To evaluate the efficacy and safety of an oxaliplatin, fluorouracil (5 FU), and folinic acid (FA) combination in treatment of patients with metastatic or advanced gastric cancer,we used oxaliplatin 130 mg/m 2 (2 hour intravenous infusion,1 d)and FA 200 mg/m 2 (2 hour intravenous infusion,1 to 5 d) followed by 5 FU 500 mg/m 2 (4 hour continuous infusion,1 to 5 d) every 3 weeks. Efficacy of treatment was evaluated after 3 cycles and the responders were confirmed 4 weeks later. In 26 case evaluated, patial release was achieved in 11 cases, stablized in 9 cases, progressed in 6 cases. The overall response rate was 42.3%. The main adverse effects were gastrointestinal tract toxicity, neurosensory toxicity and bone marrow suppression. This trail suggested that the short term curative effect of this regimen was similar to those of others and showed good efficacy and an acceptable safety profile. It is a new option for the treatment of metastatic and advanced gastric cancer.

Objective:To study the effect of ischemic postconditioning(I-postC)on the lung injury following ischemia-reperfusion(I/R)of skeletal muscle in the hind limbs of rats.Methods:The rat model of hind limbs I/R injury was established by subrenal abdominal aorta cross-clamping for 4 hours.Forty-eight rats were divided into 3 groups:I/R group,IPC and I-postC group.Each group received 4 hours of ischemia and then 12 or 24 hours of reperfusion respectively.The tissue morphology,wet-to-dry weight(W/D)ratio,malondialdehyde(MDA)and myeloperoxidase(MPO) of lung tissue were compared.The expression of ICAM-1 mRNA in lung was also studied by RT-PCR or in situ hybridization.The protein product was detected by Western blot.Results:In IPC and I-postC groups,all parameters decreased significantly compared with I/R ischemia group(P

Objective To observe the changes of proportion of NK cells,?? T cells,CD4+CD25+T cells and their FOXP3-expressed sub-population in peripheral blood of acute Plasmodium vivax infected patients.Methods The proportions of NK cells,?? T cells,CD4+CD25+T cells and FOXP3-expressed sub-population within CD4+CD25+T cells were measured by flow cytometry(FCM)in peripheral blood of 25 patients with acute infection of Plasmodium vivax(AC)and compared with those of both 14 normal controls(NC)and 13 immune controls(IC).Results The proportion of NK cells in AC(8.48%)decreased significantly compared with that in NC(15.53%)and IC(17.69%)(P0.05).Conclusions During acute Plasmodium vivax infection,the proportion of NK cells decreases and the proportion of ?? T cells increases,and CD4+CD25+FOXP3+T cells decrease a little.

To facilitate the expression of GL 7 ACA acylase gene in a recombinant E coli , a fragment of the gene, in which the signal peptide was deleted by PCR method, was inserted into a prokaryotic expression vector, pET 28a By colony PCR method screening, a recombinant plasmid pET ACY was obtained and then transformed into the expression host BL21 (DE3) The influences of induction conditions such as IPTG concentration, the time of induction and the induction temperature on the expression of the recombinant protein were investigated Under optimal condition, the enzyme activity could reach 266 U/L Finally, the recombinant GL 7 ACA acylase can be easily isolated to a purity of about 80% by a simple anion ion exchange chromatography with enzyme activity recovery of 50%

