Hydrolysis

Publication Title: 
Journal of Separation Science

A RP-HPLC method for determining fourteen components (gallic acid, chebulic acid, 1,6-di-O-galloyl-D-glucose, punicalagin, 3,4,6-tri-O-galloyl-D-glucose, casuarinin, chebulanin, corilagin, neochebulinic acid, terchebulin, ellagic acid, chebulagic acid, chebulinic acid, and 1,2,3,4,6-penta-O-galloyl-D-glucose) in the fruit of Terminalia chebula Retz. is described. The separation was achieved within 80 min using a binary gradient with mobile phases consisting of a pH 2.7 phosphoric acid solution and an 80% CH3CN solution.

Author(s): 
Juang, Lih-Jeng
Sheu, Shuenn-Jyi
Lin, Ta-Chen
Publication Title: 
Journal of Neuroscience Methods

Methylation and other covalent modifications of nucleosome core histones are key regulators of chromatin structure and function, including epigenetic control of gene expression. For the human brain, however, very little is known about the regulation of histone modifications at specific genomic loci. Furthermore, chromatin immunoprecipitation protocols applicable to postmortem tissue are lacking, and the impact of potential confounds such as autolysis time or tissue pH is unknown.

Author(s): 
Huang, Hsien-Sung
Matevossian, Anouch
Jiang, Yan
Akbarian, Schahram
Publication Title: 
Bioorganic & Medicinal Chemistry Letters

Two new GABA derivatives, 1 and 2, were synthesized and tested for their capacity to display CNS activity, which was assessed by determining the effects on the duration of pentobarbital-induced hypnosis in rats. Compound 1, peripherally injected, significantly prolonged the hypnosis time, a typical GABA-mimetic effect, while both intracerebroventricular and intravenous administration of compound 2 surprisingly shortened the hypnotic effect in an atropine-sensitive way. The study was extended also to compounds 1a, 1b and 2a, putative oxidative/hydrolytic metabolites of 1 and 2.

Author(s): 
Carelli, Vincenzo
Liberatore, Felice
Scipione, Luigi
Giorgioni, Gianfabio
Di Stefano, Antonio
Impicciatore, Mariannina
Ballabeni, Vigilio
Calcina, Francesco
Magnanini, Francesca
Barocelli, Elisabetta
Publication Title: 
Drug Metabolism and Disposition: The Biological Fate of Chemicals

beta-Artemether (AM), the O-methyl ether prodrug of dihydroartemisinin (DHA), is an endoperoxide antimalarial. The biliary metabolites of AM in adult male Wistar rats were characterized with particular reference to potential antimalarial compounds and stable derivatives of free radical intermediates. [13-(14)C]-AM (35 micromol kg(-1), i.v.) was administered to anesthetized rats. Within 0 to 3 h, 38.6 +/- 4.8% (mean +/- S.D., n = 6) of the radiolabel was recovered in bile; the 0- to 5-h recovery was 42.3 +/- 4.3%.

Author(s): 
Maggs, J. L.
Bishop, L. P.
Edwards, G.
O'Neill, P. M.
Ward, S. A.
Winstanley, P. A.
Park, B. K.
Publication Title: 
Chemical & Pharmaceutical Bulletin

Bioactivity-guided purification of n-BuOH soluble fraction from the ethanol extract of Evolvulus alsinoides resulted in the isolation of two new compounds, 2,3,4-trihydroxy-3-methylbutyl 3-[3-hydroxy-4-(2,3,4-trihydroxy-2-methylbutoxy)-phenyl]-2-propenoate (1) and 1,3-di-O-caffeoyl quinic acid methyl ester (2) along with six known compounds, caffeic acid (3), 6-methoxy-7-O-beta-glucopyranoside coumarin (4), 2-C-methyl erythritol (5), kaempferol-7-O-beta-glucopyranoside (6), kaempferol-3-O-beta-glucopyranoside (7) and quecetine-3-O-beta-glucopyranoside (8).

