Eriodictyol  (Synonyms: Huazhongilexone)

Eriodictyol ((±)-Huazhongilexone; Dihydroluteolin) is an orally active TRPV1 receptor antagonist (IC₅₀=44-47 nM, rTRPV1) with antioxidant and anti-inflammatory activities. Eriodictyol effectively inhibits lipid peroxidation and the release of proinflammatory cytokines by specifically antagonizing the TRPV1 receptor and activating the Nrf2 signaling pathway. Eriodictyol reduces the levels of ICAM-1, VEGF, eNOS and TNF-α in the retina and maintains the integrity of the blood-retinal barrier. Eriodictyol alleviates oxidative stress-induced apoptosis and hyperalgesia, enhances the activity and cytotoxicity of immune cells (such as B lymphocytes, NK cells and macrophages), and increases the levels of antioxidant enzymes simultaneously. Eriodictyol can be used in the research of diabetic retinopathy, acute lung injury and various pain-related diseases^{[1][2][3][4][5]}.

Eriodictyol inhibits LPS-induced inflammatory cytokine protein production and mRNA expression in C57BL/6 mouse bone marrow-derived macrophages^[2].
Eriodictyol (3-300 nM) acts as a functional TRPV1 antagonist in rat spinal cord synaptosomes, inhibiting capsaicin-induced calcium influx with an IC₅₀ of 44 nM, and does not alter baseline calcium levels on its own^[3].
Eriodictyol (1-300 μM; 30 min) has cell-free antioxidant activity, scavenging ABTS radicals with an IC₅₀ of 1.7 μM^[3].
Eriodictyol (2.5-20 μM; 48 h) dose-dependently inhibits LPS-induced NO production in murine peritoneal macrophages, reducing NO to 31.8 μM at 20 μM over 48 h^[4].
Eriodictyol (2.5-20 μM; 48 h) dose-dependently inhibits lysosomal enzyme activity in murine peritoneal macrophages, with significant suppression at 2.5, 5, 10, and 20 μM over 48 h^[4].
Eriodictyol (6.25-50 μM; 1 h) exhibits dose-dependent cellular antioxidant activity in murine splenocytes and macrophages, with EC₅₀ values of 13 μM and 14 μM, respectively, in the CAA assay^[4].
Eriodictyol (5-20 μM; 24 h) dose-dependently suppresses the production of proinflammatory cytokines TNF-α and IL-8 in high glucose-stimulated rat RGC-5 retinal ganglial cells^[5].
Eriodictyol (5-20 μM; 24 h) dose-dependently represses apoptosis in high glucose-stimulated rat RGC-5 retinal ganglial cells by modulating the expression of pro- and anti-apoptotic proteins^[5].
Eriodictyol (5-20 μM; 24 h) enhances activation of the Nrf2/HO-1 pathway in high glucose-stimulated rat RGC-5 retinal ganglial cells, which is required for its protective effects against oxidative stress, inflammation, and apoptosis^[5].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Eriodictyol (0.1-10 mg/kg; p.o.; daily; 10 days) dose-dependently reduces retinal inflammatory markers (TNF-α, eNOS) and plasma lipid peroxidation in streptozotocin-induced diabetic rats, with the 10 mg/kg dose suppressing blood-retinal barrier breakdown by 40% and lowering retinal VEGF and ICAM-1 levels^[1].
Eriodictyol (30 mg/kg; p.o.; single dose; 2 days prior to LPS exposure) significantly attenuates LPS-induced acute lung injury in female C57BL/6 mice via anti-inflammatory and antioxidative mechanisms, including improved survival, reduced inflammatory cytokine production, and activation of the Nrf2-Trx1 pathway^[2].
Eriodictyol (0.45-13.5 mg/kg; p.o.; single dose; 1 hour before capsaicin injection; 1-30 nmol/site; i.t.; single dose; 15 minutes before capsaicin injection) induces antinociception in intraplantar capsaicin-induced nociception in mice, with a maximal oral inhibition of 49 ± 10% (ID₅₀=2.3 mg/kg) and maximal intrathecal inhibition of 64 ± 4% (ID₅₀=2.2 nmol/site)^[3].
Eriodictyol (4.5 mg/kg; p.o.; single dose; 1 hour before intrathecal capsaicin injection) inhibits intrathecal capsaicin-induced nociception in mice by 71 ± 5%^[3].
Eriodictyol (4.5 mg/kg; p.o.; single dose; 1 hour before nociception testing) fully reverses thermal hyperalgesia and reduces mechanical allodynia by 64 ± 7% in CFA-induced inflammatory pain in mice^[3].
Eriodictyol (4.5 mg/kg; p.o.; single dose; 1 hour before intraplantar capsaicin injection) prevents intraplantar capsaicin-induced spinal oxidative stress in mice by preserving non-protein thiol levels and blocking 3-nitrotyrosine formation^[3].
Eriodictyol (combined with hesperidin and eriocitrin) enhances systemic antioxidant capacity and reduces markers of inflammation and oxidative stress in high-fat diet-fed C57BL/6J mice^[5].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

288.25

C₁₅H₁₂O₆

552-58-9

Solid

White to light yellow

O=C1C[C@@H](C2=CC=C(O)C(O)=C2)OC3=CC(O)=CC(O)=C13

Room temperature in continental US; may vary elsewhere.

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

• [1]. Bucolo C, et al. Eriodictyol prevents early retinal and plasma abnormalities in streptozotocin-induced diabetic rats. Biochem Pharmacol. 2012;84(1):88-92.  [Content Brief]

  [2]. Zhu GF, et al. Eriodictyol, a plant flavonoid, attenuates LPS-induced acute lung injury through its antioxidative and anti-inflammatory activity. Exp Ther Med. 2015;10(6):2259-2266.  [Content Brief]

  [3]. Rossato MF, et al. Eriodictyol: a flavonoid antagonist of the TRPV1 receptor with antioxidant activity. Biochem Pharmacol. 2011;81(4):544-551.  [Content Brief]

  [4]. Mokdad-Bzeouich I, et al. Investigation of immunomodulatory and anti-inflammatory effects of eriodictyol through its cellular anti-oxidant activity. Cell Stress Chaperones. 2016;21(5):773-781.  [Content Brief]

  [5]. Lv P, et al. Eriodictyol inhibits high glucose-induced oxidative stress and inflammation in retinal ganglial cells. J Cell Biochem. 2019;120(4):5644-5651.  [Content Brief]