• Bulletin of the Korean Chemical Society
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• v.27 no.8
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• pp.1194-1198
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• 2006

For the purpose of developing more effective chelating agents, we have synthesized a diethylene triamine pentaacetic acid(DTPA) analogue by using an amino acid. S-(N-Boc-aminophenyl)-Cys(t-Bu4-DTPA) methylester was prepared in 6 steps with total yield of 47.9%. For the sake of introducing a biomolecule to the DTPA derivative, a selective hydrolysis was performed with 3 M HCl/Ethylacetate = 1 : 3 ($25{^{\circ}C}$, 30 min, vigorous stirring). $^{166}Ho$-Cys-DTPA and $^{166}Ho$-Biotin-Cys-DTPA were prepared by mixing $^{166}Ho$ with DTPA derivatives at room temp in a HCl solution (pH = 5) and the radiochemical stabilities (> 99%) were maintained for over 6 hrs in vitro.

• Pediatric Infection and Vaccine
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• v.17 no.2
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• pp.156-168
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• 2010

Purpose : To compare immunogenicity and reactogenicity of a combined diphtheria-tetanus-acellular pertussis-inactivated poliovirus vaccine (DTPa-IPV, $Infanrix^{TM}$ IPV, GlaxoSmithKline Biologicals) with co-administration of commercially available DTPa and IPV vaccines at separate injection sites (DTPa+IPV). Methods : A total of 458 infants aged 8-12 weeks were randomized to receive three-ose primary vaccination at 2, 4 and 6 months with DTPa-IPV or DTPa+IPV. Blood samples were collected pre and post vaccination for measurement of immune responses. Reactogenicity was assessed following each dose using diary cards. Results : One month post-dose 3, seroprotection rates for anti-diphtheria, anti-tetanus and anti-poliovirus types 1, 2 and 3 were ${\geq}99.5%$ and vaccine response rates to pertussis antigens were at least 98.6% in both DTPa-IPV and DTPa + IPV groups. Non-inferiority between the groups was demonstrated based on pre-defined statistical criteria. Incidences of both local and systemic symptoms were within the same range across both groups with grade 3 symptoms reported following no more than 4.3% of DTPa-IPV doses and 4.5% of DTPa + IPV doses. Two serious adverse events (both pyrexia) after DTPa-IPV administration were considered vaccine-related. Both infants recovered fully. Conclusion : Combined DTPa-IPV vaccine was immunogenic and well tolerated when used as a three-dose primary vaccination course in Korean infants. DTPa-IPV could be incorporated into the Korean vaccination schedule, reducing the number of injections required to complete primary immunization.

• The Korean Journal of Nuclear Medicine
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• v.31 no.4
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• pp.427-432
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• 1997

Re-188 is useful candidate for therapeutic radionuclide because it has a physical half life of 17 hours, contains beta emissions suitable for therapy(maximum energy 2.12MeV) and emits a gamma ray that is suitable for quantitative diagnostic scanning(155keV). To use Re-188 as a radionuclide compound of angioplasty balloon radiotherapy, we investigated the labelling method and biodistribution of Re-188-DTPA We postulated that labeled Re-188-DTPA is preferable because it would be excreted via urinary system more easily than other compounds. To label Re-188 with DTPA, 1ml of 222MBq(6mCi) of Re-188 was added to DTPA solution(DTPA 20mg, $SnCl_2{\cdot}2H_2O$ 10mg, pH 3.5) and boiled at $100^{\circ}C$ for 120min in water bath. pH was adjusted to 5 with 2.3% sodium acetate. Labeling efficiency was measured using TLC-SG(acetone, saline). We evaluated biodistribution of Re-188-DTPA in sacrificed mice at 10 and 60 minutes after injection. We acquired images of kidneys, and drew time-activity curves in normal dogs and rats and calculated Tmax and Tl/2 in rats. The labelling efficiency was 95.7% on average. Labelling of Re-188-DTPA was.stable(90% after 5hours) in vitro at room temperature. According to time-activity curves of dogs and rats, it took 15 to 20 minutes after injection for Re-188-DTPA to be washed out through kidneys. In conclusion, Re-188-DTPA was successfully labeled, Re-188-DTPA was stable in vitro and was excreted early via kidneys in animals. We could recommend Re-188-DTPA as radionuclide of potential use in angioplasty balloon radiotherapy.

• Korean Journal of Soil Science and Fertilizer
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• v.48 no.4
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• pp.312-317
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• 2015

This study was conducted to evaluate effects of diethylene triamine penta acetic acid (DTPA) treatment on growth of red pepper and nutrient availability to salt accumulated soil in the plastic film house. The treatments were no application (Control), chemical fertilizers (NPK), DTPA (0.06, 0.13, and 0.19 mM) and the half of chemical fertilizers (NPK) with DTPA 0.06 mM. Fruit yield of red pepper showed no significant difference between the treatments (control, NPK, DTPA 0.06 mM, 0.13 mM, except for DTPA 0.19 mM. Red peppers were killed by DTPA 0.19 mM treatment because the high concentration of DTPA was toxic to crop. However, dry mass (stem and leave) and nutrient uptake of red pepper in DTPA 0.06 mM treatment increased significantly compared with those of control. In particular, nutrient uptake of red pepper in DTPA 0.06 mM treatment increased in the order of Fe, Mn, and Zn > Ca and Mg > K, as the magnitude of the stability constants of DTPA. Thus the application of DTPA 0.06 mM was the most effective for the alleviation of nutrient accumulation in the plastic film house soils.

