• Journal of Pharmaceutical Investigation
• /
• v.38 no.3
• /
• pp.183-189
• /
• 2008

The present study compared the feasibility of Caco-2 and MDCK cells as an efficient in-vitro model for the drug classification based on Biopharmaceutics Classification System (BCS) as well as an in-vitro model for drug interactions mediated by P-gp inhibition or P-gp induction. Thirteen model drugs were selected to cover BCS Class I{\sim}IV$ and their membrane permeability values were evaluated in both Caco-2 and MDCK cells. P-gp inhibition studies were conducted by using vinblastine and verapamil in MDCK cells. P-gp induction studies were also performed in MDCK cells using rifampin and the P-gp expression level was determined by western blot analysis. Compared to Caco-2 cells, MDCK cells required shorter period of time to culture cells before running the transport study. Both Caco-2 and MDCK cells exhibited the same rank order relationship between in-vitro permeability values and human permeability values of all tested model compounds, implying that those in-vitro models may be useful in the prediction of human permeability (rank order) of new chemical entities at the early drug discovery stage. However, in the case of BCS drug classification, Caco-2 cells appeared to be more suitable than MDCK cells. P-gp induction by rifampin was negligible in MDCK-cells while MDCK cells appeared to be feasible for P-gp inhibition studies. Taken all together, the present study suggests that Caco-2 cells might be more applicable to the BCS drug classification than MDCK-cells, although MDCK cells may provide some advantage in terms of capacity and speed in early ADME screening process.

• Journal of Microbiology
• /
• v.34 no.1
• /
• pp.7-14
• /
• 1996

Teh baculovirus gp64 glycoprotein is a major component of the envelope of budded virus (BV) and has been shown that it plays an essential role in the infection process, especially virus-cell membrane fusion. We have cloned Autographa californica Nuclear Polyhedrosis Virus (AcNPV) gp64 protein were examined for membrane fusion activity by using a synchtium formation assay under various conditions. The optimal conditions required for inducing membrane fusion are 1) form pH 4.0 to 4.8 2) 15 min exposure of cells to acidic pH 3) at least 1 .mu.g of gp64 cloned plasmid DNA per 3 * 10$^{6}$ cells 4) and an exposure of cells to acidic pH at 72 h post-transfection. In order to investigate the role of hydrophobicity of the gp64 glycoprotein for the membrane fusion, the two leucine residues (amino acid position at 229 and 230) within hydrophobic region I were substituted to alanine by PCR-derived site-directed mutagenisis and the membrane fusion activity of the mutant was anlaysed. The gp64 glycoprotein carrying double alamine substitution mutation showed no significant difference in fusion activity. This result suggested that minor changes in hydrophobicity at the amino acid position 229 and 230 does not affect the acid-induced membrane fusion activity of the gp64 glycoprotein.

• The KIPS Transactions:PartA
• /
• v.14A no.1 s.105
• /
• pp.1-14
• /
• 2007

MPICH-G2 is an MPI implementation to solve complex computational problems by utilizing geographically dispersed computing resources in grid environments. However, the computation nodes in MPICH-G2 are exposed to the external network due to the lack of supporting the private IP clusters, which raises the possibility of malicious security attacks. In order to address this problem, we propose MPICH-GP with a new relay scheme combining NAT(Network Address Translation) service and an user-level proxy. The proxy running on the front-end system of private IP clusters forwards the incoming connection requests to the systems inside the clusters. The outgoing connection requests out of the cluster are forwarded through the NAT service on the front-end system. Through the connection path between the pair of processes, the requested MPI jobs can be successfully executed in grid environments with various clusters including private IP clusters. By simulations, we show that the performance of MPICH-GP reaches over 80% of the performance of MPICH-G2, and over 95% in ease of using RANK management method.

• Journal of Life Science
• /
• v.24 no.8
• /
• pp.887-894
• /
• 2014

The screening of the microorganisms degrading chlorinated organic compounds such as PCP (pentachlorophenol) and TCE (trichloroethylene) was conducted with soil and industrial wastewater contaminated with various chlorinated organic compounds. Isolates (GP5, GP19) capable of degrading PCP and isolates (GA6, GA15) capable of degrading TCE were identified as Acetobactor sp., Pseudomonas sp., Arthrobacer sp., Xanthomonas sp. and named Acetobacter sp. GP5, Pseudomonas sp. GP19, Arthrobacer sp. GA6 and Xanthomoas sp. GA15, respectively. The microbial augmentation, OC17 formulated with the mixture of bacteria including isolates (4 strains) degrading chlorinated organic compounds and isolates (Acinetobacter sp. KN11, Neisseria sp. GN13) degrading aromatic hydrocarbons. Characteristics of microbial augmentation OC-17 showed cell mass of $2.8{\times}10^9CFU/g$, bulk density of $0.299g/cm^3$ and water content of 26.8%. In the experiment with an artificial wastewater containing PCP (500 mg/l), degradation efficiency of the microbial augmentation OC17 was 87% during incubation of 65 hours. The degradation efficiency of TCE (300 uM) by microbial augmentation OC17 was 90% during incubation of 50 hours. In a continuous culture experiment, analysis of the biodegradation of organic compounds by microbial augmentation OC17 in industry wastewater containing chlorinated hydrocarbons showed that the removal rate of COD was 91% during incubation of 10 days. These results indicate that it is possible to apply the microbial augmentation OC17 to industrial wastewaters containing chlorinated organic compounds.

