Sinomenine hydrochloride

Catalog No.S3758 Batch:S375801

Technical Data

Formula	C₁₉H₂₃NO₄.HCl
Molecular Weight	365.85	CAS No.	6080-33-7
Solubility (25°C)*	In vitro	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. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description	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].

Protocol (from reference)

Cell Assay:^{^[1]}	Cell lines Human glioma cell lines (U87, U373, U251, Hs683 and T98G) Concentrations 0-1000 μM Incubation Time 24 h, 48 h and 72 h Method 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.
Animal Study:^{^[1]}	Animal Models Nude mice (male, 5-week-old BALB/c) Dosages 50 mg/kg and 100 mg/kg Administration i.p.

Cell Assay:^{^[1]}

Cell lines
Human glioma cell lines (U87, U373, U251, Hs683 and T98G)
Concentrations
0-1000 μM
Incubation Time
24 h, 48 h and 72 h
Method
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.

Animal Study:^{^[1]}

Animal Models
Nude mice (male, 5-week-old BALB/c)
Dosages
50 mg/kg and 100 mg/kg
Administration
i.p.

References

Selleck's Sinomenine hydrochloride has been cited by 3 publications

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

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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