Author(s): 
Gupta, Prasoon
Akanksha, null
Siripurapu, Kiran Babu
Ahmad, Ausaf
Palit, Gautam
Arora, Ashish
Maurya, Rakesh
Publication Title: 
Chemical & Pharmaceutical Bulletin

Bioactivity-guided purification of n-BuOH soluble fraction from the ethanol extract of Evolvulus alsinoides resulted in the isolation of two new compounds, 2,3,4-trihydroxy-3-methylbutyl 3-[3-hydroxy-4-(2,3,4-trihydroxy-2-methylbutoxy)-phenyl]-2-propenoate (1) and 1,3-di-O-caffeoyl quinic acid methyl ester (2) along with six known compounds, caffeic acid (3), 6-methoxy-7-O-beta-glucopyranoside coumarin (4), 2-C-methyl erythritol (5), kaempferol-7-O-beta-glucopyranoside (6), kaempferol-3-O-beta-glucopyranoside (7) and quecetine-3-O-beta-glucopyranoside (8).

Author(s): 
Gupta, Prasoon
Akanksha, null
Siripurapu, Kiran Babu
Ahmad, Ausaf
Palit, Gautam
Arora, Ashish
Maurya, Rakesh
Publication Title: 
Drug Metabolism and Disposition: The Biological Fate of Chemicals

The purpose of present study was to determine the intestinal absorption and metabolism of genistein and its analogs to better understand the mechanisms responsible for their low oral bioavailability. The Caco-2 cell culture model and a perfused rat intestinal model were used for the study. In both models, permeabilities of aglycones (e.g., genistein) were comparable to well absorbed compounds, such as testosterone and propranolol.

Author(s): 
Liu, Yan
Hu, Ming
Publication Title: 
The Journal of Pharmacology and Experimental Therapeutics

Aspirin (acetylsalicylic acid) and clopidogrel are two major antithrombogenic agents that are widely used for the treatment and prevention of cerebro- and cardiovascular conditions such as stroke. Combined use produces enhanced therapeutic effect. Aspirin and clopidogrel both are esters, and hydrolysis leads to decreased or inactivated therapeutic activity. The aim of the study was to determine whether aspirin and clopidogrel are hydrolyzed by the same enzyme(s), thus reciprocally prolonging the antithrombogenic activity.

Author(s): 
Tang, Man
Mukundan, Madhu
Yang, Jian
Charpentier, Nathan
LeCluyse, Edward L.
Black, Chris
Yang, Dongfang
Shi, Deshi
Yan, Bingfang
Publication Title: 
The Journal of Pharmacology and Experimental Therapeutics

Oseltamivir is the main medicine recommended by the World Health Organization in anticipation of next influenza pandemic. This anti-influenza viral agent is an ester prodrug, and the antiviral activity is achieved by its hydrolytic metabolite: oseltamivir carboxylate. In this study, we report that the hydrolytic activation is catalyzed by carboxylesterase human carboxylesterase (HCE) 1. Liver microsomes rapidly hydrolyzed oseltamivir, but no hydrolysis was detected with intestinal microsomes or plasma.

Author(s): 
Shi, Deshi
Yang, Jian
Yang, Dongfang
LeCluyse, Edward L.
Black, Chris
You, Li
Akhlaghi, Fatemeh
Yan, Bingfang
Publication Title: 
Molecular Vision

PURPOSE: The purpose was to characterize the properties of a proteinase activity associated with betaA3-crystallin, which was isolated from the alpha-crystallin fraction of human lenses. METHODS: An inactive, Arg-bond hydrolyzing proteinase in the alpha-crystallin fraction, which was isolated from the water soluble (WS) protein fraction of 60- to 70-year-old human lenses, was activated by sodium deoxycholate treatment.

Author(s): 
Srivastava, O. P.
Srivastava, K.
Chaves, J. M.

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