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

Inhibitory and Inductive Effects of Opuntia ficus indica Extract and Its Flavonoid Constituents on Cytochrome P450s and UDP-Glucuronosyltransferases

“…Promoter reporter assays were performed to investigate the effects of E2 or OFIE on CYP2B6 or CYP3A4 gene transcription via human constitutive androstane receptor (hCAR)- or human pregnane X receptor (hPXR)-associated mechanisms in HepG2 cells. OFIE is composed of flavonol aglycones and their O -glycosides ( Figure 1 ) and cellulase and pectinase-mediated hydrolysis of OFIE leads to dramatic increases in the level of flavonol aglycones ( Figures S1 and S2 ) [ 13 ], therefore, the ability of hdl OFIE to modulate CAR and PXR promoter activity was also investigated to speculate the roles for flavonoid constituents present in OFIE. E2, OFIE, and hdl OFIE induced a 4.8-, 4.4-, and 3.8-fold increase in CAR-mediated CYP2B6 reporter activity, respectively ( Figure 4 A).…”

“…Previous studies have demonstrated that the OFI fruit contains flavonoids, including rutin, narcissin, nicotiflorin, quercetin, kaempferol, and isorhamnetin as major phenolic compounds as well as vitamins, amino acids, and fibers [ 14 , 15 , 16 ]. Narcissin, nicotiflorin, and rutin glycosides are biotransformed into their respective aglycone such as isorhamnetin, kaempferol, and quercetin, respectively ( Figure 1 ) [ 13 ]. Thus, the biological effects of OFIE are mainly attributed to flavonol aglycones rather than glycosides after oral consumption as aglycones are ready to trespass membranes [ 17 ].…”

“…The concentrations of flavonoids employed in the reported studies were in the μM range, which are approximately hundreds of fold higher compared to those of OFIE used in the present study. In addition, doses of flavonols utilized for in vivo studies ranged from 10 to 250 mg/kg/day [ 20 ], which are hundreds of folds higher compared to the estimated dose of flavonols derived from OFIE (20–40 μg/day) used in the present study [ 13 ]. Furthermore, studies conducted by other groups did not consider estrogen-deprived conditions and were performed in animals treated for a relatively shorter period (less than two weeks); whereas in the present study the duration of administration was five weeks.…”

“…The Lyophilized powder of dried OFI fruits was purchased from Jeju Cactus Town (Hallim, Jeju-do, Korea) and a representative sample (150101MC) has been deposited at the Herbarium of the College of Science, Sookmyung Women’s University, Seoul, Republic of Korea. The composition of the OFI fruit extract has been analyzed using HPLC-diode array detector (DAD) as described previously [ 12 , 13 ] ( Figure S1A and Table S3 ). Stock solutions of chemicals or OFI powder were prepared in dimethyl sulfoxide (DMSO) or olive oil and a solution of the lyophilized powder of OFI fruits was defined as OFIE in this study.…”

“…Stock solutions of chemicals or OFI powder were prepared in dimethyl sulfoxide (DMSO) or olive oil and a solution of the lyophilized powder of OFI fruits was defined as OFIE in this study. The enzyme-hydrolyzed (hdl) OFIE sample was prepared as described previously [ 13 ]. The composition of the hdl OFIE has been presented in Figure S1B and Table S3 .…”