Fupenzic acid
Fupenzic acid is a triterpenoid compound that can be found in the fruits of plants in the genus Rubus. Fupenzic acid inhibits LPS (HY-D1056)-induced NF-κB activation and reduces the expression of NO, NOS-2, COX-2, inflammatory cytokines, and chemokines. Fupenzic acid binds to RBMS1, downregulates RBMS1/cGAS/STING signaling, enhances PINK1/Parkin-mediated mitophagy, and alleviates oxidative stress and radiation-induced liver fibrosis. Fupenzic acid exhibits cytotoxic activity against various tumor cells and can inhibit melanin production. Fupenzic acid has inactivation, protective, and replication-inhibitory activities against TMV and CMV. Fupenzic acid can be used in research related to liver fibrosis, malignant glioma, colon cancer, gastric cancer, hepatocellular carcinoma, TMV, and CMV infection.
For research use only. We do not sell to patients.
- CAS No.: 119725-20-1
- Formula: C30H44O5
- Molecular Weight:484.67
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HCT-116 | IC50 |
16.31 μM
|
Cytotoxicity against human HCT116 colon carcinoma cells measured by MTT assay after 48 hrs incubation.
Cytotoxicity against human HCT116 colon carcinoma cells measured by MTT assay after 48 hrs incubation.
|
34923054 |
| BGC-823 | IC50 |
21.94 μM
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Cytotoxicity against human BGC823 gastric carcinoma cells measured by MTT assay after 48 hrs incubation.
Cytotoxicity against human BGC823 gastric carcinoma cells measured by MTT assay after 48 hrs incubation.
|
34923054 |
| HepG2 | IC50 |
23.40 μM
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Cytotoxicity against human HepG2 hepatocellular carcinoma cells measured by MTT assay after 48 hrs incubation.
Cytotoxicity against human HepG2 hepatocellular carcinoma cells measured by MTT assay after 48 hrs incubation.
|
34923054 |
In Vitro
Fupenzic acid (10-20 µM; 30 min) inhibits LPS-induced NOS-2 and COX-2 protein expression in mouse peritoneal macrophages[1].
Fupenzic acid (10-20 μM) downregulates RBMS1/cGAS/STING signaling in TGF-β1-stimulated LX-2 cells[2].
Fupenzic acid (20 μM) modulates the interaction of RBMS1 with cGAS and STING in LX-2 cells[2].
Fupenzic acid binds RBMS1 LBD in SPR with a KD of 0.51 μM[2].
Fupenzic acid (0.5-160 μM; 24 h) reduces LX-2 cell viability[2].
Fupenzic acid (10-20 μM; 24 h) inhibits TGF-β1-induced expression of fibrosis markers in LX-2 cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Mouse peritoneal macrophages
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Concentration:0, 10 and 20 μM
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Incubation Time:30 min
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Result:Suppressed LPS-induced NOS-2 and COX-2 protein expression in mouse peritoneal macrophages.
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Cell Line:Mouse peritoneal cells
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Concentration:0, 10 and 20 μM
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Incubation Time:30 min
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Result:The compound downregulated LPS-induced NOS-2, COX-2, IL-6, IL-10, IL-12, IL-18, KC, TNF-α, and IP-10 mRNA expression in mouse peritoneal cells.
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Cell Line:Human hepatic stellate LX-2 cells
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Concentration:0.5, 1, 2.5, 5, 10, 20, 40, 80 and 160 μM
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Incubation Time:24 h
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Result:Inhibited LX-2 cell viability at 40 μM; concentrations of 10 and 20 μM were selected for subsequent experiments.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 (male, 6-week-old)[2]
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Dosage:10 mg/kg/day (RT); 20 mg/kg/day (RT); 20 mg/kg/day alone without RT; 20 mg/kg/day (OE-RBMS1 rescue arm)
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Administration:p.o. gavage; daily for first month, then once every 3 days from second to sixth month; 6 months
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Result:Reduced RT-induced serum ALT, AST, and TBIL elevations.
Attenuated the RT-induced increase in liver-to-body weight ratio.
Reduced serum HA, PCIII, LN, and HYP.
Reduced H&E- and Sirius Red-detected fibrosis.
Suppressed COL-IV and Fibronectin immunofluorescence.
Downregulated Col1, Tgfb, Vim, Col4, Fn1, and Timp1 mRNA in liver tissue.
Suppressed RBMS1, cGAS, and STING protein and mRNA expression in fibrotic liver and attenuated RBMS1 immunofluorescence.
Reduced serum IL-6, TNF-α, CXCL1, and CCL1.
Decreased MDA.
Increased SOD.
Modulated Nrf2, Il6, Cxcl1, and Ccl1 mRNA.
Reduced CD86+ macrophage infiltration.
Restored Parkin mRNA.
Reversed RT-induced Parkin/PINK1 decreases and TOMM20 increase.
Preserved mitochondrial integrity by Mito-Tracker staining.
Increased LC3 puncta.
Reduced TOMM20 immunofluorescence.
Transcriptomic comparison of FA-treated versus RT liver identified 2351 differentially expressed genes, with 611 upregulated and 1741 downregulated.
In the RBMS1 overexpression/rescue arm, OE-RBMS1 increased RBMS1 protein and mRNA.
Suppressed RBMS1 protein and mRNA expression and decreased the OE-RBMS1-elevated serum ALT, AST, TBIL, HA, PCIII, and LN.
Downregulated Col1a1, Fn1, Timp1, Il6, and Cxcl1 mRNA.
Upregulated Nrf2 mRNA.
Attenuated H&E/Sirius Red-detected architectural distortion and collagen deposition.
Inhibited cGAS and STING immunofluorescence.
Enhanced Parkin immunofluorescence.
- RNA extraction experimental
- Collagen: Sirius Red Staining
- Research Protocol for Infectious Diseases
- ROS/oxidative-stress fluorescent staining
- Connective Tissue: Masson's Trichrome/Collagen Trichrome Staining
- Research Protocol for Inflammation-related Diseases
- Liver Cancer Modeling
- Liver Histomorphometry
- Cell Viability Determination by MTT Colorimetric Assay
- Fibrosis/Collagen Morphometry
- LPS-Induced Endotoxemia/Systemic Inflammation
- Cell Cytotoxicity Assay
- Mitophagy Solutions
Chemical Information
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CAS No. 119725-20-1
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Molecular Weight 484.67
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Formula C30H44O5
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SMILES
OC([C@]12[C@]([C@](O)([C@H](C)CC2)C)([H])C3=CC[C@@]([C@@]4([C@@](C(C)(C(C(O)=C4)=O)C)([H])CC5)C)([H])[C@]5(C)[C@]3(C)CC1)=O
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Structure Classification
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Initial Source
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
[2]. Guo X, et al. Fupenzic acid ameliorates radiation-induced liver fibrosis by regulating RBMS1 to inhibit the cGAS-STING pathway and restore mitochondrial function. Phytomedicine : international journal of phytotherapy and phytopharmacology. 2026 Sep;159:158399. [Content Brief]
[4]. Zhang J, et al. The triterpenoids and sesquiterpenoids from the plant of Agrimonia pilosa. Fitoterapia. 2022 Mar;157:105104. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)