The Dual Actions of Morin (3,5,7,2′,4′-Pentahydroxyflavone) as a Hypouricemic Agent: Uricosuric Effect and Xanthine Oxidase Inhibitory Activity

Abstract

Hyperuricemia is associated with a number of pathological conditions such as gout. Lowering of elevated uric acid level in the blood could be achieved by xanthine oxidase inhibitors and inhibitors of renal urate reabsorption. Some natural compounds isolated from herbs used in traditional Chinese medicine have been previously demonstrated to possess xanthine oxidase inhibitory activities. In the present investigation, morin (3,5,7,2Ј,4Ј-pentahydroxyflavone), which occurs in the twigs of Morus alba L. documented in traditional Chinese medicinal literature to treat conditions akin to gout, was demonstrated to exert potent inhibitory action on urate uptake in rat renal brushborder membrane vesicles, indicating that this compound acts on the kidney to inhibit urate reabsorption. Lineweaver-Burk transformation of the inhibition kinetics data demonstrated that the inhibition of urate uptake was of a competitive type, with a K i value of 17.4 M. In addition, morin was also demonstrated to be an inhibitor of xanthine oxidase. Lineweaver-Burk analysis of the enzyme kinetics indicated that the mode of inhibition was of a mixed type, with K i and K ies values being 7.9 and 35.1 M, respectively. Using an oxonate-induced hyperuricemic rat model, morin was indeed shown to exhibit an in vivo uricosuric action, which could explain, in part at least, the observed hypouricemic effect of morin in these rats. The potential application of this compound in the treatment of conditions associated with hyperuricemia was discussed.

Morin hydrate promotes inner ear neural stem cell survival and differentiation and protects cochlea against neuronal hearing loss

“…Moreover, morin hydrate was found to attenuate CD36 expression, as well as oxidative modification of low‐density lipoproteins and their subsequent update, in U937‐derived macrophages 13. In addition, in an oxonate‐induced hyperuricemic rat model, morin hydrate was found to act as a hypouricemic agent and xanthine oxidase inhibitor 12. It is, therefore, interesting to uncover the underlying molecular mechanisms, in order to promote its precise and controlled clinical application.…”

“…Being yellow crystalline when extracted and purified, morin hydrate has exhibited a wide range of beneficial pharmacological effects, including anti‐cancer 10 and anti‐inflammatory activities 11, xanthine oxidase inhibitor property 12, preventing oxidation of low‐density lipoprotein 13, free radical scavenging activity 14 which in turn prevented DNA damage 15. However, to date, its function in NSC growth and differentiation, as well as in preventing neuronal hearing loss, has yet to be studied.…”

Synthesis and Characterization of Fe<sub>3</sub>O<sub>4</sub> Coated on APTES as Carriers for Morin-Anticancer Drug

“…Morin (3,5,7,2',4'-pentahydroxyflavone, Figure 1), is a member of the flavonoids groups that has been reported as an important agent effective chemotherapeutic used for the treatment of cancer [11]. Furthermore, numerous reports suggest that morin has a wide range of therapeutic applications such as anti-inflammation [12], antioxidant [13], it induces apoptosis in hepatocellular carcinogenesis model [14], and xanthine oxidase inhibition activity [15]. In this study, Fe 3 O 4 magnetic nanoparticles were fabricated by co-precipitation method and coated with APTES.…”

Effects of Dietary Chrysin Supplementation on Blood Pressure and Oxidative Status of Rats Fed a High-Fat High-Sucrose Diet

“…Flavonoids have been reported to exert a wide range of biological actions, including vasodilation, antithrombotic, and antihypertensive effects (Duarte et al, 1993;Duarte et al, 2001;Yamamoto and Oue, 2006;Gryglewski et al, 1987;Yu et al, 2006;Villar et al, 2002). Most of these reports dealt with quercetin, and only one report focused on the in vivo biological effects of chrysin.…”

“…The beneficial effects of flavonoids on human health have been widely studied, and antioxidative activity was proposed as one of the most important causes of these effects (Duarte et al, 1993;Duarte et al, 2001;Yamamoto and Oue, 2006;Gryglewski et al, 1987;Yu et al, 2006;Villar et al, 2002). Quercetin is the most abundant flavonol type of flavonoid, and a wide range of biological actions including vasodilation, antihypertensive, and antithrombotic effects have been reported (Duarte et al, 1993;Duarte et al, 2001;Yamamoto and Oue, 2006).…”