Sinomenine hydrochloride

製品コードS3758 バッチS375801

印刷

化学情報

 Chemical Structure Synonyms Cucoline hydrochloride, Kukoline hydrochloride, Sabianine A hydrochloride Storage
(From the date of receipt)
3 years -20°C powder
1 years -80°C in solvent
化学式

C19H23NO4.HCl

分子量 365.85 CAS No. 6080-33-7
Solubility (25°C)* 体外 DMSO 73 mg/mL (199.53 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 Sinomenine (SN, Cucoline, Kukoline, Sabianine A), extracted from the Chinese medicinal plant, sinomenium acutum, is a potent anti-inflammatory and neuroprotective agent.
in vitro Sinomenine induces apoptotic death in U87 cells via activation of caspase-3, caspase-8 and caspase-9, and down-regulation of HIAP, Bcl-2 and survivin. Sinomenine decreases the expression of phosphorylated STAT3 (p-STAT3) both in vivo and in vitro. It has beneficial roles against several types of cancers, including breast cancer cells, esophageal carcinoma cells, hepatocellular carcinoma cells, gastric adenocarcinoma cells, lung cancer cells and colon carcinoma cells. Sinomenine treatment results in dose- and time-dependent growth inhibition in U87, and IC50 of SM ranged from 178 μM to 380 μM. Treatment of U251, U373, Hs683 and T98G with Sinomenine for 48 h obviously decreases cells viability, and IC50 are 342.7 μM, 430.2 μM, 189.6 μM and 270.3 μM, respectively[1]. Sinomenine HCl (SH) activates an autophagy-mediated cell death pathway, as indicated by the accumulated microtubule-associated protein light chain 3B (LC3B)-II, triggers autophagic flux and enhances cell viability after pretreatment with autophagy inhibitors. It induces autophagy by inhibiting the Akt-mTOR pathway and activating the JNK pathway. Sinomenine HCl (SH) dose-dependently reduces the phosphorylation of p70S6K, 4E-BP1, Akt and mTOR, while enhancing the expression levels of autophagy marker proteins in vivo and in vitro. Sinomenine HCl dose-dependently augmentes ROS generation, which is accompanied by increased autophagy in both U87 and SF767 cells. SH may promote lysosomal biogenesis by triggering the nuclear translocation of TFEB via mTOR inhibition[2].
in vivo Sinomenine has cardioprotective, anti-inflammatory activities and cancer chemopreventive property. It exhibits anti-glioma activity in vivo. Sinomenine is well tolerated by the recipient mice at therapeutic dose, and no significant cytotoxicity is accompanied[1]. Sinomenine HCl (SH) initiates the autophagy-lysosome pathway in both in vitro and in vivo experiments[2].

プロトコル(参考用のみ)

細胞アッセイ 細胞株 Human glioma cell lines (U87, U373, U251, Hs683 and T98G)
濃度 0-1000 μM
反応時間 24 h, 48 h and 72 h
実験の流れ The cells are cultured in 96-well plates with a density of 5 × 103/well, and then treated with SM for the designated time (24-72 h). Following incubation, 10 μl MTT solution (5 g/l) is added to the medium in each well, and the microplate is incubated at 37 °C for 4 h. The absorbance is read in a microplate reader at 570 nm. Cytotoxicity is expressed as the percentage of cells surviving in relation to untreated cells.
動物実験 動物モデル Nude mice (male, 5-week-old BALB/c)
投薬量 50 mg/kg and 100 mg/kg
投与方法 i.p.

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:

Sinomenine Inhibits Vasculogenic Mimicry and Migration of Breast Cancer Side Population Cells via Regulating miR-340-5p/SIAH2 Axis [ Biomed Res Int, 2022, 2022:4914005] PubMed: 35309179
Network Pharmacology-Based Approach to Investigate the Molecular Targets of Sinomenine for Treating Breast Cancer [ Cancer Manag Res, 2021, 13:1189-1204] PubMed: 33603465
Sinomenine inhibits hypoxia induced breast cancer side population cells metastasis by PI3K/Akt/mTOR pathway [ Bioorg Med Chem, 2020, 31:115986] PubMed: 33412412

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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