• Korean Journal of Clinical Pharmacy
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• v.11 no.1
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• pp.7-12
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• 2001

Cilostazol has both antithrombotic and cerebral vasodilating effects, and one of the mechanism is the selective inhibition of platalet cyclic AMP phosphodiesterase. Bioequivalence of two cilostazol tablets, the $Pletaal^{TM}$ (Korea Otsuka Pharmaceutical Co.) and the LG $Cilostazol^{TM}$ (LG Chemical Co.), was evaluated according to the guidelines of Korea Food and Drug Administration (KFDA). Sixteen normal male volunteers ($20\sim29$ years old) were randomly divided into two groups and a randomized $2\times2$ cross-over study was employed. After oral administration of $Pletaal^{TM}$ or LG $Cilostazol^{TM}$ tablet (100 mg cilostazol), blood samples were taken at predetermined time intervals and the serum cilostazol concentrations were determined using an HPLC method with UV/VIS detector. The pharmacokinetic parameters $(AUC_t,\;C_{max}\;and\;T_{max})$ were calculated and ANOVA was utilized for the statistical analysis. The results showed that the differences in AUCt, C_{max} and Tmax between two tablets based on the $Pletaal^{TM}$ tablet were $-5.39\%,\;2.32\%\;and\;4.26\%$, respectively. The powers (1-${\beta}$) for $AUC_t,\;C_{max}\;and\;T_{max}\;were\;83.81\%,\;96.02\%\;and\;91.04%$, respectively. Minimum detectable differences ($\Delta$) and $90\%$ confidence intervals were all less than $\pm20\%$. All these parameters met the criteria of KFDA for bioequivalence, indicating that LG $Cilostazol^{TM}$ tablet is bioequivalent to $Pletaal^{TM}$ tablet.

• Journal of Pharmaceutical Investigation
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• v.29 no.3
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• pp.235-240
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• 1999

Bioequivalence of two clarithromycin tablets, the $Klaricid^{TM}$ (Ciba-Geigy Korea Ltd., Seoul, Korea) and the LG clarithromycin (LG Chemical Co., Ltd., Seoul, Korea), was evaluated according to the Korean Guidelines for Bioequivalence Test (KGBT 1998). Sixteen normal male volunteers $(20{\sim}26\;years\;old)$ were randomly divided into two groups and a randomized $2{\times}2$ cross-over study was employed. After one tablet containing 250 mg of clarithromycin was orally administered, blood sample was taken at predetennined time intervals, and the concentrations of clarithromycin in serum were detennined using HPLC method with electrochemical detector. The pharmacokinetic parameters $(AUC_t,\;C_{max}\;and\; T_{max})$ were calculated and ANOVA was utilized for the statistical analysis of parameters. The results showed that the differences in $AUC_t$, $C_{max}$, and $T_{max}$ between two tablets based on $Klaricid^{TM}$ tablet were 4.06%,2.67% and -9.70%, respectively. The powers $(1-{\beta})$ for $AUC_t$, $C_{max}$ and $T_{max}$ were 83.53%, 92.34% and 96.64%, respectively. Detectable differences $({\Delta})$ and 90 % confidence intervals $(a=0.05) $were all less than ${\pm}20%$. All the parameters above met the criteria of KGBT 1998, indicating that LG clarithromycin tablet is bioequivalent to $Klaricid^{TM}$ tablet.

• Journal of Animal Science and Technology
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• v.54 no.5
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• pp.369-373
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• 2012

AMP-activated protein kinase (AMPK) maintains energy homeostasis in skeletal muscle. Nonetheless, its functional role on protein synthesis with different nutrient availability has not been elucidated. Therefore, the purpose of this study is to examine the effect of AMPK activity on protein content in C2C12 myotubes incubated with low (5 mM; LG) or high (25 mM; HG) glucose media. LG stimulated (p<0.05) AMPK and acetyl CoA carboxylase (ACC) activity compare to those in HG group. Total protein content was higher in myotubes cultured with HG than in those cultured with LG and further increased by AICAR (5-amino-1-${\beta}$-D-ribofuranosyl-imidazole-4-carboxamide). Myotubes cultured with HG showed 7.5% lower UbFL (Ubiquitin Firefly Luciferase)-to-SV40 (Simian virus40) ratio compared to those in LG. Glucose level did not change the phosphorylation level of mammalian target of rapamycin (mTOR). Interestingly, administration of AICAR significantly increased phosphorylation level of mTOR in myotubes cultured with LG but not in those with HG. Overall, this data indicate that AMPK activity and protein turnover are finely regulated in response to different glucose concentration.

