Deguelin is one of four major naturally occurring rotenoids isolated from root extracts and is best recognized as a NADH: ubiquinone oxidoreductase (complex I) inhibitor, resulting in significant alterations in mitochondrial function, and it is also a potential PI3K/AKT inhibitor[3]. As a natural agent for chemotherapy, deguelin remarkably suppresses proliferation in numerous solid cancers. Nevertheless, the molecular mechanisms of its suppression are still insufficient[4]. In the mouse skin study, deguelin reduced tumor incidence from 60% in the control group to 10% in the group treated with a dose of 33 µg, and multiplicity was reduced from 4.2 in the control group to 0.1 in the treatment group. When the dose was increased 10-fold to 330 µg, no tumors were observed in the treatment group[5]. Deguelin has been reported to elicit PD-like symptoms (degeneration of the dopaminergic pathway) in rats administered with deguelin (6 mg/kg/day for 6 days), possibly through the inhibition of mitochondrial complex I[3].
Deguelin/鱼藤素 细胞实验
Cell Line
Concentration
Treated Time
Description
References
Eca109
1, 2, 5 μM
24 h
Deguelin induced G2/M phase cell cycle arrest and polyploidy in Eca109 cells
EBioMedicine. 2017 Dec;26:100-111.
KYSE150
1, 2, 5 μM
24 h
Deguelin induced G2/M phase cell cycle arrest and polyploidy in KYSE150 cells
EBioMedicine. 2017 Dec;26:100-111.
Human Retinal Endothelial Cells (HRECs)
0~10 µM
48 h
To evaluate the cytotoxic effect of deguelin on HRECs, results showed that deguelin did not affect the viability of HRECs up to 1 µM.
J Cell Mol Med. 2008 Dec;12(6A):2407-15.
HEK 293 cells
0~10 µM
16 h
To evaluate the effect of deguelin on HIF-1α transcriptional activity, results showed that deguelin did not affect HIF-1α transcriptional activity up to 1 µM, but reduced it at 10 µM.
J Cell Mol Med. 2008 Dec;12(6A):2407-15.
PanC-1 cells
62μM
24 h
To evaluate the cytotoxicity of deguelin in pancreatic cancer cells, results showed that deguelin significantly inhibited the survival of PanC-1 cells.
Oncogene. 2013 Aug 22;32(34):3980-91.
COLO-357 cells
27μM
24 h
To evaluate the cytotoxicity of deguelin in pancreatic cancer cells, results showed that deguelin significantly inhibited the survival of COLO-357 cells.
Oncogene. 2013 Aug 22;32(34):3980-91.
L3.6pl cells
12μM
24 h
To evaluate the cytotoxicity of deguelin in pancreatic cancer cells, results showed that deguelin significantly inhibited the survival of L3.6pl cells.
Oncogene. 2013 Aug 22;32(34):3980-91.
A549
50 μM
24 h
Deguelin decreased the mRNA levels of HR molecules, especially Rad51, indicating that deguelin can inhibit the function of FBXO22
Cell Death Dis. 2024 Jan 31;15(1):104.
H1299
50 μM
24 h
Deguelin decreased the mRNA levels of HR molecules, especially Rad51, indicating that deguelin can inhibit the function of FBXO22
Cell Death Dis. 2024 Jan 31;15(1):104.
MCF-7
10^-8 M to 10^-6 M
3 days
Deguelin significantly reduced the viability of MCF-7 cells and inhibited their anchorage-dependent colony formation ability.
Cancer Lett. 2013 May 10;332(1):102-9.
MDA-MB-231
10^-8 M to 10^-6 M
3 days
Deguelin significantly reduced the viability of MDA-MB-231 cells and inhibited their anchorage-dependent colony formation ability.
Cancer Lett. 2013 May 10;332(1):102-9.
U-2 OS human osteosarcoma cells
0, 5, 10, 15, 20 μM
24 and 48 h
Deguelin significantly inhibited the migration and invasion of U-2 OS human osteosarcoma cells, which was associated with a reduction in the activities of matrix metalloproteinase-2 (MMP-2) and matrix metalloproteinase-9 (MMP-9).
Molecules. 2014 Oct 15;19(10):16588-608.
NCI-1975 cells
5, 10, 20, 50 μM
24 h
Deguelin induces apoptosis of NCI-1975 cells through a ROS-driven Akt pathway, which can be partially reversed by NAC.
Cancer Cell Int. 2015 Feb 25;15:25.
NCI-H446 cells
5, 10, 20, 50 μM
24 h
Deguelin shows similar cytotoxic effects on NCI-H446 cells as on NCI-1975 cells.
Cancer Cell Int. 2015 Feb 25;15:25.
H1299 cells
100 nM
12 h
Suppressed HIF-1α protein expression and VEGF mRNA expression, reducing the survival and angiogenic potential of radioresistant lung cancer cells
Cancer Res. 2009 Feb 15;69(4):1624-32.
H226B cells
100 nM
12 h
Suppressed HIF-1α protein expression and VEGF mRNA expression, reducing the survival and angiogenic potential of radioresistant lung cancer cells
Cancer Res. 2009 Feb 15;69(4):1624-32.
Deguelin/鱼藤素 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Nude mice
KYSE150 and Eca109 xenograft model
Intraperitoneal injection
4 mg/kg
Daily until the end of the experiment
Deguelin significantly inhibited the growth of KYSE150 and Eca109 xenograft tumors
EBioMedicine. 2017 Dec;26:100-111.
C57BL/6 mice
Oxygen-Induced Retinopathy (OIR) model
Intravitreal injection
0.1 µM
Single injection, continued until P17
To evaluate the inhibitory effect of deguelin on retinal neovascularization in the OIR model, results showed that deguelin significantly reduced retinal neovascularization.
J Cell Mol Med. 2008 Dec;12(6A):2407-15.
Nude mice
Orthotopic implantation of PanC-1-luc cells
Intraperitoneal injection
5mg/kg
Daily for 37 days
To evaluate the inhibitory effect of deguelin on pancreatic tumor growth and metastasis, results showed that deguelin significantly inhibited tumor growth and metastasis, and induced apoptosis.
Oncogene. 2013 Aug 22;32(34):3980-91.
BALB/c nude mice
Tumor xenograft model
Oral
4 mg/kg
Every other day, throughout the experimental period
Deguelin slowed the growth of xenograft tumors, especially when combined with radiotherapy, showing significant growth inhibition
Cell Death Dis. 2024 Jan 31;15(1):104.
Nude mice
MCF-7 cell xenograft model
Oral gavage
4 mg/kg
Twice daily for 45 days
Deguelin significantly inhibited the growth of MCF-7 xenograft tumors and induced apoptosis.
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