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Wielka moc w małej cząsteczce : właściwości i zastosowania bisfosfonianów

Kozicka Dominika, Socha Karolina, Szarek Jarosław, Kuźnik Anna

Wiadomości Chemiczne

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2023

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[Z] 77, 1-2

55--73

EN

Bisphosphonates (BPs) are a group of compounds that are extensively studied around the world. Bisphosphonates are organophosphorus compounds characterized by the presence of the P-C-P skeleton. They are synthetic, thermally stable, and hydrolysis-resistant pyrophosphate analogs that occur naturally in living organisms. BPs have the ability to chelate metals such as magnesium and calcium which results in their high affinity to bone tissue. [1] The above factors determine their biological properties and the wide range of related applications. Bisphosphonates have an established position on the pharmaceutical market and have been used in medicine for many years, mainly as anti-resorptive drugs. They are considered the gold standard in the prevention and treatment of many different bone diseases, such as osteoporosis or Paget disease. [1] The therapeutic potential of bisphosphonates, however, is not limited to the treatment of bone diseases, as more and more reports about their other useful biological properties appear in the literature. [2] The usefulness of bisphosphonates in imaging diagnostics and drug delivery systems is also being explored. [3-5] The following article provides a short literature review on BPs, mainly their structure, properties, and mechanism of action, as well as their current and potential applications.

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New amino bisphosphonate compound for skeletal imaging: Comparison study with methylenediphosphonic acid (MDP) and (1-hydroxyethane-1,1-diyl) diphosphonic acid (HEDP)

Assaad T.

Nukleonika

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2016

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Vol. 61, No. 1

69--74

EN

A novel bisphosphonate derivative (1-aminoethane-1,1-diyl)diphosphonic acid (AEDP) has been prepared and successfully labeled with 99mTc at high labeling yields. The in vivo biodistribution of 99mTc-AEDP has been investigated and compared with two reference compounds Tc-99m methylene diphosphonate (99mTc-MDP) and Tc-99m (1-hydroxyethylidene) diphosphonate (99mTc-HEDP). The biodistribution studies have demonstrated a high uptake of the radiotracer 99mTc-AEDP in the bone and a rapid clearance from the blood (such as the two technetium-labeled bone imaging agents in current use: 99mTc-MDP and 99mTc-HEDP). Additionally, the scintigraphic images of 99mTc-AEDP in normal rats have revealed high selective skeletal uptake.

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In vitro assay of the biological activity of bisphosphonates

Chmielewska E., Miszczyk P., Kafarski P., Kempińska K., Wietrzyk J.

Interdisciplinary Journal of Engineering Sciences

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2014

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Vol. 2, no. 1

13--16

EN

Nowadays, the use of bisphosphonates are the gold standard of treatment of bone diseases. Due to the high utility of these compounds, scientists still search for better and better structures, with a variety of substituents at carbon’s atom and create new libraries or improve methods of their synthesis. To determine the potential effect of newly discovered bisphosphonates, for example antiosteoporotic activity, there are in vitro tests which allow to determine the half maximal inhibitory concentrations (IC50) of cells. This paper describes in detail the methodology for test the biological activity of bisphosphonates. Shows the results of biological activity for synthesized bisphosphonates in relation to the commercial-incadronate and zoledronate.

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Badania nad nowymi biodegradowalnymi kompozytowymi systemami dostarczania bisfosfonianów

Sobczak M., Kolmas J., Olędzka E., Dębek C.

Engineering of Biomaterials

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2014

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Vol. 17, no. 128-129

43--45

PL

Nowe kompozytowe systemy dostarczania bisfosfonianów otrzymano z poliuretanów biodegradowalnych (PU) i nanokrystalicznego hydroksyapatytu (HAP). W pierwszym etapie, zsyntezowano PU z poli(ε-kaprolaktono) dioli (PCL), glikolu polioksyetylenowego, 1,6-diizocyjanianiu heksametylenu i butano-1,4-diolu. PCL zostały otrzymane w procesie polimeryzacji z otwarciem pierścienia katalizowanym enzymami. Następnie, otrzymano kompozytowe systemy dostarczania klodronianu. Przeprowadzono badania fizykochemiczne przygotowanych biomateriałów. Wykonano również badania cytotoksyczności zsyntezowanych polimerów. Wstępne wyniki badań wskazują, że otrzymane kompozyty stanowią perspektywiczną grupę biomateriałów, które mogą potencjalnie zostać wykorzystane w technologii implantacyjnych systemów dostarczania leków.

EN

New composite bisphosphonate delivery systems were prepared from biodegradable polyurethanes (PU) and nanocrystalline hydroxyapatite (HAP). In the first step, the PU were synthesized from poly(ε-caprolactone) diols (PCL), poly(ethylene adipate) diol, 1,6-hexamethylene diisocyanate and 1,4-butanediol. The PCL were obtained by the ring-opening polymerization catalyzed by the enzyme. Next, composite drug delivery systems for clodronate were prepared. The physico-chemical properties of the obtained biomaterials were determined. The cytotoxicity of the synthesized polymers was tested. The preliminary results show that the prepared composites are perspective biomaterials and they can be potentially applied in the technology of implantation drug delivery systems.

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Badania potencjometryczne, ESI-MS i NMR nad kompleksowaniem magnezu(II) i wapnia(II) wybranymi kwasami bisfosfonowymi w roztworze wodnym

Szpak M., Matczak-Jon E., Kurzak B.

Chemik

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2014

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Vol. 68, nr 4

321--328

PL

Przeprowadzono badania nad równowagami w roztworze układów Mg(II)/Ca(II)-L (L= kwas (cykloheksylo)aminometano-1,1-difosfonowy (1), kwas azepan-1-ylo-metano-1,1-difosfonowy (2), kwas azekan-1-ylo-metano-1,1-difosfonowy (3)) metodami pH-potencjometrii, NMR i ESI-MS. Uzyskane wyniki wskazują, że we wszystkich badanych układach preferowane jest tworzenie kompleksów jednordzeniowych o stechiometrii 1:1. Rozpatrywane związki wiążą koordynacyjnie Mg(II) i Ca(II) poprzez atomy tlenu grup fosfonianowych w szerokim zakresie wartości pH.

EN

Solution equilibrium studies on the Mg(II)/Ca(II)-L systems (L= (cyclohexyl)aminomethane-1,1-diphosphonic acid (1), azepan-1-yl-methane-1,1-diphosphonic acid (2), azecan-1-yl-methane-1,1-diphosphonic acid (3) have been performed by pH-potentiometry, NMR and ESI-MS methods. The obtained results suggest preference for the formation of mononuclear complexes of 1:1 stoichiometry in all studied systems. Compounds under consideration coordinate Mg(II) and Ca(II) through oxygen atoms of the phosphonate groups over a broad pH range.