• YAKHAK HOEJI
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• v.34 no.5
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• pp.291-295
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• 1990

A modified method was investigated for the determination of benzo(a)pyrene metabolites generated by the rat liver microsomes based on the HPLC technique with radioactive flow detection. By adding $[^3H]-dexamethasone$ to the B(a)P metabolites mixture metabolized by the microsome, the poor yield of solvent extaction of B(a)P metabolites was compensated.

• Journal of Radiopharmaceuticals and Molecular Probes
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• v.3 no.2
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• pp.98-102
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• 2017

We demonstrate a detail protocol for the radiosynthesis of a $^{125}I-labeled$ tetrazine prosthetic group and its application to the efficient radiolabeling of trans-cyclooctene-group conjugated human serum albumin (3) using inverse-electron-demand Diels-Alder reaction. Radioiodination of the stannylated precursor (2) was carried out by using [$^{125}I$]NaI and chloramine T as an oxidant at room temperature for 15 min. After HPLC purification of the crude product, the purified $^{125}I-labeled$ azide ([$^{125}I$]1) was obtained with high radiochemical yield ($65{\pm}8%$, n = 5) and excellent radiochemical purity (>99%). Inverse-electron-demand Diels-Alder reaction between ([$^{125}I$]1) and 3 gave the $^{125}I-labeled$ human serum albumin ([$^{125}I$]4) with more than 99% of radiochemical yield as determined by radio-thin-layer chromatography (radio-TLC). These results clearly indicate that the present radiolabeling method will be useful for the efficient and convenient radiolabeling of trans-cyclooctene-group containing biomolecules.

• Journal of Radiopharmaceuticals and Molecular Probes
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• v.4 no.2
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• pp.85-89
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• 2018

We demonstrate a detail protocol for the radiosynthesis of an $^{125}I$-labeled MSTP prosthetic group and its application to the efficient radiolabeling of human serum albumin (HSA). Radioiodination of the precursor (2) was carried out by using $[^{125}I]$NaI and chloramine T as an oxidant at room temperature for 15 min. After HPLC purification of the crude product, the purified $^{125}I$-labeled MSTP ($[^{125}I]1$) was obtained with high radiochemical yield ($73{\pm}5%$, n = 3) and excellent radiochemical purity (>99%). Site-specific reaction between ($[^{125}I]1$) and HSA gave the $^{125}I$-labeled human serum albumin ($[^{125}I]3$) with more than 99% of radiochemical yield as determined by radio-thin-layer chromatography (radio-TLC). These results clearly demonstrate that the present radiolabeling method will be useful for the efficient and convenient radiolabeling of thiol-bearing biomolecules.

• The Korean Journal of Nuclear Medicine Technology
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• v.22 no.2
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• pp.67-73
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• 2018

$[^{11}C]PIB$ synthesis has been performed by a loop-methylation and HPLC purification in our lab. However, this method is time-consuming and requires complicated systems. Thus, we developed an on-cartridge method which simplified the synthetic procedure and reduced time greatly by removing HPLC purification step. We compared 6 different cartridges and evaluated the $[^{11}C]PIB$ production yields and specific activities. $[^{11}C]MeOTf$ was synthesized by using TRACERlab FXC Pro and was transferred into the cartridge by blowing with helium gas for 3 min. To remove byproducts and impurities, cartridges were washed out by 20 mL of 30% EtOH in 0.5 M $NaH_2PO_4$ solution (pH 5.1) and 10 mL of distilled water. And then, $[^{11}C]PIB$ was eluted by 5 mL of 30% EtOH in 0.5 M $NaH_2PO_4$ into the collecting vial containing 10 mL saline. Among the 6 cartridges, only tC18 environmental cartridge could remove impurities and byproducts from $[^{11}C]PIB$ completely and showed higher specific activity than traditional HPLC purification method. This method took only 8 ~ 9 min from methylation to formulation. For the tC18 environmental cartridge and conventional HPLC loop methods, the radiochemical yields were $12.3{\pm}2.2%$ and $13.9{\pm}4.4%$, respectively, and the molar activities were $420.6{\pm}20.4GBq/{\mu}mol$ (n=3) and $78.7{\pm}39.7GBq/{\mu}mol$ (n=41), respectively. We successfully developed a facile on-cartridge methylation method for $[^{11}C]PIB$ synthesis which enabled the procedure more simple and rapid, and showed higher molar radio-activity than HPLC purification method.

