• Title/Summary/Keyword: No-carrier added

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Stabilization of Quercetin using Organo-hectorite and Its Application in Sunscreen Cosmetics (오가노 헥토라이트를 이용한 쿼세틴 안정화 및 자외선 차단 제품 응용에 관한 연구)

  • Sang Uk Kim;Ji Yeon Hong;Yong Woo Kim;In Ki Hong;Song Hua Xuan;Mid Eum Yun;Sung Ho Lee
    • Journal of the Society of Cosmetic Scientists of Korea
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    • v.50 no.1
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    • pp.1-10
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    • 2024
  • In this study, a quercetin benton gel (QUERPLEX) that stabilized quercetin was prepared using organo hectorite, and its efficacy was confirmed. In addition, a comparative study was conducted on the stability and effectiveness of applying this to sunscreen cosmetics. It was confirmed that QUERPLEX remained stable without showing crystal precipitation and growth for 4 weeks. As a result of measuring antioxidant activity using 2,2-diphenyl-1-picrylhydrazyl (DPPH), it showed antioxidant activity depending on the concentration, and showed a radical elimination ability of 70% or more at a concentration of 2,500 ppm or more, confirming a significant effect. Anti-inflammatory activity experiments using RAW 264.7 cells confirmed that NO production decreased in a concentration-dependent manner by reducing NO production by 8% at 25 ㎍/mL, 23% at 50 ㎍/mL, and 84% at 100 ㎍/mL. As a result of confirming the stability of the formulation according to the method of quercetin in the sunscreen formulation, the stability of the formulation was improved when quercetin was added directly to the formulation. It also improved the UV protection index on in vitro and in vivo, which is expected to have the potential as a component that can have a new boosting effect on UV protection. These results suggest that organo hectorite is very effective as a quercetin carrier and that it can be applied in cosmetic formulations by not only expressing the efficacy of quercetin but also bringing about additional effects.

Application of extraction chromatographic techniques for separation and purification of emerging radiometals 44/47Sc and 64/67Cu

  • Vyas, Chirag K.;Park, Jeong Hoon;Yang, Seung Dae
    • Journal of Radiopharmaceuticals and Molecular Probes
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    • v.2 no.2
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    • pp.84-95
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    • 2016
  • Considerably increasing interest in using the theranostic isotopes/ isotope pairs of radiometals like $^{44/47}Sc$ and $^{64/67}Cu$ for diagnosis and/or therapeutic applications in the nuclear medicine procedures necessitates its reliable production and supply. Separation and purification of no-carrier-added (NCA) isotopes from macro quantitates of the irradiated target matrix along with other impurities is a cardinal procedure amongst several other steps involved in its production. Multitudinous methods including but not limited to liquid-liquid (solvent) extraction, extraction chromatography (EXC), ion exchange, electrodeposition and sublimation are routinely applied either solitarily or in combination for the separation and purification of radioisotopes depending on their production routes, radioisotope of interest and impurities involved. However, application of EXC though has shown promises towards the numerous separation techniques have not received much attention as far as its application prospects in the field of nuclear medicine are concerned. Advances in the recent past for application of the EXC resins in separation and purification of the several medically important radioisotopes at ultra-high purity have shown promising behavior with respect to their operation simplicity, acidic and radiolytic stability, separation efficiencies and speedy procedures with the enhanced and excellent extraction abilities. In this mini review we will be talking about the recent developments in the application and the use of EXC techniques for the separation and purification of $^{44/47}Sc$ and $^{64/67}Cu$ for medical applications. Furthermore, we will also discuss the scientific and practical aspects of EXC in the view of separation of the NCA trace amount of radionuclides.

