Sanguinarine chloride, a benzophenanthridine alkaloid derived from the root of Sanguinaria Canadensis, can stimulate apoptosis via activating the production of reactive oxygen species (ROS). Sanguinarine (SANG) could induce apoptosis in a dose- and time-dependent manner in UM-SCC-22B head and neck cancer cells. Moreover, SANG-induced apoptosis was associated with the generation of reactive oxygen species (ROS) and activation of JNK and NF-κB signal pathways[3]. Sanguinarine exhibits antitumor effects in epithelial ovarian cancer cells possible via regulating CASC2-EIF4A3 axis and/or inhibiting NF-κB signaling or PI3K/AKT/mTOR pathway[4]. Sanguinarine treatment (0.25, 0.5, 1, and 2 µM) of MC3T3-E1 cells significantly increased alkaline phosphatase (ALP) activity and the phoshporalyation of AMPKα, but did not affect cell proliferation. Sanguinarine treatment promoted bone tissue growth in an ovariectomized osteoporosis rat model[5].
Sanguinarine chloride/氯化血根碱 细胞实验
Cell Line
Concentration
Treated Time
Description
References
16HBE
1 µM, 5 µM
48 hours
Assessed toxicity to normal cells
Transl Oncol. 2022 Mar;17:101345.
HT-115
3 µM
Induces cell death
Cell Death Discov. 2023 Mar 13;9(1):94.
HCT-116
3 µM
Induces cell death
Cell Death Discov. 2023 Mar 13;9(1):94.
MDA-MB-231
1 µM
14 days
SC significantly reduced the number of colonies formed by MDA-MB-231 cells in soft agar.
Cells. 2022 Apr 28;11(9):1485.
Mouse mammary epithelial cells (mMECs)
5, 25, 50 µM
1-hour pretreatment followed by 6-hours LPS stimulation
To evaluate the protective effect of SG against LPS-induced oxidative stress. Results showed that SG significantly inhibited LPS-induced ROS increase and enhanced the activities of antioxidant enzymes (SOD and GSH-Px).
Cells. 2022 Nov 18;11(22):3658.
MDA-MB-468 cells
1.5 µM
24 hours
To evaluate the effect of sanguinarine chloride on the viability of TNF-α-activated TNBC cells. Results showed that sanguinarine chloride significantly inhibited the viability of MDA-MB-468 cells with an IC50 value of 2.97 µM.
Int J Mol Sci. 2022 Jul 28;23(15):8329.
MDA-MB-231 cells
2 µM
24 hours
To evaluate the effect of sanguinarine chloride on the viability of TNF-α-activated TNBC cells. Results showed that sanguinarine chloride significantly inhibited the viability of MDA-MB-231 cells with an IC50 value of 3.11 µM.
Int J Mol Sci. 2022 Jul 28;23(15):8329.
NCI-H1688
30 µM, 10 µM, 5 µM, 1 µM
24 hours, 48 hours, 72 hours
Inhibited SCLC cell proliferation, colony formation, cell cycle, migration and invasion, and promoted apoptosis
Transl Oncol. 2022 Mar;17:101345.
Prostate cancer cells (LNCaP, VCaP, 22RV1, PC3, DU145)
0.5, 1.0 µM
24, 48 hours
To evaluate the effects of S.C on the viability and migration ability of prostate cancer cells. The results showed that S.C significantly inhibited the viability, clonogenicity, and migration ability of prostate cancer cells.
Chin Med. 2024 Jan 9;19(1):7.
HEK293T cells
1 µM
4 days
To evaluate the effect of sanguinarine on the proliferation of Rac1b cells, results showed that sanguinarine significantly inhibited the proliferation of Rac1b cells, increased the level of cleaved PARP-89, and decreased both the level of cyclin-D1 and the percentage of BrdU positive cells.
Acta Pharmacol Sin. 2015 Feb;36(2):229-40.
HTC75
1 µM
48 hours
SC inhibited telomerase activity in a dose-dependent manner with an IC50 of 1.21 μM.
Cells. 2022 Apr 28;11(9):1485.
HEK293T
1 µM
48 hours
Screening for natural hTERT inhibitors, SC significantly reduced GFP fluorescence intensity, indicating its inhibitory effect on hTERT expression.
Cells. 2022 Apr 28;11(9):1485.
