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OBJECTIVE：To study the effect of isofla vaspidicacid PB （called PB for short ）on the biofilm adhesion and the gene expression of ergosterol metabolism related enzymes in Trichophyton rubrum . METHODS ：M38-A2 method was adopted to determine MIC of PB to T. rubrum . MTT assay was used to screen the biolfilm condition and initial adhesion period of T. rubrum . The effects of different concentrations of PB （40，80，160 µg/mL）on the adhesion duration of T. rubrum （growth control group without PB was set up ，similarly hereinafter ）were evaluated and the adhesion rate was calculated by using XTT assay ；the effects of different concentrations of PB （20，40，80 µg/mL）on the biofilm formation of T. rubrum at different initial adhesion periods （3，5，9 h）were observed and the adhesion rate was calculated by using XTT assay combined with inverted microscope ；qRT-PCR method was used to detect the effects of PB （320 µg/mL）on the mRNA expression of ergosterol metabolism related enzyme gene ERG6 and ERG11 in biofilm of T. rubrum . RESULTS ：MIC of PB to T. rubrum was 20 µg/mL. The biofilm of T. rubrum in RPMI-1640 medium containing 10％ FBS was the most metabolism activity at 6 h of initial adhesion. Compared with growth control group ，after treated with different concentrations of PB ，adhesion rate and mRNA expression of ERG6 and ERG11 in biofilm were decreased significantly （P＜0.01）. Hyphae decreased or even disappeared ，and the adhesion inhibition rate （at 5 and 9 h of initial adhesion ）increased significantly （P＜0.05 or P＜0.01）. CONCLUSIONS ：PB can inhibit the adhesion of T. rubrum and reduce the hyphae ；the mechanism may be associated with the inhibition of the biofilm adhesion and mRNA expression of ergosterol metabolism related enzyme gene ERG6 and ERG11.
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OBJECTIVE：To study the toxicity mechanism of yunacotine-induced arrhythmia in rats. METHODS ：Totally 32 rats were randomly divided by random number table method into normal control group ，yunacotine low-dose and high-dose groups （0.09，0.14 mg/kg），aconitine group （positive control ，0.88 mg/kg），with 8 rats in each group. Administration groups were given the corresponding drugs once a day ，and normal control group was given the constant volume of normal saline ，for consecutive 7 d. After last intragastric administration ，the changes of electrocardiogram （ECG） were observed. The contents of adenosine triphosphate（ATP）in myocardial tissue and Ca 2+ in myocardial cells ，the activities of Na +-K+-ATPase and Ca 2+-Mg2+-ATPase as well as the protein expression of ranolidine receptor 2（RyR2）and Ca 2+-ATPase（SERCA2）in myocardial tissue were determined. RESULTS：Compared with normal control group ，time limit of QRS wave and QTc intervals of rats were prolonged significantly in yunaconitine low-dose group （P＜0.01）. The content of Ca 2 + in myocardial cells ， the ATP contents ， the activities of Ca2+-Mg2+-ATPase and Na +-K+-ATPase as well as the protein expression of SERCA 2 in myocardial tissue were reduced significantly （P＜0.05 or P＜0.01）. The heart rate of rats in yunaconitine high-dose group and aconitine group were increased significantly （P＜ 0.05 or P＜0.01），and time limit of QRS wave and QTc intervals were significantly prolonged （P＜0.01）；the content of Ca 2+ in myocardial cells was increased significantly （P＜0.01）；ATP content ，the activities of Ca 2+-Mg2+-ATPase and Na +-K+-ATPase，and protein expression of RyR 2 and SERCA 2 in myocardial tissue were decreased significantly （P＜0.01）. CONCLUSIONS ： Yunaconitine can induce arrhythmia in rats ，the mechanism of which may be associated with Ca 2+ overload that resulted from reducing the activities of Na +-K+-ATPase and Ca 2+-Mg2+-ATPase and down-regulating the expression of related calcium transporter RyR2 and SERCA 2.
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Aim To investigate the effect of SM-1 on seven main cytochrome P450(CYP450)in human liver microsomes.Methods Substrate or SM-1 was incubated with human liver microsomes for 30 min in vitro,and divided into control group and experimental group.The effects of SM-1 on the main phase I metabolic enzymes in human liver microsomes was detected by HPLC.Phenacetin,bupropion,paclitaxel,tolbutamide,omeprazole,dextromethorphan,testosterone were investigated as probe drugs.Results Inhibition rate of SM-1 on the classical substrate of human liver microsomal CYP was 0.05％,3.37％,0.08％,2.07％,4.20％,-0.15％and 10.84％,respectively.Conclusions SM-1 may have inhibitory effect on CYP3A4.Attention should be paid to the interaction of clinical drug induced by CYP enzyme inhibition.
