Bilobalide 是银杏叶中的的一种倍半萜三内酯成分,抑制 NMDA 诱导的胆碱流出,IC50值为 2.3 μM。Bilobalide 通过激活 SH-SY5Y 细胞中的 PI3K/Akt 通路来防止细胞凋亡 (apoptosis)。对神经元发挥保护和营养作用。
生物活性 | Bilobalide, a sesquiterpene trilactone constituent ofGinkgo biloba, inhibits the NMDA-induced efflux of choline with anIC50value of 2.3 μM. Bilobalide preventsapoptosisthrough activation of the PI3K/Akt pathway in SH-SY5Y cells. Exerts protective and trophic effects on neurons[1][2]. |
IC50& Target | Human Endogenous Metabolite |
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体外研究 (In Vitro) | Bilobalide (1-100 μM) completely suppresses the NMDA-evoked release of choline in a concentration-dependent manner with IC50value 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). |
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体内研究 (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. |
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来源 | - Plants
- Ginkgoaceae
- Ginkgo biloba
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运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | Powder | -20°C | 3 years | | 4°C | 2 years | In solvent | -80°C | 6 months | | -20°C | 1 month |
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溶解性数据 | In Vitro: DMSO : ≥ 100 mg/mL(306.47 mM) *"≥" means soluble, but saturation unknown. 配制储备液 1 mM | 3.0647 mL | 15.3233 mL | 30.6466 mL | 5 mM | 0.6129 mL | 3.0647 mL | 6.1293 mL | 10 mM | 0.3065 mL | 1.5323 mL | 3.0647 mL |
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以下溶剂前显示的百 分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂: 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.08 mg/mL (6.37 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (6.37 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂: 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.08 mg/mL (6.37 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (6.37 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。 3. 请依序添加每种溶剂: 10% DMSO 90%corn oil Solubility: ≥ 2.08 mg/mL (6.37 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (6.37 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。 *以上所有助溶剂都可在本网站选购。
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