Simultaneous Determination of Haloperidol and Its Metabolite, Reduced Haloperidol, in Plasma by Gas Chromatography Using Nitrogen Phosphorous Selective Detection (Gas Chromatography-Nitrogen Phosphorous Selective Detection을 이용한 혈장중 Haloperidol 및 대사체인 Reduced Haloperidol의 동시정량)

  • Park, Kyoung-Ho;Lee, Min-Hwa;Shim, Chang-Koo;Lee, Myung-Gull;Park, Jong-Sei
    • Journal of Pharmaceutical Investigation
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    • v.22 no.3
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    • pp.197-204
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    • 1992
  • A gas chromatographic method using nitrogen phosphorous selective detection was developed for simultaneous determination of haloperidol and its metabolite, reduced haloperidol, in human plasma. Combelen was used as internal standard, The method involved extraction and trimethylsilylation followed by the injection of $2-4\;{\mu}l$ of benzene layer, which was used to dissolve the trimethylsilylated derivatives of haloperidol and reduced haloperidol, onto SE-54 column [5% phenyl methyl silica fused capillary column, $16m{\times}0.22\;mm$ $(I.D.){\times}0.33\;{\mu}m$ (coated thickness)]. The temperature of column oven was programmed from $200^{\circ}C\;to\;300^{\circ}C$ at the increase rate of $10^{\circ}C/min and also the temperatures of injector and detector were set at $300^{\circ}C$. Helium was used as carrier gas and its flow rate was maintained at 30 ml/min. The detection was conducted with nitrogen phosphorous selective detector. The retention times for combelen, reduced haloperidol and haloperidol were found to be 9.14, 9.75 and 9.99 min, respectively. The detection limits for haloperidol and reduced haloperidol in human plasma were both 0.2 ng/ml. The coefficients of variation of the intra-assay were generally low (below 9.8%). The mean absolute recoveries of added haloperidol and reduced haloperidol from plasma were 72% and 84%, respectively. No interferences from endogenous substances were found.

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Selective Cytotoxicity of a Novel Platinum (II) Coordination Complex on Human Gastric Cancer Cell Lines and Normal Kidney Cells

  • Jung, Jee-Chang;Kim, Young-Kyu;Yim, Sung-Vin;Park, Seung-Joon;Chung, Joo-Ho;Chang, Sung-Goo;Lee, Kyung-Tae;Rho, Young-Soo
    • The Korean Journal of Physiology and Pharmacology
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    • v.3 no.3
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    • pp.283-291
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    • 1999
  • We have synthesized novel platinum (II) coordination complex containing cis-1,2-diaminocyclohexane (DACH) as a carrier ligand and 1,2-bis(diphenylphosphino)ethane (DPPE) as leaving group. Furthermore, nitrate was added to improve the water-solubility. A new series of [Pt(cis-DACH)(DPPE)] $2NO_3(PC)$ was evaluated its antitumor activity on various MKN-45 human gastric adenocarcinoma cell-lines and normal primary cultured kidney cells. The new platinum complex demonstrated high efficacy in the cytotoxicity on MKN-45 cell-lines as well as adriamycin-resistant (MKN-45/ADR) and cisplatin-resistant (MKN-45/CDDP) cells. The cytotoxicities of PC were found quite less than those of cisplatin in rabbit proximal renal tubular cells, human renal cortical cells and human renal cortical tissues using MTT assay, $[^3H]-thymidine$ uptake and glucose consumption tests. Based on these results, this novel platinum (II) coordination complex, was considered as better a valuable lead for improving antitumor activities with low nephrotoxicities in the development of a new clinically available anticancer chemotherapeutic agents.

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Adenyl Cyclase Activity in Cold-acclimatized Animals (한냉적응이 Adenyl Cyclase Activity에 미치는 영향)

