The Ginkgo biloba L. (GB) contains high bioactive compounds. To date, flavonoids and terpene trilactone have received the majority of attention in GB studies, and the GB has been utilized globally in functional food and pharmacological firms, with sales > $10 billion since 2017, while the other active components, for instance, polyprenols (a natural lipid) with various bioactivities have received less attention. Hence, this review focused on polyprenols' chemistry (synthesis of polyprenols and their derivatives) extraction, purification, and bioactivities from GB for the first time. The various extractions and purification methods (nano silica-based adsorbent, bulk ionic liquid membrane, etc.) were delved into, and their advantages and limitations were discussed. Besides, numerous bioactivities of the extracted Ginkgo biloba polyprenols (GBP) were reviewed. The review showed that GB contains some polyprenols in acetic esters' form. Prenylacetic esters are free of adverse effects. Besides, the polyprenols from GB have numerous bioactivities such as anti-bacterial, anti-cancer, anti-viral activity, etc. The application of GBPs in the food, cosmetics, and drugs industries such as micelles, liposomes, and nano-emulsions was delved into. Finally, the toxicity of polyprenol was reviewed, and it was concluded that GBP was not carcinogenic, teratogenic, or mutagenic, giving a theoretical justification for using GBP as a raw material for functional foods. This article will aid researchers to better understand the need to explore GBP usage.
