Biological Activity of Oleanolic Acid Derivatives HIMOXOL and Br-HIMOLID in Breast Cancer Cells Is Mediated by ER and EGFR

Breast cancer is one of the most frequently observed malignancies worldwide and represents a heterogeneous group of cancers. For this reason, it is crucial to properly diagnose every single case so a specific and efficient therapy can be adjusted. One of the most critical diagnostic parameters evaluated in cancer tissue is the status of the estrogen receptor (ER) and epidermal growth factor receptor (EGFR). Interestingly, the expression of the indicated receptors may be used in a personalized therapy approach. Importantly, the promising role of phytochemicals in the modulation of pathways controlled by ER and EGFR was also demonstrated in several types of cancer. One such biologically active compound is oleanolic acid, but due to poor water solubility and cell membrane permeability that limits its use, alternative derivative compounds were developed. These are HIMOXOL and Br-HIMOLID, which were demonstrated to be capable of inducing apoptosis and autophagy or diminishing the migratory and invasive potential of breast cancer cells in vitro. In our study, we revealed that proliferation, cell cycle, apoptosis, autophagy, and also the migratory potential of HIMOXOL and Br-HIMOLID in breast cancer cells are mediated by ER (MCF7) and EGFR (MDA-MB-231) receptors. These observations make the studied compounds interesting in the context of anticancer strategies.

Automated summary

Breast cancer is a diverse malignancy that requires accurate diagnosis for personalized and efficient therapy. The status of estrogen receptor (ER) and epidermal growth factor receptor (EGFR) is crucial in cancer diagnosis. Phytochemicals, such as oleanolic acid, have shown promise in modulating ER- and EGFR-controlled pathways in various cancers. Derivative compounds HIMOXOL and Br-HIMOLID have demonstrated apoptotic, autophagic, and anti-migratory effects in breast cancer cells. Our study reveals the involvement of ER and EGFR receptors in the effects of HIMOXOL and Br-HIMOLID, making them potential candidates for anticancer strategies.