Design, Synthesis, and Biological Evaluation of Curcumin--sitosterol Conjugate a Potential Candidate for Breast Cancer Therapy

Abstract

In this study, a novel steroidal conjugate was prepared via a convenient click chemistry technique. -sitosterol (BS), a widely distributed phytosterol throughout the plant kingdom, was chosen as a steroidal component. It is known that BS uses in the stabilization of cell membranes and has beneficial effects in different diseases. On the other hand, curcumin (CUR), a phenolic compound, was used as a phytochemical agent with a variety of biological activities. The steroidal conjugate (BS-CUR) was achieved in high yield using azide-alkyne cyclization reaction. The structure of BS-CUR was elucidated by using FTIR, NMR, HRMS, and fluorescence spectroscopy techniques. In vitro cytotoxicity assays of the BS-CUR conjugate were evaluated against human breast cancer (MDA-MB-231) and healthy mouse fibroblast cell line (L929), respectively. The preliminary evaluation indicated that BS conjugate exhibited good cytotoxicity compare with the native compounds, CUR and BS. The BS-CUR conjugate could be considered a potential compound for further design and synthesis of highly effective anticancer agents.