| CAS |
No.33570-04-6 |
| 中文名称 |
白果内酯 |
| 英文名称 |
Bilobalide |
| 别名 |
银杏内酯;(-)-Bilobalide |
| 分子式 |
C15H18O8 |
| 分子量 |
326.3 |
| 溶解性 |
Soluble in DMSO |
| 纯度 |
HPLC≥98% |
| 外观(性状) |
White to off-white Solid |
| 储存条件 |
Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year |
| MDL |
MFCD00132880 |
| SMILES |
O=C(O1)C[C@@]2([C@]1([H])C[C@]3(C(C)(C)C)O)[C@@]34[C@](OC([C@@H]4O)=O)([H])OC2=O |
| InChIKey |
MOLPUWBMSBJXER-YDGSQGCISA-N |
| InChI |
InChI=1S/C15H18O8/c1-12(2,3)14(20)4-6-13(5-7(16)21-6)10(19)23-11-15(13,14)8(17)9(18)22-11/h6,8,11,17,20H,4-5H2,1-3H3/t6-,8-,11-,13-,14+,15+/m0/s1 |
| PubChem CID |
73581 |
| 靶点 |
Others |
| 通路 |
Others |
| 背景说明 |
Bilobalide是存在于银杏中的生物活性物,具有神经保护活性。 |
| 生物活性 |
Bilobalide， a sesquiterpene trilactone constituent of Ginkgo biloba， inhibits the NMDA-induced efflux of choline with an IC50 value of 2.3 μM. Bilobalide prevents apoptosis through activation of the PI3K/Akt pathway in SH-SY5Y cells. Exerts protective and trophic effects on neurons[1][2]. |
| In Vitro |
Bilobalide (1-100 μM) completely suppresses the NMDA-evoked release of choline in a concentration-dependent manner with IC50 value of 2.3 μM[1].Bilobalide (1， 5 and 10 μM) alone for 24 h does not affect cell viability of SH-SY5Y cells. Pre-treatment of cells with Bilobalide concentration-dependently prevents Aβ 1-42-， H2O2- and serum deprivation-induced decrease of cell viability， with the best protective effect obtained at 10 μM[2].Bilobalide (5 and 10 μM; 24 h) treatment dose-dependently increases levels of p-Akt (Ser473 and Thr308) in SH-SY5Y cells[2].Western Blot Analysis：Cell Line:SH-SY5Y cells；Concentration: 5 and 10 μM；Incubation Time:24 hours；Result:Induced a significant increase in levels of p-Akt (Ser473 and Thr308). |
| In Vivo |
Bilobalide (20 mg/kg) completely suppresses the NMDA-induced release of choline in vivo while basal choline levels were not significantly affected. NMDA causes a release of choline in vivo when infused into the hippocampus of freely moving rats by retrograde dialysis. Bilobalide (20 mg/kg i.p.) completely inhibits the effect induced by NMDA[1].Animal Model: Male Wistar rats (250-350 g)[1]；Dosage: 20 mg/kg；Administration:I.p. injection 60 min before NMDA infusion；Result:Lowered basal choline efflux only slightly (by 7%) but fully antagonized the NMDA-induced increase of choline release. The convulsive effect of NMDA was almost completely suppressed. |
| 数据来源文献 |
[1]. O Weichel， et al. Bilobalide， a constituent of Ginkgo biloba， inhibits NMDA-induced phospholipase A2 activation and phospholipid breakdown in rat hippocampus. Naunyn Schmiedebergs Arch Pharmacol. 1999 Dec;360(6):609-15.
[2]. Chun Shi， et al. Bilobalide prevents apoptosis through activation of the PI3K/Akt pathway in SH-SY5Y cells. Apoptosis. 2010 Jun;15(6):715-27. |
| 规格 |
5mg 10mg 50mg 100mg |
| 单位 |
瓶 |
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英语
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