The starting material L-tryptophan reacted with 4-chlorobenzaldehyde via Pictet-Spengler condensation and followed by oxidation and decarboxylation to afford the 1-(4-chlorophenyl)-beta-carboline. The intermediate was further reacted with alkyl halogenide by N(9)-alkylation and N2-quaternarization to obtain 12 novel 1-(4-chlorophenyl)-beta-carboline derivatives. The chemical structures of all target compounds were characterized by elemental analyses, MS and 1H NMR spectra. The antitumor activities of the target compounds were evaluated by MTT method. The results demonstrated that N2-quaternarized compounds enhanced the antitumor activity significantly. In particular, compound 15 was found to be the most potent compound with IC50 values lower than 5 micromol x L(-1) against 6 human tumor cells. These results confirmed that the N2-alkyl or aralkyl substituent on the beta-carboline ring played an important role in the modulation of the antitumor activities.

Drug-Eluting Stents ; adverse effects ; Humans ; Middle Aged ; Myocardial Infarction ; etiology ; Sirolimus ; administration & dosage ; Thrombosis ; etiology

Endocardial Cushion Defects ; complications ; Female ; Humans ; Infant, Newborn ; Lung ; abnormalities ; Lung Diseases ; complications ; congenital

Objective To observe the effect of signal transduction pathway of NF-κB on tubular cell apoptosis in ischemia-reperfusion induced acute kidney injury (AKI) in mice.Methods Eighteen C57B/6 mice were randomly (random number) divided into three groups,namely control group,AKI group,and pyrrolidine dithiocarbamate (PDTC) group.AKI model of mouse was made by occlusion of bilateral renal pedicles with microvascular clamps for 45 minutes,and intraperitoneal injection of PDTC (50 mg/kg) was given immediately after modeling in mice of PDTC group.Forty-eight hours after modeling,kidney pathological changes,serum creatinine (SCr) and blood urea nitrogen (BUN) were examined,and renal tissue NF-κB,TNFR,Bcl-2 and caspase-3 levels were detected by using immunohistochemistry,and tubular cell apoptosis was observed by terminal deoxynucleotidyl transferase-mediated dUTP-biotin nick end labeling assay (TUNEL).Results (1) The pathological Pallers score of renal damage,blood urea nitrogen and serum creatinine levels in PDTC group were significantly lower than those in AKI group [(2.83 ± 0.41)vs.(4.50± 0.55),P=0.000; (61.65 ±3.06) mmol/L vs.(77.78 ±5.82)mmol/L,P=0.000and (74.33 ± 9.83) μmol/L vs.(152.00 ± 16.55) μmol/L,P =0.000,respectively].(2) The level of NF-κB in renal tissue homogenates in PDTC group was significantly lower than that in AKI group [(20.33± 2.34) ％ vs.(35.83 ± 3.06) ％,P =0.000].(3) The apoptotic index of renal tubular cells in PDTC group was significantly lower than that in AKI group [(16.67 ± 1.15) ％ vs.(28.00 ±2.01) ％,P =0.001].(4) The levels of caspase-3 and TNFR1 in renal tissue homogenates in PDTC group were significantly lower than those in AKI group [(7.00 ± 1.26) vs.(11.00 ± 1.26),P =0.000 and (5.55 ± 0.82) vs.(9.75 ± 0.76),P =0.000],and Bcl-2 level in PDTC group was significantly higher than that in AKI group [(10.50± 1.38)vs.(1.83 ±0.98),P=0.000].Conclusions NF-κB activates renal tubular cell apoptosis in acute kidney injury induced in mice after ischemia-reperfusion.Blockade of NF-κB signal transduction pathway may lessen the apoptosis of renal tubular cells,leading to renal function less compromised.

