Advances in structures required of polyphenols for xanthine oxidase inhibition

Abstract

Polyphenols have been used as natural medicaments for the management of hyperuricemia for a long history. They have been attracted many interests because of the little side effects in curing hyperuricemia, which is an important advantage over the antihyperuricemic drugs. In this review, the structure-activity relationships for polyphenols as xanthine oxidase (XO) inhibitors were discussed. It is concluded that the presence of hydroxyl groups, which influences the inhibitory effects, is closely related to whether the substitutions increase the steric hindrance or disturb the interaction of flavonoid with the catalytic site of XO, and the increased size of the molecule after glycosylation may increase the steric hindrance between flavonoid and XO, and consequently reducing the competitive inhibition behaviors. However, there is no obtained simple general rule that can comprehensively describe the effects of structural alteration on the inhibition activity because the results are varied among different subclasses of polyphenols. In addition, the inhibition mechanisms are mainly assumed as polyphenol binding to the active site of XO and hindering the entrance of xanthine or the discharge of uric acid and diffusion of O 2− radical.

Influence of In Vitro Human Digestion Simulation on the Phenolics Contents and Biological Activities of the Aqueous Extracts from Turkish Cistus Species

“…Similarly to digestive enzyme inhibition, AGE inhibitory activities of flavonoids were stimulated by C2=C3 double bond and hydroxylation of A and C rings. However, sugar attachment to the flavonoid skeleton leads to decreased inhibitory activity [ 49 ]. On the other hand, Cervantes-Lauren et al [ 50 ] suggested that flavon-3-ol glycosides possessed a greater AGE inhibition potential than the other flavonoid glycosides.…”

L‐Carnitine‐Based Bio‐Ionic Liquids as Antioxidants

“…The IL with ascorbate anion ( 1 ) had no effect on enzyme activity as well. So far, the search for new, effective XO inhibitors concerned, among others, rosmarinic, chlorogenic, caffeic and ferulic acid [71] . The low ability to inhibit XO with ILs results mainly from the properties of the acids used in their synthesis.…”

“…So far, the search for new, effective XO inhibitors concerned, among others, rosmarinic, chlorogenic, caffeic and ferulic acid. [71] The low ability to inhibit XO with ILs results mainly from the properties of the acids used in their synthesis. Despite the high antioxidant activity, the activity of gallic acid towards the XO enzyme is described as low.…”

Evaluasi Aktivitas Antihiperurisemia Ekstrak Etanol Herba Suruhan (Peperomia Pellucida L.), Herba Seledri (Apium Graveolens L.) Dan Kombinasi Ekstrak: Studi in Vivo Berbasis Bukti Ilmiah

“…Selain itu, mekanisme polifenol dalam menghambat xantin oxidase dengan cara mengikat sisi aktif dan memblok masuknya xanthine dan pelepasan asam urat dan serta difusi radikal bebas. 28 Serangkaian penelitian terus dilakukan untuk mengeksplorasi khasiat dari senyawa metabolit sekunder, khususnya berfokus pada senyawa flavonoid.…”