Hesperetin

SKU: orb1305314

Description

Hesperetin is a flavanone flavonoid commonly found as its glycoside hesperidin in citrus fruits like lemons and oranges. It is widely used in research for its antioxidant, anti-inflammatory, and potential cardioprotective properties, studied in both in vitro and in vivo models.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 520-33-2
• MW: 302.28
• Purity: 99.27% (May vary between batches)
• Formula: C₁₆H₁₄O₆
• SMILES: O=C1C=2C(O[C@@H](C1)C3=CC(O)=C(OC)C=C3)=CC(O)=CC2O
• Target: Autophagy,TGF-beta/Smad,ROS,Bcl-2 Family,p38 MAPK,5-HT Receptor,NF-κB,Apoptosis
• Solubility: Ethanol:< 1 mg/mL (insoluble or slightly soluble);DMSO:45 mg/mL (148.87 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (6.62 mM);H2O:< 1 mg/mL (insoluble or slightly soluble)

Bioactivity

• Target IC50:
  Vero cells:8.3 μM|UGT1A4:29.68-63.87 μM|PC3 cells:40 μM|CCRF-CEM cells:> 10 μM (EC50)|BJ cells:> 10 μM (EC50)|Caco-2 cells:66.67 μM|UGT1A7:29.68-63.87μM|UGT1A1:< 10 μM|RAW 264.7 cells:31.2 μM|Monocyte:2.1 μM|UGT1A8 cells:29.68 - 63.87 μM
• In Vivo:
  Pre-administration of Hesperetin (40 mg/kg b.w., oral) significantly reduces Cd-induced oxidative stress and mitochondrial dysfunction in rats’ brains, while restoring antioxidant activity and membrane-bound enzyme functions, and lessening apoptosis. At a dose of 200 mg/kg, Hesperetin diminishes Con A-induced hepatocyte apoptosis and hepatic Nos2 (iNOS) expression in mice, alongside reducing the presence of apoptotic bodies, hydropic degeneration, nuclear fragments, autolysis, and hemorrhage. Moreover, Hesperetin co-treatment notably lowers the infiltration of leukocytes in the liver tissue of mice suffering from D-GalN/LPS-induced fulminant hepatitis, demonstrating its protective effect in a murine model.
• In Vitro:
  Hesperetin has the retention of antioxidant potential in self nano-emulsifying drug delivery system. Hesperetin and NGR display broad-spectrum inhibition against human UGTs. In addition, Hesperetin exhibits strong inhibitory effects on UGT1A1, 1A3 and 1A9 (both IC50 and Ki values lower than 10 μM) and moderately inhibits UGT1A4, UGT1A7, UGT1A8 (IC50 values 29.68-63.87 μM). Hesperetin interacts with different types of proteins involving hydrogen bonds, pi-pi effects, pi-cation bonding and pi-sigma interactions with varying binding energies. Hesperetin exhibits drug-like properties which indicate its potential as a therapeutic option for CHIKV infection. Hesperetin dose-dependently reduces GCDCA-induced caspase-3 activity in cultured primary rat hepatocytes. Hesperetin also dose-dependently reduces CM-induced Nos2 (iNOS) expression in hepatocytes. Interestingly, hesperetin-induced expression of the antioxidant gene haem oxygenase 1 (HO-1) about fourfold compared with cytokine mixture alone.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

inhibit, HT, Hesperetin, Inhibitor, Autophagy, Apoptosis, 5HTReceptor, 5HT Receptor, TGFβ, TGF-β/Smad, Smad, TGFbeta/Smad, TGFbeta, TGF-beta, TGFb, TGF-b/Smad, p38MAPK, p38 MAPK

Compound Identifiers

PubChem CID

72281