• Food Science of Animal Resources
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• v.37 no.1
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• pp.62-70
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• 2017

The aim of this study was identifying a suitable food grade enzymes to hydrolyze whey protein concentrates (WPCs), to give the highest bioactivity. WPCs from ultrafiltration retentate were adjusted to 35% protein (WPC-35) and hydrolyzed by enzymes, alcalase, ${\alpha}-chymotrypsin$, pepsin, protease M, protease S, and trypsin at different hydrolysis times (0, 0.5, 1, 2, 3, 4, and 5 h). These 36 types of hydrolysates were analyzed for their prominent peptides ${\beta}-lactoglobulin$ (${\beta}-Lg$) and ${\alpha}-lactalbumin$ (${\alpha}-La$), to identify the proteolytic activity of each enzyme. Protease S showed the highest proteolytic activity and angiotensin converting enzyme inhibitory activity of IC50, 0.099 mg/mL (91.55%) while trypsin showed the weakest effect. Antihypertensive and antioxidative peptides associated with ${\beta}-Lg$ hydrolysates were identified in WPC-35 hydrolysates (WPH-35) that hydrolyzed by the enzymes, trypsin and protease S. WPH-35 treated with protease S in 0.5 h, responded positively to usage as a bioactive component in different applications of pharmaceutical or related industries.

• Archives of Pharmacal Research
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• v.24 no.6
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• pp.590-596
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• 2001

A new extended-spectrum ${\beta}-lactamase$ with an isoelectric point (pl) of 6.2 was detected in Klebsiella pneumoniae Fl 61 that was isolated from a patient with infection. This strain was highly resistant to the third or fourth generation cephalosporins such as cceftazidime ceftriaxone, cefoperzaone, and cefpirome. Analysis of this strain by the double disk diffusion test showed synergies between amoxicillin-clavulanate (AMX-CA) and cefotaxime, and AMX-CA and aztreonam, which suggested that this strain produced a extended-spectrum ${\beta}-lactamase$ (ESBL). Cenetic analysis revealed that the resistance was due to the presence of a 9.4-kb plasmic, designated as pkpl 61, encoding for new ${\beta}-lactamase$ gene (bla). Sequence analysis showed that a new bla gene of pkpl 61 differed from $bla_{TEM-1}$ by three mutations leading to the following amino acid substitutions: $Val_{84}{\rightarrow}lie,{\;}Ala_{184}{\rightarrow}Val,{\;}and{\;}Gly_{238}{\rightarrow}Ser$. These mutations have not been reported previously in the TIM type ${\beta}-lactamases$ produced by clinical strains. The novel ${\beta}-lactamase$ was overexpressed in E. coli and purified by ion exchange chromatography on Q-Sepharose and CM-Sepharose, and then further purified by gel filtration on Sehadex G-200. The catalytic activity of th8 purified ${\beta}-lactamase$ was confirmed by the nitrocefin disk.

• Bulletin of the Korean Chemical Society
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• v.33 no.9
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• pp.2976-2980
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• 2012

Nitrile-forming eliminations from (E)-2,4-$(NO_2)_2C_6H_2CH=NOC_6H_4-2-X-4-NO_2$ (1a-e) promoted by $R_3N$ in MeCN have been studied kinetically. The reactions are second-order and exhibit Br$\ddot{o}$nsted ${\beta}$ = 0.83-1.0 and ${\mid}{\beta}_{lg}{\mid}$ = 0.41-0.46. The results have been interpreted in terms of highly E1cb-like transition state with extensive $C_{\beta}$-H bond cleavage and limited $N_{\alpha}$-OAr bond cleavage. Comparison with existing data reveals that the structure of the transition state changes from E2-central to highly E1cb-like either by the change of the ${\beta}$-aryl group from Ph to 2,4-dinitrophenyl under the same condition or by the base-solvent system variation from $EtO^-$-EtOH to $Et_3N$-MeCN for a given substrate (1a-e).

• Journal of the Society of Cosmetic Scientists of Korea
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• v.37 no.4
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• pp.327-335
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• 2011

5,4'-dihydroxystilbene-3-O-${\beta}$-D-glucopyranoside (Polydatin) is one of the stilbenes found in Polygonum cuspidatum (P. cuspidatum), however, the effects of polydatin on skin biology remain to be elucidated. In this study, we obtained polydatin from P. cuspidatum and investigated the effects of polydatin in skin-derived melanocytes and fibroblasts. In melanocytes, polydatin inhibited not only the tyrosinase activity and melanin production but the expression of melanogenic factors, tyrosinase and microphthalmia-associated transcription factor (MITF). In addition, the level of type I procollagen in fibroblasts was analyzed, and polydatin significantly induced the production of type I procollagen in a dose-dependent manner. Finally we conformed that topical treatment of polydatin improved wrinkle and induced whitening of human skin in vivo. These data provide evidence that polydatin can be a potent candidate for the improvement of both skin wrinkle and whitening from the point of industry view.

