Pennogenin 3-O-α-L-rhamnopyranosyl-(1→2)-[α-L-rhamnopyranosyl-(1→4)]-β-D-glucopyranoside is a steroidal saponin glycoside studied for its diverse biological activities. It exhibits potential anti-inflammatory and immunomodulatory properties, with applications in promoting collagen synthesis for skincare and wound healing. This compound is investigated in herbal medicine formulations, derived from plants traditionally used to treat respiratory and autoimmune conditions. Additionally, it shows anti-cancer effects by inhibiting the growth of certain cancer cells through induction of apoptosis. Research also indicates hypoglycemic activity, reducing blood sugar levels in animal models, and the ability to inhibit enzymes involved in oxidative stress. These properties suggest its potential as a lead compound for developing therapeutic agents targeting chronic diseases such as cancer, diabetes, and inflammatory disorders.