Abstract

The growing interest in the chemistry of unsaturated ring-fused 1,3-heterocycles, in this particular case 1,3-oxazines, arise in part from their versatile pharmacological applications. In the present article, the evaluation of the in vitro and ex vivo antioxidant activity of two cyclohexene-fused oxazines is discussed. The in vitro antioxidant activity was evaluated by trapping the ABTS and hydroxyl radicals as well as the inhibition of the enzyme acetyl-cholinesterase and hemolysis of erythrocytes by 2,2’-Azobis(2-amidinopropane) dihydrochloride (AAPH). The results suggest that both unsaturated 1,3-oxazines are auspicious sources of biologically active compounds with good antioxidant properties. In addition, a comprehensive analysis of the interaction between these heterocycles with 2,2-diphenyl-1-picrylhydrazyl (DPPH) and 2,2’-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid) (ABTS) radicals, as well as the measurements of redox potential, provided evidence for a mechanism of antioxidant activity that takes place through electron transfer (ET) processes.

Highlights

  • Free radicals are responsible for intercellular signaling and synthesis of important biological substances in living organisms, due to their ability to facilitate the donation of their electrons to other molecules, which causes chain reactions [1,2]

  • According to the results described above, oxazines 1 and 2 were able to protect erythrocytes from damage induced by Azobis(2-amidinopropane) dihydrochloride (AAPH), since there was a decrease in the hemolysis of rat erythrocytes

  • Analysis of the results shows that Tx possesses the highest antioxidant activity/capacity

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Summary

Introduction

Free radicals are responsible for intercellular signaling and synthesis of important biological substances in living organisms, due to their ability to facilitate the donation of their electrons to other molecules, which causes chain reactions [1,2]. Some physiological processes are responsible for the antioxidant defense mechanism that catalyzes the reduction of O2 in water. Such processes control the generation of free radicals and prevent their. There are some diseases where oxidative stress is prevent their overproduction in mitochondria [9]. There are some diseases where oxidative involved in the pathophysiology, and often, the defense mechanism is not enough. It is stress is involved in the pathophysiology, and often, the defense mechanism is not enough In these necessary to find new antioxidant compounds as therapeutic agents [10]

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