Danshensu

Catalog No.S4741 Batch:S474101

Technical Data

Formula	C₉H₁₀O₅
Molecular Weight	198.17	CAS No.	76822-21-4
Solubility (25°C)*	In vitro	Water	23 mg/mL (116.06 mM)
		DMSO	Insoluble
		Ethanol	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description

Danshensu (Salvianic acid A), a herbal preparation used in traditional Chinese medicine, possesses potential antitumor and anti‑angiogenesis effects. Danshensu inhibits CYP2E1 and CYP2C9 with IC50 of 36.63 and 75.76 μm, respectively.

Targets

CYP2E1 ^[3] (Cell-free assay)	CYP2C9 ^[3] (Cell-free assay)
36.63 μM	75.76 μM

In vitro

Danshensu reduces lipid peroxidation on mitochondrial membrane by scavenging free radicals, and inhibits permeability and transmission of mitochondrial membrane by reducing thiol oxidation^[1]. Danshensu markedly improves cell viability and decreased lactate dehydrogenase (LDH) release in H9c2 cardiomyocytes. Danshensu increases phosphorylation of Akt and extracellular signal-related kinase 1/2 (ERK1/2) in H9c2 cells, and the protective effects of Danshensu are partially inhibited by phosphatidylinositol 3'-kinase (PI3K) specific inhibitor wortmannin or ERK specific inhibitor U0126. Danshensu could provide significant cardioprotection against MI/R injury, and the potential mechanisms might to suppression of cardiomyocytes apoptosis through activating the PI3K/Akt and ERK1/2 signaling pathways. Danshensu increases Bcl-2 expression and decreases Bax, active caspase-3 expression by activating Akt and ERK signaling pathways. Danshensu has been demonstrated to have biological activities in improving microcirculation, suppressing the formation of reactive oxygen species, inhibiting platelet adhesion and aggregation, protecting myocardium against ischemia, protecting endothelial cells against injury induced by inflammation^[2].

In vivo

Pretreatment with danshensu in ISO-administered rats shows a significant (P<0.001) decrease in ST-segment as compared to ISO-administered rats. Its pretreatment also shows significant (P<0.001) decrease in the levels of serum cTnI when compared to the ISO. Thus, danshensu exerts significant cardioprotective effects against ISO-induced myocardial infarction in rats^[1]. In the rat model of MI/R injury, Danshensu significantly reduces myocardium infarct size and the production of creatine kinase-MB (CK-MB), cardiac troponin (cTnI) in serum^[2].

Protocol (from reference)

Cell Assay:^{^[2]}	Cell lines Rat H9c2 cardiomyocyte cell line Concentrations 1 μM or 10 μM Incubation Time -- Method Cardiomyocytes are exposed to ischemia by replacing medium with an 'ischemic buffer', this buffer is designed to simulate the extracellular milieu of myocardial ischemia, with the approximate concentrations of potassium, hydrogen, and lactate ions occurring in vivo. Cells are incubated in the hypoxic/ischemic chamber at 37℃ for 2 h in a humidified atmosphere of 5% CO2 and 95% nitrogen. At the onset of reperfusion, cardiomyocytes are randomly exposed to one of the following treatments: vehicle, Danshensu (1 μM or 10 μM), Danshensu plus the PI3K inhibitor wortmannin (10 nM), Danshensu plus the ERK inhibitor U0126 (10 μM). Simultaneously, in the control group, H9c2 cardiomyocytes are cultured under normal conditions in CO2 incubation.
Animal Study:^{^[1]}	Animal Models Sprague-Dawley rats Dosages 160 mg/kg Administration oral administration

Cell Assay:^{^[2]}

Cell lines
Rat H9c2 cardiomyocyte cell line
Concentrations
1 μM or 10 μM
Incubation Time
--
Method
Cardiomyocytes are exposed to ischemia by replacing medium with an 'ischemic buffer', this buffer is designed to simulate the extracellular milieu of myocardial ischemia, with the approximate concentrations of potassium, hydrogen, and lactate ions occurring in vivo. Cells are incubated in the hypoxic/ischemic chamber at 37℃ for 2 h in a humidified atmosphere of 5% CO2 and 95% nitrogen. At the onset of reperfusion, cardiomyocytes are randomly exposed to one of the following treatments: vehicle, Danshensu (1 μM or 10 μM), Danshensu plus the PI3K inhibitor wortmannin (10 nM), Danshensu plus the ERK inhibitor U0126 (10 μM). Simultaneously, in the control group, H9c2 cardiomyocytes are cultured under normal conditions in CO2 incubation.

Animal Study:^{^[1]}

Animal Models
Sprague-Dawley rats
Dosages
160 mg/kg
Administration
oral administration

References

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