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Aromatase inhibitors affect the ability of estrogens production from androgens by inhibiting the aromatase enzyme activity which is a part of the estrogen pathway. [13] The two categories of AIs are based on their mechanism of action and structure.
Aromatase inhibitors (AIs) are a class of drugs used in the treatment of breast cancer in postmenopausal women and in men, [1] [2] and gynecomastia in men. They may also be used off-label to reduce estrogen conversion when supplementing testosterone exogenously .
Like the aromatase inhibitors formestane and atamestane, exemestane is a steroid that is structurally similar to 4-androstenedione, the natural substrate of aromatase. It is distinguished from the natural substance only by the methylidene group in position 6 and an additional double bond in position 1. [15]
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Letrozole is an orally active, nonsteroidal, selective aromatase inhibitor and hence an antiestrogen. It prevents aromatase from producing estrogens by competitive, reversible binding to the heme of its cytochrome P450 unit. The action is specific, and letrozole does not reduce production of corticosteroids. [citation needed
A component in various medicinal plants (e.g. Scutellaria baicalensis), chrysin is a dihydroxyflavone, a type of flavonoid. [6] It is also found in honey, propolis, the passion flowers, Passiflora caerulea and Passiflora incarnata, in Oroxylum indicum, [2] carrots, [1] chamomile, [7] many fruits, and in mushrooms, such as the mushroom Pleurotus ostreatus. [6]
[13] [6] The medication was one of the first adrenal steroidogenesis inhibitors as well as the first aromatase inhibitor to be discovered and used clinically, and led to the development of other aromatase inhibitors. [18] [4] [30] [9] Along with testolactone, it is described as a "first-generation" aromatase inhibitor. [7]
α-Naphthoflavone is a potent inhibitor of the enzyme aromatase, the enzyme that converts testosterone to estrogen. [1] [2] α-Naphthoflavone has been shown to cause abnormal testicular development in young chickens. [4]
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