Cilastatin significantly reduced gentamicin-induced apoptosis, as evidenced by preserved cell morphology and reduced cell detachment. Additionally, Cilastatin decreased caspase-3 activation and nucleosomal DNA fragmentation.
Antioxidants (Basel). 2020 Sep 3;9(9):821
rabbit primary proximal tubule cells (rPTCs)
100 µM
10 min
To evaluate the inhibitory effect of Cilastatin on Imipenem uptake in rPTCs, results showed that Cilastatin significantly inhibited Imipenem uptake.
Acta Pharm Sin B. 2019 Sep;9(5):986-996
hOAT3-HEK293 cells
100 µM
10 min
To evaluate the inhibitory effect of Cilastatin on Imipenem uptake in hOAT3-HEK293 cells, results showed that Cilastatin significantly inhibited Imipenem uptake.
Acta Pharm Sin B. 2019 Sep;9(5):986-996
hOAT1-HEK293 cells
100 µM
10 min
To evaluate the inhibitory effect of Cilastatin on Imipenem uptake in hOAT1-HEK293 cells, results showed that Cilastatin significantly inhibited Imipenem uptake.
Acta Pharm Sin B. 2019 Sep;9(5):986-996
Cilastatin sodium/西司他丁钠 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Kunming mice
Diclofenac-induced acute kidney injury model
Intraperitoneal injection
25-100 mg/kg
Single dose, duration of 24 hours
To evaluate the protective effect of Cilastatin on diclofenac-induced acute kidney injury. Results showed that Cilastatin reduced renal pathological changes, dysfunction, oxidative stress, and inflammation, and decreased the renal distribution of diclofenac and its metabolite DLF-AG.
Br J Pharmacol. 2020 May;177(9):1933-1948.
Wistar rats
Gentamicin-induced acute kidney injury model
Intraperitoneal injection
150 mg/kg
Once daily for 8 days
Cilastatin significantly ameliorated gentamicin-induced renal dysfunction, including reductions in serum creatinine, blood urea nitrogen (BUN), and kidney injury molecule-1 (KIM-1) levels. Furthermore, Cilastatin reduced morphological kidney damage, apoptosis, oxidative stress, and inflammatory responses.
Antioxidants (Basel). 2020 Sep 3;9(9):821
Wistar rats
Cisplatin-induced nephrotoxicity model
Intraperitoneal injection
150 mg/kg
Once daily for 5 days
Cilastatin significantly attenuated cisplatin-induced nephrotoxicity, including body weight loss, renal dysfunction (assessed by GFR, serum creatinine, and BUN), morphological renal lesions, apoptotic cell death, and lipid peroxidation. Additionally, Cilastatin restored cisplatin-induced alterations in renal lipid distribution.
J Lipid Res. 2018 Sep;59(9):1561-1574
New Zealand white rabbits
Imipenem-induced acute kidney injury model
Intravenous injection
200 mg/kg
Single dose, observed for 48 hours
To evaluate the protective effect of Cilastatin on Imipenem-induced nephrotoxicity, results showed that Cilastatin significantly alleviated kidney injury.
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