Enzymatic Deglycosylation of Opuntia ficus indica improves its Estrogen Receptor-Subtype Selective Transcriptional and Anti-Inflammatory Activities

Abstract

Flavonoids are polyphenols widely present as aglycone or sugar-attached glycosides in agricultural products and possess various beneficial activities. Glycosylation affects the physicochemical properties of flavonoid aglycones, leading to changes in their biological activities. Opuntia ficus indica (OFI) fruits are reported to have anti-diabetic, anti-inflammatory, and phytoestrogenic activities. In this study, the role of glycosylation in OFI grown in Jeju, Korea has been investigated, focusing on narcissin, which is the major flavonoid glycoside. Efficient and mild hydrolysis of the glycosides in extracts of Jeju OFI fruits (OFIE) was investigated using hydrolysis enzymes. The enzyme-treated OFIE displayed estrogen receptor β−selective transcriptional activity and inhibition of the nuclear factor-κB signaling pathway in cell line models. Additionally, it inhibited the enzyme that catalyzes the conversion of prostaglandin H2 to inflammatory prostaglandin D2. Our data suggests that enzymatic deglycosylation of OFIE may increase healthpromoting benefits such as the estrogen replacement effect with anti-inflammatory activity.