To discover novel fluoroquinolone lead compounds as possible anti-infective or/and antitumor chemotherapies, combination principle of pharmacophore-based drug design, a series of novel tricyclic fluoroquinolone title compounds, [1,2,4]triazino[3,4-h][1,8]naphthyridine-8-one-7-carboxylic acid derivatives ( 5a-5p), were designed and synthesized with a fused [1,2,4]-triazine ring unit. Their structures were characterized by spectral data and elemental analysis and the in vitro antibacterial and anti-cell proliferation activities were also evaluated. The results showed that the titled compounds exhibited more significant inhibitory activities against drug-resistant bacteria (Methicillin-resistant Staphylococcus aureus and multi drug-resistant Escherichia coli strains) and three tested cancer cell lines (human hepatoma SMMC-7721, murine leukemia L1210 and human murine leukemia HL60 cells). Interestingly, SAR showed that compounds with electron-donating groups attached to benzene ring had stronger antibacterial activity than antitumor activity, but electron-withdrawing compounds displayed more potential antitumor activity than antibacterial activity, especially antitumor activity of nitro compounds was comparable to comparison doxorubicin. Thus, novel triazine-fused tricyclic fluoroquinolones as potent anti-infective or/and antitumor lead compounds are valuable to pay attention and for further development.
Animals ; Anti-Bacterial Agents ; chemical synthesis ; chemistry ; Antineoplastic Agents ; chemical synthesis ; chemistry ; Carboxylic Acids ; Carcinoma, Hepatocellular ; Cell Line ; Cell Proliferation ; Drug Design ; Escherichia coli ; drug effects ; Fluoroquinolones ; chemical synthesis ; chemistry ; HL-60 Cells ; Humans ; Leukemia L1210 ; Liver Neoplasms ; Methicillin-Resistant Staphylococcus aureus ; drug effects ; Mice ; Naphthyridines ; Triazines

Objective Observation and discussion about the treatment effect with home-made vacuum drainage and Algoplaque on severe pressure ulcers. Methods The patients with severe pressure ulcers selected from Yuebei Peole′s Hospital of Shaoguan city from January to December 2016 were randomly divided into three groups:experimental group, control group A and group B (30 cases in each). The patients were treated with home-made vacuum drainage and Algoplaque in the experimental group, meanwhile a simple use of Algoplaque treatment in control group A and VSD technology in control group B only. Observed and compared the effect in the three groups on the time of dressing change, wound healing time and the total cost. Results The wound healing time of experimental group.contral group A and group B were (24.10 ± 2.12), (33.26 ± 1.71), (27.87 ± 1.95) days, the times of dressing change were 5.52 ± 0.96, 35.84 ± 1.81, 7.23 ± 1.09, dressing costs were (629.95 ± 28.10) yuan, (1354.29 ± 301.63) yuan, (10825.38±1678.21) yuan, and the differences were statistically significant (F=175.961, 5017.527, 1029.377, all P<0.01), and the wound healing time, dressing times, dressing costs were lower than the control group A and B in the observation group. Conclusion The treatment of home-made vacuum drainage and Algoplaque on patients with severe pressure ulcers can obviously reduce the time of dressing change and wound recovery, and the cost also. It is worthy to promote in clinic.

Objective To investigate the effects of propofol on intracellular free Ca2+ concentration and nitric oxide synthase (NOS) activity in PC12 cells exposed to bupivacaine. Methods The PC12 cells were provided by Shanghai Cell Biology Research Institute, Chinese Academy of Sciences and cultured in DMEM liquid culture medium. The cultured PC12 cells were seeded in 36 well plates and randomly assigned to one of 4 groups (n=9 wells each): group Ⅰ control (C);group Ⅱ propofol (P);group Ⅲ bupivacaine (B) and group Ⅳ propofol + bupivacaine (PB). In control group D-Hank solution was added. The cells were exposed to propofol 2 mmol/L and bupivacaine 0.09 mmol/L in group P and B respectively. In group PB the cells were incubated with propofol 2 mmol/L and bupivacaine 0.09 mmol/L simultaneously. After being incubated for 6 and 24 h the apoptosis in BC12 cells was assessed by flow cytometry. Apoptotic rate was calculated. NOS activity and intracellular free Ca2+ coneentration in PC12 cells were determined. Results Bupivacaine significantly increased the apoptotic rate of PC12 cells, the intracellular free Ca2+ concentration and NOS activity in PC12 cells in group B as compared with control group. Propofol significantly decreased the toxic effects of bupivacaine on PC12 cells in group PB compared with group B. Conclusion Bupivacaine is toxic to PC12 cells by increasing apoptosis, intracellular Ca+ concentration and NOS activity in the cells. The toxic effects can be prevented to some extent by concomitant administration of propofol.

