C -11 및 F - 18 표지 콜린의 합성과 체내동태에 관한 연구

전권수,유국현,김상욱,임상무,홍성운,서용섭,양승대,안순혁,허민구 대한핵의학회 2001 핵의학 분자영상 Vol.35 No.3

Objectives: Recently, [methyl-(11)^C]-(β-Hydroxyethyl)trimethylammonium ([(11)^C]choline) has been discovered to be a very effective tracer in imaging various human tumors using positron emission tomography. Because of the short half-life of C-11, it is very difficult to use in a routine imaging procedure and needs a frequent synthesis of [(11)^]choline. This can be supplemented by the substitution of [(11)^Ccholine with [methyS-18]fluorocholine. Here, we would like to report cell uptake and biodistribution of [(11)^Ccholine and [(18)^F]fluorocholine as a basic study. Methods [(11)^C]Choline was prepared by the treatment of [(11)^C]CHzI with N,N-dimethylaminoethanol and [18F]fluorocholine was synthesized from reaction of CHzBr[18F]F with N,N-dimethylaminoethanol. The radiochemical purity was checked by high performance liquid chromatography (HPLC). The biodistribution of [(11)^C]choline and [(18)^F]fluorocholine was determined in balb/c mouse at 5 min, 20 min, 40 min and 80 min. The cell uptake wa measured using glioma (9L) and colon adeocarcinoma (SW620). Results: The radiochemical purity was more than 98% after purification. In the liver, uptake did not change over time the uptake was 20/ID/g for [C]choline and 13%ID/g for [(18)^F]fluorocholine. In the kidney, radioactivity decreased over tirne the uptake was 15%1D/g for [(11)^Ccholine and 20%ID/g for [(18)^F]fluorocholine, 80 min post-injection. The cell uptake of [(11)^Ccholine was 4.93% for glioma (9L) and 18.69F for colon adenocarcinoma (SW620). For [(18)^F]fluorocholine, 1.77% for glioma (9L) and 2.77% for colon adenocarcinoma (SW620). Conclusion: [(11)^CCholine and [(18)^F]fluorocholine showed a different cell uptake tendency, depending on cancer cell line. (Korean J Nucl Med 200135:185-191)

가족성 아밀로이드성 말초신경병증 1예

양우석,서민정,권유석,유현정,노숙영,백소아 대한근전도전기진단의학회 2003 대한근전도 전기진단의학회지 Vol.5 No.2

中學 科學敎育의 探究學習에 대한 評價問項 開發 (Ⅱ)

閔庚德,楊洪準,李善行,鄭遠佑,이병교,金裕漢,羅長薰 경북대학교 과학교육연구소 1985 科學敎育硏究誌 Vol.9 No.-

This study was accomplished to develope the evaluation items for inquiry learning in the 2nd grade Middle School Science for the consecutive study of the evaluation items for inquiry learning in the 1st grade Middle School Science(U-Hang Ki et al, 1984). In this study, paper and pencil test items and performance test items are made by analyzing the abilities of inquiry according to the contents and four basic experiments from each unit in the 2nd grade Middle school science. These evaluation items were applied to tke five classes of the 2nd grade of middle school to test their validity. It is desirable that performance test schuld be used for the evaluation for the abilities of inquiry which can not be evaluated by paper and pencil test. In the evaluation methods of performance test, tester evaluation, peer evaluation and self-evaluation can be applied to the science class in a multi-student class. In higher grade, however tester evaluation is more desirable than peer and self evaluation. It is found that peer evaluation and self-evaluation make possible the perfect study by feedback.

크론병에 대한 CoPPLX의 방어효과에 대한 연구

이호학,김유림,문창기,이재일,양병윤,김종수,이정민,정재혁,안석진,박상준,김윤권,김소연,김영중,조민구,최영자,장성조 圓光大學校 醫科學硏究所 2005 圓光醫科學 Vol.20 No.1

Facile Synthesis and Radioiodine Labeling of Hypericin

Kim, Sang-Wook,Park, Jeong-Hoon,Yang, Seung-Dae,Hur, Min-Goo,Kim, Yu-Seok,Chai, Jong-Seo,Kim, Young-Soon,Yu, Kook-Hyun Korean Chemical Society 2004 Bulletin of the Korean Chemical Society Vol.25 No.8

Hypericin (1,3,4,6,8,13-hexahydroxy-10,11-dimethylphenanthro[1,10,9,8-opqra]perylene-7,14-dione), an antidepressant which is also known to be a potent protein kinase C (PKC) inhibitor was synthesized as a precursor for radioiodine labeling via two step reactions. Malignant glioma cells express higher PKC activity compared to untransformed glial cell. Here we report the synthesis and radioiodine labeling of hypericin as a potential brain tumor imaging radiopharmaceutical. The reference compound, 2-iodohypericin, and its radiolabelled analogues, 2-[$^{123}I$]iodohypericin and 2-[$^{124}I$]iodohypericin have been prepared by the reaction of hypericin with NaI or [$^{123}I$]NaI or [$^{124}I$]NaI. The labeling yield was 60-65% for each analogue and the optimal reaction time was 10 min. The purification and isolation of the labelled products were achieved by a reversed-phase HPLC.