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Objective To investigate the effects of four interior-warming drugs( galangal,cinnamon,evodia rutaecarpa,and dried ginger)on the tension of ileum smooth muscle and Ca2+-ATPase on the cell membrane in rabbits. Methods The effects of galangal,cinnamon,evodia rutaecarpa,and dried ginger were examined on normal ileum smooth muscle,in vitro intestinal muscle contraction caused by acetylcholine(ACh),barium chloride(BaCl2 )and histamine(His), and ACh-induced calcium release by using BL-420E+ biological signal collection and processing system.The average tension was measured within 1 min before delivery and within 3 minutes after the treatment,and the inhibition rate was calculated according to the average tension value.The effects of sera containing galangal,cinnamon,evodia rutaecarpa,and dried ginger on Ca2+-ATPase activity on the cell membrane of the intestinal smooth muscle were examined by phosphorus method. Results Galangal,cinnamon,evodia rutaecarpa,and dried ginger at high concentrations could restrain in vitro intestinal contraction in normal circumstances(P<0.05 or P<0.01).Significant inhibitory effects on intestinal contraction caused by ACh,His and BaCl2 were found in low,medium and high concentration groups(P<0.01).There was a dose-effectiveness relationship between the inhibition rate and final drug concentrations.The ACh-induced intracellular and extracellular calcium dependent contraction were significantly inhibited by the four interior-warming drugs( P < 0. 05 or P < 0. 01). The Ca2+-ATPase activities were( 0. 384 ± 0.070),(0.302±0.016),(0.307±0.016),(0.296±0.016),(0.313±0.003)U·mg-1 ,respectively,in intestinal smooth muscle in normal control group and high concentration groups of galangal,cinnamon,evodia rutaecarpa,and dried ginger(P<0.01). Conclusion Interior-warming drugs may relax intestinal smooth muscle by reducing the intracellular calcium release and the extracellular calcium inflow via receptor-controlled calcium channels,and inhibiting the Ca2+-ATPase activity in smooth muscle.
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Objective In this paper,we analyzed the initial review projects of clinical research during past five years in a hospital,which aims to summarize the experience and analysis existent problems,in order to provide a reference for the future hospital ethics review.Methods Summarizing and analyzing the meeting records during past five years,which were also in the field of the initial review projects of clinical research.Results Clinical trials of drug and divice,and clinical research projects exist in varying degrees of problems,which express in these two aspects:research design and ethical rational.Conclusions Ethics Committee should stengthen review the following two parts,the scientific of research project and the informed consent form.Improve their own system constantly,and ensure the efficient operation of the Ethics Committee.
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Objective To explore the application of projection pursuit model in anti-assessment on peer reviewer of scientific research project,discussing the rational of this application.Methods Establishing the projection pursuit model of anti-assessment on peer reviewer,with the best projection direction as a weight,making an evaluation on the peer reviewer,and sequencing experts by projection value.Results The projection pursuit model is stable and scientific,the importance of index ranking as correlation coefficient＞ dispersion＞ hit rate＞ synthetic dispersion＞ self dispersion ratio.Conclusions The application of projection pursuit model in anti-assessment on peer reviewer of scientific research project,is reasonable and practicable.
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OBJECTIVE@#To investigate the effects of 7-difluoromethy-5, 4'- dimethoxygenistein (DFMG) on inhibiting proliferation and inducing apoptosis of human cervical cancer HeLa cells and its possible molecular mechanism in vitro. @*METHODS@#HeLa cells were cultured in vitro. The effect of DFMG on inhibiting proliferation was determined using MTT assay. The effects of DFMG on inducing apoptosis were assessed using flow cytometry with AV-PI staining, AO/EB staining, and agarose gel electrophoresis. Multiple molecular techniques, such as RT-PCR, Western blot, siRNA transfection, and cDNA transfection, were used to explore its possible molecular mechanism. @*RESULTS@#DFMG presented with dramatically inhibiting proliferation effect of HeLa cells in a time-and dose-dependent manner ranging from 0.25 to 64 μg/mL and from 24 to 72 h in vitro, and its IC(50) was 4.62 μg/mL for 48 h. The cells treated with DFMG for 48 h showed typical morphological change of apoptosis, typical DNA ladder of agarose gel electrophoresis, and the sub-G(1) population increased in a dose-dependent manner. Simultaneously the expressions of c-myc mRNA, c-myc protein and its downstream genes, such as bax, cyto-c and caspase-9, were up-regulated, while bcl-2 protein was down-regulated. Down-regulation of c-myc by siRNA attenuated DFMG-induced cell proliferation inhibition and inducing apoptosis. Up-regulation expression of c-myc by cDNA transfection could enhance the effects of DFMG-induced cell proliferation inhibition and inducing apoptosis. @*CONCLUSION@#DFMG could inhibit the proliferation and induce the apoptosis of human cervical cancer HeLa cells in vitro, and its mechanism may be closely related to regulate c-myc and its down-stream gene expression.
