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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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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.

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Izotopy astatu w medycynie

Pruszyński M., Bilewicz A.

Postępy Techniki Jądrowej

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2003

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Vol. 46, z. 4

22--26

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Biologicznie aktywne bisfosfoniany : struktura, synteza, właściwości i działanie

Bałczewska E., Bałczewski P.

Wiadomości Chemiczne

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2000

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[Z] 54, 11-12

1075-1088

EN

The increasing interest in design and application of biologically active bisphosphonates and the lack of the relevant treatment of this subject in Polish language with emphasis of its chemical aspects, induced us, to review the literature up to April 2000 using Medline and Beilstein Cross Fire databases. Bisphosphonates are chemically and enzymatically stable analogs of physiological pyrophosphates which constitute natural inhibitors of mineralisation. Although first bisphosphonates were synthesized in the middle of XIX century, the concept of their use as inhibitors of bone resorption appeared in 1968. One group of biologically active bisphosphonates, which included the earliest bisphosphonates, constituted methylenebisphosphonates bearing simple 1-alkyl; 1,1-dihalo, 1-thiophenyl and/or 1-hydroxy substituents at the P-C-P grouping with a specific affinity to the bone tissue (etidronate, clodronate, tiludronate). The ability of bisphosphonates to bind to crystals of hydroxyapatites and to prevent both crystal growth and dissolution was enhanced when 1-chlorine atom (as in clodronate) was replaced by 1-hydroxyl group (as in etidronate). Newer bisphosphonates having a basic primary nitrogen atom in an alkyl chain (as in pamidronate and alendronate) and the recent ones containing a tertiary nitrogen (as in ibandronate and olpadronate) or a nitrogen atom within the heterocyclic ring (as in risedronate and zoledronate) are much more potent anti-resorptive compounds. The potency to inhibit bone resorption in rats increases from 1 to 10 000 in the sequence etidronate< clodronate, tiludronate< pamidronate, neridronate< alendronate, olpadronate< ibandronate, risendronate< zoledronate. Very small effective antiresorptive doses of the newest bisphosphonates clearly show that these bisphosphonates inhibit bone resorption by direct cellular effects on osteoclasts or by indirect effect through stimulation of osteoblasts to produce an osteoclast - inhibitory protein factor. In this review historically first syntheses of bisphosphonates described by Menschutkin (1865) and von Bayer-Hofmann (1898) as well as representative syntheses of clodronate, tiludronate, pamidronate, alendronate and risedronate are presented.