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Sesamin and Sesamolin: Nature's Therapeutic Lignans

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Sesame oil is commonly used as antioxidant. Sesamin (SA) and sesamolin (SO) are major lignans (a non-fat constituent) in sesame seed oil, inhibit Δ5-desaturase activity and cause accumulation of dihomo-γ- linolenic acid (DGLA), a precursor of 1-series prostaglandins, and the decreasing production of proinflammatory 2-series prostaglandins and 4-series leukotrienes. Diets supplemented with SA and/or SO, lower serum levels of interleukin (IL)-1β, IL-6 but elevate IL-10 in mice after lipopolysaccharide (LPS) exposure. Mice fed with sesame seed oil have a 65% survival rate after cecal ligation and puncture as compared with the 20% survival in the controls. SA and SO inhibit the IL-6, tumor necrosis factor (TNF)-α and nitric oxide (NO) productions from microglia under LPS stimulation. The protective effects of SA/SO to stroke-prone spontaneously hypertensive rats and hepatic ischemia-reperfusion injury have been attribute to their antioxidant and anti-inflammatory activities. The antioxidant activities of SA/SO are identified in their methylenedioxyphenyl moieties that can be changed into dihydrophenyl (catechol) moieties. Since reactive oxygen species (ROS) are mediators of a variety of pathological processes, including inflammation and ischemic/hypoxic injury, the ROS scavenging moiety may contribute as an important component to prevent cells from the free radical injury. Hypoxia or HO-induced cell injury are related with activated MAPKs and caspase-3 activities. Evidence suggests that the protective effects of SA and SO on hypoxic neuronal cells are related to suppression of ROS generation and mitogen-activated protein kinases (MAPKs). In addition, SA/SO significantly reduce LPS-activated p38 MAPK. Specific inhibitors of MAPKs dose-dependently inhibit NO and cytokine productions in LPS-stimulated microglia. Therefore, the inhibition of NO and cytokine productions may partly due to the reduction of LPS-induced p38 MAPK signal pathway by SA and SO.
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Keywords: anti-inflammation; antioxidant; hypoxia; lipopolysaccharide; mitogen-activated protein kinases; reactive oxygen species; sesamin; sesamolin

Document Type: Review Article

Affiliations: Department of Education and Research, Taichung Veterans General Hospital, Taichung, Taiwan.

Publication date: January 1, 2005

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  • Current Enzyme Inhibition aims to publish all the latest and outstanding developments in enzyme inhibition studies with regards to the mechanisms of inhibitory processes of enzymes, recognition of active sites, and the discovery of agonists and antagonists, leading to the design and development of new drugs of significant therapeutic value. Each issue contains a series of timely, in-depth reviews written by leaders in the field, covering a range of enzymes that can be exploited for drug development. Current Enzyme Inhibition is an essential journal for every pharmaceutical and medicinal chemist who wishes to have up-to-date knowledge about each and every development in the study of enzyme inhibition.
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