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Methylxanthines are chemical compounds which are derivatives of xanthine with one or more methyl groups, including: One methyl group: 1-Methylxanthine;
Xanthine (/ ˈ z æ n θ iː n / or / ˈ z æ n θ aɪ n /, from Ancient Greek ξανθός xanthós ' yellow ' for its yellowish-white appearance; archaically xanthic acid; systematic name 3,7-dihydropurine-2,6-dione) is a purine base found in most human body tissues and fluids, as well as in other organisms. [2]
A xanthine oxidase inhibitor is any substance that inhibits the activity of xanthine oxidase, an enzyme involved in purine metabolism.In humans, inhibition of xanthine oxidase reduces the production of uric acid, and several medications that inhibit xanthine oxidase are indicated for treatment of hyperuricemia and related medical conditions including gout. [1]
7-Methylxanthine (7-MX), also known as heteroxanthine, is an active metabolite of caffeine (1,3,7-trimethylxanthine) and theobromine (3,7-dimethylxanthine). [ 1 ] [ 2 ] It is a non-selective antagonist of the adenosine receptors .
IBMX (3-isobutyl-1-methylxanthine), like other methylxanthine derivatives, is both a: competitive non-selective phosphodiesterase inhibitor [1] which raises intracellular cAMP, activates PKA, inhibits TNFα [2] [3] and leukotriene [4] synthesis, and reduces inflammation and innate immunity, [4] and; nonselective adenosine receptor antagonist. [5]
Its pharmacology is similar to other methylxanthine drugs (e.g., theobromine and caffeine). [1] Trace amounts of theophylline are naturally present in tea, coffee, chocolate, yerba maté, guarana, and kola nut. [1] [3] The name 'theophylline' derives from "Thea"—the former genus name for tea + Legacy Greek φύλλον (phúllon, "leaf") + -ine.
The same protein, which in humans has the HGNC approved gene symbol XDH, can also have xanthine dehydrogenase activity (EC 1.17.1.4). [5] Most of the protein in the liver exists in a form with xanthine dehydrogenase activity, but it can be converted to xanthine oxidase by reversible sulfhydryl oxidation or by irreversible proteolytic modification.
Methylxanthines activate histone deacetylases, promoting the deacetylation of histone and subsequent DNA folding. This inhibits the synthesis of pro-inflammatory factors that induce asthma attacks and exacerbations, achieving anti-inflammatory effects. [19] For asthma maintenance therapy, methylxanthines are taken orally. [2]