Synthesis characterization and cytotoxicity studies of platinum(II) complexes with reduced amino pyridine schiff base and its derivatives as ligands.

A series of reduced amino pyridine Schiff base platinum(II) complexes were prepared as potential anticancer drugs, and characterized by NMR, IR spectroscopy, elemental analysis, and molar conductivity. UV and CD results showed the binding mode between these compounds and salmon sperm DNA may be intercalation. The cytotoxicity of these complexes was validated against A549, Hela, and MCF-7 cell lines by MTT assay. Some complexes exhibited better cytotoxic activity than cisplatin against Hela and MCF-7 cell lines.

Study of the in vitro metabolism of TJ0711 using ultra high performance liquid chromatography with quadrupole time-of-flight and ultra fast liquid chromatography with quadrupole linear ion trap mass spectrometry.

TJ0711 (1-[4-(2-methoxyethyl)phenoxy]-3-[2-(2-methoxyphenoxy)ethylamino]-2-propanol) is a novel ß-adrenoreceptor blocker with vasodilating activity. The aim of this study was to investigate the in vitro metabolic properties of TJ0711 from both qualitative and quantitative aspects using mouse, rat, dog, and human liver microsomes as well as rat hepatocytes. Two modern liquid chromatography with tandem mass spectrometry systems, ultra high performance liquid chromatography with quadrupole time-of-flight mass spectrometry and ultra fast liquid chromatography with quadrupole linear ion trap mass spectrometry, were utilized for the analysis. To better characterize the metabolic pathways of TJ0711, two major metabolites were incubated under the same conditions as that for TJ0711. TJ0711 was extensively metabolized in vitro, and a total of 34 metabolites, including 19 phase I and 15 phase II metabolites, were identified. Similar metabolite profiles were observed among species, and demethylation, hydroxylation, carboxylic acid formation, and glucuronidation were proposed as the major metabolic routes. Significant interspecies differences were observed in the metabolic stability studies of TJ0711. Furthermore, gender differences were significant in mice, rats, and dogs, but were negligible in humans. The valuable information provided in this work will be useful in planning and interpreting further pharmacokinetic, in vivo metabolism and toxicological studies of this novel ß-blocker.

Isolation, identification and characterization of a novel Rhodococcus sp. strain in biodegradation of tetrahydrofuran and its medium optimization using sequential statistics-based experimental designs.

Statistics-based experimental designs were applied to optimize the culture conditions for tetrahydrofuran (THF) degradation by a newly isolated Rhodococcus sp. YYL that tolerates high THF concentrations. Single factor experiments were undertaken for determining the optimum range of each of four factors (initial pH and concentrations of K(2)HPO(4).3H(2)O, NH(4)Cl and yeast extract) and these factors were subsequently optimized using the response surface methodology. The Plackett-Burman design was used to identify three trace elements (Mg(2+), Zn(2+)and Fe(2+)) that significantly increased the THF degradation rate. The optimum conditions were found to be: 1.80 g/L NH(4)Cl, 0.81 g/L K(2)HPO(4).3H(2)O, 0.06 g/L yeast extract, 0.40 g/L MgSO(4).7H(2)O, 0.006 g/L ZnSO(4).7H(2)O, 0.024 g/L FeSO(4).7H(2)O, and an initial pH of 8.26. Under these optimized conditions, the maximum THF degradation rate increased to 137.60 mg THF h(-1) g dry weight in Rhodococcus sp. YYL, which was nearly five times of that by the previously described THF degrading Rhodococcus strain.

Caspase-3 gene transfected with LIGHT gene: can it be used for therapy of human hepatocellular carcinoma?

BACKGROUND: The aim of this study was to detect the expression of apoptosis factor caspase-3 in transferred HepG2 cells and provide feasible evaluation of the treatment for primary liver cancer with gene methods. METHODS: The pcDNA4C-LIGHT cDNA was extracted from Escherichia coli JM-109; then, the pcDNA4C-LIGHT cDNA was transferred into the HepG2 cells by a cationic liposome mediated method. Meanwhile, the blank group was established as the control group and the HepG2 cells were collected after transfection at 12 h, 24 h, 48 h, 3 days and 5 days. The expression of caspase-3 was identified in the supernatants by ELISA. A standard curve was generated for the set of samples assayed. Statistical significance was analyzed by SPSS. RESULTS: The quantity of caspase-3 protein was the greatest at 48 h and the least on day 5. The secretion of caspase-3 did not increase in the control group. The coefficient of correlation was equal to 0.9986 and had evident significance. CONCLUSIONS: The pcDNA4C-LIGHT was effectively transfected in human HepG2 cells mediated by liposome. The expression of caspase-3 increased in the transfected group. This study provides necessary theoretic support for the treatment of liver cancer with gene methods.

Effect of tetrahydrofuran on enzyme activities in activated sludge.

Tetrahydrofuran is an important solvent with wide usage in industry and laboratory research work. However, little information was known about the influence and fate of tetrahydrofuran (THF) in the environments. Several attempts have failed to enrich microorganisms in activated sludge to degrade THF. Effects of THF on the activities of dehydrogenase, protease, phosphatase, urease and catalase in activated sludge were investigated in this paper. The activated sludge was taken from the secondary sedimentation pool in the Sibao sewage treatment plant in Hangzhou China for observation of enzyme activities variation at the existence of tetrahydrofuran. The results obtained showed that tetrahydrofuran at over the range of selected concentrations could completely inhibit dehydrogenase activity during period of incubation, in the contrary, not to the protease activity, and strongly affected the phosphatase, urease and catalase activities which declined with increasing of tetrahydrofuran concentration. EC(10), EC(50), and EC(90) of tetrahydrofuran on phosphatase, urease and catalase activities was calculated according to the equation obtained from regression model of dose-effect curve. Realizing the effect of THF on the enzymatic diversity in activated sludge can help us to understand the influence and fate of tetrahydrofuran in the environments, and help us to enrich THF-degrading pure isolates or activated sludge.

Expression of cancer-testis antigen (CTA) in tumor tissues and peripheral blood of Chinese patients with hepatocellular carcinoma.

To investigate the expression of cancer-testis antigen (CTA) in Chinese patients with hepatocellular carcinoma (HCC), and the relationship between CTA gene expression and clinical indexes, we used one-step reverse transcription polymerase chain reaction (RT-PCR). The expression of the CTA mRNA was investigated in the tissues of HCC and corresponding peripheral blood of 37 patients with HCC. Fifteen samples of cirrhotic tissues and 15 normal tissues were examined with the same method. Two kinds of CTA (SSX-2 and SSX-5) showed high-specific and high-frequent expression in HCC tissues, but neither of them could be detected in adjacent non-HCC tissues. In corresponding peripheral blood of HCC tissues, the positive expression rate of the SSX-2 and SSX-5 mRNA was not very high. No relationship was found between the expression of CTA and clinical indicators such as age, sex, tumor size, TNM staging, serum AFP level and infection with hepatitis virus. In 15 patients with cirrhosis and 15 other non-tumor patients, none of the SSX-2 and SSX-5 mRNA was detected in liver tissue or peripheral blood. High frequency and specificity of CTAs in HCC indicates that their products may be new potential promising targets for antigen-specific immunotherapy of HCC. High frequent co-expression of the two genes in HCC provides a possibility of polyvalent vaccinations for HCC. Specific expression of CTAs was observed in AFP-negative HCC, suggested applying their mRNA as tumor markers to detect circulating HCC cells as adjuvant diagnostic tool and as indicators of recurrence and prognosis.