were randomly divided into 4 groups 5 weeks after transection.Rabbits of group A re- ceived 0.3 ml of 2% high molecular weight CMCTS(H-CMCTS)once every two weeks.Rabbits in group B were treated using 2% low molecular weight(L-CMCTS)CMCTS at:the same intervals.Group C rabbits were injected intra-articularly with 0.3 ml of 1% sodium hyaluronate(Na-HA)once a week.Animals of group D were not injected.At sacrifice,11 weeks following surgery,the expression of iNOS in cartilages was analyzed by immunohistochemistry and reverse transcription-polymerase chain reaction(RT-PCR)methods.Results Both immunohistochemistry and RT-PCR showed that the level of iNOS expression of cartilage in CMCTS in- jection groups was lower than that in Na-HA injection group and the untreated group.There was no significant difference in iNOS expression between the two different molecular weight CMCTS injection groups. No signifi- cant difference of iNOS expression in cartilage was found between Na-HA injection group and the untreated group.Conclusion CMCTS suppresses iNOS expression in cartilage during the early stage of OA.Na-HA treatment has no effect on iNOS expression in cartilage.

Study on mechanism of inhibitory effect of carboxymethyl-chitosan on the chondrocytes apoptosis induced by interleukin-1? / 中华风湿病学杂志

Objective To study the influence of carboxymethyl-chitosan(CM-chitosan)on chondro- cyte apoptosis induced by recombinant human interleukin-1?(rhIL-1?)and explore its mechanism.Methods Rabbit chondrocytes were isolated and cultured.Chondrocytes were pretreated with different concentrations of CM-chitosan for 1 h,then 10 ng/ml IL-1?were added into the culture medium.After 24 h,the apoptotic rates of chondrocytes were measured by flow cytometry with AnnexinⅤ-FITC and PI staining.The morphology of nuclei was observed by fluorescent microscopy with Hoechst 33342 staining.The mitochondrial membrane po- tentials were tested by confocal laser scanning microsocopy with Rhodamine-123 and ATP contents were mea- sured by luciferase reaction.Results CM-chitosan could inhibit chondrocyte apoptosis and restore the func- tion of mitochondria induced by IL-113 in a dose-dependent manner.Conclusion CM-ehitosan can inhibit chondrocyte apoptosis by protecting mitochondrial function.