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Table 3 Summary of in vitro studies reporting effects of bisphosphonate on macrophages

From: Tumour macrophages as potential targets of bisphosphonates

Cell Type Bisphosphonate Main Findings Reference
J774 cells
RAW 264 cells
PAM, ALN, IBA, 100 μM
24 hours
Inhibited macrophage proliferation.
Reduced cell viability. Increased cell death.
Rogers et al [68]
J774 cells ALN, 25 μM or 100 μM
IBA 5 μM, 7.5 μM or 10 μM
24 hours
Dose dependent increase in accumulation of unprenylated Rap1A. Firth et al [97]
RAW 264 cells ALN 10 μM; 5, 7, 9 or 16 hours
ALN 100 μM; 1, 3, 5, 7, 9, 16 hours.
Dose and time dependent increase in accumulation of unprenylated Rap1A. Detectable after 16 hours incubation with 10 μM or 5 hours incubation with 100 μM Monkkonen et al [98]
J774 A.1 cells PAM, ZOL, ALN, RIS
1-100 μM for 72 hours.
All BPs induced significant apoptosis
ZOL > RIS > ALN > PAM.
Moreau et al [49]
Macrophage precursor from bone marrow cells and bone marrow derived macrophages PAM
2.5 × 10-7M (=0.25 μM), 96 hours
Significant inhibition M-CSF induced proliferation of bone marrow precursors Cecchini et al [69]
Activated human monocyte/macrophage PAM
100-300 μM
24 hour pre-treatment Then activated with LPS.
Dose-dependent inhibition of MMP-9 expression
Lower doses PAM increases expression.
Valleala et al [71]
Human macrophage-like cell line U937 Clodrolip
20-200 μM
2 days
Decreased cell survival Hiraoka et al [85]
Murine Macrophages Clodrolip
9 μg per well
29 hours
Decreased cell viability Gazzangia et al [86]
Murine peritoneal macrophages Clodrolip
1 mg/ml
6 hours.
Dose-dependent increase in apoptosis. Zeisberger et al [87]
Bone marrow cells from naive mice cultured with M-CSF or tumour supernatant. Zoledronic acid
0.03, 0.15, 0.3 μM
6 days
Dose-dependent inhibition in differentiation of myeloid cells to macrophages.
Decreased in M2 phenotype compared to control.
Veltman et al [89]