HTC75 cells
1 µM
48 hours
Evaluate the inhibitory effect of SC on telomerase activity, results showed SC suppresses telomerase activity in a dose-dependent manner
Cells. 2022 Apr 28;11(9):1485.
LX-2 hepatic stellate cells
0.75 µM, 1.50 µM, 3.00 µM
48 hours
To evaluate the toxicity of sanguinarine chloride and its derivatives on normal hepatic stellate cells. The results showed that the toxicity of the sanguinarine chloride derivative was lower than that of sanguinarine chloride.
Int J Mol Sci. 2023 Apr 30;24(9):8113.
Human erythroleukemia cells (HEL cells)
0.75 µM, 1.50 µM, 3.00 µM
48 hours
To evaluate the inhibitory effect of sanguinarine chloride and its derivatives on the proliferation of HEL cells. The results showed that sanguinarine chloride and its derivatives significantly inhibited the proliferation of HEL cells in a dose-dependent manner.
Int J Mol Sci. 2023 Apr 30;24(9):8113.
Sanguinarine chloride/氯化血根碱 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Caenorhabditis elegans
Wild-type N2 and mutants
Administered via NGM agar plates
0.1, 0.2, 0.4 mM
Treatment started at L4 larval stage
Sanguinarine extends healthspan and enhances innate immunity via ROS-mediated PMK-1/SKN-1 pathway activation
iScience. 2022 Feb 4;25(3):103874
Sprague-Dawley rats
Chronic constriction injury (CCI) model
Intraperitoneal injection
1.00, 2.50 and 6.25 mg/kg
Once every two days
Sanguinarine chloride alleviates neuropathic pain by suppressing p38MAPK signaling and downregulating the expression of TNF-α, IL-1β, IL-6 and NF-κB activation.
Drug Des Devel Ther. 2020 Nov 4;14:4725-4733
Nude mice
MDA-MB-231 cell-derived xenograft model
Intravenous injection
1.1 μg/kg
Every 3 days for 24 days
Evaluate the anti-tumor efficacy of SC in vivo, results showed SC significantly inhibited tumor growth
Cells. 2022 Apr 28;11(9):1485.
BALB/C nude mice
NCI-H1688 xenograft model
Intraperitoneal injection
2.5 mg/kg
Every three days for three weeks
Evaluated the anti-tumor effect of Sanguinarine chloride on SCLC in vivo
Transl Oncol. 2022 Mar;17:101345.
NCG mice
DU145 xenograft model
Intraperitoneal injection
2.5 mg/kg and 5.0 mg/kg
Every two days, total seven times
Evaluate the inhibitory effect of S.C on prostate tumor growth, results showed S.C significantly inhibited tumor growth
Chin Med. 2024 Jan 9;19(1):7.
C57BL/6J mice
Destabilization of medial meniscus (DMM)-induced osteoarthritis model
Intraarticular injection
5 μM
Every 5 days for 8 weeks
To evaluate the protective effect of Sanguinarine chloride (SC) on DMM-induced osteoarthritis, results showed that SC significantly alleviated the severity of osteoarthritis.
JCI Insight. 2023 Feb 8;8(3):e166688
BALB/c mice
LPS-induced mastitis model
Intraperitoneal injection
5, 25, 50 μM
Twice every six hours
To evaluate the protective effect of SG against LPS-induced mastitis. Results showed that SG significantly alleviated mammary tissue congestion, inflammatory cell infiltration, and acinar structure destruction, reduced TNF-α and IL-1β expression, decreased MPO activity, and enhanced the integrity of the blood–milk barrier.
Cells. 2022 Nov 18;11(22):3658.
NCr nude mice
HT-29 xenograft model
Intraperitoneal injection
6 mg/kg
Every 3 days for 24 days
Significantly suppresses tumor growth via oxeiptosis-associated features
Cell Death Discov. 2023 Mar 13;9(1):94.
Grass carp
High-fat diet-induced intestinal dysfunction model
Dietary administration
600 μg/kg and 1200 μg/kg
Three times a day for 56 days
Sanguinarine chloride enhanced the immunity of grass carp and alleviated the damage of the intestinal physical and immune barriers by regulating the MLCK and NF-κB signaling molecules. Furthermore, sanguinarine improved intestinal microbiota homeostasis by regulating the structure of the intestinal microbiota.
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