• YAKHAK HOEJI
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• v.58 no.5
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• pp.343-348
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• 2014

In the present studies, we examined effect of chamomile flowers extract (CH-Ex), which has traditionally been used as antiphlogistics in Europe for many centuries, against Candida albicans-caused septic arthritis. Candida albicans is a major etiological agent among fungal septic arthritis. This effect was investigated in a murine model of the septic arthritis. That is, mice that were given an emulsion form of C. albicans cell wall (CACW) via footpad route were treated intraperitoneally with the CH-Ex for 3 times every 3 days. Degrees of the footpad-swellings were measured with dial gauger. Data showed that the CH-Ex resulted in the reduction of swelling. For instance, at Day 9 when swelling reached the highest peak, there was up to app. 60% reduction of edema in mice injected with the CH-Ex, compared to that of the control mice that received no treatment (P<0.05). This therapeutic anti-arthritic activity appeared to be mediated by inhibitions of NO (nitric oxide) production from activated RAW264.7 macrophages and proliferation of Con A-treated T lymphocytes. Analysis by HPLC revealed that the CH-Ex contained eight polyphenolic compounds including chlorogenic acid (CRA) and rutin. We have reported the CRA and rutin respectively have the anti-arthritic activity. This correlation implicates that CRA and rutin in the CH-Ex may be responsible for the activity. Combined all together, the CH-Ex has anti-arthritic activity against C. albicans-caused septic arthritis, possibly by inhibiting NO production and proliferation of T cells. This activity seems to be contributed by, at least, CRA and rutin among the compounds in the CH-Ex.

• Archives of Pharmacal Research
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• v.22 no.2
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• pp.165-172
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• 1999

In the present work , the transport mechanism of a capsaicin derivative, DA-5018, through blood-brain barrier (BBB) has been investigated to evaluate the feasibility of potential drug development. The result of pharmacokinetic parameters obtained from the intravenous injection of plasma volume marker,$[3^H]RSA$ and $[{14}^C]DA-5018$, indicated that both AUC, area under the plasma concentration curve and VD, volume of distribution in brain of $[3^H]RSA$ agreed with those reported ($1620{\pm}10 $percentage injected dose minute per milliliter (%IDmin/ml) and $12.0{\pm}0.1{\mu}l/g$, respectively). Elimination half-life and AUC of $[{14}^C]DA-5018$is corrected by the PHLC analysis, 19.6$\pm$1.2 min and 7.69$\pm$0.85% IDmin/ml, respectively. The metabolic rate of $[{14}^C]DA-5018$was very rapid. The blood-brain barrier permeability surface area (PS) product of $[{14}^C]DA-5018$ was calculated to be 0.24$\pm$0.05 $\mu$l/min/g. The result of internal carotid artery perfusion and capillary depletion suggested that [14C]DA-5018 pass through BBB with the time increasingly. Investigation of transport mechanism of $[{14}^C]DA-5018$ using agonist and antagonist suggested that vanilloid (capsaicin) receptor did not exist in the BBB, and nutrient carrier system in the BBB has no effect on the transport of DA-5018. In conclusion, despite the fact that penetration of DA-5018 through BBB is significant, the intact drug found in the brain tissue is small because of a rapid metabolism. Therefore, for the central analgesic effect of DA-5018, the method to increase the metabolic stability in plasma and the brain permeability should be considered.

• Archives of Pharmacal Research
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• v.27 no.7
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• pp.806-810
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• 2004

Metformin is a biguanide antihyperglycemic agent often used for the treatment of non-insulin dependent diabetics (NIDDM). In this study, the pharmacokinetics and pharmacodynamics of metformin were investigated in Korean healthy volunteers during a fasting state for over 10 h. In order to evaluate the amount of glucose-lowering effect of metformin, the plasma concentrations of glucose were measured for a period of 10 h followed by the administration of metformin (oral 500 mg) or placebo. In addition, the concentration of metformin in blood samples was determined by HPLC assay for the drug. All volunteers were consumed with 12 g of white sugar 10 minutes after drug intake to maintain initial plasma glucose concentration. The time courses of the plasma concentration of metformin and the glucose-lowering effect were analyzed by nonlinear regression analysis. The estimated $C_{max}$, $T_{max}$, $CL_{t}$/F (apparent clearance), V/F(apparent volume of distribution), and half-life of metformin were 1.42$\{pm}$0.07 $\mu\textrm{g}$/mL, 2.59$\{pm}$0.18h, 66.12$\{pm}$4.6 L/h, 26.63 L, and 1.54 h respectively. Since a significant counterclock-wise hysteresis was found for the metformin concentration in the plasma-effect relationship, indirect response model was used to evaluate pharmacodynamic parameters for metformin. The mean concentration at half-maximum inhibition $IC_{50}$, $k_{in}$, $k_{out}$ were 2.26 $\mu\textrm{g}$/mL, 83.26 $H^{-1}$, and 0.68 $H^{-1}$, respectively. Therefore, the pharmacokinetic-pharmacodynamic model may be useful in the description for the relationship between plasma concentration of metformin and its glucose-lowering effect.