  • Kang, Bok-Soon;Lee, Sang-Ho;Kang, Doo-Hee
    • The Korean Journal of Physiology
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    • v.8 no.2
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    • pp.67-74
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    • 1974
  • The object of this research is aimed to determine the activity of adenyl cyclase in both skeletal muscle sarcolemma and fat cell ghost of epididymal adipose tissue isolated from rats exposed to cold for various length of time in an attempt to evaluate whether the tissue sensitivity to catecholamine is increased when rats are exposed to cold for long periods of time Methods: a)Animals: Albino rats ranging in weight from 150 to 200 gm were used throughout this study. For experimental purposes, the rats are divided into two groups: experimental animals were place4 in a cold room at $4^{\circ}C$, controls being kept at $25^{\circ}C$. At the end of 2, 4, 6, 12, and 16 weeks. exposure to cold the rats were used to measure the adenyl cyclase activity. b) Isolation of plasma membrane from skeletal muscle and adipose tissue: The Plasma membrane of skeletal muscle from hind limbs of rats are prepared by the method employed by Rosenthal et at. and fat cell ghost of epididymal adipose tissue of rats by the method employed by Rodbell. c) Adenyl cyclase assay: Adenyl cyclase activity were measured by the method employed by Marinetti et al. Briefly, plasma membrane was incubated with $3^H-ATP$, various amount of noradrenaline and other incubation mixture at $37^{\circ}C$ for 20 minutes. After stopping the enzyme reaction by immersion in boiling water, carrier 3',5'-AMP was added to the system as a marker and $100\;{\mu}1$ aliquots of incubation mixture were pipetted on $20{\time}20$ Whatman No. 3 MM filter paper for one dimensional chromatography. The cyclic AMP spots were cut off and placed in counting vials containing 10ml of Bray's scintillation cocktail. Radioactivity was determined with a Packard Tri-Carb liquid scintillation counter. The enzyme activity is expressed as nanomoles of cyclic AMP produced per mg of membrane per hour. Result: 1. Average adenyl cyclase activity in the plasma membrane of skeletal muscle before and after noradrenaline administration was significantly higher in the cold-exposed rats as compared to the control. Continuous exposure to cold Produced an increased adenyl cyclase activity before and after noradrenaline administration. Adenyl cyclase activity reached peak levels at the 6 weeks exposure to told and level of adenyl cyclase activity remained high. Noradrenaline administration to the incubation medium induced a significant increase in adenyl cyclase activity and the degree of stimulation were proportional to the hormonal concentration But the rate of inclement in adenyl cyclase activity by noradreasline was the same in both groups. 2. Adenyl cyclase activity in fat cell ghost between cold exposed and control rats showed no significant differences before and after noradreualine administration. In summary, it can be concluded that cold adaptation give rise an increased activity of adenyl cyclase in plasma membrane of skeletal muscle in rats.

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Synthesis and Small Animal Brain PET Study of a Serotonin Receptor Radiotracer, 18F-Mefway (세로토닌 5-HT1A수용체 방사성 추적자 18F-Mefway의 합성과 소동물 뇌 PET 연구)

  • Ahn, Sung-Min;Hong, Tae-Kee;Ryu, Young-Hoon;Choi, Jae-Yong;Kim, Sung-Chul
    • The Journal of the Korea Contents Association
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    • v.9 no.11
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    • pp.262-270
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    • 2009
  • $^{18}F$-mefway has been developed as radioligand for serotonin receptor 5-$HT_{1A}$. The object of this study was to obtain the mefway precursor with the higher yield than previous method and to identify whether $^{18}F$-mefway can bind to 5-$HT_{1A}$ or not. from microPET imaging of small animal brain. Precursor was prepared by a modification of the reported procedure then [$^{18}F$] labeling was performed by adding $^{18}F$ ion at $130^{\circ}C$ in the hot cell for 30min. After purification of reaction mixture using alumina Sep-pak and HPLC, microPET images of small animal brain were determined. The chemical yield of precursor was increased from 9% to 34% using oxalyl chloride and LAH/diethylether. We synthesized a precursor which was successfully labeled with no-carrier-added $^{18}F$-by new synthetic route. This research suggest that $^{18}F$-mefway will be used a radiopharmaceutical for evaluation of central nerve system disorder as imaging a gent for 5-$HT_{1A}$ receptor.

