Synthesis and Biocompatibility Studies of New Iminodiacetic Acid Derivatives
Background: Iminodiacetic acid (IDA) derivatives can be used as ligands to form complexes with technetium, with potential application as hepatobiliary diagnostic agents. The aim of this study was to synthesize five novel IDA derivatives and to compare their effects on plasma haemostasis with clinica...
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MDPI AG
2017-12-01
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Online Access: | https://www.mdpi.com/1420-3049/22/12/2265 |
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author | Magdalena Markowicz-Piasecka Piotr Dębski Elżbieta Mikiciuk-Olasik Joanna Sikora |
author_facet | Magdalena Markowicz-Piasecka Piotr Dębski Elżbieta Mikiciuk-Olasik Joanna Sikora |
author_sort | Magdalena Markowicz-Piasecka |
collection | DOAJ |
description | Background: Iminodiacetic acid (IDA) derivatives can be used as ligands to form complexes with technetium, with potential application as hepatobiliary diagnostic agents. The aim of this study was to synthesize five novel IDA derivatives and to compare their effects on plasma haemostasis with clinically approved ligands for technetium complexation. Methods: The influence of synthesized IDA derivatives on plasma haemostasis was evaluated spectrophotometrically by clot formation and lysis test (CL-test), coagulation assay, Prothrombin Time and Activated Partial Tromboplastin Time. The effects of the tested compounds on erythrocytes were assessed using haemolysis assays, microscopy and flow cytometry studies. Results: Despite their significant influence on the kinetic parameters of the process of clot formation and fibrinolysis, the tested ligands, at potential diagnostic concentrations, did not alter the overall potential of clot formation and lysis (CLAUC). At potential diagnostic concentrations (0.4 μmol/mL) all the tested compounds showed no adverse effects on the membranes of RBCs (Red Blood Cells). Conclusion: IDA derivatives with methoxy substituents in aromatic ring, exert multidirectional effects on plasma haemostasis and should be considered safe as their significant impacts were mostly observed at 4 μmol/mL, which is about 10-fold higher than the theoretical plasma concentrations of these compounds. |
first_indexed | 2024-12-21T20:32:12Z |
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id | doaj.art-f97fe134c8784a4580e552a94e99b9d1 |
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issn | 1420-3049 |
language | English |
last_indexed | 2024-12-21T20:32:12Z |
publishDate | 2017-12-01 |
publisher | MDPI AG |
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series | Molecules |
spelling | doaj.art-f97fe134c8784a4580e552a94e99b9d12022-12-21T18:51:12ZengMDPI AGMolecules1420-30492017-12-012212226510.3390/molecules22122265molecules22122265Synthesis and Biocompatibility Studies of New Iminodiacetic Acid DerivativesMagdalena Markowicz-Piasecka0Piotr Dębski1Elżbieta Mikiciuk-Olasik2Joanna Sikora3Laboratory of Bioanalysis, Department of Pharmaceutical Chemistry, Drug Analysis and Radiopharmacy, Medical University of Lodz, ul. Muszyńskiego1, 90-151 Lodz, PolandStudents Research Group, Laboratory of Bioanalysis, Department of Pharmaceutical Chemistry, Drug Analysis and Radiopharmacy, Medical University of Lodz, ul. Muszyńskiego 1, 90-151 Lodz, PolandDepartment of Pharmaceutical Chemistry, Drug Analysis and Radiopharmacy, Medical University of Lodz, ul. Muszyńskiego 1, 90-151 Lodz, PolandLaboratory of Bioanalysis, Department of Pharmaceutical Chemistry, Drug Analysis and Radiopharmacy, Medical University of Lodz, ul. Muszyńskiego1, 90-151 Lodz, PolandBackground: Iminodiacetic acid (IDA) derivatives can be used as ligands to form complexes with technetium, with potential application as hepatobiliary diagnostic agents. The aim of this study was to synthesize five novel IDA derivatives and to compare their effects on plasma haemostasis with clinically approved ligands for technetium complexation. Methods: The influence of synthesized IDA derivatives on plasma haemostasis was evaluated spectrophotometrically by clot formation and lysis test (CL-test), coagulation assay, Prothrombin Time and Activated Partial Tromboplastin Time. The effects of the tested compounds on erythrocytes were assessed using haemolysis assays, microscopy and flow cytometry studies. Results: Despite their significant influence on the kinetic parameters of the process of clot formation and fibrinolysis, the tested ligands, at potential diagnostic concentrations, did not alter the overall potential of clot formation and lysis (CLAUC). At potential diagnostic concentrations (0.4 μmol/mL) all the tested compounds showed no adverse effects on the membranes of RBCs (Red Blood Cells). Conclusion: IDA derivatives with methoxy substituents in aromatic ring, exert multidirectional effects on plasma haemostasis and should be considered safe as their significant impacts were mostly observed at 4 μmol/mL, which is about 10-fold higher than the theoretical plasma concentrations of these compounds.https://www.mdpi.com/1420-3049/22/12/2265iminodiacetic acidradiopharmaceuticalsbiocompatibilityhaemostasis |
spellingShingle | Magdalena Markowicz-Piasecka Piotr Dębski Elżbieta Mikiciuk-Olasik Joanna Sikora Synthesis and Biocompatibility Studies of New Iminodiacetic Acid Derivatives Molecules iminodiacetic acid radiopharmaceuticals biocompatibility haemostasis |
title | Synthesis and Biocompatibility Studies of New Iminodiacetic Acid Derivatives |
title_full | Synthesis and Biocompatibility Studies of New Iminodiacetic Acid Derivatives |
title_fullStr | Synthesis and Biocompatibility Studies of New Iminodiacetic Acid Derivatives |
title_full_unstemmed | Synthesis and Biocompatibility Studies of New Iminodiacetic Acid Derivatives |
title_short | Synthesis and Biocompatibility Studies of New Iminodiacetic Acid Derivatives |
title_sort | synthesis and biocompatibility studies of new iminodiacetic acid derivatives |
topic | iminodiacetic acid radiopharmaceuticals biocompatibility haemostasis |
url | https://www.mdpi.com/1420-3049/22/12/2265 |
work_keys_str_mv | AT magdalenamarkowiczpiasecka synthesisandbiocompatibilitystudiesofnewiminodiaceticacidderivatives AT piotrdebski synthesisandbiocompatibilitystudiesofnewiminodiaceticacidderivatives AT elzbietamikiciukolasik synthesisandbiocompatibilitystudiesofnewiminodiaceticacidderivatives AT joannasikora synthesisandbiocompatibilitystudiesofnewiminodiaceticacidderivatives |