Pakistan Journal of Pharmaceutical Sciences

Abstract: Background: Notoginseng Radix et Rhizoma (NRR), derived from Panax notoginseng, serves as both a functional food and a key medicinal material in traditional Chinese medicine. Its bioactivity is largely attributed to saponins, which undergo significant chemical transformations during processing (e.g., steaming), altering its pharmacological profile. Objective: This review aims to systematically consolidate experimentally verified metabolites from authenticated NRR, elucidate the chemical transformations induced by processing and clarify the resulting shift in pharmacological effects, thereby providing a scientific basis for its targeted application. Method: A comprehensive literature search was conducted using CNKI, Wanfang Data, National Science and Technology Library, the Pharmacopoeia of the People’s Republic of China, PubMed and Web of Science. Keywords included Panax notoginseng (Burk.) F. H. Chen; Pharmacological activities; Phytochemisity; Saponin transformation; Traditional processing; Traditional Chinese medicine. Data were also sourced from classic texts, dissertations and unpublished materials. Results: Processing, particularly steaming, converts high-polarity saponins into less polar ones via deglycosylation, dehydration and hydroxylation. This chemical shift underlies a functional transition: raw NRR primarily promotes blood activation and stasis dispersion, while processed NRR exhibits enhanced blood-nourishing, antioxidant, anti-inflammatory and immunomodulatory activities. Conclusion: The integration of ethnopharmacological knowledge with modern scientific perspectives clarifies the metabolite pathways and mechanistic basis for processing-induced changes in NRR. This review provides a reliable foundation for the precise use and further development of NRR in functional foods, nutraceuticals and evidence-based therapy.