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Wichitnithad W O'Callaghan JP Miller DB Train BC Callery PS 《Bioorganic & medicinal chemistry》2011,19(24):7482-7492
A novel class of N-substituted tetrahydropyridine derivatives was found to have multiple kinetic mechanisms of monoamine oxidase A inhibition. Eleven structurally similar tetrahydropyridine derivatives were synthesized and evaluated as inhibitors of MAO-A and MAO-B. The most potent MAO-A inhibitor in the series, 2,4-dichlorophenoxypropyl analog 12, displayed time-dependent mixed noncompetitive inhibition. The inhibition was reversed by dialysis, indicating reversible enzyme inhibition. Evidence that the slow-binding inhibition of MAO-A with 12 involves a covalent bond was gained from stabilizing a covalent reversible intermediate product by reduction with sodium borohydride. The reduced enzyme complex was not reversible by dialysis. The results are consistent with slowly reversible, mechanism-based inhibition. Two tetrahydropyridine analogs that selectively inhibited MAO-A were characterized by kinetic mechanisms differing from the kinetic mechanism of 12. As reversible inhibitors of MAO-A, tetrahydropyridine analogs are at low risk of having an adverse effect of tyramine-induced hypertension. 相似文献
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Chawanphat Muangnoi Ponsiree Jithavech Pahweenvaj Ratnatilaka Na Bhuket Wiwat Supasena Wisut Wichitnithad Pasarapa Towiwat 《Bioscience, biotechnology, and biochemistry》2018,82(8):1301-1308
In this work, a curcumin-diglutaric acid (CurDG) prodrug was synthesized by conjugation of curcumin with glutaric acid via an ester linkage. The water solubility, partition coefficient, release characteristics, and antinociceptive activity of CurDG were compared to those of curcumin. The aqueous solubility of CurDG (7.48 μg/mL) is significantly greater than that of curcumin (0.068 μg/mL). A study in human plasma showed that the CurDG completely releases curcumin within 2 h, suggesting the ability of CurDG to serve as a prodrug of curcumin. A hot plate test in mice showed the highest antinociceptive effect dose of curcumin at 200 mg/kg p.o., whereas CurDG showed the same effect at an effective dose of 100 mg/kg p.o., indicating that CurDG significantly enhanced the antinociceptive effect compared to curcumin. The enhanced antinociceptive effect of CurDG may be due to improved water solubility and increased oral bioavailability compared to curcumin. 相似文献
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Tracing the origin of a cryptic invader: phylogeography of the Euwallacea fornicatus (Coleoptera: Curculionidae: Scolytinae) species complex 下载免费PDF全文
Richard Stouthamer Paul Rugman‐Jones Pham Q. Thu Akif Eskalen Tim Thibault Jiri Hulcr Liang‐Jong Wang Bjarte H. Jordal Chi‐Yu Chen Miriam Cooperband Ching‐Shan Lin Naoto Kamata Sheng‐Shan Lu Hayato Masuya Zvi Mendel Robert Rabaglia Sunisa Sanguansub Hsin‐Hui Shih Wisut Sittichaya Shixiang Zong 《Agricultural and Forest Entomology》2017,19(4):366-375
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