Systematic review evaluates asperosaponin VI metabolism, processing effects, and biological activities.

The purpose of this review is to systematically categorize and critically evaluate the chemical metabolites, processing methods, and pharmacological effects of the core active ingredient asperosaponin VI (ASD VI) sourced from Dipsacus asper. By following the principles of systematic review and best practices of ethnopharmacology, we analyzed available literature up to the year 2025. The results indicate that more than one hundred metabolites have been identified and reported in D. asper, including triterpenoid saponins, iridoids, phenolic acids, and alkaloids, among which ASD VI is the main active marker. Traditional wine-frying, salt-frying, and sweating processes have been known to significantly elevate the content and dissolution rate of ASD VI through biological transformations or physical and chemical changes, which enhance its effects of strengthening bones, tonifying the kidney, and hemostasis. ASD VI itself exhibits multiple pharmacological activities, such as promoting bone formation, offering neuroprotection, improving metabolic liver disease, enhancing myocardial protection, and preventing miscarriage. Its roles involve regulation of key signaling pathways like BMP/Smad, Wnt/β-catenin, and PI3K/AKT. However, our critical analysis reveals that current research efforts have some common limitations like the use of single model approaches, mechanisms mostly being evaluated at the correlation level, and missing data regarding the critical pharmacokinetics and clinical transformations. As a pilot effort, we systematically review the chemical composition, processing modifications, and component pharmacology of D. asperoides within a common framework that not only integrates existing knowledge but also reveals the core scientific bottlenecks from traditional experience to modern drug development; this is expected to provide a clear roadmap for in-depth research and development of ASD VI in the future.