Brevilin A

SKU: orb1219361

Description

Brevilin A is a sesquiterpene lactone isolated from Centipeda minima, inhibits janus kinase activity and blocks STAT3 signaling in cancer cells with anti-tumor activity. Brevilin A is a selective inhibitor of JAK-STAT signal pathway by attenuating the JAKs activity and blocking STAT3 signaling (IC50 = 10.6 μM) in Cancer Cells.Brevilin A induces apoptosis and autophagy via mitochondrial pathway and PI3K/AKT/mTOR inactivation in colon adenocarcinoma cell CT26.antitumourIn vitro activity against Giardia intestinalis was used for bioassay-guided fractionation of crude extracts from C. minima. The sesquiterpene lactone, Brevilin A was isolated and found to have antigiardial activity (IC50 = 16.1 μM) and was similarly active in vitro against Entamoeba histolytica (IC50 between 4.5 and 9 μM) and against Plasmodium falciparum (IC50 = 9.42 μM).

Key Properties

• CAS Number: 16503-32-5
• MW: 346.41
• Purity: >98% (HPLC)
• Formula: C₂₀H₂₆O₅
• SMILES: C/C=C(C)\C(O[C@H]1[C@@]([C@@H]2C)([H])[C@@](OC2=O)([H])C[C@@H](C)[C@@]3([H])[C@]1(C(C=C3)=O)C)=O
• Target: Antifection
• Solubility: DMSO:100 mg/mL (288.67 mM; Need ultrasonic)

Bioactivity

• In Vivo:
  Animal model: Male BALB/c nude mice injected with CNE-2 cells. Dosage: 10 and 20 mg/kg. Administration: Oral gavage; 10 and 20 mg/kg; once daily; 16 days. Result: Decreased average tumor volumes and weights treated with 20 mg/kg by 36.3% and 46.0%, respectively, compared to vehicle control. Inhibited the protein expression of p-AKT and p-STAT3 at both low and high doses.
• In Vitro:
  Cell Viability Assay Cell line: A549R cells. Concentration: 1-20 μM. Incubation time: 24 hours. Result: Exhibited STAT3 signaling inhibition in a dose dependent manner with IC50 value of 10.6 μM. Cell Proliferation Assay Cell line: CNE-2 cells. Concentration: 0-50 μM. Incubation time: 24, 48, and 72 hours. Result: Showed IC50 values in CNE-2 cells with treatment times of 24, 48, and 72 h of 7.93, 2.60, and 22.26 μM, respectively. Apoptosis Analysis Cell line: DU145 and MDA-MB-468 cells. Concentration: 10 μM. Incubation time: 24 and 48 hours. Result: Decreased c-Myc and CyclinD1 after 24 h and 48 h treatment, increased cleaved PARP after 24 h treatment. Western blot analysis. Cell line: A549R cells. Concentration: 12.5 and 25 μM Incubation time: 24 hours. Result: Inhibits STAT3 phosphorylation in A549R cells.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Quick Database Links

Gene Symbol

Antifection