Betulin caffeate is primarily investigated for its potential biological and pharmacological applications, especially in the field of anticancer research. It exhibits cytotoxic activity against various cancer cell lines, making it a candidate for development in oncology therapeutics. The compound combines structural features of betulin, a natural triterpene, with caffeic acid, known for its antioxidant properties, resulting in enhanced bioactivity.

It has shown promise in inducing apoptosis and inhibiting proliferation of tumor cells, particularly in studies involving liver, lung, and cervical cancer models. Additionally, due to the presence of caffeic acid moiety, the compound may possess anti-inflammatory and antioxidant effects, which could support its role in protective or adjuvant therapies.

Research is ongoing to improve its solubility and bioavailability for potential use in drug formulations. Betulin caffeate is also explored in cosmeceuticals for its skin-protective properties, leveraging its natural origin and multifunctional activity.