Cardioprotective Effects of BMS-180448, a Prototype mitoK$_{ATP}$ Channel Opener, and the Role of Salvage Kinases, in the Rat Model of Global Ischemia and Reperfusion Heart Injury

Lee, Ju-Han,Jung, In-Sang,Lee, Sung-Hun,Yang, Min-Kyu,Hwang, Ji-Hye,Lee, Hak-Dong,Cho, Yu-Sun,Song, Min-Jin,Yi, Kyu-Yang,Yoo, Sung-Eun,Kwon, Suk-Hyung,Kim, Bo-Kyung,Lee, Chang-Soo,Shin, Hwa-Sup 대한약학회 2007 Archives of Pharmacal Research Vol.30 No.5

To investigate the involvement of reperfusion-induced salvage kinases (RISK) as possible signaling molecules for the cardioprotective effects of BMS-180448, a prototype mitochondrial ATP-sensitive K$^*$ (mitoK$_{ATP}$ ) channel opener, we measured its cardioprotective effects in a rat model of jschemia/reperfusion (1/R) heart injury, together with western blotting analysis of five different signaling proteins. in isolated rat hearts subjected to 30-min global ischemia followed by 30-min reperfusion, BMS-180448 (1, 3 and 10 K${\mu}$M) significantly increased reperfusion left ventricular developed pressure (LVDP) and 30-min reperfusion double product (heart rate x LVDP) in a concentration-dependent manner, while decreasing left ventricular end-diastolic pressure (LVEDP) throughout reperfusion period in a concentration-dependent manner. SDS-PAGE/western blotting analysis of left ventricle reperfused for 30 min revealed that BMS-180448 significantly decreased phospho-GSK3K${\beta}$ at high concentration, whereas it tended toincrease slightly phospho-eNOS and phospho-p70S6K with concentration. However, BMS-180448 had re effect on phospho-Akt and phospho-Bad. These results suggest that the car-dioprotective effects of BMS-180448 against 1/R heart injury may result from direct activation of mitoK$_{ATP}$ channel in cardiomyocytes, with the minimal role of RISK pathway in the activation of this channel and the cardioprotective effects of BMS-180448.

TRPM7 Is Essential for RANKL-Induced Osteoclastogenesis

Yang, Yu-Mi,Jung, Hwi-Hoon,Lee, Sung Jun,Choi, Hyung-Jun,Kim, Min Seuk,Shin, Dong Min The Korean Society of Pharmacology 2013 The Korean Journal of Physiology & Pharmacology Vol.17 No.1

The transient receptor potential melastatin type 7 (TRPM7) channel is a widely expressed non-selective cation channel with fusion to the C-terminal alpha kinase domain and regarded as a key regulator of whole body $Mg^{2+}$ homeostasis in mammals. However, the roles of TRPM7 during osteoclastogenesis in RAW264.7 cells and bone marrow-derived monocyte/macrophage precursor cells (BMMs) are not clear. In the present study, we investigate the roles of TRPM7 in osteoclastogenesis using methods of small interfering RNA (siRNA), RT-PCR, patch-clamp, and calcium imaging. RANKL (receptor activator of NF-${\kappa}B$ ligand) stimulation did not affect the TRPM7 expression and TRPM7-mediated current was activated in HEK293, RAW264.7, and BMM cells by the regulation of $Mg^{2+}$. Knock-down of TRPM7 by siTRPM7 reduced intracellular $Ca^{2+}$ concentration ($[Ca^{2+}]_i$) increases by 0 mM $[Mg^{2+}]_e$ in HEK293 cells and inhibited the generation of RANKL-induced $Ca^{2+}$ oscillations in RAW264.7 cells. Finally, knock-down of TRPM7 suppressed RANKL-mediated osteoclastogenesis such as activation and translocation of NFATc1, formation of multinucleated cells, and the bone resorptive activity, sequentially. These results suggest that TRPM7 plays an essential role in the RANKL-induced $[Ca^{2+}]_i$ oscillations that triggers the late stages of osteoclastogenesis.

Alteration of RANKL-induced osteoclastogenesis in primary cultured osteoclasts from SERCA2+/- mice.

