Prostaglandin E1 是一种前列腺素类似物，具有血管舒张特性（对 EP3/EP4/EP2/IP/EP1 的 Ki 值分别为 1.1/2.1/10/33/36 nM），常用于勃起功能障碍及外周血管功能的研究。
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Prostaglandin E1 (Alprostadil) is a ligand for prostanoid receptors, exhibiting Kis of 1.1 nM, 2.1 nM, 10 nM, 33 nM, and 36 nM for mouse EP3, EP4, EP2, IP, and EP1 receptors respectively. It induces vasodilation and inhibits platelet aggregation, being researched as a vasodilator for peripheral vascular diseases[1].[2].[3].
体内研究
Subcutaneously administered at 20 ng/animal/day for four days, it significantly inhibits FGF-induced angiogenesis in mice[2].
体外研究
In experiments, Prostaglandin E1 at concentrations ranging from 1 nM to 10 μM over 48 hours, reduces proliferation of HUVECs (up to 100% inhibition) in the presence of VEGF (20 ng/mL) with an IC50 of 400 nM[2].
Prostaglandin E1 also inhibits VEGF-induced HUVECs migration at doses from 0.01 μM to 10 μM over 6 hours, with an IC50 of 500 nM[2], and restricts in vitro angiogenesis at 1-5 μM over 12-18 hours[2].
Additionally, Prostaglandin E1 increases intracellular cAMP levels in HUVECs within 20 minutes when administered at concentrations from 0.01 μM to 10 μM[2].
Prostaglandin E1/前列腺素E1 细胞实验
Cell Line
Concentration
Treated Time
Description
References
H9c2 cells
0.5 µM
12 hours hypoxia followed by 12 hours reoxygenation
To investigate the effects of PGE1 on the H/R model, results showed that PGE1 treatment significantly reduced apoptosis in H9c2 cells, inhibited mPTP opening, and decreased cytochrome c and cleaved caspase-3 expression.
Mol Med Rep. 2021 Feb;23(2):110.
Mesenchymal stem cells
10 ng/mL
24 hours
PGE1 reduces MSC apoptosis and increases CXCR4 expression, MSC migration, and VEGF secretion by activating the HIF-1α pathway
Stem Cell Res Ther. 2022 Jul 16;13(1):316.
Human umbilical vein endothelial cells (HUVECs)
0.25, 0.50, 1.00 µM
24 hours
To investigate the protective effects of PGE1 against H2O2-induced oxidative damage. PGE1 markedly restored the viability of HUVECs under oxidative stress, scavenged intracellular reactive oxygen species induced by H2O2, suppressed the production of lipid peroxides such as MDA, restored the activities of endogenous antioxidants including SOD and GSH-Px, and inhibited cell apoptosis. Additionally, PGE1 significantly increased NO content, eNOS protein, and mRNA expression.
Acta Pharmacol Sin. 2010 Apr;31(4):485-92.
Mouse trigeminal ganglion neurons
100 nM
3 minutes
To investigate the effect of PGE1 on Ih current, results showed that PGE1 significantly enhanced the amplitude of Ih current
Int J Mol Sci. 2021 Dec 16;22(24):13534.
PTEN-knockdown PASMCs
100 nM
30 minutes to 24 hours
PGE1 induced pCREB expression at 30 min, increased PTEN expression at 6 h, and decreased pAKT levels from 6 to 24 h.
Sci Rep. 2017 Aug 30;7(1):9974.
HK-2 cells
0.1 –100 µM
48 hours
To evaluate the effect of PGE1 on HK-2 cell viability under high glucose conditions, results showed PGE1 significantly enhanced cell viability
Acta Pharmacol Sin. 2020 Apr;41(4):561-571.
K562 cells
10 µM
6 hours
Repressed AP-1 factors expression, simulating the effect of Tcf1/Lef1 deficiency
Cell Stem Cell. 2017 Sep 7;21(3):359-373.e5.
Primary cardiomyocytes
2.0 µM
6 hours hypoxia followed by 6 hours reoxygenation
PGE1 protected primary cardiomyocytes against H/R-induced injuries, increased the viability of H/R-induced primary cardiomyocytes, and decreased LDH levels in a dose-dependent manner.
Biosci Rep. 2019 Dec 20;39(12):BSR20190597.
