Esomeprazole magnesium ((S)-Omeprazole magnesium) is a potent orally active inhibitor of H+, K+-ATPase, offering therapeutic potential for research into upper intestinal disorders and gastroesophageal reflux disease[1].[2]. Additionally, it functions as an exosome inhibitor by blocking the release of exosomes through the inhibition of V-H+-ATPases[4].
体内研究
In experimental studies involving A/J mice, treatment with Esomeprazole magnesium (0.5-50 mg/kg; oral gavage; daily for 10 days) has been shown to enhance gastric total antioxidant capacity and Cu/Zn-superoxide dismutase activity[1].
体外研究
Esomeprazole magnesium originates from its strontium counterpart, Esomeprazole strontium tetrahydrate (EST), which includes esomeprazole as the S-enantiomer of omeprazole in a salt-exchanged form with Esomeprazole magnesium trihydrate[3].
Esomeprazole Magnesium/埃索美拉唑镁 细胞实验
Cell Line
Concentration
Treated Time
Description
References
Human microvascular endothelial cells (HMVECs)
3–100 μM
24 hours
To study the effect of omeprazole on DDAH1 and DDAH2 protein expression, results showed omeprazole did not regulate the expression of DDAH1 or DDAH2
Circulation. 2013 Aug 20;128(8):845-53
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
5-200 μM
24 hours
To evaluate the effect of different V-ATPase inhibitors on macrophage uptake of targeted or non-targeted lipid vesicles. ESO pretreatment significantly reduced the endocytosis of both targeted and non-targeted vesicles by macrophages.
Int J Nanomedicine. 2020 Aug 25;15:6385-6399
LNCaP cells
140 µM
24 and 48 hours
To evaluate the effect of Esomeprazole on LNCaP cell viability and extracellular pH. Results showed that Esomeprazole only caused cell death at the highest concentration and increased extracellular pH from 6.5 to 6.95.
Cancers (Basel). 2022 Oct 7;14(19):4916
PC3 cells
140 µM
24 and 48 hours
To evaluate the effect of Esomeprazole on PC3 cell viability and extracellular pH. Results showed that Esomeprazole caused 50% cell death after 48 hours and increased extracellular pH from 6.8 to 7.1.
Cancers (Basel). 2022 Oct 7;14(19):4916
Esomeprazole Magnesium/埃索美拉唑镁 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Nude mice
A549 tumor model
Intravenous injection
3 mg/kg
Single dose, vesicles injected 24 hours later
To evaluate the effect of ESO pretreatment on the biodistribution of nanocarriers. ESO pretreatment significantly reduced the liver and spleen distribution of targeted vesicles and enhanced their accumulation in tumors.
Int J Nanomedicine. 2020 Aug 25;15:6385-6399
Athymic nude mice
PC3 prostate cancer subcutaneous and orthotopic models
Gavage
2.5 mg/kg body weight
Every other day for three weeks
To evaluate the effect of Esomeprazole on tumor growth and acidosis in PC3 prostate cancer models. Results showed that acute administration increased tumor pH from 6.86 to 7.05 after 3 hours, but long-term treatment did not significantly alter tumor growth or acidosis.
Cancers (Basel). 2022 Oct 7;14(19):4916
Mice
Radiation-induced brain injury model
Intraperitoneal injection
10 mg/kg
Once daily for 8 weeks
Inhibiting the enzymatic activity of AEP to alleviate radiation-induced brain injury
iScience. 2024 Apr 9;27(5):109698
Mice
Cotton smoke-induced lung injury model
Oral
30 mg/kg and 300 mg/kg
Daily administration for 21 days
To evaluate the prophylactic and therapeutic potential of esomeprazole in a mouse model of cotton smoke-induced lung injury. Results showed that therapeutic esomeprazole significantly inhibited the progression of fibrosis and reduced circulating markers of inflammation and fibrosis.
搜索