Anthracosis ; complications ; Bacterial Proteins ; genetics ; Humans ; Methicillin Resistance ; genetics ; Methicillin-Resistant Staphylococcus aureus ; drug effects ; genetics ; Penicillin-Binding Proteins ; Respiratory Tract Infections ; complications ; microbiology ; Sputum ; microbiology

Adult ; Arsenic Poisoning ; etiology ; Female ; Humans ; Male ; Middle Aged ; Organotin Compounds ; poisoning ; Water Pollution ; Young Adult

Objective With ordinary acupuncture as the control, to observe the feasibility and effectiveness of electroacupuncture at Jiaji (EX-B2) points in treating primary trigeminal neuralgia.Method Forty patients with primary trigeminal neuralgia were randomized into a group of electroacupuncture at Jiaji points and an ordinary acupuncture group, 20 cases in each group. In the electroacupuncture group, Jiaji of C2and T1on the affected side were selected, while the points were selected by following the Acupuncture-moxibustion Therapeuticsin the ordinary acupuncture group. Carbamazepine (CBZ) was taken as the basic treatment for the two groups. A treatment course (3 weeks) was observed, and follow-up study was conducted every 4 weeks for a total of 12 weeks. The dose of CBZ, Visual Analogue Scale (VAS) and Short-form McGill Pain Questionnaire (SF-MPQ) scores at each time point were recorded. The changes of the index in the two groups at each time point were compared.ResultAt the end of the treatment (the third week), the dose of CBZ, VAS and SF-MPQ scores all declined in the two groups, and the between-group differences were statistically insignificant (P>0.05). The follow-up study in the 7th week showed that the data of the observed indexes all decreased in the two groups, while the electroacupuncture group presented a more significant efficacy, and the between-group differences were statistically significant (P<0.05). The follow-up studies in the 11th and 15th weeks showed that the data of the observed indexes continued to decline in the electroacupuncture group but began to increase in the ordinary acupuncture group, and the between-group differences were statistically significant (P<0.001).Conclusion Electroacupuncture at Jiaji points and ordinary acupuncture both can reduce the dose of CBZ for patients with primary trigeminal neuralgia, improve pain and other discomforts as well as the negative emotions, but electroacupuncture at Jiaji can produce a more significant long-term efficacy compared to the ordinary acupuncture.

Objective:To explore influence of nasal continuous positive airway pressure (nCPAP)on maximal oxygen uptake (V · O2 max )etc.in patients with chronic congestive heart failure (CHF)complicated moderate-to-severe ob-structive sleep apnea-hypopnea syndrome (OSAHS)and explore its significance.Methods:A total of 83 CHF com-plicated moderate-to-severe OSAHS patients were selected and randomly divided into routine treatment group (n=40)and nCPAP group (n = 43).Both groups were treated for six months.Left ventricular ejection fraction (LVEF),apnea hyponea index (AHI)and V · O2 max were measured and compared between two groups before and af-ter treatment.Results:Compared with routine treatment group after six-month treatment,there was significant re-duction in AHI [(27.5±6.2)vs.(6.8±1.2)],and significant rise in LVEF [(0.45±0.07)vs.(0.48±0.05)]and · V O2 max [(16.5±3.5)ml·kg-1 ·min-1 vs.(19.2±3.4)ml·kg-1 ·min-1 ]in nCPAP group,P <0.05 all.Con-· clusion:The nCPAP can improve ventilation function,heart function and V O2 max in patients with CHF complicated moderate-to-severe OSAHS,who have received basic medication.

Objective To investigate the prevalence rate of healthcare-associated infection(HAI)in a hospital,so as to provide reference for making HAI control measures.Methods The cross-sectional survey on HAI was carried out among all hospitalized patients on May 26,2010,December 12,2012 and December 4,2013,respectively,sur-veyed data were analyzed.Results The prevalence rate was 6.66%(n =116),6.67%(n =113)and 6.33%(n =120)in 2010,2012 and 2013 respectively,and case rate was 7.29%(n=127),7.38%(n=125)and 6.97%(n=132) respectively,intensive care unit(ICU )had the highest infection rate,internal medicine ICU was up to 71 .43%. The main infection site was lower respiratory tract(44.53%),followed by surgical site infection (9.11 %)and uri-nary tract infection (9.11 %).The isolation rate of gram-negative bacteria,gram-positive bacteria and fungi was 60.81 %,20.38% and 18.81 % respectively.Usage rate of antimicrobial agents in three years was 32.95%, 29.87% and 25.59% respectively (χ2 = 13.16,P <0.01 ).Conclusion Prevalence rate of HAI in this hospital is high ,the main pathogen is gram-negative bacteria,the main infection site is lower respiratory tract ,antimicrobial use decreased year by year.Monitor on high risk departments,main sites and pathogens should be intensified.

To observe the effects of serum containing Xiaotan Sanjie Decoction, a compound traditional Chinese herbal medicine, on proliferation and apoptosis of human gastric cancer cell line MKN-45.