Phenolic antioxidants: a rationale for design and evaluation of novel antioxidant drug for atherosclerosis.
With increasing evidence that shows the involvement of active oxygen and nitrogen species in a variety of disorders, cancer, and aging, the role of antioxidant against oxidative stress has received renewed attention. In this review article, a rationale for design of lipophilic, radical-scavenging antioxidant is presented and the potency of a novel antioxidant, 2,3-dihydro-5-hydroxy-2,2-dipentyl-4, 6-di-tert-butylbenzofuran (BO-653), as an inhibitor of LDL oxidation was evaluated by considering various factors such as reactivity toward radicals, localization, and mobility in the lipoprotein, and fate of its radical. The anti-atherogenic activity of BO-653 was compared with those of alpha-tocopherol, probucol, and its metabolites. Furthermore, a novel function of phenolic antioxidants such as cell regulation and induction of phase II defense antioxidants are also discussed.
Noguchi
N
N
University of Tokyo, Research Center for Advanced Science and Technology, Komaba, Meguro, Tokyo, Japan.
Niki
E
E
D000818:Animals; D000975:Antioxidants / Q000737:chemistry / Q000494:pharmacology*; D001161:Arteriosclerosis / Q000188:drug therapy* / Q000378:metabolism / Q000517:prevention & control; D001572:Benzofurans / Q000737:chemistry / Q000494:pharmacology*; D015195:Drug Design; D004355:Drug Stability; D016166:Free Radical Scavengers / Q000494:pharmacology; D006801:Humans; D014810:Vitamin E / Q000494:pharmacology
C106512:2,3-dihydro-5-hydroxy-2,2-dipentyl-4,6-di-tert-butylbenzofuran; D000975:Antioxidants; D001572:Benzofurans; D016166:Free Radical Scavengers; D014810:Vitamin E