Carbonic anhydrase I and II inhibition with natural products: caffeine and piperine

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 IC₅₀ values of caffeine against hCA I was of 55 mM, whereas that of piperine of 60 mM. The IC₅₀ 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.

Keywords::

• Carbonic anhydrase
• enzyme inhibitor
• natural product
• caffeine
• piperine

Acknowledgements

This work is acknowledged to our Principal and Dean Dr. P. Suresh GITAM Institute of Pharmacy, GITAM University, Visakhapatnam who has given all the opportunity of laboratory and instruments. The authors are greatly indebted to Dr. C. T. Supuran for the enzyme assay.

Declaration of interest

The authors report no conflict of interest. The authors alone are responsible for the content and writing of the article.