Stachydrine

製品コードS3771 バッチS377101

印刷

化学情報

Chemical Structure Synonyms Proline betaine, L-stachydrine, Methyl hygrate betaine Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C7H13NO2
分子量 143.18 CAS No. 471-87-4
Solubility (25°C)* 体外 DMSO 28 mg/mL (195.55 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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 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.
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].

プロトコル(参考用のみ)

細胞アッセイ 細胞株 Endothelial cells
濃度 0.1 mM
反応時間 72 h
実験の流れ

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.
動物実験 動物モデル Transverse aortic constriction animal model (Wistar rats)
投薬量 8 mg/kg
投与方法 by oral gavage

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

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

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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