Abstract
Novel chemotypes with carbonic anhydrase (CA; EC 4.2.1.1) inhibitory action, in addition to the sulphonamide and sulphamate were discovered, many of which are based on natural products. Caffeine and piperine were extracted and tested for inhibition of the human (h) cytosolic isoforms hCA I and II. The IC(50) values of caffeine against hCA I was of 55 mM, whereas that of piperine of 60 mM. The IC(50) values of caffeine and piperine against hCA II were of 2 mM. Although these are quite weak inhibitors they may constitute leads for developing tighter binding compounds.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Alkaloids / chemistry
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Alkaloids / isolation & purification
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Alkaloids / pharmacology*
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Benzodioxoles / chemistry
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Benzodioxoles / isolation & purification
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Benzodioxoles / pharmacology*
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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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Caffeine / chemistry
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Caffeine / isolation & purification
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Caffeine / pharmacology*
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Carbonic Anhydrase I / antagonists & inhibitors*
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Carbonic Anhydrase I / metabolism
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Carbonic Anhydrase II / antagonists & inhibitors*
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Carbonic Anhydrase II / metabolism
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Dose-Response Relationship, Drug
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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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Fruit / chemistry
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Humans
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Piperaceae / chemistry
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Piperidines / chemistry
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Piperidines / isolation & purification
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Piperidines / pharmacology*
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Plant Leaves / chemistry
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Polyunsaturated Alkamides / chemistry
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Polyunsaturated Alkamides / isolation & purification
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Polyunsaturated Alkamides / pharmacology*
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Structure-Activity Relationship
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Theaceae / chemistry
Substances
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Alkaloids
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Benzodioxoles
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Biological Products
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Enzyme Inhibitors
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Piperidines
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Polyunsaturated Alkamides
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Caffeine
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Carbonic Anhydrase I
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Carbonic Anhydrase II
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piperine