Hexahydrocurcumin is one of the major metabolites of curcumin and a selective, orally active COX-2 inhibitor. Hexahydrocurcumin is inactive against COX-1. Hexahydrocurcumin has antioxidant, anticancer and anti-inflammatory activities^[1][2]. In Vitro: Hexahydrocurcumin (0-25 μM; 24-48 hours; HT-29 cells) treatment significantly decreased the viability of HT-29 colon cancer cells in a time- and concentration-dependent. The respective IC₅₀ values for 24 and 48 h of Hexahydrocurcumin exposureare 77.05 and 56.95, respectively^[1].
Hexahydrocurcumin (0-25 μM; 24-48 hours; HT-29 cells) combined with 5-fluorouracil (5-FU; 5 µM) markedly reduces the COX-2 expression. The level of COX-1 is not altered^[1].
Hexahydrocurcumin (0-25 μM; 24-48 hours; HT-29 cells) combined with 5-fluorouracil (5-FU; 5 µM) markedly reduces the COX-2 protein. The level of COX-1 protein is not altered^[1].
Hexahydrocurcumin (7-14 μM; 24 hours) attenuates lipopolysaccharide (LPS)-elicited increase of prostaglandin E₂ (PGE₂) in murine macrophages (RAW 264.7) in a concentration-dependent manner^[2]. In Vivo: Hexahydrocurcumin (50 mg/kg; oral administration; daily; for 16 weeks; male Wistar rats) treatment significantly reduces the numbers of aberrant crypt foci (ACF) in colon cancer rats. Hexahydrocurcumin also markedly decreases COX-2 protein expression. The levels of COX-1 protein is not different from normal rats^[3].