Ginkgetin is a natural biflavonoid compound extracted from Ginkgo biloba leaves, inhibits the Wnt signaling pathway (IC₅₀=5.92μM)[1]. Ginkgetin exhibits multiple pharmacological activities, including anticancer, anti-inflammatory, antimicrobial, antioxidant, and neuroprotective effects[2]. Ginkgetin can be used to treat coronary heart disease, angina pectoris, and hypertension[3-4].
In vitro, co-treatment of A549, NCI-H460, and SPC-A-1 non-small cell lung cancer cells with Ginkgetin (5μM) and Cisplatin (5μM) for 48 hours significantly induces ferroptosis and enhances the cytotoxic effects of Cisplatin[5]. Treatment of ovarian cancer cells A2780, SK-OV-3, and CP70 with Ginkgetin (0.625–80μM) for 24 hours significantly inhibits cell proliferation, induces apoptosis, and reduces cell migration and invasion capabilities[6].
In vivo, intraperitoneal injection of Ginkgetin (5mg/kg) every other day for 2 months in a Doxorubicin (Dox; 10mg/kg)-induced aging C57BL/6J mouse model significantly alleviates aging-related pathological changes in multiple tissues (including kidney, liver, muscle, and spleen) and improves motor function[7]. Oral administration of Ginkgetin (25, 50, 100mg/kg) twice weekly for 8 weeks in ovariectomized (OVX) C57BL/6J mice significantly attenuates bone loss[8].
References:
[1] Ye ZN, Yu MY, Kong LM, et al. Biflavone Ginkgetin, a Novel Wnt Inhibitor, Suppresses the Growth of Medulloblastoma. Nat Prod Bioprospect. 2015 Mar 29;5(2):91–7.
[2] Liu XG, Lu X, Gao W, et al. Structure, synthesis, biosynthesis, and activity of the characteristic compounds from Ginkgo biloba L. Nat Prod Rep. 2022 Mar 23;39(3):474-511.
[3] Xiong B, Lu JJ, Guo H, et al. Ginkgetin from Ginkgo biloba: mechanistic insights into anticancer efficacy. Nat Prod Bioprospect. 2025 Aug 5;15(1):50.
[4] Adnan M, Rasul A, Hussain G, et al. Ginkgetin: A natural biflavone with versatile pharmacological activities. Food Chem Toxicol. 2020 Nov;145:111642.
[5] Lou JS, Zhao LP, Huang ZH, et al. Ginkgetin derived from Ginkgo biloba leaves enhances the therapeutic effect of cisplatin via ferroptosis-mediated disruption of the Nrf2/HO-1 axis in EGFR wild-type non-small-cell lung cancer. Phytomedicine. 2021 Jan;80:153370.
[6] Liu Y, Ye J, Fan Z, et al. Ginkgetin Alleviates Inflammation and Senescence by Targeting STING. Adv Sci (Weinh). 2025 Jan;12(2):e2407222.
[7] Geng Z, Zuo L, Li J, et al. Ginkgetin improved experimental colitis by inhibiting intestinal epithelial cell apoptosis through EGFR/PI3K/AKT signaling. FASEB J. 2024 Jul 31;38(14):e23817.
[8] Wei G, Liang X, Wu F, et al. Ginkgetin attenuates bone loss in OVX mice by inhibiting the NF-κB/IκBα signaling pathway. PeerJ. 2024 Jul 10;12:e17722.
Ginkgetin一种从银杏叶中提取的双黄酮类天然化合物，能够抑制Wnt信号通路（IC₅₀=5.92μM）[1]。Ginkgetin有抗癌、抗炎、抗菌、抗氧化和神经保护等多种药理活性[2]。Ginkgetin可用于治疗冠心病、心绞痛以及高血压等疾病[3-4]。
在体外，Ginkgetin（5μM）与Cisplatin（5μM）联合处理A549、NCI-H460和SPC-A-1非小细胞肺癌细胞48小时，显著诱导铁死亡，同时增强Cisplatin的细胞毒性作用[5]。Ginkgetin（0.625–80μM）处理卵巢癌细胞A2780、SK-OV-3和CP70 24小时，显著抑制细胞增殖并诱导细胞凋亡，同时降低细胞迁移和侵袭能力[6]。
在体内，Ginkgetin（5mg/kg）每隔一天腹腔注射一次，持续2个月，用于处理经Doxorubicin（Dox；10mg/kg）诱导的衰老C57BL/6J小鼠。Ginkgetin显著减轻了多个组织（包括肾脏、肝脏、肌肉和脾脏）的衰老相关病理变化，并改善了小鼠的运动能力[7]。Ginkgetin（25、50、100mg/kg）每周两次口服给药，持续8周，用于处理卵巢切除（OVX）的C57BL/6J小鼠，显著减轻了小鼠的骨丢失[8]。