Synthesis of (4-$[^{18}F]$Fluorophenyl)triphenylphosphonium as a Mitochondrial Voltage Sensor for PET (PET영상용 미토콘드리아 막전위 감지기 (4-$[^{18}F]$Fluorophenyl)triphenylphosphonium의 합성)

  • Kim, Dong-Yeon;Yu, Kook-Hyun;Bom, Hee-Seung;Min, Jung-Joon
    • Nuclear Medicine and Molecular Imaging
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    • v.41 no.6
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    • pp.561-565
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    • 2007
  • Purpose: Lipophilic cations including tetraphenylphosphonium (TPP) salts penetrate the hydrophobic barriers of the plasma and mitochondrial membranes, resulting in accumulation in mitochondria in response to the negative inner transmembrane potentials. The development of radiolabeled phosphonium cations as a noninvasive imaging agent may serve as a new molecular "voltage sensor" probe to investigate the role of mitochondria in the pathophysiology and diagnosis of cancer. Materials and Methods: We have synthesized a reference compound (4-fluorophenyl)triphenylphosphonium (TPP) and a labeled compound $[^{18}F]$TPP via two step nucleophilic substitution of no-carrier-added $[^{18}F]$fluoride with the precursor, 4-iodophenyltrimethylammonium iodide, in the presence of Kryptofix-2.2.2 and $K_2CO_3$. Result: The reference compound (4-fluorophenyl)triphenylphosphonium (TPP) was synthesized in 60% yield. The radiolabeled compound $[^{18}F]$TPP was synthesized in $10\sim15%$ yield. The radiochemical purity of the $[^{18}F]$TPP was $95.57{\pm}0.51%$ (n=11). Conclusion: $[^{18}F]$TPP was successfully synthesized that might have a potential to be utilized as a novel myocardial or cancer imaging agent for PET. However, it is required to improve the radiochemical yield to apply $[^{18}F]$TPP in preclinical or clinical researches.

Development of an exclusive column method for 82Sr/82Rb generator using a 100 MeV proton linear accelerator of KOMAC

  • Kye-Ryung Kim;Yeong Su Ha;Sang-Pil Yoon;Yeon-ji Lee;Yong-Sub Cho;Hyeongi Kim;Sang-Jin Han;Jung Young Kim;Kyo Chul Lee;Jin Su Kim
    • Journal of Radiopharmaceuticals and Molecular Probes
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    • v.7 no.2
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    • pp.119-125
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    • 2021
  • 82Sr for 82Rb generator was produced through the irradiation of the proton beam on the nat.RbCI target at the target irradiation facility installed at the end of the Rl-dedicated beamline of the 100 MeV proton linear accelerator of KOMAC (Korea Multi-purpose Accelerator Complex). The average current of the proton beam was 1.2 µA for irradiation time of 150 min. For the separation and purification of the 82Sr from nat.RbCI irradiated, Chelex-100 resin was used. The activities of 82Sr in the irradiated nat.RbCI target solution and after purification were 45.29 µCi and 43.4 µCi, respectively. The separation and purification yield was 95.8%. As an adsorbent to be filled in the generator for 82Sr adsorption hydrous tin oxide was selected. The adsorption yield of 82Sr into the generator adsorbent was > 99 %, and the total amount of 82Sr adsorbed to the generator was 21.6 µCi as of the day of the 82Rb elution experiment. When the elution amount was 22 mL, the maximum82Rb elution yield was 93.3%, and the elution yield increased as the flow rate increased. After the eluted 82Rb was filled in the correction phantom of the small PET for animals, a PET image was taken. The image scan time was set to 5 min, and the phantom PET image was successfully obtained. As results of impurity analysis on eluted 82Rb using ICP-MS, nat.Rb stable isotopes that compete in vivo of 82Rb were identified as undetected levels and were determined to be No-Carrier-Added (NCA).

