Ginkgo biloba L., an ancient dioecious gymnosperm, is now cultivated worldwide for landscaping and medical purposes. A novel biflavonoid—amentoflavone 7′′-O-β-d-glucopyranoside (1)—and four known biflavonoids were isolated and identified from the male flowers of Ginkgo. The anti-proliferative activities of five biflavonoids were evaluated on different cancer lines. Bilobetin (3) and isoginkgetin (4) exhibited better anti-proliferative activities on different cancer lines. Their effects were found to be cell-specific and in a dose and time dependent manner for the most sensitive HeLa cells. The significant morphological changes validated their anticancer effects in a dose-dependent manner. They were capable of arresting the G2/M phase of the cell cycle, inducing the apoptosis of HeLa cells dose-dependently and activating the proapoptotic protein Bax and the executor caspase-3. Bilobetin (3) could also inhibit the antiapoptotic protein Bcl-2. These might be the mechanism underlying their anti-proliferation. In short, bilobetin (3) and isoginkgetin (4) might be the early lead compounds for new anticancer agents.

Ginkgo biloba L. has always been a popular area of research due to its various active ingredients and pharmacological effects. Ginkgo biloba is rich in ginkgo flavonoids, ginkgolides, and ginkgolic acid, with anti-inflammation, antioxidation, neuroprotection, anti-platelet agglutination, hypolipidemic effect, anti-cancer, and anti-radiation properties. There are many methods to extract and separate the active components of ginkgo. Among them, supercritical carbon dioxide fluid extraction (SFE-CO₂) is known for its green, clean, and environment-friendly properties. In this paper, the pharmacological activities, the active components, and structures of different parts of ginkgo, the extraction methods of its effective ingredients, and the application of the SFE-CO₂ method for the extraction and separation of active ingredients in Ginkgo biloba from leaves, seeds, pollen, and roots were reviewed, in order to make best use of ginkgo resources, and provide support and references for the development of SFE-CO₂ of active components from Ginkgo biloba.

Two new compounds, ardisiapunine B (1) and ardisiapunine C (2), were isolated from Ardisia lindleyana D. Dietr. Their structures were examined using HR–ESI–MS, IR, (1D, 2D) NMR spectroscopic analyses, single–crystal X–ray diffraction, and ECD calculation. It was found that the two new compounds belong to unusual oleanane-type triterpenes, with compound 1 bearing an acetal unit and a C–13–C–18 double bond, and compound 2 bearing a C–28 aldehyde group and a C–18–C–19 double bond. The anti-inflammatory properties of compounds 1 and 2 were tested on NO production and cellular morphology using RAW264.7 cells, and their anti-tumor properties were tested on cytotoxic activities, cellular morphology, cell apoptosis, and cell cycle. The results showed that compound 1 exhibited a potent cytotoxicity against HepG2 cell lines with an IC₅₀ of 12.40 μM. Furthermore, it is possible that compound 1 inhibits cell proliferation by blocking the cell G2/M phase and promoting cell apoptosis. Compound 2 exhibited a potential anti-inflammatory activity by decreasing the production of NO in LPS–stimulated RAW264.7 cells. Comparative analysis of the structures of compounds 1 and 2 revealed that the acetal structure and double bond positions were the main differences between them, and these are presumed to be the main reasons for the extreme differences in their cytotoxicity and anti-inflammatory activities. From these new findings, two promising lead compounds were identified for the future development of potential anti–inflammatory or anti–tumor agents.

Backgrounds: Ginkgo biloba L. has attracted much attention for its unique chemical composition and pharmacological properties, and most of the research focused on Ginkgo biloba leaves (GBL). Our preliminary research found that Ginkgo biloba flowers (GBF) were superior to GBL in terms of anti-radiation activity, but the underlying cause of this discrepancy in activity remains elusive. Objectives: The aim of this study was to systematically compare the chemical and nutritional composition of Ginkgo biloba flowers and leaves, to further elucidate the material basis of the medicinal and nutritional value of Ginkgo biloba flowers, and to conduct further comparative studies on the anti-ferroptosis activity and anti-radiation activity of the two. Methods: In this study, the chemical constituents of GBF and GBL were identified by UPLC-Q-orbitrap HRMS, and the contents of amino acids, fatty acids, inorganic elements, purines, and ceramides of both were determined. Meanwhile, the anti-iron death activity and anti-radiation activity of GBF and GBL were comparatively studied by cellular experiments. Results: The results showed that the content of chemical components such as flavonoids and other nutrients such as amino acids, fatty acids, and ceramides were richer in GBF than in GBL, and GBF was indeed superior to GBL in terms of anti-radiation and anti-ferroptosis activity. Conclusion: Through in-depth analyses of the chemical and nutritional compositions of Ginkgo biloba flowers and leaves, the present study reveals the possible material basis for the stronger activity of GBF and provides theoretical support for its application in nutraceuticals and pharmaceuticals, especially in the development of functional nutraceuticals and anti-radiation drugs with higher health benefits.