Bisacylphosphonates Inhibit Hydroxyapatite Formation and Dissolution in Vitro and Dystrophic Calcification in Vivo

Gershon Golomb*, Ada Schlossman, Hanan Saadeh, Matilda Levi, Joel M. Van Gelder, Eli Breuer

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

47 Scopus citations

Abstract

Some geminal bisphosphonates are used clinically for a number of important bone/calcium related diseases; however, side effects and lack of selectivity impede their wide use. This work reports the synthesis and evaluation of bisacylphosphonates (e.g., adipoyl- and suberoylbisphosphonate). These compounds were found to inhibit significantly hydroxyapatite formation and dissolution in vitro and the calcification of bioprosthetic tissue implanted subdermally in rats. These are the first instances of nongeminal bisphosphonates [P–(C) n– P, n ≥ 2] that have been reported to be active in calcium-related disorders. The reported bisacylphosphonates possess apparent lower toxicity, and their calcium complexes/salts have improved solubility properties. Therefore, they are of potential importance for clinical applications.

Original languageEnglish
Pages (from-to)143-148
Number of pages6
JournalPharmaceutical Research
Volume9
Issue number1
DOIs
StatePublished - Jan 1992

Keywords

  • acylphosphonates
  • bisphosphonates
  • calcification
  • calcinosis
  • hydroxy apatite
  • ketophosphonates
  • phosphonates

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