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Chrysin and aromatase

Chrysin is a flavonoid that has been purported especially in the bodybuilding world to be an effective inhibitor of an enzyme known as aromatase. Aromatase is the enzyme that causes the conversion of testosterone into estradiol and androstenedione into estrone. This would have a definite theoretical advantage to bodybuilders especially those who are taking high doses of potent anabolic steroids.

However, if true, it would have significant advantages for many outside the bodybuilding community, as well.

Aromatase levels are known to rise with age. This increase often causes a relative imbalance of estrogen and testosterone in men as they grow older. In addition to having a decreased output of testosterone with age , the age-related increase of aromatase causes older men to convert what testosterone they do produce into estrogen. This is not a desirable phenomenon for aging men, and explains part of the interest in finding an effective inhibitor of aromatase.

Chrysin and PGE2

Inflammation and oxidative stress are associated with cancer, atherosclerosis, and other chronic diseases. Dietary flavonoids have been reported to possess antiinflammatory and antioxidant properties, but their mechanisms of action and structure-activity relations have not been fully investigated. We hypothesized that differences in antioxidant activity between the structurally similar flavones, luteolin and chrysin (differing only in B-ring hydroxylation patterns), would differentially affect inflammation-associated Cox-2 expression and PGE2 formation. Pretreatment of RAW 264.7 macrophage-like cells with 25, 50, or 100 µmol/L concentrations of luteolin inhibited lipopolysaccharide (LPS)-induced Cox-2 protein expression (P < 0.0001). Chrysin pretreatment did not reduce LPS-induced Cox-2 protein expression at any level tested. Conversely, both luteolin and chrysin completely suppressed LPS-induced PGE2 formation (P < 0.001). Luteolin, but not chrysin, inhibited xanthine/xanthine oxidase-generated superoxide formation at 100 µmol/L in a cell-free system (P < 0.001). Although both luteolin and chrysin reduced LPS-induced hydroxyl radical formation relative to the positive control (P < 0.001), luteolin was superior to chrysin (P = 0.003). In summary, luteolin and chrysin suppressed PGE2 formation equally well, despite differential effects on Cox-2 protein expression and on superoxide and hydroxyl radical scavenging. These data indicate that flavones may display similar antiinflammatory activity via different mechanisms.