Critical Analysis on Characterization, Systemic Effect, and Therapeutic Potential of Beta-Sitosterol: A Plant-Derived Orphan Phytosterol

The document from 2016 provides a detailed review of beta-sitosterol (BS), a plant-derived phytosterol with a structure similar to cholesterol and a wide range of reported pharmacological effects. It is noted for its antioxidant, antimicrobial, angiogenic, immunomodulatory, antidiabetic, anti-inflammatory, anticancer, and antinociceptive activities, with minimal toxicity. However, the exact functions of BS in plants and its mechanisms of action in humans remain unclear. The review calls for more research to understand BS's cellular and molecular effects in humans and to substantiate claims made by commercial entities. It also discusses BS's sources, properties, analytical methods, synthesis, systemic effects, pharmacokinetics, therapeutic potentials, and toxicity. Despite evidence of beneficial effects in clinical trials, there is a lack of long-term studies and human trials for many of the effects observed in animal models. The document emphasizes the need for further studies to clarify the mechanisms of action, long-term effects, and clinical applications of BS, and it points out the challenges in studying BS due to regulatory agencies often not differentiating between individual phytosterols. The FDA has approved claims of BS's benefits against coronary heart disease, but its efficacy for other conditions like alopecia and BPH requires more convincing long-term data. The document suggests that future research should focus on improving BS's drug delivery and absorptivity and conducting extensive risk-benefit studies.