Abstract
A library consisting of characterized marine natural products as well as synthetic derivatives was screened for compounds capable of inhibiting the production of hydrogen sulfide (H2S) by cystathionine beta-synthase (CBS). Eight hits were validated and shown to inhibit CBS activity with IC50 values ranging from 83 to 187μM. The majority of hits came from a series of synthetic polyandrocarpamine derivatives. In addition, a modified fluorogenic probe for H2S detection with improved solubility in aqueous solutions is reported.
Keywords:
Fluorogenic probe; Hydrogen sulfide; Inhibitor screen; Sulfur metabolism.
Copyright © 2015 Elsevier Ltd. All rights reserved.
Publication types
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Research Support, N.I.H., Extramural
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Research Support, Non-U.S. Gov't
MeSH terms
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Amines / chemistry*
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Amines / isolation & purification
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Amines / pharmacology
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Animals
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Biological Products / chemistry
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Biological Products / isolation & purification
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Biological Products / pharmacology
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Cystathionine beta-Synthase / antagonists & inhibitors*
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Cystathionine beta-Synthase / metabolism
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Enzyme Inhibitors / chemistry*
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Enzyme Inhibitors / isolation & purification
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Enzyme Inhibitors / pharmacology
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Humans
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Hydrogen Sulfide / analysis
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Hydrogen Sulfide / metabolism*
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Imidazoles / chemistry*
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Imidazoles / isolation & purification
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Imidazoles / pharmacology
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Urochordata / chemistry*
Substances
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Amines
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Biological Products
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Enzyme Inhibitors
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Imidazoles
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polyandrocarpamine A
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polyandrocarpamine B
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Cystathionine beta-Synthase
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Hydrogen Sulfide