Ginkgo biloba L., an ancient medicinal tree with origins tracing back over 280 million years, holds a unique place in both traditional and modern therapeutic systems. Widely used in East Asian ethnomedicine, and increasingly validated by pharmacological research, it serves as a rich source of bioactive compounds like terpene trilactones (ginkgolides, bilobalide), flavonoids (quercetin, kaempferol), alkaloids, proanthocyanidins, alkyl phenols, and organic/phenolic acids. This review provides a critical synthesis of Ginkgo biloba’s traditional uses, phytochemical constituents, and pharmacological activities, and highlights its anti-oxidant, anti-inflammatory, anticancer, neuroprotective, and vasoprotective properties. In addition, recent advances in the structural transformation and semi-synthetic modification of ginkgolides are presented to offer insights into their structure–activity relationships. Beyond therapeutic roles, Ginkgo biloba exhibits notable potential in non-pharmaceutical domains, which include its use as a natural colorant and photoprotective agent in cosmetics, and as a bio-based material in textile dyeing. Through a systematic examination of peer-reviewed literature, this review underscores Ginkgo biloba’s multifaceted value as a promising botanical resource for both medicinal and industrial innovation.
Rather et al. (2025) studied this question.