Research Highlights

doi:10.1038/nindia.2016.58 Published online 26 April 2016

New therapy for heart disease

Researchers have discovered that the triterpenoid arjunolic acid inhibits the activity of carbonic anhydrase II, an enzyme that has been linked to cardiac hypertrophy1. This acid is thus potentially useful for treating heart disease.

Carbonic anhydrase II converts carbon dioxide into bicarbonate and hydrogen ions in various physiological processes. However, this enzyme also play roles in cellular processes that lead to diseases such as cardiac hypertrophy in which heart muscle tissue thickens.

To find a way to stop such enzyme-induced heart damage, the researchers probed the efficiencies of arjunolic acid to block the activity of carbonic anhydrase II in both solutions and mice heart cells and compared them with those for similar triterpenoids.

Of all the triterpenoids tested, arjunolic acid exhibited the maximum efficiency for blocking the enzyme’s activity. In mice heart cells, arjunolic acid inhibited the activity of carbonic anhydrase II by reducing a process known as acidosis in cells. In addition, the acid also reduced the loads of calcium and sodium ions in cells.

These reduced intracellular ion loads also protected vital cellular organelles such as mitochondria, suggesting that arjunolic acid could help prevent cardiac hypertrophy.

This ability to protect cells by increasing levels of antioxidant enzymes makes arjunolic acid a promising compound for designing effective drugs for treating cardiac hypertrophy, the researchers say.


References

1. Kalyanavenkataraman, S. et al. Discovery of arjunolic acid as a novel non-zinc binding carbonic anhydrase II inhibitor. Bioorg. Chem. 66, 72–79 (2016)