Photohuperzine A—A new photoisomer of huperzine A: Structure elucidation, formation kinetics and activity assessment

Marques, Lygia Azevedo; Giera, Martin; Kanter, Frans J. J. de; Niessen, W.M.A.; Lingeman, H.; Irth, H.

doi:10.1016/j.jpba.2010.01.013

Cited by 5 publications

(3 citation statements)

References 20 publications

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“…The AChE activity was determined according to [11] with some modifications: 10 mM stock solutions in MeOH of the isolated degradation products, formed under acidic conditions, were prepared from the purified material and used for further dilutions. The AChE bioactivity assay was measured in a 96-well plate using AChE dissolved in 20 mM Tris-HCl buffer pH 7.5, 2 g/l PEG 6000 and 1 g/l ELISA blocking reagent.…”

Section: Acetylcholinesterase Inhibition Assaymentioning

confidence: 99%

Stability-indicating study of the anti-Alzheimer's drug galantamine hydrobromide

Marques

Maada

Kanter

et al. 2011

Journal of Pharmaceutical and Biomedical Analysis

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Section: Acetylcholinesterase Inhibition Assaymentioning

confidence: 99%

Stability-indicating study of the anti-Alzheimer's drug galantamine hydrobromide

Marques

Maada

Kanter

et al. 2011

Journal of Pharmaceutical and Biomedical Analysis

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“… Structure of huperzine A ( 6 ) and its photodegradation product photohuperzine A (adapted with permission from Marques et al ., 2010b). …”

Section: Huperzine Amentioning

confidence: 99%

“…Marques et al . studied the stability of 6 under irradiation; it was significantly transformed to a new compound called photohuperzine A (Marques et al ., 2010b). Its activity against AChE was found to be 100 times lower when compared with 6 (Ashani et al ., 1992).…”

Section: Huperzine Amentioning

confidence: 99%

Analysis of acetylcholinesterase inhibitors: bioanalysis, degradation and metabolism

Marques¹,

Giera²,

Lingeman³

et al. 2010

Biomedical Chromatography

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Alzheimer's is a neurodegenerative disease. Its symptoms are attributed to a deficiency of cholinergic neurotransmission. The drugs of choice for the treatment of Alzheimer's disease are acetylcholinesterase (AChE) inhibitors. Starting in the 1980's from non-specific AChE inhibitors, the first-generation drugs such as physostigmine, a second generation of more selective and better tolerated products has been developed. Methods to detect and quantify these drugs and their metabolites in biological samples have been developed for analysis in plasma, blood, urine and cerebrospinal fluid. Diverse detection techniques have been used, such as ultraviolet, fluorescence, electrochemical and mass spectrometry. In this review, the methods applied to the analysis of these drugs and their metabolites in different biological matrices are reviewed and discussed. The stability of these drugs in biological matrices and under stress-conditions is also included in the discussion.

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Advances in mass spectrometry-based post-column bioaffinity profiling of mixtures

Kool¹,

Giera²,

Irth³

et al. 2010

Anal Bioanal Chem

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In the screening of complex mixtures, for example combinatorial libraries, natural extracts, and metabolic incubations, different approaches are used for integrated bioaffinity screening. Four major strategies can be used for screening of bioactive mixtures for protein targets—pre-column and post-column off-line, at-line, and on-line strategies. The focus of this review is on recent developments in post-column on-line screening, and the role of mass spectrometry (MS) in these systems. On-line screening systems integrate separation sciences, mass spectrometry, and biochemical methodology, enabling screening for active compounds in complex mixtures. There are three main variants of on-line MS based bioassays: the mass spectrometer is used for ligand identification only; the mass spectrometer is used for both ligand identification and bioassay readout; or MS detection is conducted in parallel with at-line microfractionation with off-line bioaffinity analysis. On the basis of the different fields of application of on-line screening, the principles are explained and their usefulness in the different fields of drug research is critically evaluated. Furthermore, off-line screening is discussed briefly with the on-line and at-line approaches.Schematic view of an on-line bioaffinity analysis or HRS setup with MS based bioassay detection

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Photohuperzine A—A new photoisomer of huperzine A: Structure elucidation, formation kinetics and activity assessment

Cited by 5 publications

References 20 publications

Stability-indicating study of the anti-Alzheimer's drug galantamine hydrobromide

Stability-indicating study of the anti-Alzheimer's drug galantamine hydrobromide

Analysis of acetylcholinesterase inhibitors: bioanalysis, degradation and metabolism

Advances in mass spectrometry-based post-column bioaffinity profiling of mixtures

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