Synthesis and Biodistribution of Flumazenil Derivative [F-18](3-(2-Fluoro) flumazenil for Imaging Benzodiazepine Receptor (벤조디아제핀 수용체 영상용 양전자 방출 핵종 표지 플루마제닐 유도체 [F-18](3-(2-Fluoro)flumazenil의 합성과 생체 내 분포)

  • Hong, Sung-Hyun;Jeong, Jae-Min;Chang, Young-Soo;Lee, Dong-Soo;Chung, June-Key;Cho, Jung-Hyuck;Lee, Sook-Ja;Kang, Sam-Sik;Lee, Myung-Chul
    • The Korean Journal of Nuclear Medicine
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    • v.33 no.6
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    • pp.527-536
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    • 1999
  • Purpose: Radiotracers that bind to the central benzodiazepine receptor are useful for the investigation of various neurological and psychiatric diseases. [C-11]Flumazenil, a benzodiazepine antagonist, is the most widely used radioligand for central benzodiazepine receptor imaging by PET. We synthesized 3-(2-[F-18]fluoro)flumazenil, a new fluorine-18 ($t_{1/2}$= 110 min) labeled analogue of benzodiazepine receptor imaging agent, and evaluated in vivo for biodistribution in mice. Materials and Methods: Flumazenil (Ro 15-1788) was synthesized by a modification of the reported method. Precursor of 3-(2-[F-18]fluoro)flumazenil, the tosylated flumazenil derivative was prepared by the tosylation of the ethyl ester by ditosylethane. [F-18] labeling of tosyl substitued flumazenil precursor was performed by adding F-18 ion at $85^{\circ}C$ in the hot ceil for 20 min. The reaction mixture was trapped by C18 cartridge, washed with 10% ethanol, and eluted by 40% ethanol. Bidistribution in mice was determined after intravenous injection. Results: The total chemical yield of tosylated flumazenil derivative was ${\sim}40%$. The efficiency of labeling 3-(2-[F-18]fluoro)flumazenil was 66% with a total synthesis time of 50 min. Brain uptakes of 3-(2-[F-18]fluoro)flumazenil at 10, 30, 60 min after injection, were $2.5{\pm}0.37,\;2.2{\pm}0.26,\;2.1{\pm}0.11$ and blood activities were $3.7{\pm}0.43,\;3.3{\pm}0.07,\;3.3{\pm}0.09%ID/g$, respectively. Conclusion: We synthesized a tosylated flumazenil derivative which was successfully labeled with no-carrier-added F-18 by nucleophilic substitution.

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Effect of K2CO3 Loading on the Adsorption Performance of Inorganic Adsorbent for H2S Removal (K2CO3 첨가에 따른 H2S 제거용 무기계 흡착제의 흡착성능 영향에 관한 연구)

  • Jang, Kil Nam;Song, Young Sang;Hong, Ji Sook;You, Young-Woo;Hwang, Taek Sung
    • Clean Technology
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    • v.23 no.3
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    • pp.286-293
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    • 2017
  • The goal of this paper was to improve the performance of the adsorbent to remove $H_2S$. Pellet type adsorbents were prepared by using four kinds of materials ($Fe_2O_3$, $Ca(OH)_2$, Activated carbon, $Al(OH)_2)$ for use as a basic carrier. As the results of $H_2S$ adsorption tests, $Fe_2O_3$ and Activated Carbon improved the adsorption performance of $H_2S$ by 1.5 ~ 2 times, and $Ca(OH)_2$ and $Al(OH)_2$ showed no effect on $H_2S$ adsorption performance. Four basic materials were as carriers, and 5 wt% of KI, KOH and $K_2CO_3$ were added on the carriers, respectively. As the results of $H_2S$ adsorption tests, adsorbent containing $K_2CO_3$ showed the best performance. As a result of $H_2S$ adsorption test with varying $K_2CO_3$ content from 5 to 30 wt%, it was confirmed that adsorption performance was increased up to 20 wt% of $K_2CO_3$ and adsorption performance decreased to 30 wt%. The $H_2S$ adsorption performance was modeled by using Thomas model with varying $K_2CO_3$ contents and the results were used for the adsorption tower design. It was shown that the experimental values and the simulated values were in good agreement with the contents range of $K_2CO_3$ up to 20 wt%. Based on these results, it is expected that not only the adsorption performance of $H_2S$ adsorbent is improved but also life time of the adsorbent is increased.