• Journal of Pharmaceutical Investigation
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• v.39 no.6
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• pp.393-400
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• 2009

PHEA (hydroxyethyl-aspartamide)-mPEG (methoy-polyethyleneglycol)-$C_{16}$ (hexadecylamine)-ED (ethylenediamine) was prepared as a drug delivery carrier. The structure and molecular weight of polymers were characterized by $^1H$-NMR and gel permeation chromatography. Micelle size and shape were measured by electro-photometer light scattering and transmission electron microscope. The mean diameter of micelles was 23 nm in aqueous solution. To evaluate the potential of these polymeric micelles as a drug carrier, PSI-mPEG-$C_{16}$-ED was conjugated with Cy5.5 for Near-Infrared Fluorescent (NIRF) based optical imaging. PSI-mPEG-$C_{16}$-ED-Cy5.5 was injected intravenously into mice (n=5) and in vivo NIRF imaging was performed during 48 h after injection. The biodistribution study at 24 h after injection showed the longcirculation property of PSI-mPEG-$C_{16}$-ED-Cy5.5. Therefore, PSI-mPEG-$C_{16}$-ED micelles could be a promising drug carrier and imaging agent.

• Development and Reproduction
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• v.7 no.2
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• pp.113-118
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• 2003

Follicular fluid(FF) of mammalian Graafian follicles contains various kinds of proteins and proteinases that are believed to play important roles during follicular growth oocyte maturation and ovulation of mature oocytes. Previous studies of human FF(hFF) demonstrated the presence of many serine/threonine proteinases and matrix metalloproteinases such as gelatinases, however, little is known about the caseinases. Present study was aimed to examine the presence and the property of caseinolytic enzyme in hFF. Using casein zymographic method, it was found that hFF, human adult serum and cord serum exhibited one intense 80 kDa and another weak 78 kDa bands having caseinolytic activity. When inhibitors were added to the zymographic substrate buffer, caseinolytic activity of both 80 kDa and 78 kDa proteins were inhibited by othylenediarnine tetraacetic acid(EDTA) or soybean trypsin inhibitor(SBTI), but not by E-64, phenylmethylsulfonyl fluoride(PMSF) or 1,10-phenanthroline. Thus both enzymes appear to belong to a family of trypsin-like enzyme. Addition of EDTA to the zymographic substrate buffer almost abolished the caseinolytic activity of both enzymes. However, further addition of a divalent metal ion such as CaC $l_2$, MgC $l_2$, MnC $l_2$ or ZnC $l_2$ to the same buffer fully restored the enzyme activity at 5 mM concentration despite the presence of EDTA. Based upon these observations, 80 kDa and 78 kDa caseinolytic enzymes are present in human follicular fluid and they appear to be trypsin-like enzymes of which caseinolytic activity needs the presence of $Ca^{++}$, aM $g^{++}$, M $n^{++}$ or Z $n^{++}$././././.

• Bulletin of the Korean Chemical Society
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• v.26 no.1
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• pp.146-150
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• 2005

Two new barium vanadium borophosphate compounds, $(NH_4)_2(C_2H_{10}N_2)_6[Ba(H_2O)_5]_2[V_2P_2BO_{12}]_6{\cdot}8H_2O$, Ba- VBPO1 and $(NH_4)_8(C_3H_{12}N_2)_4[Ba(H_2O)_7][V_2P_2BO_{12}]_6{\cdot}17H_2O$, Ba-VBPO2 have been synthesized by interdiffusion methods in the presence of diprotonated ethylenediamine and 1,3-diaminopropane. Compound Ba-VBPO1 has an infinite chain anion (${[BaH_2O)_5]_2[V_2P_2BO_{12}]_6}$$^{14-}$, whereas Ba-VBPO2 has a discrete cluster anion {[$Ba(H_2O)_7][V_2P_2BO_{12}]_6$}$^{16-}$. Crystal Data: $(NH_4)_2(C_2H_{10}N_2)_6[Ba(H_2O)_5]_2[V_2P_2BO_{12}]_6{\cdot}8H_2O$, triclinic, space group P$\overline{1}$ (no. 2), a = 13.7252(7) $\AA$, b = 15.7548(8) $\AA$, c = 15.8609(8) $\AA$, α = 63.278(1)$^{\circ}$, $\beta$ = 75.707(1)$^{\circ}$, $\gamma$ = 65.881(1)$^{\circ}$, Z = 1; $(NH_4)_8(C_3H_{12}N_2)_4[Ba(H_2O)_7][V_2P_2BO_{12}]_6{\cdot}17H_2O$, monoclinic, space group C2/c (no. 15), a = 31.347(2) $\AA$, b = 17.1221(9) $\AA$, c = 22.3058(1) $\AA$, $\beta$ = 99.303(1)$^{\circ}$, Z = 4.

