Resveratrol Is a Potent Inhibitor of the Dioxygenase Activity of Lipoxygenase

Abstract

Resveratrol is a naturally occurring phytoalexin, present in grapes and other food products, with important antioxidant properties. Although still under debate, it is generally assumed that resveratrol has protective effects against heart diseases and probably tumor development. Lipoxygenase is a dioxygenase with peroxidase activity involved in the synthesis of mediators in inflammatory, atherosclerotic, and carcinogenic processes. Lipoxygenase activity is also involved in the generation of flavors and aromas in foods from animal or vegetal sources. The results presented here show that resveratrol was a potent inhibitor of the dioxygenase activity of lipoxygenase, with an IC(50) = 13 microM. Simultaneously, resveratrol was oxidized by the peroxidase activity of lipoxygenase with a V(max) = 0.28 microM min(-1) and a k(M) = 16.6 microM. Furthermore, oxidized resveratrol was as efficient a lipoxygenase inhibitor as in its reduced form. From the data obtained it can be concluded that both resveratrol and its oxidized form can act as inhibitors of the dioxygenase activity of lipoxygenase. In contrast, the hydroperoxidase activity of lipoxygenase was not inhibited by resveratrol. These results suggest that resveratrol may be used as an antioxidant food additive and as a pharmacological agent to prevent the generation of eicosanoids involved in pathological processes.

Resveratrol improves reproductive parameters of adult rats varicocelized in peripuberty

“…Although oxidative stress (OS) is an important factor in the sperm lesion caused by varicocele (Aitken et al 2014) and in spite of the known efficacy of resveratrol as an antioxidant (Pinto et al 1999, Saiko et al 2008, its capability to decrease lipid peroxidation caused by varicocele in the testicular environment and in the epididymal level were not yet investigated. In the present research, we observed a favorable action of resveratrol on reproduction of rats submitted to a left-sided surgical varicocele.…”

Resveratrol as a Chemopreventive Agent: A Promising Molecule for Fighting Cancer

“…In the presence of the substrate (linoleic acid), resveratrol inhibits both 5-lipoxygenase and 15-lipoxygenase as a competitive inhibitor [85,112]. Resveratrol prolongs the lag phase of both enzymes, indicating a possible reduction of Fe(III) to Fe(II) at the catalytic site [96].…”

Antimutagenic effect of resveratrol

“…Resveratrol can modulate signal transduction pathways by the inhibitory effect on the activation of transcription factors such as NF-κB and AP1 (KUNDU & SURH 2004). Resveratrol, as a selective inhibitor of cyclooxygenase 2 (COX-2), is also a strong inhibitor of the dioxygenase activity of lipoxygenase (LOX) (PINTO et al 1999). …”