Isobavachalcone (IBC) is a potent inhibitor of Akt signaling pathway, which induces apoptosis in human cancer cells (Inhibits OVCAR-8 cell growth with an IC50 value of 7.92 μM). Isobavachalcone also induces Reactive Oxyen Species (ROS) generation in OVCAR-8 cells and has exhibited cancer anti-promotive and anti-proliferative activity[3]. Isobavachalcone inhibited massive granulomas, decreased inflammatory cells infiltration and oxidative stress markers level, but it can increase antioxidant enzymes level. Isobavachalcone decreased TNF-α production in BALF and lung tissue. Isobavachalcone can inhibit NF-κB pathway that may be mediated by upregulation of A20. Isobavachalcone can activate NRF2/HO-1 pathway and inhibit adhesion molecule expression[4]. IBC is able to significantly inhibit proliferation and induce apoptosis of Tca8113 (tongue squamous cell carcinoma) cells in vitro. IBC treatment resulted in typical apoptotic morphology of nuclear fragmentation and apoptotic bodies in Tca8113 cells[5].
Isobavachalcone/异补骨脂查尔酮 细胞实验
Cell Line
Concentration
Treated Time
Description
References
THP-1 cells
30 μM
48 h
Induces apoptosis and differentiation, inhibits cell proliferation
Haematologica. 2018 Sep;103(9):1472-1483.
HL60 cells
30 μM
48 h
Induces apoptosis and differentiation, inhibits cell proliferation
Haematologica. 2018 Sep;103(9):1472-1483.
S. aureus JAR
6.25 μg/ml
24 h
Synergistic biofilm eradication
Front Microbiol. 2022 Sep 23;13:958132.
MRSA USA300
6.25 μg/ml
24 h
Synergistic with gentamicin against planktonic MRSA
Front Microbiol. 2022 Sep 23;13:958132.
MSSA ATCC25923
1.56 μg/ml
24 h
Synergistic with gentamicin against planktonic MSSA
Front Microbiol. 2022 Sep 23;13:958132.
Human neuroglioma H4 cells
10, 25, 50 μM
6 h
To evaluate the effect of ISO on autophagy, the results showed that ISO induced the formation of GFP-LC3 puncta, indicating the activation of autophagy.
Cell Death Dis. 2020 Nov 26;11(11):1015.
Human osteosarcoma U2OS cells
25 μM
6 h
To evaluate the effect of ISO on autophagy, the results showed that ISO induced the formation of GFP-LC3 puncta, and this effect was abolished in ATG5 knockout cells, indicating that ISO acts through the autophagy pathway.
Cell Death Dis. 2020 Nov 26;11(11):1015.
MCF-7 cells
15 μM
24 h
IBC increased γ-H2AX signal, indicating induction of replication stress
Elife. 2025 Jan 31;13:RP104718.
MCF-7 cells
15 μM
2 h
IBC inhibited CPT-induced autophosphorylation of CHK2
Elife. 2025 Jan 31;13:RP104718.
BJ cells
15 μM
24 h
No increase in γ-H2AX signal was observed
Elife. 2025 Jan 31;13:RP104718.
Aml-12 cells
10.09 μM
72 h
Evaluate the cytotoxic activity of compound 16 against Aml-12 cells, showing low toxicity to normal cells.
J Enzyme Inhib Med Chem. 2024 Dec;39(1):2292006.
PC9 cells
16.12 μM
72 h
Evaluate the cytotoxic activity of compound 16 against PC9 cells, showing significant cytotoxicity.
J Enzyme Inhib Med Chem. 2024 Dec;39(1):2292006.
A549 cells
14.21 μM
72 h
Evaluate the cytotoxic activity of compound 16 against A549 cells, showing significant cytotoxicity.
J Enzyme Inhib Med Chem. 2024 Dec;39(1):2292006.
H1975 cells
4.35 μM
72 h
Evaluate the cytotoxic activity of compound 16 against H1975 cells, showing significant cytotoxicity.
J Enzyme Inhib Med Chem. 2024 Dec;39(1):2292006.
SW480 cells
0-100 µM
24, 48, 72 h
To evaluate the cytotoxicity of IBC against CRC cell lines. IBC significantly decreased CRC cell viability in a dose- and time-dependent manner.
Drug Des Devel Ther. 2019 May 1;13:1449-1460.
HCT116 cells
0-100 µM
24, 48, 72 h
To evaluate the cytotoxicity of IBC against CRC cell lines. IBC significantly decreased CRC cell viability in a dose- and time-dependent manner.
Drug Des Devel Ther. 2019 May 1;13:1449-1460.
Candida albicans SC5314
8 mg/mL (MIC)
12-24 h
To evaluate the antifungal activity of IBC against Candida albicans SC5314, results showed that IBC disrupted cell membrane integrity, inhibited biofilm formation, and induced apoptosis and autophagy-associated cell death.
albicans by disrupting cell wall/membrane integrity and inducing apoptosis and autophagy. Front Cell Infect Microbiol.
Cryptococcus neoformans H99
8 µg/mL
24 h
IBC significantly inhibited the growth of C. neoformans H99, indicating strong antifungal activity.
Microb Cell Fact. 2024 Apr 12;23(1):107.
Isobavachalcone/异补骨脂查尔酮 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
NOD/SCID mice
MCF-7/Luc xenograft model
Intraperitoneal injection
1.5 mg/kg
Three times per week for 3 weeks
IBC significantly inhibited tumor growth and extended mouse survival
Elife. 2025 Jan 31;13:RP104718.
Mouse
HL60 xenograft model
Oral
15 and 30 mg/kg
18 days
Suppresses tumor growth without obvious toxicity
Haematologica. 2018 Sep;103(9):1472-1483.
C57BL/6J mice
Femoral implant-related infection model
Intraperitoneal injection
20 mg/kg
Once daily for 4 weeks
Reduced inflammatory osteolysis and maintained trabecular bone microarchitecture, while enhancing reduction of MDSC M1 polarization and eradication of USA300 biofilm
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