Kanou, Masanobu; Saeki, Ken-ichi; Kato, Taka-aki; Takahashi, Kazuhiko; Mizutani, Takaharu published the artcile< Study of in vitro glucuronidation of hydroxyquinolines with bovine liver microsomes>, HPLC of Formula: 112-63-0, the main research area is hydroxyquinoline glucuronidation bovine liver microsome.
Glucuronidation of drugs by UDP-glucuronosyltransferase (UGT) is a major phase II conjugation reaction. Defects in UGT are associated with Crigler-Najjar syndrome and Gilbert’s syndrome with severe hyperbilirubinemias and jaundice. We analyzed the reactivities of some hydroxyquinoline derivatives, which are naturally produced from quinoline by cytochrome P 450. The analyses were carried out using a microassay system for UGT activity in bovine liver microsomes in the range 0.5-100 pmol/assay with the highly sensitive radio-image analyzer Fuji BAS2500 (Fujifilm, Tokyo, Japan). 3-Hydroxylquinoline is a good substrate for glucuronidation, and the relative Kcat values were 3,1-fold higher than the values for p-nitrophenol. 5,6-Dihydroquinoline-5,6-trans-diol gave a similar Km value to that of 3-hydroxyquinoline, but the Vmax value was approx. 1/15 of that of p-nitrophenol and showed weak reactivity. Quinoline N-oxide gave a low Vmax value and showed marginal activity. The Kcat values of 6-hydroxyquinoline and 5-hydroxyquinoline were 2.1- and 1.2-fold higher than that of p-nitrophenol, resp. Fluoroquinoline (FQ) derivatives, such as 3FQ, 7,8diFQ and 6,7,8triFQ, did not show any substrate activities. These results suggest that there are therapeutic problems in administration of some quinoline drugs to patients with jaundice.
Fundamental & Clinical Pharmacology published new progress about Bos taurus. 112-63-0 belongs to class esters-buliding-blocks, and the molecular formula is C19H34O2, HPLC of Formula: 112-63-0.
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