Aloperine

Catalog No.S2420 Batch:S242012

Technical Data

Formula	C₁₅H₂₄N₂
Molecular Weight	232.36	CAS No.	56293-29-9
Solubility (25°C)*	In vitro	DMSO	46 mg/mL (197.96 mM)
		Ethanol	46 mg/mL (197.96 mM)
		Water	4 mg/mL (17.21 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.)

Preparing Stock Solutions

Biological Activity

Description	Aloperine is an isolated alkaloid in sophora plants such as Sophora alopecuroides L, and exhibits anti-inflammatory, antibacterial, antiviral, and anti-tumor properties.
In vitro	Compared with other alkaloids including sophoridine, sophocarpine, matrine, oxymatrine and cytisine, Aloperine treatment exerts the most potent cytotoxic activity against human cancer cell lines of differing tissue origins, including leukaemia cell lines HL-60, U937 and K562, oesophageal cancer EC109 cells, lung cancer A549 cells and the hepatocellular carcinoma HepG2 cell line with IC50 of 0.04 mM, 0.27 mM, 0.36 mM, 1.11 mM, 1.18 mM, and 1.36 mM, respectively. The strongest cytotoxic effect of Aloperine on HL-60 cells is observed at 72 hours with the inhibition rate of 94.1%.In contrast to the effect on leukaemia cells, up to 1 mM of Aloperine does not significantly reduce the viability of normal PBMNCs at 72 hours. Aloperine treatment at 20 μM for 48 hours significanlty induces apoptosis and autophagy in HL-60 cells in a dose-dependent manner. ^[2]
In vivo	Topical application of 1% Aloperine suppresses 2, 4-dinitrofluorobenzene (DNFB)-induced increase in ear thickness and ear erythema in BALB/c mice, and significantly decreases the up-regulated mRNA and protein levels of tumor necrosis factor-alpha (TNF-α), interleukin-1beta (IL-1β) and interleukin-6 (IL-6) induced by DNFB in ear biopsy homogenates. ^[1] Topical application of Aloperine reduces the DNFB-induced dermatitis (dermatitis index and ear thickness) in NC/Nga mice at day 13 and day 14 in a dose-dependent manner. Aloperine treatment reduces DNFB-induced lymphocytes infiltration and eosinophils infiltration in a dose-dependent manner. Aloperine treatment also reduces the DNFB-induced infiltration of mast cells in a dose-dependent manner. Aloperine reduces the plasma level of IgE in a dose-dependent manner. Aloperine markedly reduces DNFB-induced increase in IL-4, IL-13 and IFN-γ productions, while it increases the IL-10 level in a dose-dependent manner. Aloperine treatment significantly reduces the cytokine levels of TNF-α, IL-1β and IL-6 in ear biopsies homegenates of NC/Nga mice in a dose-dependent manner. ^[3]

Protocol (from reference)

Cell Assay:^{^[2]}	Cell lines K562, U937, HL-60, EC109, A549 and HepG2 Concentrations Dissolved in DMSO, final concentrations ~2 mM Incubation Time 24, 48, and 72 hours Method Cells are seeded in 96-well plates in 100-μL culture medium. After incubation of 4 hours for leukaemia cells and of 24 hours for solid cancer cells, experimental media containing either excipient control or Aloperine are added to appropriate wells. Five concentrations of Aloperine for 48-hour treatment are used to determine the in vitro IC50 growth inhibitory values of Aloperine in cancer cells. After incubation, 10 μL of MTT solution (5 mg/mL) is added to each well. The plates are then incubated for 4 hours at 37 °C. Intracellular formazan crystals are dissolved by addition of 100 μL of isopropanol-HCI-SDS solution to each well. After an overnight incubation at 37 °C, the optical density of the samples is determined at 570 nm. DNA fragmentation is analysed after the extraction of DNA from cells exposed to the indicated doses of Aloperine for 48 hours using apoptotic DNA ladder kit. For autophagy detection, cells are collected and incubated with PBS containing 5 μM acridine orange for 15 minutes. The acridine orange is removed and the cells are resuspended in 100 μL of PBS. Fluorescent micrographs are obtained with an inverted fluorescent microscope. Autophagy is quantified based on the mean number of cells displaying intense red staining for three fields (containing at least 50 cells per field) for each experimental condition.
Animal Study:^{^[1]}	Animal Models Female BALB/c mice with DNFB-induced allergic contact dermatitis Dosages 1% (w/w) Administration Topical application

Cell Assay:^{^[2]}

Cell lines
K562, U937, HL-60, EC109, A549 and HepG2
Concentrations
Dissolved in DMSO, final concentrations ~2 mM
Incubation Time
24, 48, and 72 hours
Method
Cells are seeded in 96-well plates in 100-μL culture medium. After incubation of 4 hours for leukaemia cells and of 24 hours for solid cancer cells, experimental media containing either excipient control or Aloperine are added to appropriate wells. Five concentrations of Aloperine for 48-hour treatment are used to determine the in vitro IC50 growth inhibitory values of Aloperine in cancer cells. After incubation, 10 μL of MTT solution (5 mg/mL) is added to each well. The plates are then incubated for 4 hours at 37 °C. Intracellular formazan crystals are dissolved by addition of 100 μL of isopropanol-HCI-SDS solution to each well. After an overnight incubation at 37 °C, the optical density of the samples is determined at 570 nm. DNA fragmentation is analysed after the extraction of DNA from cells exposed to the indicated doses of Aloperine for 48 hours using apoptotic DNA ladder kit. For autophagy detection, cells are collected and incubated with PBS containing 5 μM acridine orange for 15 minutes. The acridine orange is removed and the cells are resuspended in 100 μL of PBS. Fluorescent micrographs are obtained with an inverted fluorescent microscope. Autophagy is quantified based on the mean number of cells displaying intense red staining for three fields (containing at least 50 cells per field) for each experimental condition.

Animal Study:^{^[1]}

Animal Models
Female BALB/c mice with DNFB-induced allergic contact dermatitis
Dosages
1% (w/w)
Administration
Topical application

References

Selleck's Aloperine has been cited by 7 publications

Aloperine inhibits the progression of non-small-cell lung cancer through the PI3K/Akt signaling pathway [ Cancer Cell Int, 2021, 21(1):662]	PubMed: 34895234
Aloperine inhibits colorectal cancer cell proliferation and metastasis progress via regulating miR-296-5p/STAT3 axis [ Tissue Cell, 2021, 74:101706]	PubMed: 34883316
Aloperine in combination with therapeutic adenoviral vector synergistically suppressed the growth of non-small cell lung cancer. [ J Cancer Res Clin Oncol, 2020, 10.1007/s00432-020-03157-2]	PubMed: 32088783
Autophagy Modulation in Human Thyroid Cancer Cells following Aloperine Treatment [ Int J Mol Sci, 2019, 20(21)E5315]	PubMed: 31731481
Identification of Aloperine as an anti-apoptotic Bcl2 protein inhibitor in glioma cells. [ PeerJ, 2019, 7:e7652]	PubMed: 31534865
In Vitro Antitumor Activity of Aloperine on Human Thyroid Cancer Cells through Caspase-Dependent Apoptosis [ Int J Mol Sci, 2018, 19(1)E312]	PubMed: 29361731
Aloperine executes antitumor effects through the induction of apoptosis and cell cycle arrest in prostate cancer in vitro and in vivo. [ Onco Targets Ther, 2018, 11:2735-2743]	PubMed: 29785122

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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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