• Journal of Radiopharmaceuticals and Molecular Probes
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• v.1 no.1
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• pp.53-61
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• 2015

Lutetium-177 ($T_{1/2}=6.71day$) is an adequate radionuclide for therapy, which has both beta emission ($E_{max}=497keV$) for therapeutic effect and gamma emission (113 and 208 keV) for imaging. $^{177}Lu$ labeled ethylenediamine-N,N,N',N'-tetrakis (methylene phosphonic acid) (EDTMP) and 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraaminomethylenephosphonate (DOTMP) have been proposed as radiopharmaceuticals for bone pain palliation. In this study, we compared radiochemistry and biodistribution of $^{177}Lu$-EDTMP and $^{177}Lu$-DOTMP. EDTMP and DOTMP were synthesized, and 1 mg of each was labeled with $^{177}Lu$ at pH 7~8 with high efficiency (>98%). For comparative biodistribution studies, $^{177}Lu$-EDTMP or $^{177}Lu$-DOTMP were injected into ICR-mice through tail vein, and then biodistribution data were obtained as percentages of injected dose per gram of tissue (% ID/g). Urine excretions of both agents in mice were checked for 7 days. Rat images were also obtained after injection of $^{177}Lu$-EDTMP or $^{177}Lu$-DOTMP. $^{177}Lu$-DOTMP (100% at 1 min) showed faster labeling than $^{177}Lu$-EDTMP (100% at 30 min). Both of them were stable at least for 21 days at room temperature. High bone uptakes were found for both $^{177}Lu$-EDTMP and $^{177}Lu$-DOTMP: 38.0 and 34.1% ID/g at 3 hr, respectively; and 33.2 and 18.8% ID/g at 7 day, respectively. Rapid excretions to urine were found for both agents ($^{177}Lu$-EDTMP: 56%, $^{177}Lu$-DOTMP: 63% at 1 day). Other organs showed very low uptakes. Rat images of both $^{177}Lu$-EDTMP and $^{177}Lu$-DOTMP showed high bone uptakes and low soft tissue uptakes. In conclusion, both $^{177}Lu$-EDTMP and $^{177}Lu$-DOTMP showed high potential as bone pain palliation agents. $^{177}Lu$-EDTMP showed higher bone uptake and slower bone clearance in mice than those of $^{177}Lu$-DOTMP.

• Journal of Ginseng Research
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• v.31 no.3
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• pp.154-158
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• 2007

In order to increase the content of germanium in ginseng adventitious roots, the effects of chelating agents on germanium content and root growth were investigated in the submerged cultures of ginseng adventitious roots. Chelating agents such as citric acid, oxalic acid, phosphoric acid, EDTA (Ethylenediamine tetraacetic acid) or EGTA (Ethylene glycol-bis $({\beta}-aminoethylether)-tetraacetic$ acid) were administrated in the submerged culture of ginseng root containing 50 ppm $GeO_2$. After 6 weeks of cultivation, fresh weight, germanium and saponin contents in the roots were analyzed. Among chelating agents, addition of 1.0mM phosphoric acid was found to be best for germanium accumulation. Under this condition, germanium content increased 1.4 times as compared to that of the control. The germanium content in the adventitious roots also increased with addition of EDTA or EGTA, while they inhibited the growth of ginseng adventitious root. Citric and oxalic acids were not effective for increasing germanium content in adventitious roots. As the results, it suggests that the phosphoric acid can be proved as the optimal agent for the enhancement of germanium accumulation in ginseng adventitious roots. These results can be served as a guideline for the mass production of ginseng adventitious roots containing germanium by large-scale production.

