GLPBio

Gambogenic acid

Catalog No.: GC38062Purity:>98.00%
COASDSData Sheet
GambogensÄure ist ein Wirkstoff in Gamboge mit krebsbekÄmpfender Wirkung. GambogensÄure wirkt als wirksamer Inhibitor von EZH2, bindet spezifisch und kovalent an Cys668 innerhalb der EZH2-SET-DomÄne und induziert die EZH2-Ubiquitinierung.

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Gambogenic acid
Cas No.: 173932-75-7
10mM (in 1mL DMSO)In Stock
$175.00
1
1mgIn Stock
$42.00
1
5mgIn Stock
$126.00
1
10mgIn Stock
$202.00
1
25mgIn Stock
$343.00
1
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    618, 1017–1023 (2023)
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    610, 366–372 (2022)
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    Cell
    187(9):2288-2304 (2024)
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    Cell
    183(7):1867-1883 (2020)
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    31, 1291–1307 (2021)

Beschreibung (Description)

Gambogenic acid, the main active component of gamboge, inhibits Aurora A kinase, with an IC50 value of 1.425μM[1]. Gambogenic acid triggers endoplasmic reticulum (ER) stress-mediated apoptosis through the reactive oxygen species/IRE1α/c-Jun N-terminal kinase signalling pathway[2]. Gambogenic acid has been widely used as an anticancer agent to inhibit the growth of different cancer cells[3].

In vitro, Gambogenic acid treatment for 72h significantly inhibited the proliferation of HCC827, H1650, and HCC827 erlotinib-resistant (HCC827ER) cells with IC50 values of 1.510, 1.328, and 0.909μM, respectively[4]. Treatment of HepG2 cells with 3μM Gambogenic acid for 24h promoted apoptosis, accompanied by a decrease in Bcl-2 levels and an increase in Bax expression levels[5]. Treatment with 1μM Gambogenic acid for 48h inhibited the invasion and migration of A375 cells and induced ferroptosis in A375 cells treated with TGF-β1 (5ng/ml; 48h)[6].

In vivo, Gambogenic acid treatment via intraperitoneally injection at a dose of 2mg/kg/day for 21 days significantly reduced tumor volume and weight in HCT116 cell-xenograft mice, without affecting body weight[7]. Intraperitoneal injection of Gambogenic acid (10mg/kg/day) for 7 consecutive days in male Sprague-Dawley rats can prevent liver oxidative damage caused by acetaminophen (APAP) and alleviate liver histopathological changes caused by APAP[8].

References:
[1] Liu C, Xu J, Guo C, et al. Gambogenic acid induces endoplasmic reticulum stress in colorectal cancer via the aurora a pathway[J]. Frontiers in Cell and Developmental Biology, 2021, 9: 736350.
[2] Zhao Q, Zhong J, Bi Y, et al. Gambogenic acid induces Noxa-mediated apoptosis in colorectal cancer through ROS-dependent activation of IRE1α/JNK[J]. Phytomedicine, 2020, 78: 153306.
[3] Mi L, Xing Z, Zhang Y, et al. Unveiling gambogenic acid as a promising antitumor compound: a review[J]. Planta Medica, 2024, 90(05): 353-367.
[4] Xu L, Meng X, Xu N, et al. Gambogenic acid inhibits fibroblast growth factor receptor signaling pathway in erlotinib-resistant non-small-cell lung cancer and suppresses patient-derived xenograft growth[J]. Cell death & disease, 2018, 9(3): 262.
[5] Yan F, Wang M, Li J, et al. Gambogenic acid induced mitochondrial-dependent apoptosis and referred to phospho-Erk1/2 and phospho-p38 MAPK in human hepatoma HepG2 cells[J]. Environmental toxicology and pharmacology, 2012, 33(2): 181-190.
[6] Wang M, Li S, Wang Y, et al. Gambogenic acid induces ferroptosis in melanoma cells undergoing epithelial-to-mesenchymal transition[J]. Toxicology and applied pharmacology, 2020, 401: 115110.
[7] Zhao Q, Zhong J, Bi Y, et al. Gambogenic acid induces Noxa-mediated apoptosis in colorectal cancer through ROS-dependent activation of IRE1α/JNK[J]. Phytomedicine, 2020, 78: 153306.
[8] Ding Z, Li Y, Tang Z, et al. Role of gambogenic acid in regulating PI3K/Akt/NF-kβ signaling pathways in rat model of acute hepatotoxicity[J]. Bioscience, Biotechnology, and Biochemistry, 2021, 85(3): 520-527.

