In Vitro and In Vivo Inhibition of Hydroxyapatite Formation and Dissolution by Bisacylphosphonates and Bishydroxyiminophosphonates

E. Breuer, G. Golomb, A. Hoffman, A. Schlossman, J. M. Van Gelder, H. Saadeh, M. Levi, Y. Eitan

Research output: Contribution to journalArticlepeer-review

5 Scopus citations
Original languageAmerican English
Pages (from-to)167-170
Number of pages4
JournalPhosphorus, Sulfur and Silicon and the Related Elements
Issue number1-4
StatePublished - 1 Mar 1993

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The results show that both bisacylphoephonatee and biehydroxyimino-phosphonates inhibited the calcification. The anticalcification effect of the various compounds was not associated with adverse effects on somatic growth, as could be seen from the weight gain obeerved in all experimental groups. 4. Inhibition of tetracycline (TC) releaee from bone The influence of adipoylbiephosphonate (AdBP) on bone resorption in viva was determined by monitoring the rate of release of tetracycline from the bone by measuring the amount of TC in the blood of rats which were pretreated by injections of tritiated TC. The reeulte which will be presented show that this new bisphosphonate inhibite bone reeorp-tion in viva, without having the adverse side effect6 of the currently used bisphosphonate ADP: namely impairment of bone mineralization, nephrotoxicity and inhibition on somatic growth. In addition, preliminary acute toxicological studies on bisacylphoephonatee also show that the tolerated dose found (neither death6 nor weight lose) for AdBP was ...u :'.t.Jly k.L*L=< + ?.&2 *k.!-Z G? "R.2. T?,e are^.^ i a . w r v T ; ~ S L V L Lãil;~ the better solubility propertiee of the newly reported biaacylphoepho-nates clearly indicate their potential for clinical applications. Acknowledgment Supported in part by the German-Ieraeli Foundation for Scientific Research & Development. References 1. H. Fleisch, Bone 8:S23 (1987); F. J. Schoen, H. Harasaki, K. M. Kim, H. C. Anderson, and R. J. Levy. J. Biomed. Mater. Res. 22:ll-36 (1988). 2. M. D. Francis and R. R. Martodam, In R. L. Hilderbrand (ed. ), The Role of PhOsphonates in Living Systems, CRC Pram, Boca Raton, 1903, pp. 55-96. 3. R. Karaman, A. Goldblum, E. Breuer, and H. Leader. J. Chem. Sac. Perkin Trans. 1 765-774 (1989). 4. E. Breuer, R. Karaman, A. Goldblum, D. Gibson, H. Leader, B.V.L. Potter, and J.H. Cumins, J. Chem. Sac. Perkin Trans. 1, 1988, 3047 - 3057. 5. R.

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