Synthesis and anti-cancer activity of acetals of arjunolic acid

Abstract

Arjunolic acid (AA) is a pentacyclic triterpene acid with various potent biological activities. In this work, arjunolic acid was isolated from the heartwood of Terminalia arjuna, and a series of novel arjunolic acid acetals were synthesized and characterized. The anti-cancer activity of the synthesized acetals was investigated against sixty cell lines from nine different types of cancers at the National Cancer Institute (NCI). Compounds AA-2, AA-4, AA-9, and AA-18 demonstrated significant activity against colon cancer. These compounds were selected for further studies against murine colon cancer cell line CT-26. Mechanistic studies of the most active compound AA-9 on CT-26 cells revealed cell cycle arrest in the G₂/M phase, which induces ROS generation in cells, leading to cell death. Additionally, compound AA-9 showed better selectivity for tumour cells and non-tumour cells.