Rat H9C2 cells
0.5, 1.0, and 2.0 µM
6 hours hypoxia followed by 6 hours reoxygenation
PGE1 significantly diminished the cell cytotoxicity and apoptosis induced by the 6H/6R regimen, and also decreased expression of IL-2, IL-6, P-p65, TNF-α, and cleaved-caspase-3. In addition, PGE1 up-regulated miR-21-5p expression and reduced the apoptosis ability of H/R-injured rat cardiomyocytes by affecting the miR-21-5p/FASLG axis.
Biosci Rep. 2019 Dec 20;39(12):BSR20190597.
Prostaglandin E1/前列腺素E1 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Wistar rats
Asphyxia-induced cardiac arrest model
Intravenous injection
1 µg/kg
Single dose
To evaluate the protective effects of PGE1 on post-cardiac arrest myocardial dysfunction, results showed that PGE1 significantly increased ejection fraction and cardiac output, improved survival rate, and reduced cardiomyocyte apoptosis.
Mol Med Rep. 2021 Feb;23(2):110.
Wistar rats
Diabetic kidney disease model
Intravenous injection
10 µg/kg
Once daily for 10 consecutive days
To evaluate the effect of PGE1 on kidney injury in diabetic kidney disease rats, results showed PGE1 significantly reduced proteinuria and renal tubular apoptosis
Acta Pharmacol Sin. 2020 Apr;41(4):561-571.
C57BL/6 mice
Orofacial pain model
Subcutaneous injection
10 ng/10 μL and 20 ng/10 μL
Single injection, observed for 90 minutes
To investigate PGE1-induced orofacial pain behavior, results showed that PGE1 induced mechanical allodynia in a dose-dependent manner
Int J Mol Sci. 2021 Dec 16;22(24):13534.
Wistar rats
Pulmonary arterial hypertension model
Tail vein injection
10 ng/mL
Single injection
After transplantation of PGE1-preconditioned MSCs, the pulmonary artery systolic pressure, mean pulmonary artery pressure, right ventricular hypertrophy index, %WT, and %WA decreased in rats with PAH, showing better therapeutic effects than non-preconditioned MSCs
Stem Cell Res Ther. 2022 Jul 16;13(1):316.
Wistar rats
Hypoperfused rat liver model
Perfusion
100 μg/liter
20 min pretreatment followed by 25% low flow perfusion
Prostaglandin E1 significantly attenuated hypoperfusion-induced early reductive stress and mitochondrial dysfunction, and diminished subsequent oxidative injury and cell death
J Clin Invest. 1994 Jan;93(1):155-64
Mice
CML model
Intraperitoneal injection
2.5-5 mg/kg
Once daily for the duration of treatment
Significantly reduced the number of leukemic stem cells, prolonged survival, and showed synergistic effects when combined with imatinib
Cell Stem Cell. 2017 Sep 7;21(3):359-373.e5.
Wistar P7 rats
Neonatal ischemia-reperfusion model
Intraperitoneal injection
20 µg/kg
Every 5 minutes for 4 times, lasting 50 minutes
To evaluate whether prostaglandin E1 improves collateral recruitment and brain damage after ischemia in neonatal rats. Results showed that prostaglandin E1 delayed and improved ipsilateral reperfusion by decreasing thromboxane A synthase-1 gene expression, reducing the density of reactive astrocytes and lesion volume.
Int J Mol Sci. 2018 Sep 30;19(10):2995
Sprague-Dawley rats
Permanent middle cerebral artery occlusion model
Intravenous injection
22.6 nmol/kg or 45.2 nmol/kg
Single administration
To examine the effects of a mixed formulation composed of prostaglandin E1 and lithium (PGE1+Li mixture) on brain damage after cerebral ischemia. The results showed that the mixture significantly reduced infarct volume and neurological deficits, and upregulated cytoprotective HSP70, GRP78, HSP60, and Bcl-2 protein levels, while decreasing p53 expression.
Acta Pharmacol Sin. 2011 Mar;32(3):303-10
Sprague-Dawley rats
Monocrotaline-induced pulmonary arterial hypertension (PAH) model
Intraperitoneal injection
5 mg/kg
Once daily for 3 weeks
PGE1 prevented pulmonary arterial remodeling and improved hemodynamics via the induced expression of PTEN.
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