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.
| 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 |
| Molecular Weight | 566.51 |
| Formula | C32H22O10 |
| CAS Number | 481-46-9 |
| Solubility (25°C) | DMSO ≥ 20 mg/mL |
| Storage | 2-8°C, dry, sealed |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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