• Analytical Science and Technology
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• v.32 no.3
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• pp.96-104
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• 2019

Agastache rugosa, known as Korean mint, is a medicinal plant with many beneficial health effects. In this study, a simple and reliable HPLC-UV method was proposed for the quantification of rosmarinic acid (RA) in the aqueous extracts of A. rugosa. RA was selected as a quantification marker due to its easiness in procurement and analysis. The developed method involved chromatographic separation on a $C_{18}$ column ($250{\times}4.6mm$, $5{\mu}m$) at room temperature. The mobile phase consisted of water and acetonitrile both containing 2 % acetic acid and was run at a flow rate of $1mL\;min^{-1}$. The method was validated for specificity, linearity, precision, and accuracy. It was specific to RA and linear in the range of $50-300{\mu}g\;mL^{-1}$ ($r^2=0.9994$). Intra-day, inter-day, and inter-analyst precisions were ${\leq}0.91%\;RSD$, ${\leq}1.40%\;RSD$, and 1.94 % RSD, respectively. Accuracy was 93.3-95.9 % (${\leq}1.21%\;RSD$). The method could be applied to three batches of bulk samples and three batches of lab scale samples, which were found to be $0.64({\pm}0.04)mg\;g^{-1}$ and $0.48({\pm}0.02)mg\;g^{-1}$ for the dried raw materials of A. rugosa. The results show that the proposed method can be used as a readily applicable method for QC of health functional foods containing the aqueous extracts of A. rugosa.

• Korean Journal of Pharmacognosy
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• v.50 no.2
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• pp.141-147
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• 2019

The aim of this study was to investigate the potential of Acanthopanax sieboldianum (Makino) Koidz (ACS) as a potent antioxidant and antidiabetic agent. The antioxidative and alpha-glucosidase inhibitory activities were examined using the methanol extracts and solvent fractions from ACS-leaf and ACS-stem. Antioxidative activities were measured by in vitro methods such as DPPH and ABTS radical scavenging activity and superoxide dismutase (SOD) activity. When the chloroform and ethyl acetate fractions of ACS-leaf and ethyl acetate fractions of ACS-stem were compared with the control, the SOD-like activity was impaired even at the low treatment concentrations. In addition, the ethyl acetate fractions of ACS-leaf and ACS-stem showed alpha-glucosidase inhibition activities at low treatment concentrations. Analysis of the major components in the fractions of ACS-leaf and ACS-stem was also performed using HPLC. Finally, astragalin, isoqurecetin, chlorogenic acid and caffeic acid contents were measured. Based on this work, we propose that ACS-leaf and ACS-stem have great potential as natural antioxidant and antidiabetic materials related to health benefits.

• Journal of Biomedical and Translational Research
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• v.19 no.4
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• pp.130-139
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• 2018

This study aimed to analyze a high-performance liquid chromatography (HPLC) separation using a pentafluorophenyl column of parent drug hydroxychloroquine (HCQ) and its active metabolite, desethylhydroxchloroquine (DHCQ) applying to determine bioequivalence of two different formulations administered to patients. A rapid, simple, sensitive and specific liquid chromatography-tandem mass spectrometry (LC-MS/MS) method has been developed and validated for bioanalysis of HCQ and its metabolite DHCQ in human whole blood using deuterium derivative $hydroxychloroquine-D_4$ as an internal standard (IS). A triple-quadrupole mass spectrometer was operated using electrospray ionization in multiple reaction monitoring (MRM) mode. Sample preparation involves a two-step precipitation of protein techniques. The removed protein blood samples were chromatographed on a pentafluorophenyl (PFP) column ($50mm{\times}4.6mm$, $2.6{\mu}m$) with a mobile phase (ammonium formate solution containing dilute formic acid) in an isocratic mode at a flow rate of 0.45 mL/min. The standard curves were found to be linear in the range of 2 - 500 ng/mL for HCQ; 2 - 2,000 ng/mL for DHCQ in spite of lacking a highly sensitive MS spectrometry system. Results of intra- and inter-day precision and accuracy were within acceptable limits. A run time of 2.2 min for HCQ and 2.03 min for DHCQ in blood sample facilitated the analysis of more than 300 human whole blood samples per day. Taken together, we concluded that the assay developed herein represents a highly qualified technology for the quantification of HCQ in human whole blood for a parallel design bioequivalence study in a healthy male.