To discover novel antitumor rhodanine unsaturated ketones, a series of fluoroquinolone (rhodanine α, β-unsaturated ketone) amine derivatives (5a-5r) were designed and synthesized with fluoroquinolone amide scaffold as a carrier. The structures of eighteen title compounds were characterized by elemental analysis, 1H NMR and MS. The in vitro anti-proliferative activity against Hep-3B, Capan-1 and HL60 cells was evaluated by MTT assay. The results showed that the title compounds not only had more significant anti-proliferative activity against three tested cancer cell lines than that of the parent ciprofloxacin 1, but also exhibited the highest activity against Capan-1 cells. The SAR revealed that some compounds carrying aromatic heterocyclic rings or phenyl attached to an electron-withdrawing carboxyl or sulfonamide substituent were comparable to or better than comparison doxorubicin against Capan-1 cells. As such, it suggests that fluoroquinolone (rhodanine α, β-unsaturated ketone) amines are promising leads for the development of novel antitumor fluoroquinolones or rhodanine analogues.

Objective To evaluate the surgical techniques and clinical efficacy of retroperitoneoscopic ligation of renal lymphatic vessels outside adipose capsule and inside adipose capsule for comparison in the treatment of chyluria.Methods Retrospective anal-ysis of the retroperitoneal laparoscopic adipose capsule of kidney pedicle lymphatic duct ligation(group Ⅰ)and adipose capsule pathways in the kidney totally or subtotally free renal pedicle lymphatic ligation(group Ⅱ)and 1 1 1 patients with chyluria clinical data,compared two groups of operation time,bleeding volume,the rate of analgesia,postoperative gastrointestinal function recovery time,drainage time,postoperative recovery time,postoperative hospital stay and postoperative complications and other index differ-ence.Results Retroperitoneal laparoscopic operation group of adipose capsule in operation time,bleeding volume,postoperative an-algesia,postoperative gastrointestinal function recovery time,drainage time,postoperative recovery time,postoperative hospital stay and postoperative complications were better than the adipose capsule of kidney totally or subtotally free operation group,the differ-ence was statistically significant(P<0.05).Conclusion Retroperitoneal laparoscopic renal adipose capsule of kidney pedicle lym-phatic disconnection for the treatment of chyluria effect,and adipose capsule operation ways,the method less trauma,quicker recov-ery,can completely replace the renal adipose capsule total or Sub-total of free kidney pedicle lymphatic disconnection operation,wor-thy of clinical application.

To optimize the synthetic method and antibacterial activity of fused heterocyclic thiadiazole compounds, cyclocondensation of 2-(4-methoxyphenyl)-5-amino-1,3,4-thiadiazole (2) with alpha-chloro-4-chloro acetophenone (3) resulted in a key intermediate (4), 6 -(4-chlorophenyl)-2-(4-methoxyphenyl)-imidazo-[2,1-b][1,3,4]thiadiazole, which was carried out an nucleophilic substitution with substituted piperazine to give the corresponding free bases of piperazine (5a-5c), then followed by Mannich reaction with heterocyclicamines and formaldehyde to yield the corresponding Mannich bases, (1a-11) as respective hydrochloride salts. The structures were confirmed by IR, 1H NMR, MS and elemental analysis and the antibacterial activities in vitro of fifteen newly synthesized compounds were also tested against Gram positive bacteria and Gram negative bacteria with the standard 2-fold agar dilution method. The antibacterial results showed that the introduction of a polar group resulted in the enhancement of antibacterial activity in vitro. Thus, the structures of these fused compounds could further be investigated.
Anti-Bacterial Agents ; chemical synthesis ; chemistry ; pharmacology ; Bacillus subtilis ; drug effects ; Escherichia coli ; drug effects ; Imidazoles ; chemical synthesis ; chemistry ; pharmacology ; Mannich Bases ; chemistry ; Microbial Sensitivity Tests ; Molecular Structure ; Pseudomonas aeruginosa ; drug effects ; Staphylococcus aureus ; drug effects ; Thiadiazoles ; chemical synthesis ; chemistry ; pharmacology