- Pharmacokinetic alteration of paclitaxel by ferulic acid derivative
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P-glycoprotein (P-gp) is known to be involved in multidrug resistance (MDR) and modulation of pharmacokinetic (PK) profiles of substrate drugs. Here, we studied the effects of synthesized ferulic acid (FA) derivatives on P-gp function in vitro and examined PK alteration of paclitaxel (PTX), a well-known P-gp substrate drug by the derivative. Compound 5c, the FA derivative chosen as a significant P-gp inhibitor among eight FA candidates by in vitro results, increased PTX AUCinf as much as twofold versus the control by reducing PTX elimination in rats. These results suggest that FA derivative can increase PTX bioavailability by inhibiting P-gp existing in eliminating organs.
- Lee, Jaeok,Chae, Song Wha,Ma, Lianji,Lim, So Yeon,Alnajjar, Sarah,Choo, Hea-Young Park,Lee, Hwa Jeong,Rhie, Sandy Jeong
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- Compositions for the prevention or treatment of neurodegenerative disease containing alkoxyphenylpropenone derivatives or pharmaceutically acceptable salts thereof as an active ingredient
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PURPOSE: An alkoxyphenylpropenone derivative is provided to efficiently use as a pharmaceutical composition for preventing or treating a degenerative brain disease; or pharmaceutical composition for protecting a brain cell by having an excellent protecting effect of the brain cell. CONSTITUTION: An alkoxyphenylpropenone derivative or a pharmaceutically acceptable salt thereof is indicated as below chemical formula 1; and R^1 is hydrogen or O-R^4; R^2 is hydrogen or O-R^5; R^3 is hydroxy, O-R^6 or -NR^7R^8; R^4, R^5 and R^6 are C_1-C_12 straight chain or a side chain alkyl, C_2-C_12 straight chain or a side chain alkenyl, and unsubstituted or C_5-C_6 aryl which is substituted as C_1-C_4 straight chain, or a side chain alkoxy, C_5-C_6 aryl C_1-C_4 alkyl; R^7 is hydrogen, C_1-C_4 straight chain, or a side chain alkyl; R^8 is hydrogen, the C_1-C_4 straight chain or the side chain alkyl, and the C5-C6 aryl which is unsubstituted or hydroxy-substituted, the C1-C4 alkyl or the C5-C6.
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Paragraph 0166-0167; 0171-0176
(2021/05/28)
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- Tacrine-ferulic acid-nitric oxide (no) donor trihybrids as potent, multifunctional acetyl- and butyrylcholinesterase inhibitors
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In search of multifunctional cholinesterase inhibitors as potential anti-Alzheimer drug candidates, tacrine-ferulic acid-NO donor trihybrids were synthesized and tested for their cholinesterase inhibitory activities, release of nitric oxide, vasodilator properties, cognition improving potency, and hepatotoxicity. All of the novel target compounds show higher in vitro cholinesterase inhibitory activity than tacrine. Three selected compounds (3a, 3f, and 3k) produce moderate vasorelaxation in vitro, which correlates with the release of nitric oxide. Compared to its non-nitrate dihybrid analogue (3u), the trihybrid 3f exhibits better performance in improving the scopolamine-induced cognition impairment (mice) and, furthermore, less hepatotoxicity than tacrine.
- Chen, Yao,Sun, Jianfei,Fang, Lei,Liu, Mei,Peng, Sixun,Liao, Hong,Lehmann, Jochen,Zhang, Yihua
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scheme or table
p. 4309 - 4321
(2012/07/27)
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