• Asian-Australasian Journal of Animal Sciences
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• v.16 no.10
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• pp.1397-1401
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• 2003

The aim of this study was to determine genotypes of four genetic markers and to investigate their association with milk production traits in Brown Swiss cattle imported to Slovakia. The bovine $\kappa$-casein, $\beta$-lactoglobulin, growth hormone and prolactin genotypes of 107 cows were identified by polymerase chain reaction. Effects all four genetic markers on milk, fat, protein and lactose yields and fat, protein and lactose percentage were estimated from a data set of 249 lactations. The frequency of desirable B allele of $\kappa$-casein gene to milk production was 0.46, alleles A of $\beta$-lactoglobulin gene was 0.55, allele and L of growth hormone gene was 0.45 and allele A and B of bovine prolactin gene were 0.61 and 0.39. The results of milk production obtained in our work showed that BB genotypes of $\kappa$-CN gene, AA genotypes of $\beta$-LG gene, LL genotypes of bGH gene were significantly associated with better milk production traits, mainly about the fat content. Association of a bovine prolactin genotypes with milk production were not found.

• Bulletin of the Korean Chemical Society
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• v.35 no.7
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• pp.2135-2138
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• 2014

A kinetic study is reported for the SNAr reaction of 1-Y-substituted-phenoxy-2,4-dinitrobenzenes (1a-1h) with OH- in 80 mol % $H_2O$/20 mol % DMSO at $25.0{\pm}0.1^{\circ}C$. The second-order rate constant ($k_{OH^-}$) increases as the substituent Y in the leaving group changes from an electron-donating group (EDG) to an electronwithdrawing group (EWG). The Br${\o}$nsted-type plot for the reactions of 1a-1h is linear with ${\beta}_{lg}$ = -0.16, indicating that the reactivity of substrates 1a-1h is little affected by the leaving-group basicity. A linear Br${\o}$nsted-type plot with ${\beta}_{lg}=-0.3{\pm}0.1$ is typical for reactions reported previously to proceed through a stepwise mechanism in which formation of a Meisenheimer complex is the rate-determining step (RDS). The Hammett plot correlated with ${\sigma}_Y{^{\circ}}$ constants results in a much better correlation than that correlated with ${\sigma}_Y{^-}$constants, implyng that no negative charge is developing on the O atom of the leaving group (or expulsion of the leaving group is not advanced at all in the TS). This excludes a possibility that the $S_NAr$ reaction of 1a-1h with $OH^-$ proceeds through a concerted mechanism or via a stepwise pathway with expulsion of the leaving group being the RDS. Thus, the current reactions have been concluded to proceed through a stepwise mechanism in which expulsion of the leaving group occurs rapidly after the RDS.

• Asian-Australasian Journal of Animal Sciences
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• v.17 no.5
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• pp.712-718
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• 2004

This study was carried out to separate the calcium-binding protein derived from enzymatic hydrolysates of cheese whey protein. CWPs (cheese whey protein) heated for 10 min at $100^{\circ}C$ were hydrolyzed by trypsin, papain W-40, protease S, neutrase 1.5 and pepsin, and then properties of hydrolysates, separation of calcium-binding protein and analysis of calcium-binding ability were investigated. The DH (degree of hydrolysis) and NPN (non protein nitrogen) of heated-CWP hydrolysates by commercial enzymes were higher in trypsin than those of other commercial enzymes. In the result of SDS-PAGE (sodium dodecyl sulphate polyacrylamide gel electrophoresis), $\beta$-LG and $\alpha$-LA in trypsin hydrolysates were almost eliminated and the molecular weight of peptides derived from trypsin hydrolysates were smaller than 7 kDa. In the RP-HPLC (reverse phase HPLC) analysis, $\alpha$-LA was mostly eliminated, but $\beta$-LG was not affected by heat treatment and the RP-HPLC patterns of trypsin hydrolysates were similar to those of SDS-PAGE. In ion exchange chromatography, trypsin hydrolysates were shown to peak from 0.25 M NaCl and 0.5 M NaCl, and calcium-binding ability is associated with the large peak, which was eluted at a 0.25 M NaCl gradient concentration. Based on the results of this experiment, heated-CWP hydrolysates by trypsin were shown to have calcium-binding ability.