• Korean Journal of Soil Science and Fertilizer
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• v.46 no.6
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• pp.665-672
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• 2013

This study was conducted to evaluate the effects of a chelating agent on cucumber growth and changes in soil nutrients availability in polytunnel greenhouse fields. Diethylene triamine penta acetic acid (DTPA) was selected as a chelating agent. Two experiments were carried out as follows: i) For field experiment in the autumn season of 2010, each plot was treated by varying the concentration and the number of times being applied with DTPA; [DTPA (0.5 mM, 1 time/3 months), DTPA (0.06 mM, 1 time/1 week), DTPA (0.13 mM, 1 time/2 weeks), DTPA (0.06 mM, 1 time/1 week)+N]. Conventional practice was also investigated. ii) In the spring and summer seasons of 2011, each plot was treated by varying the concentration (0, 0.06, 0.13, 0.19 mM) of DTPA, chemical fertilizers (NPK), and combination of chemical fertilizers and DTPA 0.06 mM. The fruit yields of cucumber and soil chemical properties had no significant differences between treatments. However, in the spring season of 2011, DTPA 0.06 mM plot added 1 time per 2 weeks increased the yield of cucumber, but caused the reduction of yield in next cultivation season. This result showed that excess use of DTPA can cause the damage of crop growth. The inorgainc contents such as Ca and Mg absorbed by cucumber plant had significant differences between DTPA 0.19 mM (2 times/1 week) and fertilizers plus DTPA treatments [DTPA 0.06 mM (2 times/1 week) + 1/2 NPK, DTPA 0.06 mM (2 times/1 week) + NPK]. The input cost of fertilizers was saved when the concentration and the number of times added with DTPA was 0.06 mM and 1 time a week, respectively. This treatment used 67% less of applied fertilizers cost than the plot of conventional practice did. Thus, this research suggested that the application of DTPA 0.06 mM by 1 time a week can be effective for sustainability of crop production and reduction of fertilizers usage in polytunnel greenhouse.

• The Korean Journal of Nuclear Medicine
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• v.27 no.2
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• pp.270-276
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• 1993

$Technetium-^{99m}$ labeling method using bifunctional chelating agent cyclic DTPA has been evaluated with human polyclonal nonspecific IgG. IgG was conjugated with cyclic DTPA with various molar ratio. Reduction of $^{99m}Tc$ was done with $Na_2S_2O_4$ with various molar excess. Labeling efficiency and identification of polymer was confirmed with HPLC using TSK4000 SW column. Polymer was purified with 100 cm Sepharose 6LB column. Cultured $1{\times}10^9$ Staphylococcus aureus were injected into rat thigh 24 hours later labeled IgG was injected, and in vivo distribution was observed 4 and 24 hours thereafter. Reduction of $^{99m}Tc$ was optimal with the 10000-50000 times molar excess of $Na_2S_2O_4$. Polymer formation increased with increasing mloar excess of cyclic DTPA to IgG. Three step labeling-labeling DTPA conjugated IgG after reduction of $^{99m}Tc$-made more polymer than two two step labeling-simultaneous mixing DTPA conjugated IgG, $^{99m}Tc$ and $Na_2S_2O_4$. $^{99m}Tc$ blood clearance and lower uptake in the abscess and other organs. IgG conjugated with 200 times molar excess of cyclic DTPA showed slower blood clearance with 200 times molar excess of cyclic DTPA showed slower blood clearance than that of 200 times molar excess of cyclic DTPA showed slower blood clearance than that of 20 times molar excess. In the $^{99m}Tc$ labeling of IgG with cyclic DTPA for the immunoscintigraphy, obtimal labeling condition should be chosen, and effect of the $^{99m}Tc$ labeled IgG polymer should be considered.

• Investigative Magnetic Resonance Imaging
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• v.6 no.2
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• pp.158-165
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• 2002

