Effect of zoledronic acid on oral fibroblasts and epithelial cells: a potential mechanism of bisphosphonate-associated osteonecrosis.

Article Details

Citation

Scheper MA, Badros A, Chaisuparat R, Cullen KJ, Meiller TF

Effect of zoledronic acid on oral fibroblasts and epithelial cells: a potential mechanism of bisphosphonate-associated osteonecrosis.

Br J Haematol. 2009 Mar;144(5):667-76. doi: 10.1111/j.1365-2141.2008.07504.x. Epub 2008 Nov 20.

PubMed ID
19036117 [ View in PubMed
]
Abstract

Osteonecrosis of the jaw secondary to bisphosphonate infusion (zoledronic acid-ZA) is assumed to be a bone disease. This study investigated the effects of ZA on soft tissues using oral mucosal cells as an in vitro model of soft tissue cell death in the pathogenesis of bone necrosis. Human gingival fibroblast and keratinocyte cell lines were exposed to different concentrations of ZA (0.25-3 micromol/l), using 1 micromol/l as the expected baseline concentration. A dose-response effect on apoptosis and cell proliferation [Terminal deoxynucleotidyl transferase-mediated dUTP-Biotin End Labelling and Annexin V or Coulter counter and 3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2H-tetr azolium), respectively] was observed with increasing ZA concentrations; both reversed using siRNA against caspase 3 or 9. Gene expression analysis using RT(2) Profiler polymerase chain reaction Arrays demonstrated the differential expression of multiple genes involved in apoptosis including those that encode TNF, BCL-2, Caspase, IAP, TRAF and Death Domain families. Western blot analysis confirmed the presence of activated forms of caspase 3 and 9 and underexpression of survivin protein expression. This study demonstrated that low concentrations of ZA rapidly and directly affected the oral mucosal tissues though the induction of a gene-regulated apoptotic process. These findings support the potential for soft tissue injury as an initiating/potentiating event for osteonecrosis.

DrugBank Data that Cites this Article

Pharmaco-transcriptomics
DrugDrug GroupsGeneGene IDChangeInteractionChromosome
Zoledronic acidApprovedBAD572
upregulated
zoledronic acid results in increased expression of BAD mRNA11q13.1
Zoledronic acidApprovedBAG1573
upregulated
zoledronic acid results in increased expression of BAG1 mRNA9p13.3
Zoledronic acidApprovedBAG39531
upregulated
zoledronic acid results in increased expression of BAG3 mRNA10q26.11
Zoledronic acidApprovedBAX581
downregulated
zoledronic acid results in decreased expression of BAX mRNA19q13.33
Zoledronic acidApprovedBCL2A1597
downregulated
zoledronic acid results in decreased expression of BCL2A1 mRNA15q25.1
Zoledronic acidApprovedBCL2L1598
upregulated
zoledronic acid results in increased expression of BCL2L1 mRNA20q11.21
Zoledronic acidApprovedBCL2L2599
upregulated
zoledronic acid results in increased expression of BCL2L2 mRNA14q11.2
Zoledronic acidApprovedBID637
upregulated
zoledronic acid results in increased expression of BID mRNA22q11.21
Zoledronic acidApprovedBIRC2329
downregulated
zoledronic acid results in decreased expression of BIRC2 mRNA11q22.2
Zoledronic acidApprovedBIRC657448
downregulated
zoledronic acid results in decreased expression of BIRC6 mRNA2p22.3
Zoledronic acidApprovedBIRC8112401
downregulated
zoledronic acid results in decreased expression of BIRC8 mRNA19q13.42
Zoledronic acidApprovedBNIP3664
downregulated
zoledronic acid results in decreased expression of BNIP3 mRNA10q26.3
Zoledronic acidApprovedCASP1423581
downregulated
zoledronic acid results in decreased expression of CASP14 mRNA19p13.12
Zoledronic acidApprovedCASP8841
upregulated
zoledronic acid results in increased expression of CASP8 mRNA2q33.1
Zoledronic acidApprovedCD40LG959
downregulated
zoledronic acid results in decreased expression of CD40LG mRNAXq26.3
Zoledronic acidApprovedDAPK11612
downregulated
zoledronic acid results in decreased expression of DAPK1 mRNA9q21.33
Zoledronic acidApprovedFAS355
upregulated
zoledronic acid results in increased expression of FAS mRNA10q23.31
Zoledronic acidApprovedLTBR4055
upregulated
zoledronic acid results in increased expression of LTBR mRNA12p13
Zoledronic acidApprovedTNF7124
upregulated
zoledronic acid results in increased expression of TNF mRNA6p21.33
Zoledronic acidApprovedTNFRSF10A8797
upregulated
zoledronic acid results in increased expression of TNFRSF10A mRNA8p21.3
Zoledronic acidApprovedTNFRSF11B4982
upregulated
zoledronic acid results in increased expression of TNFRSF11B mRNA8q24.12
Zoledronic acidApprovedTNFRSF1A7132
upregulated
zoledronic acid results in increased expression of TNFRSF1A mRNA12p13.31
Zoledronic acidApprovedTNFRSF2127242
upregulated
zoledronic acid results in increased expression of TNFRSF21 mRNA6p12.3
Zoledronic acidApprovedTNFRSF258718
downregulated
zoledronic acid results in decreased expression of TNFRSF25 mRNA1p36.31
Zoledronic acidApprovedTNFRSF93604
downregulated
zoledronic acid results in decreased expression of TNFRSF9 mRNA1p36.23
Zoledronic acidApprovedTRADD8717
upregulated
zoledronic acid results in increased expression of TRADD mRNA16q22.1
Zoledronic acidApprovedTRAF27186
upregulated
zoledronic acid results in increased expression of TRAF2 mRNA9q34.3
Zoledronic acidApprovedTRAF37187
upregulated
zoledronic acid results in increased expression of TRAF3 mRNA14q32.32
Zoledronic acidApprovedXIAP331
downregulated
zoledronic acid results in decreased expression of XIAP mRNAXq25