Objective To study the protective effect of(-)clausenamide on the damage of PC12 cells induced by serum deprivation and to explore its related mechanism. Methods The cell viability was detected by MTT assay and morphological observation. The effect of(-)clausenamide on the PC12 cell apoptosis was analyzed by flow cytometry. Then western blotting and confocal microscope was used for the further study of effect of(-)clausenamide on the protein expression of GSK-3?,Bax and Bcl-2. Results(-)Clausenamide remarkably increased PC12 cell survival rate through inhibiting the PC12 cell apoptosis induced by serum deprivation at the concentration of 1 or 10 ? mol/L(P

OBJECTIVETo investigate the effects of the quinoline derivative PQ1 combined with cisplatin on the proliferation and gap junction communication of prostate cancer PC3 cells.

METHODSWe cultured in vitro prostate cancer PC3 cells and divided them into DMSO blank control, cisplatin control, and cisplatin (10 mg/ml) plus PQ1 (1, 2, 5, 10, and 15 μmol/L) groups. We measured the proliferation of the prostate cancer PC3 cells, determined the expressions of the connexin 43 (Cx43) mRNA and protein by RT-PCR and Western blot, and compared the indexes among different groups.

RESULTSCisplatin combined with PQl at 1 - 10 μmol/L significantly inhibited the proliferation of the PC3 cells and the inhibition rate rose in a concentration- and time-dependent manner, from (48.72 ± 0.98)% vs (50.33 ± 0.62)% at 0 μmol/L to (77.38 ± 1.12)% vs (83.50 ± 1.05)% at 15 μmol/L at 24 and 48 hours (P < 0.05). Compared with the cisplatin control, cisplatin combined with PQ1 at 1, 2, 5, 10, and 15 μmol/L increased the expression of Cx43 mRNA from 0.379 ± 0.113 to 0.669 ± 0.031, 0.831 ± 0. 127, 0.769 ± 0.100, 0.532 ± 0.086, and 0.475 ± 0.134, respectively (P < 0.05), and cisplatin combined with PQ1 at 1, 2, 5, and 10 μmol/L elevated that of Cx43 protein from 0.138 ± 0.146 to 0.263 ± 0.111, 0.306 ± 0.152, 0.415 ± 0.280, and 0.643 ± 0.310, respectively (P < 0.05).

CONCLUSIONThe quinoline derivative PQ1 can promote the gap junction communication of prostate cancer PC3 cells and enhance the killing effect of cisplatin on PC3 cells by upregulating the expressions of Cx43 mRNA and protein.

Aminoquinolines ; pharmacology ; Antineoplastic Combined Chemotherapy Protocols ; pharmacology ; Cell Line, Tumor ; Cell Proliferation ; drug effects ; Cisplatin ; pharmacology ; Connexin 43 ; genetics ; metabolism ; Dose-Response Relationship, Drug ; Gap Junctions ; drug effects ; physiology ; Humans ; Male ; Prostatic Neoplasms ; metabolism ; pathology ; physiopathology ; RNA, Messenger ; metabolism ; Time Factors

The conventional oral drug delivery frequently results in the drug elimination before its complete release due to rapid gastric emptying and short gastrointestinal transport time, thus reducing the bioavailability of drug. In order to maintain an effective concentration of drug in the body and maximize its optimal efficacy, the frequency of administrations often needs to be increased. By contrast, gastric retention drug delivery system (GRDDS), as an innovative method of drug delivery, prolongs the retention time of the drug in the stomach and reduces irritation to the gastrointestinal tract. Consequently, it enhances the bioavailability of drug, reduces dosing frequency for patients and improves treatment adherence. In recent years, domestic and foreign studies have been conducted on gastric retention drug delivery systems. Here, we provide a comprehensive overview of the relevant literature published in recent years, examining their current marketing status, various types, as well as in vivo and in vitro evaluation methods.

