Gambogenic acid binds to Cys668 within the EZH2-SET domain, triggering EZH2 degradation through COOH terminus of Hsp70‐interacting protein (CHIP)‐mediated ubiquitination.
Gambogenic acid/新藤黄酸 细胞实验
Cell Line
Concentration
Treated Time
Description
References
BEAS-2B cells
10 µM (IC50)
24 hours
Inhibited proliferation of BEAS-2B cells
Pharmaceuticals (Basel). 2025 Mar 6;18(3):374.
H1650 cells
3.8 µM (IC50)
24 hours
Inhibited proliferation of H1650 cells
Pharmaceuticals (Basel). 2025 Mar 6;18(3):374.
A549 cells
5 µM
18 hours
Evaluate the effect of Gambogenic acid on TGFβ-induced A549 cell migration, results showed that Gambogenic acid significantly inhibited TGFβ-induced cell migration.
J Mol Cell Biol. 2024 Apr 10;15(11):mjad068.
HEK293T cells
5 µM
18 hours
Evaluate the effect of Gambogenic acid on TGFβ-induced SBE4-luc reporter activity, results showed that Gambogenic acid significantly reduced TGFβ-induced SBE4-luc activity.
J Mol Cell Biol. 2024 Apr 10;15(11):mjad068.
TF-1 cells
8 µM
24 hours
Evaluate the apoptosis and proliferation inhibitory effects of Gambogenic acid on TF-1 cells. Results showed that GNA significantly increased caspase 3/7 activity and inhibited cell proliferation.
Cancer Biol Ther. 2024 Dec 31;25(1):2427374.
SKM-1 cells
6 µM
24 hours
Evaluate the apoptosis and proliferation inhibitory effects of Gambogenic acid on SKM-1 cells. Results showed that GNA significantly increased caspase 3/7 activity and inhibited cell proliferation.
Cancer Biol Ther. 2024 Dec 31;25(1):2427374.
MDS-L cells
4 µM
24 hours
Evaluate the apoptosis and proliferation inhibitory effects of Gambogenic acid on MDS-L cells. Results showed that GNA significantly increased caspase 3/7 activity and inhibited cell proliferation.
Cancer Biol Ther. 2024 Dec 31;25(1):2427374.
HN-6 cells
2 µM
24 hours
Screening compounds to reduce EZH2 immunofluorescent signals, GNA was one of the most effective compounds
EMBO J. 2017 May 2;36(9):1243-1260.
HT29 cells
0-5 µM
24 hours
GNA significantly inhibited HT29 cell proliferation and induced apoptosis
Front Cell Dev Biol. 2021 Oct 6;9:736350.
HCT116 cells
0-5 µM
24 hours
GNA significantly inhibited HCT116 cell proliferation and induced apoptosis
Front Cell Dev Biol. 2021 Oct 6;9:736350.
Murine primary peritoneal macrophages
0, 0.25, 0.5, 1.0, 1.5 µM
24 hours
To assess the effect of GEA on LPS-induced NO production, results showed that GEA significantly inhibited LPS-induced NO production
Acta Biochim Biophys Sin (Shanghai). 2016 May;48(5):454-61.
THP-1 cells
0, 0.25, 0.5, 1.0, 1.5 µM
24 hours
To evaluate the effect of GEA on IL-1β secretion in human THP-1 cells, results showed that GEA effectively diminished IL-1β secretion
Acta Biochim Biophys Sin (Shanghai). 2016 May;48(5):454-61.
J774A.1 cells
0, 0.25, 0.5, 1.0, 1.5 µM
24 hours
To assess the cytotoxic effect of GEA, results showed that GEA at concentrations below 1.5 μM did not affect the viability of J774A.1 cells
Acta Biochim Biophys Sin (Shanghai). 2016 May;48(5):454-61.
HCC1833 cells
1 µM, 2 µM
24, 48, 72 hours
Inhibited proliferation and migration of HCC1833 cells, arrested cell cycle in G0/G1 phase, and promoted apoptosis
Pharmaceuticals (Basel). 2025 Mar 6;18(3):374.
A549 cells
2 µM, 4 µM
24, 48, 72 hours
Inhibited proliferation and migration of A549 cells, arrested cell cycle in G0/G1 phase, and promoted apoptosis
Pharmaceuticals (Basel). 2025 Mar 6;18(3):374.
HEK293 cells
1.6 µM
4 hours
To study the effect of GB on HSP90-HSF1/HSF2 interaction, results showed GB disrupts the interaction between HSP90 and HSF1/HSF2
Cell Stress Chaperones. 2021 Sep;26(5):819-833.
HeLa cells
4 µM
4 hours
To study the effect of GB on HSF1, results showed GB induces HSF1 localization to nuclear stress bodies
Cell Stress Chaperones. 2021 Sep;26(5):819-833.
U2OS cells
2.5 µM
4.5 hours
To study the effect of GBA on HSF1 and HSF2, results showed GBA induces HSF1-dependent heat shock response
Cell Stress Chaperones. 2021 Sep;26(5):819-833.
MM.1S cells
0.51 µM and 0.90 µM
48 hours and 72 hours
To evaluate the effect of Gambogenic acid on the proliferation and apoptosis of MM.1S cells. Results showed that Gambogenic acid inhibited cell growth and induced apoptosis in a dose- and time-dependent manner.
J Cancer. 2017 Mar 7;8(5):839-851.
Gambogenic acid/新藤黄酸 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Sprague-Dawley rats
Healthy male Sprague-Dawley rats
Lateral tail vein injection
1.5 mg/kg
Single dose
Evaluate the pharmacokinetic properties of GNA-loaded PMs. The results showed that the AUC0→t value of GNA-loaded PMs was 3.94 times that of free GNA, indicating that PMs significantly improved the bioavailability of GNA.
Polymers (Basel). 2019 May 7;11(5):820
BALB/c nude mice
HCC827 and HCC827ER xenograft models
Intraperitoneal injection
10 mg/kg
Once daily for 27 days
To evaluate the inhibitory effect of GNA alone or in combination with erlotinib on tumor growth, GNA alone or in combination with erlotinib significantly suppressed tumor growth in the HCC827ER xenograft model
Cell Death Dis. 2018 Feb 15;9(3):262
NOG hIL-3 GM-CSF transgenic mice
MDS-L/Akaluc cell xenograft model
Intraperitoneal injection
16 mg/kg
Twice a week for 15 weeks
Evaluate the anti-tumor effects of Gambogenic acid in the MDS xenograft model. Results showed that GNA significantly inhibited MDS-L cell growth and prolonged the survival of mice.
Cancer Biol Ther. 2024 Dec 31;25(1):2427374.
BALB/c nude mice
MM.1S xenograft model
Intravenous injection
2.0 mg/kg
Every two days for two weeks
To evaluate the antitumor effect of Gambogenic acid on MM.1S xenograft models. Results showed that Gambogenic acid significantly inhibited tumor growth and synergistically enhanced the antitumor effect with bortezomib.
J Cancer. 2017 Mar 7;8(5):839-851.
BALB/c nude mice
U266 xenograft model
Intravenous injection
5 mg/kg
Every other day for two weeks
To evaluate the inhibitory effect of GNA on the growth of U266 xenograft tumors in vivo. The results showed that GNA significantly inhibited tumor growth without affecting the body weight of mice.
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