(-)-Epicatechin

(-)-Epicatechin (Epicatechin) belongs to natural products and is a COX-1 inhibitor (IC50 = 3.2 μM) with cell permeability. By blocking the nuclear localization of the p65 subunit of NF-κB, this compound inhibits IL-1β-induced iNOS expression and possesses significant anti-inflammatory activity.

COX-1:3.2 μM, MDA-MB-231 cells:85 μM

Methods: Panc-1, U87, and MIA PaCa-2 cancer cells as well as normal human fibroblasts were treated with (-)-epicatechin to detect mitochondrial respiration, oxygen consumption, radiation sensitivity under combined irradiation, and levels of Chk2 phosphorylation and p21 induction.
Results: (-)-Epicatechin stimulated mitochondrial respiration and oxygen consumption only in Panc-1 cells; selectively enhanced radiation sensitivity in cancer cells (REF 1.7, 1.5, and 1.2 for Panc-1, U87, and MIA PaCa-2, respectively) without enhancement in normal fibroblasts (REF = 0.9); and increased Chk2 phosphorylation and p21 induction only in cancer cells when combined with irradiation.[1]

Methods: 26-month-old C57BL/6 aged mice were administered (-)-epicatechin (1 mg/kg, twice daily) by gavage for 2 weeks (vehicle: water). Additionally, 6 middle-aged subjects (41 ± 5 years) were given (-)-epicatechin capsules (25 mg, twice daily) for 7 days. Muscle regulatory factors and hand grip strength were measured.
Results: (-)-Epicatechin reduced elevated myostatin and β-galactosidase, and increased follistatin and Myf5 in aged mice; in humans, it increased hand grip strength (~7%) and plasma follistatin/myostatin ratio, reversing aging-related changes.[2]
Methods: 5-month-old C57BL/6 male mice were randomly divided into control group, training group, detraining + placebo (water) group, and detraining + (-)-epicatechin (1 mg/kg, gavage, twice daily) group. Skeletal muscle capillary density, VEGF-A/TSP-1 expression, oxidative enzyme activity, and endurance were measured.
Results: Compared with the placebo group, (-)-epicatechin significantly increased skeletal muscle capillary density and oxidative enzyme activity in detrained mice, maintained mitochondrial complex IV and cytochrome c oxidase activity, reduced the decline in VEGF-A/TSP-1 ratio, and preserved endurance comparable to the training group.[3]

Panc-1 cells are seeded into T-150 flasks and on the next day, cells are treated with different concentrations of (-)-epicatechin for 1 h, then harvested and solubilized in 10 mM HEPES (pH 7.4), 40 mM KCl, 1%Tween-20, 1 μM oligomycin, 1 mM PMSF,10 mM KF, 2 mM EGTA, and 1 mM Na3VO4. COX activity is measured in the presence of 20 mM ascorbate and 200 μM substrate cytochrome c from cow heart.(Only for Reference)

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

H2O: 2.25 mg/mL (7.75 mM), Sonication is recommended.

DMSO: 80 mg/mL (275.61 mM), Sonication is recommended.

50% PEG300+50% Saline: 5 mg/mL (17.23 mM)

0.5% CMC-Na: 5 mg/mL (17.23 mM), Sonication is recommended.