Demethylzeylasteral is primarily studied for its potential anti-cancer properties, particularly in inhibiting the growth and spread of tumor cells. It has shown activity in inducing apoptosis and suppressing metastasis in various cancer cell lines, including liver, breast, colorectal, and lung cancers. The compound also exhibits anti-inflammatory effects by modulating key signaling pathways such as NF-κB and MAPK, including inhibition of inflammatory mediators like cytokines and prostaglandins. It helps reduce symptoms in chronic inflammation models, such as rheumatoid arthritis.

Due to these properties, it is being explored as a candidate for adjuvant cancer therapy. Additionally, demethylzeylasteral may support immune regulation and has been investigated for use in autoimmune and inflammatory conditions.

Furthermore, it has neuroprotective potential, which may be useful in developing treatments for neurological disorders such as Alzheimer's disease, by reducing oxidative stress and inflammation in the brain.

Most research remains in preclinical stages, focusing on its mechanism of action and therapeutic potential, and it is not yet widely used in clinical settings.