Zoledronic acid monohydrate (Zoledronate monohydrate) is a third-generation bisphosphonate (BP) with potent anti-resorptive activity. It inhibits the differentiation and apoptosis of osteoclasts and also exhibits anti-cancer effects [1].
体内研究
Zoledronic Acid monohydrate (0.05 mg/kg; i.p.; weekly; for 3 weeks) enhances bone mineral density and content [5].
Zoledronic Acid monohydrate (0.5-1 mg/kg; i.p.; weekly; for 3 weeks) disrupts both osteoclast and osteoblast function, impacting bone remodeling in vivo and influencing bone mechanical properties [5].
体外研究
Zoledronic Acid monohydrate (0.1-1 µM; 48 hours) upregulates receptor activator of nuclear factor kB ligand (RANKL) and sclerostin mRNA expressions in osteocyte-like MLO-Y4 cells [2].
Zoledronic Acid monohydrate increases the expression of osteoclastogenesis supporting factor from MLO-Y4 cells [2].
Zoledronic Acid monohydrate enhances RANKL expression via the IL-6/ JAK2/STAT3 pathway in MLO-Y4 cells [2].
Zoledronic Acid monohydrate regulates osteoclast differentiation and function by modulating NF-κB and JNK signaling pathways [3].
Zoledronic Acid monohydrate exhibits inhibitory effects on the differentiation and maturation of MC3T3-E1 cells at concentrations <1 µM [4].
Zoledronic acid monohydrate/唑来磷酸一水化合物 细胞实验
Cell Line
Concentration
Treated Time
Description
References
γδ T cells
3 μg/mL
5 days
Activate γδ T cells for subsequent experiments
Nat Commun. 2021 Feb 4;12(1):792.
U-2OS cells
1 µM
24 h
To investigate the effect of Zoledronic acid on Ras/Akt/mTOR and Ras/ERK1/2/HIF-1α signaling pathways, it was found to inhibit these pathways, increase ABCA1 expression, and restore immune sensitivity.
Cells. 2020 Mar 6;9(3):647.
Saos-2 cells
1 µM
24 h
To investigate the effect of Zoledronic acid on Saos-2 cells, it was found to increase ABCA1 expression and restore immune sensitivity.
Cells. 2020 Mar 6;9(3):647.
leukemia cells
1 μM or 10 μM
48 h
To evaluate the effect of Zoledronic acid on the viability of leukemia cells, results showed that Zoledronic acid had no direct effect on the viability and colony-forming capacity of leukemia cells.
Leukemia. 2018 Nov;32(11):2326-2338.
γδ T cells
2 μM
24 h
To expand γδ T cells, results showed that zoledronic acid effectively promoted the expansion of γδ T cells.
MAbs. 2022 Jan-Dec;14(1):2115205.
Cervical cancer cells derived CSCs
5, 10, 20, 40, 80 μM
1, 2, 3, 4, 5 days
Zoledronic acid inhibited the proliferation of cervical cancer cells derived CSCs, with an IC50 of 23.39 μM at 72 h
J Exp Clin Cancer Res. 2019 Feb 21;38(1):93.
HeLa cells derived CSCs
10, 20, 30 μM
72 h
Zoledronic acid induced apoptosis in HeLa cells derived CSCs, with the apoptotic proportion increasing from 3.2% to 36.2%
J Exp Clin Cancer Res. 2019 Feb 21;38(1):93.
Zoledronic acid monohydrate/唑来磷酸一水化合物 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
C57BL/6 mice
B16-F10 tumor model
Intraperitoneal injection
5 mg/kg
Every 4 days for a total of 5 times
To reduce the population of tumor-associated macrophages (TAMs), thereby decreasing the accumulation of DOX-AS-M-NPs in tumors
Mol Pharm. 2014 Dec 1;11(12):4425-36
BALB/c nude mice
Bone metastasis model
Intraperitoneal injection
100 μg/kg
On days 1, 3 and 7
Zoledronic acid combined with PTX and 4D3 enhanced the antitumor effect, significantly inhibiting tumor growth.
Cancer Sci. 2020 May;111(5):1840-1850
Mice
Hu-CD34+ mouse model
Intravenous injection
20 µg/mice
Administered on days 3, 9, and 15, lasting 21 days
To investigate the therapeutic effect of Zoledronic acid on chemo-immune-resistant osteosarcoma, it was found to slow tumor growth, increase intratumor necrosis and apoptosis, and enhance the ABCA1/ABCB1 ratio and Vγ9Vδ2 T-cell infiltration.
Cells. 2020 Mar 6;9(3):647.
Mice
Osteoporosis model
Intraperitoneal injection
0.25 mg/kg
Twice a week for 2 weeks
ZA prevented CLP-induced bone loss
Sci Rep. 2017 Feb 1;7:41358
Mice
Sfrp4 knockout mice
Intraperitoneal injection
20 µg/kg
Single dose, male mice observed up to 68 weeks, female mice observed up to 24 weeks
Zoledronic acid treatment does not interfere with the development of elevated trabecular bone mass with Sfrp4 disruption and does not differentially affect cortical bone width or thickness.
Bone Res. 2023 Feb 20;11(1):9
Mice
BCR-ABL1+ pre-B ALL model
Intraperitoneal injection
2 μg
5 days a week for 2 weeks
To evaluate the therapeutic effect of Zoledronic acid on leukemia-induced bone loss, results showed that Zoledronic acid inhibited the activity of osteoclasts, restored the bone loss, reduced the bone resorption activity, and prolonged the survival of mice.
Leukemia. 2018 Nov;32(11):2326-2338.
BALB/c nude mice
Xenograft model of cervical cancer cells derived CSCs
Intraperitoneal injection
20, 40, 80 μg/kg
Once daily for 21 days
Zoledronic acid suppressed the growth of xenografts derived from HeLa cells derived CSCs, significantly reducing tumor volume and weight
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