• Korean Journal of Agricultural Science
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• v.46 no.1
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• pp.85-92
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• 2019

This study was intended to provide basic data for a health functional food study by exploring antioxidant activity of reflux extract according to the concentration of ethanol and the extract of ultrasonic waves extracted and reflux extracted under the same solvent conditions. In the same solvent condition, the reflux extract ($75.10{\pm}1.99mg$) showed a higher total phenol content than the ultrasonic wave extract ($51.74{\pm}2.28mg$). Flavonoids also had a higher reflux extract ($25.05{\pm}1.53mg$) than did ultrasonic extracts ($16.23{\pm}1.95mg$). Reflux extract according to ethanol concentration was found to have a higher phenol content than the 70% ethanol extract ($40.60{\pm}1.49mg$) in 60% ethanol extract. Flavonoid content was also similar to phenol content in reflux extract as determined by ethanol concentration from 60% ethanol ($25.05{\pm}1.53mg$) to 70% ethanol extract ($6.60{\pm}0.46mg$). In addition, the antioxidant activity (DPPH, TEAC, FRAP, ORAC) of the reflux extract in the same solvent conditions tended to be higher than that of ultrasonic extracts. Also, 60% ethanol extract had better antioxidant activity than 70% ethanol extract. However, an analysis of phenolic acid content through HPLC showed that the ultrasonic extract had a higher content in the same solvent condition than did the reflux extract. Not only the presence of phenolic acid, but also those of other compounds are believed to be attributed to the activity of antioxidants. Therefore, further studies are needed to clarify this phenomenon.

• Korean Journal of Medicinal Crop Science
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• v.26 no.6
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• pp.471-476
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• 2018

Background: Astragalus membranaceus belonging to the Leguminosae family is often utilized as a traditional medicine. The aim of this study was to elucidate the basic breeding information required to develop short stem A. membranaceus cultivars. Methods and Results: Roots of A. membranaceus advanced yield trial (AYT) lines were harvested in late October 2017. Root yield of six AYT lines were increased in a range of 8.9 - 74.8% compared with 'Aseong' as control (check variety). The height of seven AYT lines were shorter than that of 'Aseong'. In addition, stem diameter of nine AYT lines was thicker than that of 'Aseong'. Consequently, 1502-56, 1503-90, and 1510-80 were selected as elite lines for the development of short stem cultivars. HPLC analysis was perfromed to identify lines with high level active components such as calycosin-7-O-${\beta}$-D-glucoside and calycosin. The levels of both active components were higher in 1502-56, and 1503-90, but not in 1510-80 compared to 'Aseong'. In addition, 2,2-Diphenyl-1-picryl hydrazyl (DPPH) radical scavenging activity was higher in the 1502-56 compared to 'Aseong'. Considering these results, two AYT lines, 1502-56 and 1503-90 were selected as short stem lines with high calycosin-7-O-${\beta}$-D-glucoside and calycosin content. Conclusions: Taken together, Two short stem lines were identified in this study. In our future study, regional yield trial (RYT) will be conducted using these selected lines to develop new cultivars.

• Korean Journal of Medicinal Crop Science
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• v.27 no.3
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• pp.194-201
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• 2019

Background: The Ministry of Environment, Korea recognizes Cotoneaster wilsonii Nakai as a second-class endangered plant. It is a native species that grows in Ulleung-do, Korea. To our knowledge, the bioactivity of this plant has not yet been reported. Therefore, in this study, we have reported the bioactivity of C. wilsonii Nakai. Methods and Results: The anti-oxidant activities of C. wilsonii methanolic extract were investigated in vitro. The anti-oxidant activity was evaluated using the 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical assay, and the total phenolic and flavonoid content were measured. The leaf methanolic extract had the highest DPPH radical scavenging activity ($IC_{50}$; $15.74{\mu}g/m{\ell}$), and it also had the highest total phenolic and flavonoid content ($220.95mg{\cdot}GAE/g$, and $36.46mg{\cdot}QE/g$ extract respectively). Through high performance liquid chromatography (HPLC) analysis, chlorogenic acid was found to be the predominant among all phenolic compounds, showing a concentration of 84.24 mg/g extract. More than 60% decrease in nitric oxide (NO) production was found in the leaf methanolic extract. Conclusions: To the best of our knowldege, this is the first report of the bioactivities of C. wilsonii. The results demonstrate that the leaf methanolic extract of C. wilsonii shows potent anti-oxidant, and anti-inflammatory activities.

• Korean Journal of Pharmacognosy
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• v.49 no.4
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• pp.349-361
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• 2018

Socheongryong-tang (SCRT) was one of the major traditional herbal medicines wildly used in the treatment of respiratory disease. SCRT is being commercially produced in the form of mix extracts powder and soft dry extract by different extract methods in the Korean Herbal Pharmacopeia (KHP). In this study, the contents of marker components and biological activities of the SCRT mix extract powder were compared with those of the SCRT decoction. To analyze the marker components of SCRT, nine marker from eight herbal preparations were chosen. And the method using high performance liquid chromatography (HPLC) with diode-array detector method was established for the simultaneous analysis. Method validation was accomplished by linearity, precision test, and recovery test. The contents of nine marker components in this extract was ascertained by ratio. The biological activities were examined the effect of SCRT on anti-oxidation and pro-inflammation mediated by LPS-stimulation. We confirmed that both of SCRT mix extrct powder and decoction have the similar contents on total polyphenol and flavonoid and inhibited the secretion of nitric oxide (NO), $IL-1{\beta}$, IL-6, tumor necrosis factor $(TNF)-{\alpha}$ and the expression of iNOS, COX-2, $IL-1{\beta}$, IL-6, $TNF-{\alpha}$. These results suggest that SCRT mix extract powder and decoction have a significant correlation.