Yang, Yu-Mi,Kim, Min Seuk,Son, Aran,Hong, Jeong Hee,Kim, Kyung-Ho,Seo, Jeong Taeg,Lee, Syng-Ill,Shin, Dong Min Mary Ann Liebert, Inc 2009 Journal of bone and mineral research Vol.24 No.10

<P>RANKL is essential for the terminal differentiation of monocytes/macrophages into osteoclasts. RANKL induces long-lasting oscillations in the intracellular concentration of Ca(2+) ([Ca(2+)](i)) only after 24 h of stimulation. These Ca(2+) oscillations play a switch-on role in NFATc1 expression and osteoclast differentiation. Which Ca(2+) transporting pathway is induced by RANKL to evoke the Ca(2+) oscillations and its specific role in RANKL-mediated osteoclast differentiation is not known. This study examined the effect of a partial loss of sarco/endoplasmic reticulum Ca(2+) ATPase type 2 (SERCA2) on osteoclast differentiation in SERCA2 heterozygote mice (SERCA2(+/-)). The BMD in the tibias of SERCA2(+/-) mice increased >1.5-fold compared with wildtype mice (WT). RANKL-induced [Ca(2+)](i) oscillations were generated 48 h after RANKL treatment in the WT mice but not in the SERCA2(+/-) bone marrow-derived macrophages (BMMs). Forty-eight hours after RANKL treatment, there was a lower level of NFATc1 protein expression and markedly reduced translocation of NFATc1 into the nucleus during osteoclastogenesis of the SERCA2(+/-) BMMs. In addition, RANKL treatment of SERCA2(+/-) BMMs incompletely induced formation of multinucleated cells, leading to reduced bone resorption activity. These results suggest that RANKL-mediated induction of SERCA2 plays a critical role in the RANKL-induced [Ca(2+)](i) oscillations that are essential for osteoclastogenesis.</P>

Influence of Caramel Colorant on Level of 4(5)-Methylimidazole in Coo

Min-Chul Jung,Seong Min Hong,Yu-Jin Kim,So-Jeong Yang,Min-Seon Park,Kwang-Geun Lee 한국산업식품공학회 2016 학술대회 및 심포지엄 Vol.2016 No.10

4(5)-methylimidazole (4(5)-MI) is carcinogenic, nitrogen-containing compound, mainly found during the manufacturing of caramel coloring. Hence, presence of 4(5)-MI is well-known in any food products with addition of caramel coloring for desirable sensory characteristics, such as cookies. Limited work has been conducted to develop suitable analytical method and to investigate effect of caramel coloring in cookies. This study aimed at developing the analytical method for quantification of 4(5)-MI and confirming influence of caramel coloring on level of 4(5)-Mi in cookies. Gas chromatography-mass spectrometry (GC-MS) was utilized for qualification and quantification of 4(5)-MI. Sample preparation procedure specialized in bakery products was fully developed in this study. The concentration of 4(5)-MI in 15 commercial cookies and biscuits ranged from 71.5 to 1254.8 ng/g. Correlation equation (y = 706.42x + 21.792) was obtained to estimate effect of caramel colorant on level of 4(5)-MI in cookies. Further, analytical method developed and results of correlation equation can be utilized in future studies on reduction of 4(5)-MI in many food.

Realgar transforming solution-induced differentiation of NB4 cell by the degradation of PML/RARa partially through the ubiquitin–proteasome pathway

Yang Hai,Xin Wang,Peng Song,Jian-yin Li,Longhe Zhao,Fei Xie,Xiang-min Tan,Qin-Jian Xie,Lan Yu,Yang Li,Zhengrong Wu,Hong Yu Li 대한약학회 2019 Archives of Pharmacal Research Vol.42 No.8

PML/retinoic acid receptor alpha (RARa), as ahallmark of acute promyeloid leukemia (APL), is directlyrelated to the outcome of clinical APL remedy. It isreported that arsenicals can effectively degrade PML/RARa, such as arsenic trioxide and realgar. However, thehigh toxicity or insolubility have hampered their clinicalapplications. Realgar transforming solution (RTS) wasproduced from realgar by bioleaching process in our lab. Previous studies demonstrated that RTS had a significantanti-cancer ability on chronic myeloid leukemia throughoncoprotein degradation. The capacity of RTS on treatingAPL is what is focused on in this study. The results showedthat RTS had a noticeable sensitivity in NB4 cell, and RTSremarkably down-regulated PML/RARa expression andinduced cell differentiation. Further, RTS could accumulatePML/RARa into the nuclear bodies and then executedegradation, which could be reversed by proteasomeinhibitor MG132. The results also exhibited that thereduction of RTS-induced PML/RARa expression accompaniedby the elevation of ubiquitin and SUMO-1 proteinexpression. Finally, PML and SUMO-1 had been demonstratedto be co-localized after RTS treatment byimmunofluorescence co-localization assay and immunoprecipitationassay. In conclusion, these results suggestedthat RTS-induced cell differentiation may attribute to thePML/RARa degradation partially through the ubiquitin–proteasome pathway.