Stachydrine

Catalog No.S3771 Batch:S377102

Technical Data

Formula	C₇H₁₃NO₂
Molecular Weight	143.18	CAS No.	471-87-4
Solubility (25°C)*	In vitro	DMSO	29 mg/mL (202.54 mM)
		Water	29 mg/mL (202.54 mM)
		Ethanol	15 mg/mL (104.76 mM)
* <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

Stachydrine (Proline betaine, L-stachydrine, Methyl hygrate betaine) is a quaternary ammonium derivative of proline that occurs widely in Medicago species. It is an osmoprotective compound found in urine. Stachydrine is a major constituent of Chinese herb leonurus heterophyllus sweet used to promote blood circulation and dispel blood stasis. Stachydrine can inhibit the NF-κB signal pathway.

Targets

NF-κB ^[5]

In vitro

Stachydrine inhibits cell proliferation and induces primary apoptosis and ROS production in T47D and MCF-7 cells in time- and dose-dependent manner. Its treatment induces caspase-3 activation and decreases the expression of the anti-apoptotic protein Bcl-2. Stachydrine simultaneously inhibits the phosphorylation of Akt and ERK proteins^[1]. Stachydrine ameliorates the detrimental effect of high-glucose on EC (endothelial cells) and that its beneficial effect occurs through the modulation of cell senescence signaling and SIRT1 expression^[2]. Stachydrine inhibits AngII-induced excessive autophagy within H9c2 cells. Stachydrine blocks the over phosphorylation of the p47phox subunit, decreases the translocation of p47phox and p67phox to the membrane, inhibits the activity of NOX2, and reduces the generation of ROS^[3].

In vivo

Stachydrine ameliorates transverse aortic constriction (TAC)-induced cardiac hypertrophy, dysfunction and excessive autophagy in vivo^[3]. It shows significantly pharmacological properties including low toxicity, anti-inflammatory activities by improving the cellular membrane permeability, decreasing the levels of inflammatory factors and reducing the lipid peroxidation, and anti-oxidant activities by reducing plasma LDH activity and MDA levels, and protection against myocardial ischemia reperfusion injury in rats. The mean pharmacokinetic parameters of stachydrine after oral administration of Herba Leonuri extract: Tmax=0.75 h, t1/2z=1.64 h^[4].

Protocol (from reference)

Cell Assay:^{^[2]}	Cell lines Endothelial cells Concentrations 0.1 mM Incubation Time 72 h Method The cell proliferation is determined by XTT after treatment with high-glucose (30 mM) in the presence or absence of stachydrine (0.1 mM) up to 72 h. Briefly, Endothelial cells (EC) are seeded in 96-well at a density of 4000 cells/well and incubated for 12, 24, 48, and 72h at 37 ºC with high-glucose alone or with high-glucose in the presence of stachydrine (0.1 mM). Control cells received normal glucose concentration or stachydrine (0.1 mM) alone. At the end of incubations, XTT assay is performed. The absorbance was measured at 492 nm in a spectrophotometer.
Animal Study:^{^[3]}	Animal Models Transverse aortic constriction animal model (Wistar rats) Dosages 8 mg/kg Administration by oral gavage

Cell Assay:^{^[2]}

Cell lines
Endothelial cells
Concentrations
0.1 mM
Incubation Time
72 h
Method
The cell proliferation is determined by XTT after treatment with high-glucose (30 mM) in the presence or absence of stachydrine (0.1 mM) up to 72 h. Briefly, Endothelial cells (EC) are seeded in 96-well at a density of 4000 cells/well and incubated for 12, 24, 48, and 72h at 37 ºC with high-glucose alone or with high-glucose in the presence of stachydrine (0.1 mM). Control cells received normal glucose concentration or stachydrine (0.1 mM) alone. At the end of incubations, XTT assay is performed. The absorbance was measured at 492 nm in a spectrophotometer.

Animal Study:^{^[3]}

Animal Models
Transverse aortic constriction animal model (Wistar rats)
Dosages
8 mg/kg
Administration
by oral gavage

References

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Selleck's Stachydrine has been cited by 3 publications

Stachydrine alleviates lipid-induced skeletal muscle insulin resistance via AMPK/HO-1-mediated suppression of inflammation and endoplasmic reticulum stress [ J Endocrinol Invest, 2022, 10.1007/s40618-022-01866-8]	PubMed: 35834165
Stachydrine is effective and selective against blast phase chronic myeloid leukaemia through inhibition of multiple receptor tyrosine kinases [ Pharm Biol, 2022, 60(1):700-707]	PubMed: 35348419
Stachydrine prevents LPS-induced bone loss by inhibiting osteoclastogenesis via NF-κB and Akt signalling. [ J Cell Mol Med, 2019, 10.1111/jcmm.14551]	PubMed: 31328430

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SHIPPING AND STORAGE
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