Lansoprazole (AG 1749) is an oral proton pump inhibitor that effectively suppresses gastric acid secretion. Additionally, Lansoprazole (AG 1749) demonstrates potent inhibition of neutral sphingomyelinase (N-SMase), making it a brain-penetrant exosome inhibitor[1][2].
体内研究
Lansoprazole treatmentat doses ranging from 20 to 40 mg/kg significantly reduced memory deficits and attenuated biochemical and histopathological alterations induced by STZ and HFD[3].
Lansoprazole administered orally at doses of 20 mg/kg and 40 mg/kg significantly decreases the STZ and HFD-induced elevation in AChE activity[3].
Lansoprazole, administered orally at doses of 20 mg/kg and 40 mg/kg, significantly reduces the STZ and HFD-induced increase in brain MPO level[3].
HFD-fed mice treated with lansoprazole (20 mg/kg and 40 mg/kg, orally) exhibit a significant reduction in body weight compared to the control animals[3].
体外研究
Lansoprazole inhibits gastric acid secretion in a concentration-dependent manner, with an IC50 value of 0.76 μM, over a range of 0.3 to 3 μM[4].
Lansoprazole induces concentration-dependent, reversible, and reproducible relaxations of arteries within the range of 30 to 300 μM[5].
Lansoprazole/兰索拉唑 细胞实验
Cell Line
Concentration
Treated Time
Description
References
HEK293 cells
20 μM
30 minutes
Enhances polyubiquitination of TRAF6
EBioMedicine. 2015 Nov 17;2(12):2046-61.
Human primary white adipocytes
10 μmol/L
LPZ treatment induced the expression of thermogenic markers UCP1 and PPARGC1A
Acta Pharm Sin B. 2024 Apr;14(4):1711-1725.
Mouse primary subcutaneous white adipocytes
10 μmol/L
LPZ treatment significantly increased basal, maximal and proton leak respiration and elevated the expression of thermogenic genes
Acta Pharm Sin B. 2024 Apr;14(4):1711-1725.
Mouse primary brown adipocytes
10 μmol/L
LPZ treatment significantly increased basal, maximal and proton leak respiration and elevated the expression of thermogenic genes
Acta Pharm Sin B. 2024 Apr;14(4):1711-1725.
MRC-5 lung fibroblasts
10 µM
72 hours
Lansoprazole showed intracellular activity against Mycobacterium tuberculosis in MRC-5 lung fibroblasts with an IC50 of 1.47 µM
Nat Commun. 2015 Jul 9;6:7659.
Human microvascular endothelial cells (HMVECs)
20 μM
24 hours
To study the effect of PPIs on intracellular ADMA concentration, results showed PPIs increased intracellular ADMA by ~30%
Circulation. 2013 Aug 20;128(8):845-53.
RAW 264.7 cells
1-2.5 μM
4 days
Significantly increased the proportion of large osteoclasts
EBioMedicine. 2015 Nov 17;2(12):2046-61.
Human mesenchymal stromal cells
20 μM
2 days
Enhances nuclear accumulation of Runx2 and induces osteoblastogenesis
EBioMedicine. 2015 Nov 17;2(12):2046-61.
NIH3T3 fibroblasts
160 μM
180 seconds
To test the inhibitory effect of lansoprazole on swelling-dependent chloride channels (IClswell), results showed that lansoprazole could block IClswell with an IC50 of 160 μM.
Br J Pharmacol. 2000 Feb;129(3):598-604.
Candida auris AR0390
40 µg/mL (108 µM/mL) LNP + 2 µg/mL AmB
6 hours
To assess the killing kinetics of the AmB/LNP combination, lansoprazole restored the fungicidal properties of AmB against resistant C. auris within 6 hours.
Emerg Microbes Infect. 2024 Dec;13(1):2322649.
Candida auris AR0390
16 µM/mL
24 hours
To screen for drugs that enhance AmB's antifungal activity, lansoprazole was identified as a potent enhancer of AmB against C. auris AR0390.
Emerg Microbes Infect. 2024 Dec;13(1):2322649.
Aβ42 fibrils
2.5–10 μM
750 s
Evaluation of binding kinetics of lansoprazole with Aβ42 fibrils, showing multiple binding sites
Eur J Nucl Med Mol Imaging. 2024 Nov;51(13):3960-3977.
ΑSyn fibrils
2.5–10 μM
750 s
Evaluation of binding kinetics of lansoprazole with αSyn fibrils, showing multiple binding sites
Eur J Nucl Med Mol Imaging. 2024 Nov;51(13):3960-3977.
Lansoprazole/兰索拉唑 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
C57BL/6J male mice
High-fat diet (HFD)-induced obesity model
Subcutaneous injection
10 mg/kg
Daily until the completion of the experiments
LPZ treatment slowed body weight gain, reduced fat mass accumulation, increased energy expenditure, improved glucose tolerance and insulin sensitivity, and alleviated hepatic steatosis
Acta Pharm Sin B. 2024 Apr;14(4):1711-1725.
BALB/c mice
Acute tuberculosis model
Oral
300 mg/kg
Twice daily for 9 days
Oral administration of lansoprazole sulfide significantly reduced the bacterial burden of Mycobacterium tuberculosis-infected mice
Nat Commun. 2015 Jul 9;6:7659.
Sprague–Dawley rats
Femoral fracture model
Oral
7.5 mg/kg/day
Once daily for 4 weeks
Increased osteoblastogenesis and accelerated fracture healing
EBioMedicine. 2015 Nov 17;2(12):2046-61.
C57BL/6J mice
Subcutaneous injection
30 mg/kg/day
Once daily for 5 weeks
To study the effect of lansoprazole on serum ADMA levels, results showed lansoprazole increased serum ADMA by ~20%
Circulation. 2013 Aug 20;128(8):845-53.
Female CD-1 mice
Disseminated C. auris infection model
Oral
300 mg/kg
Once daily for two days
To evaluate the therapeutic efficacy of the AmB/LNP combination in vivo, the combination significantly reduced fungal burden in the kidneys (1.7-log reduction) and improved mouse health.
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