ObjectiveTo study the cardioprotective effects of ischemic post-conditioning on elderly patients with ST-elevation acute myocardial infarction (STEM1).MethodsConsecutive 215 patients with STEMI undergoing emergency percutaneous coronary intervention(PCI) were randomly assignedto receive ischemicpost-conditioningorconventional PCItreatment.The ischemic postconditioning (n=38) were conducted by 3 episodes of 30-second occlusion followed by 30-second reperfusion, while the control group (n= 46) was without any intervention after PCI.Reperfusion arrhythmias, corrected TIMI frame count (cTFC) and TIMI myocardial perfusion grade (TMPG)were compared between the two groups, respectively.Results The incidence of reperfusion arrythmias was less frequent in ischemic postconditioning group (21.1％ ,8/38) than in control group (45.7％ ,21/46) after PCI (x2 = 5.571, P＜0.05). The TIMI grade 3 flow was similar between two groups [(94.7％(36/38) vs. 82.6％( 38/46), x2= 2.919, P＞0.05], the cTFC levels (23.6±3.7vs. 26.1 ±5.9) and TMPG 3 perfusion [ 89.5％ (34/38) vs.69.6％ (32/46)] were significantly different (t= 5.434, P＜0.05; x2 = 4.899, P＜0.05, respectively) between two groups.ConclusionsIschemic postconditioning may reduce myocardial reperfusion injury in elderly patients with STEMI undergoing emergent PCI.

BACKGROUND: It is easy and feasible to treat anterior urethral stricture using internal urethrotomy, however, its drawback is high recurrence in the long-term follow-up. OBJECTIVE: To evaluate the effect of submucosal injected verapamil on prevention of anterior urethral stricture recurrence after internal urethrotomy. METHODS: Totally 60 consecutive males with anterior urethral stricture underwent internal urethrotomy with or without urethral submucosal injection of verapamil, in the Department of Urology, First Affiliated Hospital of Fujian Medical University, from December 2006 to April 2008, were selected. All cases were followed up at least 24 months.RESULTS AND CONCLUSION: All cases were followed up for 24-39 months, with an average of 28.5 months. Urethral stricture recurred in two cases in the verapamil-treated group but 8 cases in the untreated group. This difference in stricture recurrence between the two groups was statistically significant (P < 0.05). The results demonstrated that submucosal injection of verapamil at the stricture site significantly reduces the stricture recurrence rate after internal urethrotomy. Further studies involving larger number of cases and longer follow-up are warranted to confirm the efficacy and safety of this therapy.

Objective To study the application of individualized dressing change on tumor patients with PICC. Methods We made different methods of dressing change in accordance with the status of the patients and the seasons, and observed the color and the integrity of the local skin around the puncture points. Results With the exception of 2 cases requested extubation because of tetter on skin around the puncture point, the local skin infection or systemic infection didn't occur in the other 97 cases by individualized dressing change. Conclusions It can reduce the rate of local infection, extends time of catheter retaining, and improves quality of life of tumnor patients with PICC by individualized dressing change

OBJECTIVETo observe the clinical efficacy on spastic pelvic floor syndrome (SPFS) treated with electroacupuncture (EA) at Shangliao (BL 31), Ciliao (BL 32), Zhongliao (BL 33) and Xialiao (BL 34).

METHODSThirty-six cases of SPFS were treated with EA at Shangliao (BL 31), Ciliao (BL 32), Zhongliao (BL 33) and Xialiao (BL 34), intermittent wave, 60 times/min in frequency, retained for 20 min. In general, the acupoints on one side were stimulated in each treatment. The bilateral acupoints stimulation was applied in serious cases. The treatment was given once every two days, five treatments made one session and totally three sessions were required. Before and after treatment, the clinical symptoms, anal kinetic indices defecation radiographic changes were observed. The follow-up observation was done in three months after the end of treatment.

RESULTSIn three-months follow-up after treatment, 14 cases were cured, 18 cases improved and 4 cases failed. The total effective rate was 88. 9%. After treatment, the cases of incomplete defecation, difficult defecation, anal pain and anal obstruction were reduced apparently as compared with those before treatment, indicating the statistically significant differences (all P<0.01). After treatment, rectal anal reflex threshold (ARA) was increased, anal maximal contraction pressure (AMCP) was reduced to (16.62±1.54) kPa and anal rest pressure (ARP) was significantly reduced to (7.22±0.36) kPa, indicating the statistical differences as compared with those before treatment (all P<0.01). After treatment, anorectal angle (ARA) in forceful defecation was increased to (116.55±9.42)°, the distance between the anorectal junction and the pubococcygeal line was decreased, and the impression of puborectal muscle was alleviated apparently as compared with that before treatment (P<0.01).

CONCLUSIONEA at Shangliao (BL 31), Ciliao (BL 32), Zhongliao (BL 33) and Xialiao (BL 34) achieves definite efficacy on SPFS and this therapeutic method obviously relieves the symptoms and deserves to be promoted in clinic.

