Ginkgetin

Biological Activity

Ginkgetin is a natural biflavonoid isolated from leaves of Ginkgo biloba L. with effects of anti-inflammation and anticancer activity. Ginkgetin inhibits COX-2 dependent phases of prostaglandin D(2) (PGD(2)) generation in bone marrow-derived mast cells (BMMC) in a concentration-dependent manner with IC(50) values of 0.75 microM. Ginkgetin consistently inhibited the production of leukotriene C(4) (LTC(4)) in a dose dependent manner, with an IC(50) value of 0.33 microM. Ginkgetin also inhibited degranulation reaction in a dose dependent manner, with an IC(50) value of 6.52 microM. Ginkgetin is also a potent inhibitor of Wnt signaling, with an IC50 of 5.92 μΜ.

In vivo, Ginkgetin inhibited tumor growth in xenografted nude mice and down-regulated p-STAT3Tyr705 and survivin in tumor tissues. At total doses of 1,000 microg/site on the dorsal skin (15 mm x 15 mm), ginkgetin inhibited prostaglandin E2 production by 65.6 % along with a marked suppression of COX-2 induction.

Protocol (for reference only)

Cell Experiment
Cell lines	Daoy and D283 cell lines
Preparation method	Cell Viability Assay Daoy and D283 cells were treated with Ginkgetin for 48 h. Cell viability was detected by MTS assay and represented with relative viability versus control. The calculated IC50 values were 14.65 ± 0.07 and 15.81 ± 0.57 μM, towards Daoy and D283 cells respectively.
Concentrations	2.5, 5, 10, 20 μM
Incubation time	48 hours

Animal Experiment
Animal models	Male Sprague-Dawley rats (200-220 g)
Formulation	vehicle (0.9% (w/v) NaCl solution)
Dosages	25, 50, 100 mg/kg
Administration	i.p. 2 hours after the onset of ischemia

Chemical Information

Molecular Weight	566.51
Formula	C32H22O10
CAS Number	481-46-9
Solubility (25°C)	DMSO ≥ 20 mg/mL
Storage	2-8°C, dry, sealed

References

[1] Qin Li, et al. Biosci Biotechnol Biochem . Ginkgetin exerts anti-inflammatory effects on cerebral ischemia/reperfusion-induced injury in a rat model via the TLR4/NF-κB signaling pathway

[2] Yoon Jung Jeon, et al. Cancer Sci. Ginkgetin Inhibits the Growth of DU-145 Prostate Cancer Cells Through Inhibition of Signal Transducer and Activator of Transcription 3 Activity

[3] Ok Heui You, et al. Bioorg Med Chem Lett. Ginkgetin Induces Apoptosis via Activation of Caspase and Inhibition of Survival Genes in PC-3 Prostate Cancer Cells

[4] Jong Keun Son, et al. Biol Pharm Bull. Ginkgetin, a Biflavone From Ginko Biloba Leaves, Inhibits cyclooxygenases-2 and 5-lipoxygenase in Mouse Bone Marrow-Derived Mast Cells