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Female , Humans , Apoptosis , Caspase 9 , Metabolism , Cell Proliferation , Down-Regulation , Gene Expression Regulation, Neoplastic , Genistein , Pharmacology , HeLa Cells , Proto-Oncogene Proteins c-bcl-2 , Metabolism , Proto-Oncogene Proteins c-myc , Metabolism , Up-Regulation , Uterine Cervical Neoplasms , Pathology , bcl-2-Associated X Protein , MetabolismABSTRACT
Objective To observe the therapeutic effect of adjunctive treatment with Qiangzhu Recipe for ankylosing spondylitis(AS). Methods Forty-eight AS patients were evenly randomized into observation group and control group according to the admission order. The observation group was given Qiangzhu Recipe together with sulfasalazine and celecoxib orally, and the control group received oral use of sulfasalazine and celecoxib. Four weeks constituted one treatment course, and the treatment covered 3 courses. The main clinical outcomes of the patients included Bath AS functional index ( BASFI) , Bath AS disease activity index ( BASDAI) , pain visual analog scale ( VAS) scores, global VAS scores, spinal mobility indexes ( finger-to-floor distance, occiput -wall distance, thoracic mobility, Schober test, scoliolosis test) , and laboratory inflammatory indicators of erythrocyte sedimentation rate (ESR) and C-reactive protein. Moreover, the incidence of adverse reaction was also recorded. Results (1) After treatment for 4, 8, and 12 weeks, the percentage of the patients arriving at the degree of ASAS20 was 16.67%, 33.34%, and 70.83% respectively in the observation group, and was 8.33%, 29.17%, and 58.33% in the control group; the percentage of the patients arriving at the degree of ASAS40 was 4.17%, 20.83%, and 37.50% respectively in the observation group, and was 0.00%, 12.50%and 25.00% in the control group. The differences of the percentage of the patients arriving at the degree of ASAS20 and ASAS40 were insignificant between the two groups (P>0.05). (2) After treatment, symptoms were much relieved, spinal mobility was improved, and inflammatory indicators of ESR and CRP were alleviated in the two groups ( P0.05 compared with the control group). Conclusion Adjunctive treatment with Qiangzhu Recipe exerts certain synergistic action on sulfasalazine and celecoxib in treating ankylosing spondylitis.
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Objective To compare the pharmacokinetics difference of methotrexate ( MTX) alone or MTX combined with the decoction of Radix Salviae Miltiorrhizae ( RSM) in rats, and to investigate the possible impact of RSM on the efficacy and pharmacokinetics of MTX after oral administration. Methods Sprague-Dawley rats were given MTX (7 mg/kg) alone or MTX together with RSM (3.085 g/kg) respectively. At different time points, blood was sampled from orbital venous plexus and then was precipitated by perchloric acid. The serum concentration of MTX was determined by using high performance liquid chromatography ( HPLC) method. Chromatographic separation was achieved on a reversed-phase Diamonsil C18 (2) column with the mobile phase of methanol-formic acid water solution (formic acid in volume fraction of 0.1%) in gradient elution. The column temperature was 27 ℃, flow rate was 1 mL/min, detection wavelength was 302 nm, and the injection volume was 10 μL. The results were analyzed by pharmacokinetic software DAS ( 2.1.1) by non-compartment model. Results The linearity of the calibration curve for MTX was good in the range of 0.097 6 ~ 12.5 mg/L, the detection limit was 0.097 6 mg/L and the recovery was in the range of 77.5% ~ 86.6%. Compared with MTX group, the peak-arriving time of MTX-RSM group was advanced, and the clearance of MTX was delayed. Area under concentration-time curve at 0-t (AUC(0-t)) was increased by 0.609 times, and AUC(0-∞) was increased by 0.786 times. Conclusion The decoction of RSM exerts an effect on promoting the absorption of MTX, delaying the clearance of MTX and enhancing the bioavailability of MTX in vivo.
