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Isoginkgetin, a natural biflavonoid from Ginkgo biloba, inhibits inflammatory response in endothelial cells via suppressing NF-κB activation

Acta Pharmacologica Sinica volume 46, pages 3396–3398 (2025)Cite this article

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Isoginkgetin (ISOGK), a naturally occurring biflavonoid first isolated from Ginkgo biloba leaves in 1983, is a member of the biflavonoid subclass characterized by two acacetin monomers linked by a 3’-8” carbon-carbon bond to form a dimeric structure [1]. ISOGK exhibits multifunctional bioactivities (including antioxidative and antitumor properties) across various experimental models. Mechanistically, ISOGK activates the nuclear factor erythroid 2-related factor 2/antioxidant response element (NRF2/ARE) pathway, upregulating heme oxygenase-1 (HO-1) and NAD(P)H quinone oxidoreductase 1 (NQO1) expression, which attenuates oxidative damage and enhances mitochondrial bioenergetics in cardiomyocytes, thereby protecting against obesity-induced cardiac dysfunction [2]. In oncology, ISOGK acts as a broad-spectrum spliceosome inhibitor (IC50 ~30 μM), disrupting tumor gene expression and inducing cytotoxic effects [3]. In glioblastoma U87MG cells, ISOGK inhibited cell proliferation in a dose- and time-dependent manner, triggering S-phase cell cycle arrest, and activating both apoptotic and autophagic pathways [4]. Although the anti-inflammatory effects of Ginkgo biloba have been documented [5], the potential anti-inflammatory activity of its biflavonoid constituent ISOGK remains to be elucidated.

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Fig. 1: Isoginkgetin inhibits endothelial inflammation via suppressing NF-κB activation.

Data availability

RAW data of RNA-seq was deposited in Gene Expression Omnibus with accession number: GSE293694.

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Acknowledgements

This study was supported by the National Natural Science Foundation of China (82370444, 12411530127). This work was also supported by the Program for Innovative Research Team of The First Affiliated Hospital of USTC (CXGG02), USTC Research Funds of the Double First-Class Initiative (YD9110002089), and the Research Funds of the Center for Leading Medicine and Advanced Technologies of IHM.

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Author notes

  1. These authors contributed equally: Mei-jie Chen, Zhi-dan Zhang

Authors and Affiliations

  1. Department of Endocrinology, Centre for Leading Medicine and Advanced Technologies of IHM, The First Affiliated Hospital of USTC, Division of Life Sciences and Medicine, University of Science and Technology of China, Hefei, 230001, China

    Mei-jie Chen, Zhi-dan Zhang, Fan-shun Zhang & Suo-wen Xu

  2. William Harvey Research Institute, Barts and The London Faculty of Medicine and Dentistry, Queen Mary University of London, London, UK

    Paul C. Evans

  3. Centre for Cardio-metabolic Research in Africa, Division of Medical Physiology, Faculty of Medicine and Health Sciences, Stellenbosch University, Cape Town, South Africa

    Hans Strijdom

  4. Anhui Provincial Key Laboratory of Metabolic Health and Panvascular Diseases, Hefei, 230001, China

    Suo-wen Xu

Authors
  1. Mei-jie Chen
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  2. Zhi-dan Zhang
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  3. Fan-shun Zhang
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  4. Paul C. Evans
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  6. Suo-wen Xu
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Contributions

MJC, ZDZ, and FSZ designed and performed experiments. ZDZ analyzed the data and wrote the manuscript. PCE, HS, and SWX reviewed and edited the manuscript. SWX conceptualized and supervised the project.

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Correspondence to Suo-wen Xu.

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Chen, Mj., Zhang, Zd., Zhang, Fs. et al. Isoginkgetin, a natural biflavonoid from Ginkgo biloba, inhibits inflammatory response in endothelial cells via suppressing NF-κB activation. Acta Pharmacol Sin 46, 3396–3398 (2025). https://doi.org/10.1038/s41401-025-01612-9

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