• Restorative Dentistry and Endodontics
• /
• v.31 no.2
• /
• pp.133-139
• /
• 2006

The purposes of this study were firstly to identify the microbial species on gutta-percha (GP) cones exposed at outpatient clinics using polymerase chain reaction, and secondly to evaluate the rapid sterilization effect of two chemical disinfectants at chair side. It also evaluated the alteration of surface texture of GP cones after 5-min soaking into two chemical disinfectants. A total of 100 GP cones from two endodontic departments were randomly selected for microbial detection using PCR assay with universal primer. After inoculation on the sterilized GP cones with the same microorganism identified by PCR assay, they were soaked in two chemical disinfectants: 5% NaOCl and 2% chlorhexidine for 1, 3, 5, and 10 minutes. The sterilization effect was evaluated by turbidity and subculture. The change of surface textures using a scanning electron microscope was also examined after 5 min-soaking in two chemical disinfectants. Results showed that four bacterial species were detected in 17 GP cones, and all the species belonged to the genus Staphylococcus. Two chemical disinfectants were effective in sterilization with just 1 minute soaking. On the SEM picture of NaOCl-soaked GP cone, a cluster of cuboidal crystals was seen on the cone surface. Present data demonstrate that two chemical disinfectants are useful for rapid sterilization of GP cone just before obturation at chair side, while CHX-soaked GP cone has cleaner surface without crystal precipitation than that of NaOCl-treated cone.

• Bulletin of the Korean Chemical Society
• /
• v.33 no.4
• /
• pp.1123-1127
• /
• 2012

P-gp (P-glycoprotein) is a member of the ATP binding cassette (ABC) family of transporters. It transports many kinds of anticancer drugs out of the cell. It plays a major role as a cause of multidrug resistance (MDR). MDR function may be a cause of the failure of chemotherapy in cancer and influence pharmacokinetic properties of many drugs. Hence classification of candidate drugs as substrates or nonsubstrate of the P-gp is important in drug development. Therefore to identify whether a compound is a P-gp substrate or not, in silico method is promising. Recursive Partitioning (RP) method was explored for prediction of P-gp substrate. A set of 261 compounds, including 146 substrates and 115 nonsubstrates of P-gp, was used to training and validation. Using molecular descriptors that we can interpret their own meaning, we have established two models for prediction of P-gp substrates. In the first model, we chose only 6 descriptors which have simple physical meaning. In the training set, the overall predictability of our model is 78.95%. In case of test set, overall predictability is 69.23%. Second model with 2D and 3D descriptors shows a little better predictability (overall predictability of training set is 79.29%, test set is 79.37%), the second model with 2D and 3D descriptors shows better discriminating power than first model with only 2D descriptors. This approach will be used to reduce the number of compounds required to be run in the P-gp efflux assay.

• Journal of Korean Society of Rural Planning
• /
• v.26 no.3
• /
• pp.91-102
• /
• 2020

The purpose of study was analyze the pumping characteristics, Irrigation Efficiency(IE), and irrigation pattern by period of rice growing stage with based on the performance of design irrigation water requirement and operational Galshin Pumping(GP) station in GP irrigation district constructed under rural water development project master plan. GP station was located in Yedang reservoir, Yesan-gun, Chungcheongnam-do and has been supplying irrigation water since 2006. The research data are the Irrigation Water Requirement(IWR) and the Pumping Water Amount(PWA) from 2006 to 2015 at the GP station, which is the supplied amount. The IWR were calculated using the Blaney-Criddle formula of the HOMWRS program, Hydrological Operation Model for Water Resource System, developed by Korea Rural Community Corporation. The Blaney-Criddle formula was used to calculate design irrigation water requirement of Galshin rural water development project master plan. During 2006-2015, the study period, the annual average IWR is 763.2(±149.1)mm, the annual PWA of the GP station is 397.4mm to 1,056.9mm, and those average annual PWA is 643.4(±208.4)mm. The annual IE of GP station 96.5% to 169.0%, and the average annual IE is 124.3%, which is higher than the research results conducted in other pumping stations. Analyzing the irrigation patterns of the GP irrigation district, the IWR Ratio per 10days(IWRR) and the PWA Ratio per 10days(PWAR) of the G P station were obtained. The IWRR is the percentage of IWR for each 10 days of a month to total IWR per year, and the PWAR is the percentage of PWA for each 10 days of a month to total PWA per year. The Kolmogorov- Smirnov(K-S) test results of IWRR and PWAR showed the characteristics classification by rice growing stage and stable normal distribution characteristics. Average IWRR(AIWRR) and Average PWAR(APWAR) are presented as irrigation patterns. Irrigation pattern analysis will be able to standardize comparison, analysis and probability calculation of the pumping station characteristics of different pumping stations and apply to objective evaluation of the pumping station district.

