Inhibition of catechol-O-methyltransferase by natural pentacyclic triterpenes: structure–activity relationships and kinetic mechanism
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چکیده
منابع مشابه
Inhibition of catechol-O-methyltransferase by hydroxybenzenes and related compounds.
The inhibitory action of 1, 2, 3-trihydroxybenzene (pyrogallol) on the activity of catechol-O-methyltransferase (COMT) is well known (1-4). Recently, 1, 3, 5,-trihydroxy benezene (phloroglucinol) and 2, 4, 6-trihydroxy-l-propiophenom~ (THPP) have been shown to exert spasmolytic action in experimental animals and to relieve spastic disorders of the urinary tract and biliary ducts in patients (5-...
متن کاملKinetic and inhibition studies on catechol-O-methyltransferase affinity labelling by N-(3,4-dihydroxyphenyl)maleimide.
Initial velocity and product inhibition studies have been performed on soluble catechol-O-methyltransferase which has been partially purified from pig liver. The results are consistent with an ordered reaction mechanism, in which S-adenosyl-L-methionine (AdoMet) is the leading substrate. The enzyme is irreversibly inhibited by maleimide derivatives in a biphasic manner, which suggests a differe...
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SCOPE Inhibiting human neutrophil elastase (HNE) is a promising strategy for treating inflammatory lung diseases, such as H1N1 and SARS virus infections. The use of sivelestat, the only clinically registered synthesized HNE inhibitor, is largely limited by its risk of organ toxicity because it irreversibly inhibits HNE. Therefore, potent reversible HNE inhibitors are promising alternatives to s...
متن کاملMetabolism of catechol estrogens by erythrocyte catechol-O methyltransferase.
Fishman and Tulchinsky (1) present evidence that the catechol estrogen 2hydroxyestrone suppresses serum prolactin in normal ovulatory young women. However, in 3 of the 12 subjects studied the authors were unable to suppress serum prolactin and suggested that prolactin response to 2-hydroxyestrone is subjectand not time-dependent. In a study designed to evaluate the kinetics of catechol estrogen...
متن کاملSerotonin-Induced Hypersensitivity via Inhibition of Catechol O-Methyltransferase Activity
The subcutaneous and systemic injection of serotonin reduces cutaneous and visceral pain thresholds and increases responses to noxious stimuli. Different subtypes of 5-hydroxytryptamine (5-HT) receptors are suggested to be associated with different types of pain responses. Here we show that serotonin also inhibits catechol O-methyltransferase (COMT), an enzyme that contributes to modultion the ...
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ژورنال
عنوان ژورنال: Journal of Enzyme Inhibition and Medicinal Chemistry
سال: 2021
ISSN: 1475-6366,1475-6374
DOI: 10.1080/14756366.2021.1928112