• Archives of Pharmacal Research
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• v.18 no.6
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• pp.449-453
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• 1995

The search for patinum (II)-based compounds with improved therapeutic properties was prompted to design and synthesize a new family of water-soluble, third generation cis-diamminedichlorplatinum (II) complexes linked to uracil and uridine. Six heretofore undescribed uracil and uridine-platinum (II) complexes are ; [N-(2-aminoethyl)uracil-5-carboxamide]dichloroplatinum (II)(3a), [N-2(2-aminoethyl)uracil-6-carboxmide]dichloroplatinum (II) (3b),[5-(2-aminorthyl)carbamoyl-2',3',5',-tri-O-acetyluridine] dichloroplatinum (II) (6b), [5-(2-aminoethyl)-carbamoyl]-2',3',5',-tri-O-acetyluridine] dichloroplatinum (II) (6b), [5-(2-aminoethyl)carbamoylu-ridine]dihloroplatinum (II) (7a), [6-(2-aminoethyl)carbamoyluridine]dichloroplatinum (II) (7b). These analogues were prepared from the key starting materials, 5-carboxyuracil (1a) and 6-carboxyuracil (1b) which were reacted with ethylenediamine to afford the respective N-(2-aminoethyl)uracil-5-carboxmide (2a) land N-(2-aminoethyl)uracil-6-carboxamide (2b). The cisplatin complexes 3a and 3b were obtained through the reaction of the respective 2a and 2b ficiently introduced on the .betha.-D-ribose ring via a Vorbruggen-type nucleoside coupling procedure with hexamethyldisilazane, trimethylchlorosilane and stannicchloride under anhydrous acetonitfile to yield the sterospecific .betha.-anomeric 5-carboxy-2',3',5'-tri-O-acetyluridine (4a) and 6-carboxy-2',3',5'-tri-O-acetyluridine (4b), respective 5-(2-aminoethyl)carbamoyl-2',3',5'-tri-O-acetyluridine (5a) and 6-(2-aminoethyl)carbamoyl-2',3',5'-tri-O-acetyluridine (5b). The diamino-uridines 5a and 5b were reacted with potassium tetrachloroplatinate (II) to give the novel nucleoside complexes, 6a and 6b respectively which were deacetylated into the free nucleosides, 7a and 7b by the treatment with CH/sub 3/ONa. The antitumor activities were evaluated against three cell lines (K-562, FM-3A and P-388).

• Journal of the Korean Chemical Society
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• v.29 no.6
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• pp.629-636
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• 1985

The rates of solvolysis of trans-$[Co(AA)_2Cl_2]^+$ in which AA indicates ethylenediamine(en), N-ethylethylenediamine (N-eten), N-methylethylenediamino (N-meen) and trimethylenediamine(tn) respectively have been investigated using conductometric and spectrophotometric methods at various pressure up to 2,000 bar in acetone-water mixture. The activation volumes (${\Delta}V^{\neq}) obtained from the pressure effect on rate constants were -0.2∼0.9 $cm^3mole^{-1}$ for en, -0.2∼0.6 $cm^3mole^{-1}$ for N-eten, -0.8∼6.0 $cm^3mole^{-1}$ for N-meen and 0.7∼7.0$cm^3mole^{-1}$ for tn. The rates of solvolysis of these complexes were analyzed by comparing with the results obtained from excess free energy ($G^E$) and free energy cycle. It was found that $S_N1$ character was increased with decreasing the pressure and increasing the content of acetone in the mixture solvent. In addition to that, the effect of charge separation on the mechanism of solvolysis was discussed.

• Journal of Periodontal and Implant Science
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• v.32 no.1
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• pp.1-12
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• 2002

The periodontal ligament(PDL) is a unique tissue that is crucial for tooth function. However, little is known of the molecular mechanisms controlling PDL function. PDL-specific protein;PDLs22 had been previously identified as a novel protein isolated from cultured human PDL fibroblasts using subtraction hybridization between human gingival fibroblasts and PDL fibroblasts. The aim of this study was to examine the expression pattern and tissue localization of PDLs22 protein in embryonic and various postnatal stages of developing mouse using immunohistochemical staining. Embryos (E18) and postnatal (P1, P4, P5, P15, P18) were decapitated and the heads were fixed overnight in a freshly prepared solution of 4% paraformaldehyde. Some specimens were decalcified for $2{\sim}4$ weeks in a solution containing 10% of the disodium salt of ethylenediamine-tetraacetic acid (EDTA). Next, tissues were dehydrated, embedded in paraffin and sectioned serially at $6{\mu}m$ in thickness. Polyclonal antiserum raised against PDLs22 peptides, ISNKYLVKRQSRD, were made. The localization of PDLs22 in tissues was detected by polyclonal antibody against PDLs22 by means of immunohistochemical staining. The results were as follows; 1. Expression of PDLs22 protein was not detected in the tooth germ of bud and cap stage. 2. At the late bell stage and root formation stage, strong expression of PDLs22 protein was observed in developing tooth follicle, osteoblast-like cells, and subodontoblastic cells in the tooth pulp, but not in gingival fibroblasts, ameloblasts and odontoblasts of tooth germ 3. In erupted tooth, PDLs22 protein was intensely expressed in PDL and osteoblast-like cells of alveolar bone, but not in gingival fibroblasts, mature osteocytes and adjacent salivary glands. 4. In the developing alveolar bone and mid-palatal suture, expression of PDLs22 protein was seen in undifferentiated mesenchymal cells and osteoblast-like cells of developing mid-palatal suture, but not in mature osteocytes and chondrocytes. These results suggest that PDLs22 protein may play an important role in the differentiation of undifferentiated mesenchymal cells in the bone marrow and PDL cells, which can differentiate into multiple cell types including osteoblasts, cementoblasts, and PDL fibroblasts. However, more researches should be performed to gain a better understanding of the exact function of PDLs22 protein which related to the PDL cell differentiation.