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This article reviewed the theories and current researches of Ryodoraku Diagnostic System and pointed out its value in clinical studies, as well as the feasibility and significance of applying this system on the studies of electricity of meridians and collaterals.
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OBJECTIVE: To establish the method for the dissolution determination of Eslicarbazepine acetate tablets.METHODS: Samples were collected at 30 min with phosphate buffer solution(pH=4.5) as solvent and rotation speed of 50 r?min-1 according to second dissolution determination method(slurry method) stated in Chinese Pharmacopeia(2010 edition).The absorbance of 3 batches of samples was determined by UV spectrophotometry at detection wavelength of 288 nm.RESULTS: The method showed a good linear relationship in the range of 5～30 ?g?mL-1(r=0.999 8) with an average recovery of 99.74%(RSD=0.47%).The dissolutions of 3 batches of samples were 82.06%,82.72% and 82.64%,respectively.CONCLUSIONS: Established method is simple and reliable for the dissolution determination of Eslicarbazepine acetate tablets.
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OBJECTIVE: To study the effect of total flavonoids from Alpinia officinarum on gastrointestinal motility.METHODS: Gastric emptying method was applied to observe the effect of total flavonoids from A.officinarum on gastric emptying of normal mice and sthenic gastric emptying induced by pyridostigmine bromide.Effect of total flavonoids from A.officinarum on gastric smooth muscle of rats was observed through in vitro test and small intestine advancement was used to observe the influence of total flavonoids from A.officinarum on intestinal motility.RESULTS: Total flavonoids from A.officinarum had no significant influence on gastric emptying of normal mice,but distinctly inhibited sthenic gastric emptying induced by pyridostigmine bromide(P
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OBJECTIVE:To establish the quality standard of Dibiling.METHODS:Rhizoma Coptidis in the formulation was identified qualitatively by TLC,and the content of ephedrine hydrochloride was determined by RP - HPLC.RESULTS: The TLC spots of Rhizoma Coptidis were clear and distinctive.The linear range of ephedrine hydrochloride was 0.088～3.520?g(r = 0.996 0) with an average recovery rate of 100.82%(RSD = 1.19%,n = 6).CONCLUSION:The established standard is applicable for the quality control of Dibiling.
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OBJECTIVE: To prepare Flu mixture and establish its quality standard. METHODS: The methods of decoction- boiling and distillation were adopted to prepare the flu mixture; TLC was used to identify Radix Et Rhizoma Rhei and Rhizoma Curcumae Longae, and HPLC was used to determine the content of Artemisinin. RESULTS: The spots characteristic of Radix Et Rhizoma Rhei and Rhizoma Curcumae Longae. were clearly identified with TCL. A good linearity was seen of Artemisinin in the range of 0. 42～ 2. 10? g( r=0. 999 3) . The recovery rate was 99. 84% ( RSD=2. 15% ) . CONCLUSIONS: The preparation is simple in preparation technique and good in stability. The TLC method is highly exclusive. The HPLC method is simple, accurate, and can be used for the quality control of flu mixture.
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[ Objective] To compare the protective mechanism of Zuojin Pill (Rhizoma Coptidis: Fructus Evodiae = 6:1) and Fan Zuojin Pill (Rhizoma Coptidis: Fructus Evodiae = 1: 6) on gastric secretion and gastric mucosal barrier. [Methods] Pylorus - ligated rat model was applied. Rats were divided into normal saline group, Zuojin Pill groups (1.4 g/kg and 2.8 g/kg) and Fan Zuojin Pill groups (1.4g/kg and 2.8g/kg) and then the drugs were given by duodenal feeding. Gastric secretion and gastric mucus synthesis were examined. [Results] Zuojin Pill and Fan Zuojin Pill (1.4 g/kg and 2.8 g/kg) both inhibited gastric secretion and decreased total acid output and pepsin activity in a dose- effect manner. Zuojin Pill and Fan Zuojin Pill also increased the content of gastric adherent mucus (GAM) and tended to elevate the mucus level in gastric juice. [Conclusion] The preventive mechanism of Zuojin Pill and Fan Zuojin Pill on gastric mucosa may be related to the regulation of gastric secretion and gastric mucus synthesis.