Bilobalide 是银杏叶的倍半萜三内酯成分，可抑制 NMDA 诱导的胆碱流出，IC50 值为 2.3 μM。
| Cas No. | 33570-04-6 |
| 别名 | 白果内酯; (-)-Bilobalide |
| Canonical SMILES | O=C1O[C@]([C@]([C@@](C2([H])[H])(C(C([H])([H])[H])(C([H])([H])[H])C([H])([H])[H])O[H])([C@@]3([H])O[H])[C@](C4([H])[H])1[C@@]2([H])OC4=O)([H])OC3=O |
| 分子式 | C15H18O8 |
| 分子量 | 326.3 |
| 溶解度 | ≥ 16.3 mg/mL in DMSO, ≥ 98.2 mg/mL in EtOH with gentle warming |
| 储存条件 | Store at -20℃ |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request |
| 产品描述 | Description:
IC50 Value: 3.33 (pIC50 Value) [1]
Bilobalide is a biologically active terpenic trilactone present in Ginkgo biloba. An increasing number of studies have demonstrated its neuroprotective effects.
in vitro: Inhibition by BB and GB was abolished in mutant receptors containing T6'S and S12'A substitutions, but their potencies were enhanced (42- and 125-fold, respectively) in S2'A mutant receptors [1]. BB enhanced the secretion of α-secretase-cleaved soluble amyloid precursor protein (sAPPα, a by-product of non-amyloidogenic processing of APP) and decreased the β amyloid protein (Aβ, a by-product of amyloidogenic processing of APP) via PI3K-dependent pathway [2].
in vivo: Oral administration of bilobalide (10-30 mg/kg) significantly inhibited thermal hyperalgesia in response to carrageenan, capsaicin and paw incision, independent of dose, with an efficacy similar to that of diclofenac. In the carrageenan model, mechanical hypersensitivity and paw oedema were also significantly reduced after treatment with bilobalide (10-30 mg/kg) [3]. BB(4 and 8 mg/kg) significantly protected VD rats against cognitive deficits in the Morris water maze. Biochemical assessment showed that BB (4 and 8 mg/kg) increased superoxide dismutase (SOD) activity and glutathione (GSH) content, and decreased nitric oxide synthase (NOS) activity and malondialdehyde (MDA) content [4].
Clinical trial: N/A |
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