Effect of phenolic compounds from the rind of Punica granatum on the activity of three metabolism‐related enzymes

Abstract

Enzyme activity modulation by synthetic compounds provide strategies combining the inhibitory and therapeutic mode of action of the confirmed inhibitors. However, natural modulators could offer a valuable alternative for synthetic ones for the treatment of different chronic diseases (diabetes, hypertension, cancer) due to the numerous side effects of the latter. In vitro screening assays were conducted for Punica granatum rind methanolic extract against three metabolism‐related enzymes: α‐amylase, tyrosinase, and hyaluronidase. The obtained results showed that the examined extract retained high multitarget inhibition with inhibition percentages 31.5 ± 1.3%, 75.9 ± 4.7%, and 68.5 ± 5.3% against α‐amylase, tyrosinase, and hyaluronidase, respectively. Bioguided fractionation of P. granatum rind extract revealed that quercetin is the major active compound with inhibitory activities: 54.3 ± 2.7%, 94.2 ± 3.5%, and 90.9 ± 2.7% against α‐amylase, tyrosinase, and hyaluronidase, respectively. Kinetic studies of enzymes showed that quercetin inhibition was noncompetitive, uncompetitive, and competitive for α‐amylase, tyrosinase, and hyaluronidase, respectively. The molecular docking of quercetin with α‐amylase and hyaluronidase showed high binding energy with different bonds stabilizing the ligand–protein complex. Compiling all obtained results led to conclude that both P. granatum rind extract and quercetin have multitarget activities with potential therapeutic applications in many metabolic disorders.

Effect of phenolic compounds from the leaves of Psidium guajava on the activity of three metabolism‐related enzymes

“…Table 1 contains the detailed information about 27 plants and agricultural wastes that were extracted in methanol and investigated for their inhibitory activity against α-amylase, tyrosinase, and hyaluronidase (results are not included). Among the 27 plants extracts, Punica granatum results were illustrated in our previous publication [58] and it was concluded that Punica granatum extract and some of its fractions exhibited multitarget inhibition against α-amylase, tyrosinase, and hyaluronidase along with quercetin. In this study, we aim to illustrate the multitarget inhibition of P. guajava (guava) for the same target enzymes.…”