Ginkgolide B
(Synonyms: 银杏内酯 B; 白果苦内酯 B; BN-52021) 目录号 : GN10453
Ginkgolide B是从银杏叶中提取的一种萜内酯，是血小板活化因子（PAF）的特异性拮抗剂, IC50为 3.6μM。
Cas No.:15291-77-7
Sample solution is provided at 25 µL, 10mM.
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Ginkgolide B is a terpene lactone extracted from Ginkgo biloba leaves and is a specific antagonist of platelet activating factor (PAF), with an IC50 of 3.6μM[1]. Platelet activating factor (PAF) is a phospholipid inflammatory mediator that rapidly activates platelets, white blood cells and endothelial cells by binding to PAFR, amplifying inflammatory and thrombotic responses[2]. Ginkgolide B has antioxidant, anti-inflammatory, anti-tumor, and anti-apoptotic activities and is commonly used for research on ischemia/reperfusion injury, neuroinflammation, and tumors[3-5].
In vitro, treatment of Human umbilical vein endothelial cells (HUVECs) with Ginkgolide B (30–300μM; 24h) dose-dependently increased PXR nuclear translocation, upregulated CYP3A4 and MDR1 expression, attenuated doxorubicin- or staurosporine-induced apoptosis, and suppressed TNF-α-induced THP-1 cell adhesion and expression of VCAM-1 and E-selectin[6].
In vivo, in rat model of cerebral ischemia/reperfusion injury, Ginkgolide B(20mg/kg; i.p.; 14days) significantly reduce the volume of cerebral infarction and the neurological deficit score, increased the proportion of nestin-, neuron-specific enolase- and glial fibrillary acid protein-positive cells, increased the mRNA expression of brain-derived neurotrophic factor(BDNF) and epidermal growth factor(EGF), and increased the expression levels of BDNF and suppressor of cytokine signaling 2(SOCS2) in the ischemic penumbra[7]. In pentobarbitone or ethyl carbamate-anaesthetized guinea-pigs, Ginkgolide B (1mg/kg; i.v.; 1h) inhibited bronchoconstriction, the hematocrit increase and the accompanying thrombopenia and leukopenia induced by PAF-acether[8].
References:
[1] Lamant V, Mauco G, Braquet P, Chap H, Douste-Blazy L. Inhibition of the metabolism of platelet activating factor (PAF-acether) by three specific antagonists from Ginkgo biloba. Biochem Pharmacol. 1987;36(17):2749-2752.
[2] Venable ME, Zimmerman GA, McIntyre TM, Prescott SM. Platelet-activating factor: a phospholipid autacoid with diverse actions. J Lipid Res. 1993;34(5):691-702.
[3] Koltai M, Tosaki A, Hosford D, Braquet P. Ginkgolide B protects isolated hearts against arrhythmias induced by ischemia but not reperfusion. Eur J Pharmacol. 1989;164(2):293-302.
[4] Lee CW, Lin HC, Wang BY, et al. Ginkgolide B monotherapy reverses osteoporosis by regulating oxidative stress-mediated bone homeostasis. Free Radic Biol Med. 2021;168:234-246.
[5] Ahlemeyer B, Krieglstein J. Pharmacological studies supporting the therapeutic use of Ginkgo biloba extract for Alzheimer's disease. Pharmacopsychiatry. 2003;36 Suppl 1:S8-S14.
[6] Zhou T, You WT, Ma ZC, et al. Ginkgolide B protects human umbilical vein endothelial cells against xenobiotic injuries via PXR activation. Acta Pharmacol Sin. 2016;37(2):177-186.
[7] Zheng PD, Mungur R, Zhou HJ, Hassan M, Jiang SN, Zheng JS. Ginkgolide B promotes the proliferation and differentiation of neural stem cells following cerebral ischemia/reperfusion injury, both in vivo and in vitro. Neural Regen Res. 2018;13(7):1204-1211.
[8] Desquand S, Touvay C, Randon J, et al. Interference of BN 52021 (ginkgolide B) with the bronchopulmonary effects of PAF-acether in the guinea-pig. Eur J Pharmacol. 1986;127(1-2):83-95.
