Preparation, purification and pharmacological effects of the ginkgolide B: A review

Ginkgolide B (GB), a unique cage-structured diterpenoid lactone from Ginkgo biloba, exerts potent multi-target pharmacological effects (anti-platelet aggregation, anti-inflammation, antioxidant, anti-apoptosis, ferroptosis-inhibiting) with high safety, holding great promise for treating complex diseases such as cardio-cerebrovascular and neurodegenerative disorders. However, its clinical translation and industrialization are severely hindered by inherent bottlenecks, namely low oral bioavailability, poor blood-brain barrier penetration, and extremely low natural extraction yield. Distinct from existing fragmented reviews, this work focuses on constructing an integrated framework of from structure-activity relationship and preparation/purification technology to pharmacological mechanism and clinical transformation strategy. It systematically summarizes the structural basis of multi-pathway synergistic effects centered on platelet-activating factor receptor (PAFR) antagonism, compares the advantages and limitations of extraction, biosynthesis and chemical synthesis technologies, and clarifies the core molecular mechanisms of its pharmacological activities through in vitro/in vivo evidence. Key conclusions highlight that novel formulation strategies, rational structural modification, and standardized experimental protocols are critical to overcoming GB's defects. This review provides novel insights for clinical translation: guiding the development of brain-targeted or organ-specific delivery systems, offering structural guidance for high-bioavailability derivatives, and establishing a standardized research system to reduce inter-study heterogeneity. Ultimately, it bridges the gap between basic research and clinical application, laying a foundational reference for GB's rational utilization in precision medicine and the development of novel GB-based therapeutics.