• Advances in Traditional Medicine
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• v.7 no.1
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• pp.51-64
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• 2007

Mucus is an aqueous gel complex with a constitution of about 95% water, high molecular weight glycoprotein (mucin), lipid, salts etc. Mucus appears to represent a significant barrier to the absorption of some compounds. Natural mucoadhesive agent was isolated and purified from the aqueous extract of the seeds of prosopis pallida (PP). Formulated tablet with the isolated material by wet granulation method. Some natural edible substances are in consideration for candidates as mucoadhesive agents to claim more effective controlled drug delivery as an alternative to the currently used synthetic mucoadhesive polymers. Subjected the materials obtained from natural source i.e. PP and standard synthetic substance, sodium carboxymethyl cellulose for evaluation of mucoadhesive property by various in vitro and in vivo methods. Through standard dissolution test and a model developed with rabbit, evaluated in vitro controlled release and bioadhesive property of theophylline formulation. Mucoadhesive agent obtained from PP showed good mucoadhesive potential in the demonstrated in vitro and in viνo models. The results suggest that the mucoadhesive agent showed controlled release properties by their application, substantially. In order to assess the gastrointestinal transit time in vivo, a radio opaque X-ray study performed in healthy rabbit testing the same controlled release formulation with and without bioadhesive polymer. Plasma levels of theophylline determined by the HPLC method and those allowed correlations to the in vitro mucoadhesive study results. Better correlation found between the results in different models. PP may acts as a better natural mucoadhesive agent in the extended drug delivery system.

• Journal of Nutrition and Health
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• v.29 no.8
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• pp.889-898
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• 1996

This study estimated the re!ation between psychological stress and stress hormones, nu­t tritional status of patients with non-insulin dependent diabetes mellitus(NIDDM). Psycho­l logical stress such as depr'ession and anxiety in 34 diabetics was analyzedin relation to nutrient intake, blood components such as fasting blood sugar(FBS), hemoglobin AIC, stress hormones a and amino acids. The IeveIs of depression and anxiety were measured by The center for ep­i idemiological studies-depc$pm$111.49pg/ml for total catecholamine ( (norepmephrine and epinephrine) and 233.95 $pm$73.99pg/ml for norepinephrine, 94.03$pm$75. 9 97pg/ml for epinephrine, 13.lS$pm$5.55pl/dl for cortisol and 171.50$pm$62.50pg/ml for gul c cagon respectlveIy. The leveIs of stress hormones in diabetics such as total catecholamine, norep­i mephrine cortisol and glucagon were significantly higher than those in normal control. The lev­el of epmephrine was higher in diabetics but the diffierenee was not significant. The calorie m t take in diabetics was 1762$pm$292keal which is S1.4% lower than Korean recommended dietary a allowances(RDA). Calcium intake was slightly low but other nutrients intakeswere higher than R RDA. The value of fasting blood sugar(FBS), usual fasting blood sugar(usual FBS) which refteet a average FBS during 3 months and hemoglobin Al C in diabetics was 1S4.1S$pm$74.22mg/dl, 177.76$pm$42.77mg/dl and S.S4$pm$2.S2% respec디VeIy. The distribution of plasma amino acids in d diabetics was generally in the normal range. The leveI of anxiety in diabetics was positively cor­related with norepinephrine, concentration and usual FBS. The levels of glucagon, usual FBS a and hemoglobin Aj C were pOSI디veIy correlated with the branched chaimamino acid(BCM : leucme, isoleucme and valine)

• The Korean Journal of Pesticide Science
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• v.19 no.3
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• pp.174-184
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• 2015

In the present study, the metabolism of [$^{14}C$]butachlor was investigated in rice plant according to the OECD test guideline No. 501. [$^{14}C$]Butachlor was treated as granule to paddy water by application of 1.5 kg ingredient (a.i.)/ha at the 3~4 leave stage of rice plant. At 85 days after treatment (DAT), samples of panicle, foliage, and roots were taken for radioactivity analysis. Upon harvest at 126 DAT, rice plants were separated into brown rice, husk, straw, and root parts. Amounts of total radioactivity absorbed by rice plant ranged from 8.6 to 9.8% of applied radioactivity (AR). Total radioactive residues (TRRs) of rice plant at 126 DAT was the highest as 4.0421 mg/kg (7.3% AR) in the straw followed by 1.4595 mg/kg (2.4% AR) in the root, 0.7257 mg/kg (0.1% AR) in the husk. The lowest level recording 0.1020 mg/kg (0.1% AR) was found in brown rice. Each part was extracted with various solvents and solvent/water mixtures. Greater than 70% of TRRs was readily extractable from foliage, panicle, husk and straw. Only 34.0% of the brown rice and 43% of root based on TRRs were extractable showing that the residues were completely assimilated in the plant tissue. The level of non-extractable radioactivity was ranged from 26.2 to 66.0% of TRRs. From this study, five tentative major metabolites (M1, M2, M3, M4 and M5) were observed in rice extracts. Among the metabolites, 2,6-diethylaniline assigned as M4 was identified in rice plant by comparing to retention time of reference standard. Un-metabolized butachlor was not detected in any fractions. In soil extracts, N-(butoxymethyl)-N-(2,6-diethyl phenyl)acetamide, 2,6-diethylaniline, M2, M3 and M5 were observed. And the concentration of butachlor was low level (ca. 0.03 mg/kg).