• Journal of Korean Society of Occupational and Environmental Hygiene
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• v.6 no.2
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• pp.292-300
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• 1996

Hexavalent chromium($Cr^{+6}$) compounds are considered to be particularly hazardous, primarily because of the associated risk of allergic reaction and cancer. The analytic method of hexavalent chromium such as the s-diphenylcarba-zide(DPC) method and all ether previously used methods are often made uncertain due to significant interferences from organic components. This report can provide a technique for the more rapid and simple determination of total hexavalent chromium. than other currently using methods. The s-diphenylcarbazide method proposed by the U.S. National Institute for Occupational Safety and Health has low recovery rate(15.67 - 48.20%) due to interference, iron chloride and nickel chloride. A microwave oven technique has high recovery rate(about 70%) of insoluble hexavalent chromium. For the difference of ionic charges of $Cr^{+3}$-ethylenediamine tetraacetic acid(EDTA) chelate and $CrO_4{^{-2}}$, we could detect them simultaneously by ion exchanged high performance liquid chromatography. The confirmation of $Cr^{+3}$ and $Cr^{+6}$ were checked by fraction collector and flameless atomic absorption spectrometer. We observed that the small amount of hexavalent chromium is converted to trivalent chromium due to enhancement of chromium reduction by $Fe^{+3}$ or $Ni^{+2}$. As a result of this study, on the analysis of insoluble hexavalent chromium with microwave oven was used for, it may be better and more precise analysis after pretreatment by 2% NaOH-3% $Na_2CO_3$ and then analysis UV-spectrophotometer. It should be done for various studies on insoluble hexavalent chromium on the basis work environmental monitoring so called welding, painting etc.

• Nutrition Research and Practice
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• v.2 no.2
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• pp.74-79
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• 2008

Zinc plays a protective role in anti-atherosclerosis but the clear mechanism has not been proposed yet. In the present study, we evaluated whether zinc modulates atherosclerotic markers, VACM-1 and ICAM-1 and cell viability both in endothelial cells in vitro and mouse aortic cell viability ex vivo. In study 1, as in vitro model, endothelial EA.hy926 cells were treated with $TNF{\alpha}$ for 5 hours for inducing oxidative stress, and then treated with Zn-adequacy ($15\;{\mu}M$ Zn) or Zn-deficiency ($0\;{\mu}M$ Zn) for 6 hours. Pro-atherosclerosis factors, VCAM-1 and ICAM-1 mRNA expression and cell viability was measured. In study 2, as ex vivo model, mouse aorta ring was used. Mourse aorta was removed and cut in ring then, cultured in a 96-well plate. Aortic ring was treated with various $TNF{\alpha}$ (0-30 mg/ml) and intracellular zinc chelator, N, N, N', N', -tetrakis (2-pyridylmethyl) ethylenediamine (TPEN, $0-30\;{\mu}M$) for cellular zinc depletion for 2 days and then cell viability was measured. The results showed that in in vitro study, Zn-adequate group induced more VCAM-1 & ICAM-1 mRNA expression than Zn-deficient group during 6-hour zinc treatment post-5 hour TNF-$\alpha$ treatment, unexpectedly. These results might be cautiously interpreted that zinc would biologically induce the early expression of anti-oxidative stress through the increased adhesion molecule expression for reducing atherosclerotic action, particularly under the present 6-hour zinc treatment. In ex vivo, mouse aortic ring cell viability was decreased as TNF-$\alpha$ and TPEN levels increased, which suggests that mouse aortic blood vessel cell viability was decreased, when oxidative stress increases and cellular zinc level decreases. Taken together, it can be suggested that zinc may have a protective role in anti-atherosclerosis by cell viability in endothelial cells and aorta tissue. Further study is needed to clarify how pro-atherosclerosis molecule expression is modulated by zinc.