• Journal of Pharmaceutical Investigation
• /
• v.40 no.5
• /
• pp.291-296
• /
• 2010

This study was to investigate the effect of baicalein, an antioxidant, on the bioavailability of nicardipine after orally or intravenously administered nicardipine in rats. Nicardipine was administered orally (12 mg/kg) or intravenously (4 mg/kg) with or without orally administered baicalein (0.4, 2 or 10 mg/kg) to rats. In the inhibitory effect of baicalein on CYP3A4 activity, baicalein inhibited CYP3A4 activity with $IC_{50}$ values of 9.2 ${\mu}M$. The cell-based P-gp activity test using rhodamine-123 also showed that baicalein (30-10 ${\mu}M$, p<0.01) significantly inhibited P-gp activity. Compared with the control group (given nicardipine alone), the area under the plasma concentration-time curve (AUC) was significantly (2 mg/kg, P<0.05; 10 mg/kg, P<0.01) increased by 25.9-60.0%, and the peak concentration ($C_{max}$) was significantly (10 mg/kg, P<0.01) increased by 40.0% in the presence of baicalein after orally administration of nicardipine. Consequently, the relative bioavailability (R.B.) of nicardipine was increased by 1.26- to 1.60-fold and the absolute bioavailability (A.B.) was significantly (2 mg/kg, P<0.05; 10 mg/kg, P<0.01) increased by 26.0-59.9%. Compared to the i.v. control, baicalein did not significantly change pharmacokinetic parameters of nicardipine in i.v. administration. Accordingly, the enhanced oral bioavailability of nicardipine might be mainly due to increased intestinal absorption caused by P-gp inhibition rather than to reduced elimination of nicardipine by baicalein. The increase in the oral bioavailability might be mainly attributed to enhanced absorption in the small intestine via the inhibition of P-gp and reduced first-pass metabolism of nicardipine via the inhibition of the CYP3A subfamily in the small intestine and/or in the liver by baicalein. Based on these results, nicardipine dosage should be adjusted when given concomitantly with baicalein.

• Journal of Ginseng Research
• /
• v.44 no.1
• /
• pp.154-160
• /
• 2020

Background: Korean ginseng (Panax ginseng Meyer) powder is in rising demand because powder forms of foods are convenient to handle and are highly preservable. However, ginseng powder (GP) manufactured using the conventional process of air drying and dry milling suffers nutrient destruction and a lack of microbiological safety. The objective of this study was to prepare GP using a novel process comprised of UV-TiO₂ photocatalysis (UVTP) as a prewashing step, wet grinding, high hydrostatic pressure (HHP), and freeze-drying treatments. Methods: The effects of UVTP and HHP treatments on the microbial population, ginsenoside concentration, and physiological characteristics of GP were evaluated. Results: When UVTP for 10 min and HHP at 600 MPa for 5 min were combined, initial 4.95 log CFU/g-fw counts of total aerobes in fresh ginseng were reduced to lower than the detection limit. The levels of 7 major ginsenosides in UVTP-HHP-treated GP were significantly higher than in untreated control samples. Stronger inhibitory effects against inflammatory mediator production and antioxidant activity were observed in UVTP-HHP-treated GP than in untreated samples. There were also no significant differences in CIELAB color values of UVTP-HHP-treated GP compared with untreated control samples. Conclusion: Combined processing of UVTP and HHP increased ginsenoside levels and enhanced the microbiological safety and physiological activity of GP.

• Asian Pacific Journal of Cancer Prevention
• /
• v.16 no.5
• /
• pp.2043-2049
• /
• 2015

Background: Serum Golgi protein 73 (GP73) as a novel and potential marker for diagnosing hepatocellular carcinoma (HCC) have been found to be elevated in HCC patients and associated with clinical variables representing tumor growth and invasiveness. The aim of this study was to prepare a pair of monoclonal antibodys (mAbs) against GP73 and develop a newly designed double-antibody sandwich enzyme-linked immunosorbent assay (s-ELISA), which would be used in the detection of serum GP73 (sGP73) as well as in the diagnosis of HCC. Materials and Methods: Produced by prokaryotic expression, the purified recombinant GP73 (rGP73), produced by prokaryotic expression, was used to immunize the Balb/c mice. Two hybridoma cell lines against GP73 were obtained by fusing mouse Sp2/0 myeloma cells with spleen cells from the immunized mice. The titers of anti-GP73 mAb reached 1:243,000. Western blotting analysis and Immunohistochemistry staining revealed that anti-GP73 mAb could recognize GP73 protein. The double-antibody s-ELISA was successfully established and validated by 119 HCC and 103 normal serum samples. Results: showed that the detection limit of this method could reach 1.56 ng/ml, and sGP73 levels in HCC group (mean=190.6 ng/ml) were much higher than those of in healthy controls (mean=70.92 ng/ml). Conclusions: Results of our study not only showed that sGP73 levels of HCC patients were significantly higher than those of healthy controls, but also indicated that the laboratory homemade anti-GP73 mAbs could be the optimal tool used in evaluating sGP73 levels, which would provide a solid foundation for subsequent clinical applications.