Kolaviron Inhibition of Aromatase of Breast Cancer, a Step-ahead of Exemestane, Letrozole, and Anastrozole: A Molecular Docking Studies

Abstract

Aromatase is a cytochrome P450 enzyme that synthesizes estrogen from androgen. Estrogen causes the proliferation of cancerous cells. However, inhibition of aromatase has proven to be helpful in the treatment of breast cancer in post-menopausal woman. Aromatase inhibitors (exemestane, letrozole and anastrozole) that are presently being used as first-line treatment of breast cancer have been reported to have side effects. In view of these, we have identified kolaviron a natural anti-aromatase biflavonoid from garcinia kola through molecular docking studies with the help of autodock software, to have the best interaction with amino residues of aromatase (-10.5Kcal/mol) on comparison with the third-generation aromatase inhibitors (exemestane -10.3Kcal/mol, letrozole -8.5 Kcal/mol and anastrozole – 8.2 Kcal/mol). Hence, kolaviron may be a novel and potent compound for the treatment of estrogen receptor positive breast cancer. However, there is need for further confirmation through wet experiment.