Azelnidipine is a calcium blocker that has been shown to have antioxidant effects in endothelial cells and cardiomyocytes. Azelnidipine inhibited TGF-β1- and Ang II-induced HSC (hepatic stellate cells) activation in vitro and attenuated CCl4- and TAA-induced liver fibrosis, and it accelerated regression of CCl4-induced liver fibrosis in mice[3]. Cultures of human mononuclear leukocytes collected from six healthy volunteers showed 100 nM of azelnidipine caused significant inhibition of formyl-methyonyl leucyl phenylalanine (fMLP)-induced production of IL-8. These results suggest that azelnidipine has anti-inflammatory effects independent of its anti-hypertensive action[4]. Moreover, beneficial effect of Azelnidipine in diabetic cardiomyopathy via altering intracellular Ca2+ handling proteins and preventing apoptosis by its antioxidant property[5]. Acute administration of azelnidipine could prevent a sudden drop of cardiac function after acute stress like IMO (immobilization stress: IMO). Azelnidipine might have a protective effect on stress-induced cardiac dysfunction like α and β adrenergic blockers[6]. Azelnidipine has potent antiatherosclerotic properties by inhibition of macrophage activation through Cav1.2[7].
Azelnidipine/阿折地平 细胞实验
Cell Line
Concentration
Treated Time
Description
References
LX-2 cells
100 nM
6 h
Azelnidipine significantly reduced the increase in intracellular ROS levels induced by TGF-β1, Ang II, or H2O2
Br J Pharmacol. 2012 Feb;165(4b):1173-87.
LX-2 cells
100 nM
24 h
Azelnidipine significantly reduced the up-regulation of COL1A1 mRNA expression induced by 5 ng·mL-1 TGF-β1 alone
Br J Pharmacol. 2012 Feb;165(4b):1173-87.
guinea-pig portal vein myocytes
300 nM
7 min
To investigate the inhibitory effects of Azelnidipine on voltage-dependent L-type Ca2+ channels, results showed persistent inhibition of IBa
Br J Pharmacol. 2006 Nov;149(6):786-96.
SHEE
0, 1, 2.5, 5, 10, 15, 20 μM
24, 48, 72, 96 h
To evaluate the effect of Azelnidipine on SHEE cell proliferation, results showed that Azelnidipine did not significantly inhibit SHEE cell proliferation.
Mol Ther Oncolytics. 2022 Sep 26;27:61-72.
KYSE450
0, 1, 2.5, 5, 10, 15, 20 μM
24, 48, 72, 96 h
To evaluate the inhibitory effect of Azelnidipine on ESCC cell proliferation, results showed that Azelnidipine significantly inhibited ESCC cell proliferation in a concentration- and time-dependent manner.
Mol Ther Oncolytics. 2022 Sep 26;27:61-72.
KYSE150
0, 1, 2.5, 5, 10, 15, 20 μM
24, 48, 72, 96 h
To evaluate the inhibitory effect of Azelnidipine on ESCC cell proliferation, results showed that Azelnidipine significantly inhibited ESCC cell proliferation in a concentration- and time-dependent manner.
Mol Ther Oncolytics. 2022 Sep 26;27:61-72.
CT26 cells
20 μM
24 h
To test the effect of azelnidipine on the expression of CD47 and PVR in CT26 cells. Results showed that azelnidipine could inhibit the expression of PVR but not CD47.
Biomolecules. 2021 May 10;11(5):706.
BMDM cells
20 μM
4 h
To test the effect of azelnidipine on macrophage phagocytosis of tumor cells. Results showed that azelnidipine significantly enhanced the phagocytosis of MC38, CT26, and B16-OVA tumor cells by BMDM cells.
Biomolecules. 2021 May 10;11(5):706.
Azelnidipine/阿折地平 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Wistar rats
STZ-induced diabetic model
Oral gavage
5 mg/kg
Once daily for 12 weeks
To investigate the protective effect of Azelnidipine on hyperglycemia-induced cardiac damage. Results showed that AZL treatment significantly reduced levels of cardiac damage markers (e.g., Troponin-1, CK-MB, CK-NAC, uric acid, LDH, and alkaline phosphatase), improved inflammatory cytokine and lipid profiles, and decreased oxidative stress markers.
Cardiovasc Diabetol. 2010 Dec 1;9:82
Wistar rats
STZ-induced diabetic model
Oral gavage
5 mg/kg
Once daily for 12 weeks
To evaluate the effect of Azelnidipine on diabetic cardiomyopathy. Results showed that Azelnidipine significantly improved cardiac contractile function, calcium handling protein expression, oxidative stress, and apoptosis.
Cardiovasc Diabetol. 2011 Nov 4;10:97
C57BL/6 mice
CCl4- or TAA-induced liver fibrosis model
Oral
10 mg/kg
6 days a week for 6 weeks
Azelnidipine significantly decreased inflammatory cell infiltration, pro-fibrotic gene expressions, HSC activation, lipid peroxidation, oxidative DNA damage and fibrosis in the livers of CCl4- or TAA-treated mice
Br J Pharmacol. 2012 Feb;165(4b):1173-87.
SCID/CB17 mice
Esophageal cancer patient-derived xenograft (PDX) model
Oral gavage
2, 20 mg/kg
Daily for 18 or 42 days
To evaluate the inhibitory effect of Azelnidipine on esophageal cancer growth in vivo, results showed that Azelnidipine significantly inhibited tumor growth and reduced the levels of Ki67 and p-ERK1/2 T202/Y204.
Mol Ther Oncolytics. 2022 Sep 26;27:61-72.
Mice
MC38 and CT26 tumor models
Intraperitoneal injection
2 or 5 mg/kg
Once daily for two weeks
To test the inhibitory effect of azelnidipine on the growth of MC38 and CT26 tumors. Results showed that azelnidipine significantly inhibited tumor growth and enhanced the infiltration and function of CD8+ T cells.
Biomolecules. 2021 May 10;11(5):706.
Wistar rats
Hypertension model
Oral
9.7 mg/day
14 days
Azelnidipine alleviated NA-induced blood pressure variability augmentation and preserved baroreceptor reflex sensitivity despite a smaller reduction in blood pressure
Japan
... 展开 >> Department of Cardiovascular Medicine Graduate School of Medical Science Kumamoto University
1-1-1 Honjyo, Kumamoto-City, Kumamoto, Japan, 860-8556
OSCAR-Study Data Center
ShinjukuParkTower30FN, 3-7-1 Nishi-Shinjuku, Shinjuku-ku, Tokyo, Japan, 163-1030 收起 <<
Japan
... 展开 >> Department of Cardiovascular Medicine Graduate School of Medical Science Kumamoto University
1-1-1 Honjyo, Kumamoto-City, Kumamoto, Japan, 860-8556
OSCAR-Study Data Center
ShinjukuParkTower30FN, 3-7-1 Nishi-Shinjuku, Shinjuku-ku, Tokyo, Japan, 163-1030 收起 <<
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