Protokoll (Protocol)

Cell experiment [1]:

Cell lines

HepG2 cells

Preparation Method

HepG2 cells were cultured in Dulbecco's modified Eagle's medium (DMEM) supplemented with 10% fetal bovine serum, 100units /ml penicillin, and 100μg/ml streptomycin. Cells were cultured at 37°C in a humidified atmosphere with 5% CO2. Subsequently, HepG2 cells in the logarithmic growth phase were collected and seeded in 96-well culture plates overnight at a density of approximately 6×104 cells/ml. Cells were incubated with different concentrations of Gambogenic acid (0, 0.75, 1.5, 3, 6, and 12μM). At various time points of 24, 48, or 72h, 5.0mg/ml MTT was added, and cells were then incubated at 37°C for 4h and measured at a wavelength of 570nm.

Reaction Conditions

0, 0.75, 1.5, 3, 6, and 12μM; 24, 48, and 72h

Applications

Gambogenic acid treatment reduced the percentage of viable HepG2 cells in a concentration- and time-dependent manner.
Animal experiment [2]:

Animal models

Female BALB/c-nu mice

Preparation Method

Female BALB/c-nu mice (4 weeks of age) were maintained under specific pathogen free (SPF) conditions and provided with sterile food and water. HCT116 cells (1×106 cells per mouse) were injected subcutaneously into the right abdomen of each mouse. When the tumor volume was approximately 100mm3, mice were randomly divided into a vehicle group, a 2mg/kg Gambogenic acid group, and a positive control 15mg/kg paclitaxel (PTX) group (n=6 mice in each group). Mice were intraperitoneally injected with Gambogenic acid daily and PTX three times a week. Tumor size was measured and calculated using the standard formula: 0.5×length×width2. The body weight of mice was measured at the same time. After 21 days, all mice were euthanized, and tumors were collected for analysis.

Dosage form

2mg/kg/day for 21 days; i.p.

Applications

Gambogenic acid treatment significantly reduced tumor volume and weight in mice without affecting body weight.

References:
[1] Yan F, Wang M, Li J, et al. Gambogenic acid induced mitochondrial-dependent apoptosis and referred to phospho-Erk1/2 and phospho-p38 MAPK in human hepatoma HepG2 cells[J]. Environmental toxicology and pharmacology, 2012, 33(2): 181-190.
[2] Zhao Q, Zhong J, Bi Y, et al. Gambogenic acid induces Noxa-mediated apoptosis in colorectal cancer through ROS-dependent activation of IRE1?/JNK[J]. Phytomedicine, 2020, 78: 153306.

Produktdokumente (Product Documents)

Purity:>98.00%Appearance:A solid
COASDSData Sheet

Chemische Eigenschaften (Chemical Properties)

CAS-Nr.
173932-75-7
SMILES
O=C(O)/C(C)=C\C[C@@]1(C2=O)OC(C)(C)[C@]([C@]31OC4=C5C(O)=C(C/C=C(C)/CC/C=C(C)\C)C(O)=C4C/C=C(C)\C)([H])C[C@@]2([H])C=C3C5=O
Summenformel
C38H46O8
Molekulargewicht
630.77
Löslichkeit
DMSO: 250 mg/mL (396.34 mM)
Lagerung
4°C, protect from light
Allgemeine Hinweise
Wählen Sie anhand der Löslichkeitsdaten des Produkts ein geeignetes Lösungsmittel. Aliquotieren Sie die Stammlösung nach der Herstellung, um wiederholte Gefrier-Auftau-Zyklen zu vermeiden.
Verwenden Sie Stammlösungen bei Lagerung bei -80°C innerhalb von 6 Monaten bzw. bei -20°C innerhalb von 1 Monat.
Zur Verbesserung der Löslichkeit das Röhrchen auf 37°C erwärmen und für eine angemessene Dauer beschallen.
Versandbedingungen
Evaluierungsmuster werden mit Kühlakkus versandt. Andere verfügbare Größen werden bei Raumtemperatur oder auf Anfrage mit Kühlakkus versandt.

Rechner (Calculators)Molarität / Verdünnung / Molekulargewicht / Einheitenumrechnung / In-vivo-Formulierung / Löslichkeit

g/mol

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