Acupuncture Points ; Adult ; Aged ; Anus Diseases ; physiopathology ; therapy ; Constipation ; physiopathology ; therapy ; Defecation ; Electroacupuncture ; Female ; Humans ; Male ; Middle Aged ; Muscle Spasticity ; physiopathology ; therapy ; Pelvic Floor ; pathology

Objective:To observe the influence of radiofrequency catheter ablation of the fat pad at the right pulmonary vein- atria junction(RPV fat pad)on Bezold-Jarisch reflex(BJR)induced by veratridine in canine.Methods:Ten mongrel dogs were anesthetized and their chest were opened through a right thoracotomy to expose the RPV fat pad.Veratridine was injected into the left ventricle at bolus doses of 10?g/kg through a catheter to induce BJR.The sinus cycle length(SCL),systolic arterial pressure(SAP),diastolic arterial pressure(DAP),mean arterial pressure(MAP),left ventricle systolic pressure(LVSP), left ventricle diastolic pressure(LVDP)and mean left ventricle pressure(MLVP)were measured under the baseline and after ablation of the RPV fat pad;the changes of the above parameters(?SCL,?SAP,?DAP,?MAP,?LVSP,?LVDP,and?MLVP)were calculated.Then the same dose of veratridine was injected under the pad after ablation and the changes of the a- bove parameters were observed.Results:BJR was successfully induced in the 8 animals;the animals has prolonged sinus cycle length(SCL)and decreased MAP and MLVP.After ablation,the prolongation of SCL after injection of veratridine was markedly reduced([229.2?92.3]ms vs[39.3?14.1]ms,P

Objective To investigate the effects of TLR7 on imiquimod induced apoptosis of THP-1 derived macrophages.Methods Three cell lines ( THP-1 derived macrophages, MDCK cell line and HUVEC cell line) with different capabilities of expressing TLR7 were selected.The survival rates of cells af-ter the treatment with different concentrations of imiquimod were detected by MTT assay.The levels of IL-6 in the supernatants of TLR7 inhibitor chloroquine or TLR7-siRNA treated cells were detected by enzyme-linked immunosorbent assay.The apoptosis of cells was detected by flow cytometry after inhibiting the ex-pression of TLR7.Results Imiquimod induced the apoptosis of THP-1 derived macrophages, MDCK cell lines and HUVEC cell lines.The levels of IL-6 were significantly decreased as the expression of TLR7 was inhibited by treating THP-1 derived macrophages with chloroquine or TLR7-siRNA.Treating THP-1 derived macrophages with chloroquine or TLR7-siRNA did not affect the cell apoptosis induced by imiquimod.Con-clusion Imiquimod could induce the apoptosis of THP-1 derived macrophages through TLR7 independent pathway.

OBJECTIVE Leukotriene B4 (LTB4) biosynthesis and subsequently neutrophilic inflam?mation may provide a potential strategy for the treatment of acute lung injury (ALI) or idiopathic pulmonary fibrosis (IPF). To provide a potential strategy for the treatment of ALI or IPF, we identified potent inhibi?tors of Leukotriene A4 hydrolase (LTA4H), a key enzyme in the biosynthesis of LTB4. METHODS In this study, we identified two known histone deacetylase (HDAC) inhibitors, suberanilohydroxamic acid (SAHA) and its analogue 4-(dimethylamino)-N-〔7-(hydroxyamino)-7-oxoheptyl〕benzamide (M344), as effective inhibitors of LTA4H using enzymatic assay, thermofluor assay, and X- ray crystallographic investigation. We next tested the effect of SAHA and M344 on endogenous LTB4 biosynthesis in neutrophils by ELISA and neutrophil migration by transwell migration assay. A murine experimental model of ALI was induced by lipopolysaccharide(LPS) inhalation. Histopathological analysis of lung tissue using H&E staining revealed the serious pulmonary damage caused by LPS treatment and the effect of the SAHA. We next examined mRNA and protein levels of pro-inflammatory cytokines in lung tissue and bronchoalveolar lavage fluid using qRT- PCR and ELISA to further investigate the underlying mechanisms of anti-inflammatory activities by SAHA. We also investigated the effects of SAHA and M344 on a murine experimental model of bleomycin (BLM)-induced IPF model. RESULTS The results of enzymatic assay and X-ray crystallography showed that both SAHA and M344 bind to LTA4H, signif?icantly decrease LTB4 levels in neutrophil, and markedly diminish early neutrophilic inflammation in mouse models of ALI and IPF under a clinical safety dose. CONCLUSION Collectively, SAHA and M344 would provide promising agents with well-known clinical safety for potential treatment in patients with ALI and IPF via pharmacologically inhibiting LAT4H and blocking LTB4 biosynthesis.