New derivatives of 11-keto-β-boswellic acid (KBA) induce apoptosis in breast and prostate cancers cells

A series of new 11-keto-beta-boswellic acid were partially-synthesized by modifying the hydroxyl and carboxylic acid functional groups of ring A. The structures of the new analogs were confirmed by detailed spectral data analysis. Compounds 4, 5 and 9 exhibited potent anti-cancer results against two human tumor cancer cell lines having IC50 value of MCF-7 (breast) and LNCaP (prostate): 123.6, 9.6 and 88.94 mu M and 9.6, 44.12 and 12.03 mu M, respectively. Additionally, a maximum nuclear fragmentation was observed for 4 (78.44%) in AKBA treated cells after 24 hr followed by 5 and 9 with (74.25 and 66.9% respectively). This study suggests that the presence of hydrazone functionality (4 and 9) has effectively improved the potency of AKBA. Interestingly, compound 5 with a lost carboxylic acid group of ring A showed comparable potent activity. Highly selective AKBA requires further modification to improve its bioavailability and solubility inside the cancer cells.

Automated summary

A series of new 11-keto-beta-boswellic acid analogs were synthesized by modifying the hydroxyl and carboxylic acid functional groups of ring A, showing potent anti-cancer activity against breast and prostate cancer cell lines. This study suggests that chemical modification of the functional groups in these analogs can effectively enhance their biological activity.