Purpose : To evaluate the effect of Gd-DTPA on signal intensity of diffusion-weighted magnetic resonance(MR) image and apparent diffuse coefficient (ADC) in dog brain with hype racute stroke. Materials and methods : Experimental canine model of hyperacute cerebral infarction was made by selective intraarterial embolization with particulate embolic material. Diffusion-weighted MR imaging was performed in five dogs at 1 hour after the embolization of internal carotid artery. After intravenous bolus injection of Gd- DTPA, additional 11 diffusion-weighted MR images were serially obtained from 2 minutes to 90 minutes after injection in each dog. The author evaluated findings of hyperacute cerebral infarction on diffusion-weighted MR imaging, and calculated mean signal intensity and mean ADC in infarcted region and contralateral normal region. Statistical analysis of mean signal intensity, mean ADC and contrast-noise ratio before and after Gd-DTPA injection was performed. Results : Hyperacute cerebral infarction developed in all five dogs on diffusion-weighted MR images obtained 1 hour after embolization. The area of hyperacute infarction had steady increase in signal intensity on diffusion-weighted MR image and decrease in ADC. In normal perfusion area, decrease in signal intensity was observed at 2 minutes the Gd-DTPA injection, whereas ADC did not changed. Conclusion : Intravenous injection of Gd-DTPA had no influence on ADC in both hyperacute infarction and normally perfused are a, but caused initial transient signal reduction in normally perfused area on diffusion-weighted MR image due to susceptibility effect of Gd-DTPA. It is important to calculate ADC in evaluating the effect of diffusion after injection of Gd-DTPA.

• The Korean Journal of Nuclear Medicine Technology
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• v.14 no.2
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• pp.45-49
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• 2010

Purpose: Several radiopharmaceuticals were used for cisternography. But recently, due to more short acquisition time, high resolution than other radiopharmaceuticals like In-111 DTPA, we were using Tc-99m DTPA in cisternography. Using of Tc-99m DTPA for intrathecal, was not officially recognised by the FDA. And there are matters of aseptic meningitis, muscular tetany, seizures by inappropriate radiopharmaceuticals handling. So, it is necessary to prevent adverse reactions while handling the radiopharmaceuticals using in cisternography. Therefore, this study aims to evaluation of usefulness and procedures for safety of radiopharmaceuticals in cisternography. Materials and Methods: Subjects were 12radioactive tracer vials using in cisternography in 2008 Dec. 16 - 2009 Dec. 30. (1) Radioactive tracer Vial test - We were measured NaPertechnetate radiation dose and volume, normal saline volume for dilution, source volume and dose activity for patient injection. And then, calculated mass of pure DTPA. (2) Bacterial endotoxin test - We performed pyrogen test using by negative/positive control vials which was added normal saline 0.2 mL and added normal saline 0.1 mL, Tc-99m DTPA 0.1 mL in test control vial. And then, reacted by digital hot plate in $37.5^{\circ}C$ for 1 hour and compared of gel-clot in each control vials. (3) Compliance safety procedure - We were checked safety issues and wrote out a safety procedure exam sheet. Results: (1) Radioactive tracer Vial test - Mass of DTPA per dose for patient injection (mg) was 0.88 (mg) on average, and Mass of DTPA per volume for patient injection (mg) was 0.74 (mg) on average. (2) Bacterial endotoxin test - All control test vials showed negative reactions. (3) Compliance safety procedure - We were checked safety issues and wrote out a safety exam sheet in all the exams. So, there were no adverse reactions. Conclusion: We could examine easier to safety tests using by Techscan - DTPA (Mallinckrodt): CaNa3. Each test results were passed the safety tests and there are no adverse reactions. The use of Tc-99m DTPA for cisternography, always has been become an issue. Since it has occur adverse reaction while examine the cisternography using by Tc-99m DTPA, it needs to set up the 'Standard Operating procedures'.

• Journal of the Korean Chemical Society
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• v.49 no.4
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• pp.355-362
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• 2005

• The Korean Journal of Nuclear Medicine
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• v.31 no.4
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• pp.440-451
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• 1997

This study was designed to prospect the $^{111}In$-labelled paclitaxel as tumor imaging agent. In order to provide a taxol molecule with a functional group which is able to chelate In-111, taxol-DTPA conjugate and 2'-hemisuccinyltaxol were synthesized by esterification of taxol at C-2'on C-13 carbon with DTPA anhydride and succinic anhydride, respectively. Synthesis yield of the taxol derivatives was 34% for taxol-DTPA and 80% for 2'-hemisuccinyltaxol. Cytotoxicity of the taxol derivatives were measured by MTT method toward cell lines HT29, B16, P388, and CT26. The cytotoxic activities of the taxol derivatives were maintained, although less active than taxol. Radiolabelling of the taxol derivatives were proceeded directly with $^{111}InCl_3$ or indirectly with $^{111}In$-citrate(ligand-exchange method). The ligand-exchange method was not suitable because some precipitates appeared during the reaction. On the contrary, by direct radiolabelling method, we were able to obtain taxol-DTPA-$^{111}In$ in 100% radiochemical yield. However, 2'-hemisuccinyltaxol was not labelled by both methods. Yield and radiochemical purity of the radiolabelled com-pound were determined by HPLC, paper chromatography and instant thin layer chromatography. Taxol-DTPA-$^{111}In$ was characterized to be hydrophilic by lipophilicity test, and nearly non-adhesive to HT29, B16, P388, and CT26 by cell binding affinity test. Binding affinity of the taxol-DTPA-$^{111}In$ complex to serum proteins was also examined by protein precipitation with 30% trichloroacetic acid. The results showed that 30% of the taxol-DTPA-$^{111}In$ complex binds with serum proteins.