Obacunone belongs to a class of unique triterpenoids called limonoids, present in Citrus species. Obacunone possesses antivirulence activity and demonstrates inhibition of cell-cell signaling in Vibrio harveyi and Escherichia coli O157:H7[3]. Obacunone inhibited SW480 cell proliferation with IC50 values of 97 μM at 24h. Sequence of events such as decreased ratio of bcl2/bax gene transcription, activation of caspase-3, fragmentation of DNA in cells treated with obacunone demonstrated induction of apoptosis by limonoids[4]. Obacunone stimulated the transcriptional activity of the bile acids-specific G protein-coupled receptor, TGR5, in a dose-dependent manner. In addition, obacunone inhibited adipocyte differentiation in 3T3-L1 cells and antagonized ligand-stimulated peroxisome proliferator-activated receptor γ (PPARγ) transcriptional activity[5].
Obacunone/黄柏酮 细胞实验
Cell Line
Concentration
Treated Time
Description
References
Mature osteoclasts
20 μM
To evaluate the effect of OB on the morphological changes of osteoclasts. Results showed that OB-treated groups had significantly reduced osteoclast area and number of nuclei.
J Adv Res. 2023 Nov;53:235-248.
Bone marrow macrophages (BMMs)
0, 1, 5, 10, 20 μM
6 days
To evaluate the inhibitory effect of OB on RANKL-induced osteoclast differentiation. Results showed that OB dose-dependently inhibited osteoclast formation.
J Adv Res. 2023 Nov;53:235-248.
Bone marrow macrophages (BMMs)
0, 1, 5, 10, 20 μM
48 h
To evaluate the cytotoxicity of OB on BMMs. Results showed that OB had little effect on BMMs proliferation at the tested concentrations.
J Adv Res. 2023 Nov;53:235-248.
BEAS-2B cells
10, 20, 40 μM
4 h
To evaluate the protective effects of OB against LPS-induced BEAS-2B cell injury. Results showed that OB increased cell viability and inhibited LDH release in a dose-dependent manner, and reduced the secretion of inflammatory cytokines IL-1β, IL-6, and TNF-α.
Cell Mol Biol Lett. 2022 Mar 19;27(1):29.
Madin-Darby canine kidney (MDCK) cells
3.12, 12.5, 50 μM
6 days
Obacunone significantly inhibited cyst formation and expansion of MDCK cysts in a dose-dependent manner.
Antioxidants (Basel). 2021 Dec 24;11(1):38.
NCM460 human colonic epithelial cells
0–100 μM
24 h
Evaluate the effect of obacunone on cell viability, results showed obacunone markedly increased cell viability
Front Microbiol. 2020 Mar 31;11:497.
RAW264.7 mouse macrophage cells
0–100 μM
24 h
Evaluate the effect of obacunone on LPS-stimulated NO production, results showed obacunone significantly suppressed NO production
Front Microbiol. 2020 Mar 31;11:497.
RAW264.7 mouse macrophage cells
0–100 μM
24 h
Evaluate the effect of obacunone on cell viability, results showed almost no cytotoxicity at concentrations up to 100 μM
Front Microbiol. 2020 Mar 31;11:497.
Caco-2 cells
100 μg/ml
3 h
To evaluate the effect of Obacunone on Salmonella adhesion and invasion. Results showed that Obacunone significantly reduced the number of adherent and invasive Salmonella cells.
Appl Environ Microbiol. 2012 Oct;78(19):7012-22.
Obacunone/黄柏酮 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
B6 mice
Bleomycin-induced lung fibrosis model
Intraperitoneal injection
10 mg/kg
Detected after 48 hours
Obacunone inhibits bleomycin-induced lung fibrosis by activating the Nrf2 pathway
Protein Cell. 2016 Sep;7(9):684-8
C57BL/6J female mice
Ovariectomy-induced osteoporosis model
Intraperitoneal injection
5 mg/kg
Every two days for six weeks
To evaluate the therapeutic effect of OB on ovariectomy-induced osteoporosis. Results showed that OB treatment significantly prevented bone loss and inhibited osteoclast activity.
J Adv Res. 2023 Nov;53:235-248.
C57BL/6 mice
LPS-induced acute lung injury model
Intraperitoneal injection
2.5, 5, 10 mg/kg
48 hours
To evaluate the protective effects of OB against LPS-induced acute lung injury. Results showed that OB significantly alleviated LPS-induced lung histopathological injury, reduced inflammatory cytokine secretion and Fe2+ and 4-HNE levels, and upregulated GPX4, SLC7A11, and Nrf2 expression.
Cell Mol Biol Lett. 2022 Mar 19;27(1):29.
Mice
Kidney-specific Pkd1 knockout mouse (PKD) model
Intraperitoneal injection
100 mg/kg
Once daily for 4 days
Obacunone significantly retarded renal cyst development in PKD mice.
Antioxidants (Basel). 2021 Dec 24;11(1):38.
C57BL/6 mice
CFA-induced inflammatory pain model
Intraperitoneal injection
10 mg/kg
Once daily for three consecutive days
OB alleviates inflammatory pain by promoting microglial polarization from M1 to M2 and activating the Nrf2/HO-1 signaling pathway.
Drug Des Devel Ther. 2024 Apr 18;18:1265-1275
C57BL/6 mice
DSS-induced ulcerative colitis model
Oral gavage
25, 50, 100 mg/kg/day
Once daily, starting from 2 days before DSS treatment and continuing to the end of the experiment
Evaluate the protective effect of obacunone on DSS-induced colitis, results showed obacunone significantly attenuated disease symptoms including weight loss, diarrhea, bloody stool, and colonic shortening
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