Ginkgolide B是从银杏叶中提取的一种萜内酯，是血小板活化因子（PAF）的特异性拮抗剂, IC50为3.6μM[1]。 血小板活化因子（PAF）是一种磷脂类炎症介质，通过与PAFR结合迅速激活血小板、白细胞和内皮细胞，放大炎症与血栓反应[2]。Ginkgolide B具有抗氧化、抗炎、抗肿瘤和抗凋亡活性，常用于缺血/再灌注损伤、神经炎症及肿瘤等研究[3-5]。
体外实验中，用Ginkgolide B（30–300μM；24小时）处理人脐静脉内皮细胞（HUVECs），剂量依赖性地增加PXR核转位，上调CYP3A4和MDR1的表达，减轻多柔比星或司他霉素诱导的细胞凋亡，并抑制TNF-α诱导的THP-1细胞黏附以及VCAM-1和E-选择素的表达[6]。
体内实验中，在大鼠脑缺血/再灌注损伤模型中，Ginkgolide B（20mg/kg；腹腔注射；连续14天）显著减少脑梗死体积和神经功能缺损评分，增加巢蛋白、神经特异性烯醇化酶和胶质纤维酸性蛋白阳性细胞的比例，提高脑源性神经营养因子（BDNF）和表皮生长因子（EGF）的mRNA表达水平，并增加缺血半暗带中BDNF和细胞因子信号转导抑制因子2（SOCS2）的表达水平[7]。在用戊巴比妥或乙基卡巴明麻醉的豚鼠中，Ginkgolide B（1mg/kg静脉注射；1小时）抑制了PAF-乙醚诱导的支气管收缩、血细胞比容增加以及伴随的血小板减少和白细胞减少[8]。
| Cell experiment [1]: | |
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Cell lines |
Human umbilical vein endothelial cells |
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Preparation Method |
Human umbilical vein endothelial cells (HUVECs) were cultured in RPMI-1640 supplemented with 10% (v/v) FBS and grown in a humidified incubator containing 5% CO2 at 37°C. Ginkgolide B or RIF was dissolved in DMSO and diluted with RPMI-1640. The final concentration of DMSO never exceeded 1‰ of the total culture volume. The cells were seeded in 6-, 12-, or 24-well culture plates for each experiment and treated with various concentrations(30–300μM) of ginkgolide B for 24h. Then cells were collected for further analyses. |
|
Reaction Conditions |
30–300μM; 24h |
|
Applications |
Ginkgolide B dose-dependently increased PXR nuclear translocation, upregulated CYP3A4 and MDR1 expression, attenuated doxorubicin- or staurosporine-induced apoptosis, and suppressed TNF-α-induced THP-1 cell adhesion and expression of VCAM-1 and E-selectin. |
| Animal experiment [2]: | |
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Animal models |
Sprague-Dawley rats |
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Preparation Method |
A total of 150 male clean healthy Sprague-Dawley rats, weighing 250–280g and aged 8 weeks were randomly assigned to three groups: sham, middle cerebral artery occlusion (MCAO) and MCAO + Ginkgolide B (n = 50 per group). A cerebral ischemia/reperfusion model was established. In brief, a 4-0 monofilament nylon thread was inserted into the right common carotid artery to obstruct the middle cerebral artery (MCA) for 90 minutes, and then the thread was withdrawn. In the sham group, the thread was inserted into the right common carotid artery without reaching the bifurcation between the MCA and anterior cerebral artery. Ginkgolide B at 20mg/kg was intraperitoneally administered immediately and 6 hours after ischemia, and thereafter once daily. In the sham and MCAO groups, an equal volume of normal saline (2mL) was intraperitoneally administered with the same schedule. In each group, rats received intraperitoneal injection of bromodeoxyuridine (BrdU) at 50mg/kg three times (once every 4 hours) within 12 hours. Then, 4 hours after the last injection of BrdU, the rats were sacrificed for assessing the proliferation of NSCs. At 3, 7 and 14 days after surgery, neurological function was evaluated (n=5 per time point for each of the three groups). These rats were then sacrificed for immunohistochemistry, real-time quantitative polymerase chain reaction (RT-PCR) and western blot assay (n=5 per group, for a total of 45 rats for each of the three assays). |
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Dosage form |
20mg/kg/day for 14 days; i.p. |
|
Applications |
Ginkgolide B significantly reduce the volume of cerebral infarction and the neurological deficit score. |
|
References: |
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| Cas No. | 15291-77-7 | SDF | |
| 别名 | 银杏内酯 B; 白果苦内酯 B; BN-52021 | ||
| Canonical SMILES | O=C1O[C@@]2([H])C([C@@]([C@]([C@@]3([H])OC4=O)([C@]4([H])C([H])([H])[H])O[H])1O[C@]5([H])OC6=O)(C3([H])O[H])C5([C@@]6([H])O[H])C(C(C([H])([H])[H])(C([H])([H])[H])C([H])([H])[H])([H])C2([H])[H] | ||
| 分子式 | C20H24O10 | 分子量 | 424.4 |
| 溶解度 | DMF: 25 mg/ml,DMF:PBS(pH 7.2)(1:1): 0.5 mg/ml,DMSO: 14 mg/ml | 储存条件 | Store at 2-8°C Dry, sealed and protect from light |
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.3563 mL | 11.7813 mL | 23.5627 mL |
| 5 mM | 0.4713 mL | 2.3563 mL | 4.7125 mL |
| 10 mM | 0.2356 mL | 1.1781 mL | 2.3563 mL |
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