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• W2376278384 abstract "In order to increase stability of quercetin, its metabolically and chemically susceptible hydroxyl groups 7-OH and 3-OH respectively were transiently blocked with a pivaloxymethyl (POM) promoiety to provide two novel quercetin conjugates [7-O-POM-Q (2), 3-O-POM-Q (3)]. In the absence of stabilizer (ascorbic acid), the synthesized conjugates showed significantly increased stability in cell culture media [t1/2 = 4 h (2), 52 h (3)] compared with quercetin (t1/2 < 30 min) and quercetin prodrug 1 (t1/2 = 0.8 h). In addition, the quercetin conjugate 2 underwent efficient cellular uptake and intracellular levels of its hydrolysis product, quercetin, were maintained up to 12 h. Stability and intracellular accumulation of 2 were demonstrated by its stabilizer-independent cytostatic effect and induction of apoptotic cell death. Even though 3 was more stable than 2, it failed to penetrate cell membranes. However, the remarkable stability of 3 warrants further investigation of quercetin conjugates with various promoieties at the 3-OH position." @default.
• W2376278384 created "2016-06-24" @default.
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• W2376278384 date "2010-11-19" @default.
• W2376278384 modified "2023-10-14" @default.
• W2376278384 title "Enhanced Stability and Intracellular Accumulation of Quercetin by Protection of the Chemically or Metabolically Susceptible Hydroxyl Groups with a Pivaloxymethyl (POM) Promoiety" @default.
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• W2376278384 doi "https://doi.org/10.1021/jm101252m" @default.
• W2376278384 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/21090565" @default.
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