三七皂苷Ft1(Notoginsenoside Ft1)是植

Notoginsenoside Ft1  (Synonyms: 三七皂苷FT1)

三七皂苷Ft1(Notoginsenoside Ft1)是植物分离三七皂苷，刺激血管生成。

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生物活性    
Notoginsenoside Ft1 is a saponin isolated from Panax notoginseng; stimulator of angiogenesis. IC50 value: Target: angiogenesis stimulator in vitro: Ft1 increases translocalization of hypoxia-inducible factor-1α (HIF-1α) from cytoplasm to nuclei, where it binds to the vascular endothelial growth factor (VEGF) promoter, increasing the expression of VEGF mRNA and the subsequent secretion of the growth factor. Ft1 induces the activation of PI3K/AKT and Raf/MEK/ERK signaling pathways [1]. Among the saponins examined, Ft1 was the most potent procoagulant and induced dose-dependent platelet aggregation. Ft1 reduced plasma coagulation indexes, decreased tail bleeding time and increased thrombogenesis. Moreover, it potentiated ADP-induced platelet aggregation and increased cytosolic Ca(2+) accumulation, effects that were attenuated by clopidogrel. Ft1 binds to platelet P2Y12 receptors. The increase in intracellular Ca(2+) evoked by Ft1 in HEK293 cells overexpressing P2Y12 receptors could be blocked by ticagrelor [2]. Ft1 caused endothelium-dependent relaxations, which were abolished by l-NAME (inhibitor of nitric oxide synthases) and ODQ (inhibitor of soluble guanylyl cyclase). Ft1 increased the cGMP level in rat mesenteric arteries. GR and ER were present in the endothelial layer and their antagonism by RU486 and PHTPP, respectively, inhibited Ft1-induced endothelium-dependent relaxations and phosphorylations of eNOS, Akt and ERK1/2 [3]. Ft1 showed the best inhibitory effect on cell proliferation of SH-SY5Y cells with IC50 of 45μM. Ft1 not only arrested the cell cycle at S, G2/M stages, but also promoted cell apoptosis. Ft1 up-regulated the protein expressions of cleaved caspase 3, phospho-p53, p21, and cyclin B1, but down-regulated that of Bcl-2. Moreover, Ft1 enhanced the phosphorylation of ERK1/2, JNK and p38 MAPK [4]. in vivo: Ft1 promotes the formation of blood vessels in Matrigel plug and wound healing in mice [1].

分子量    
917.13

性状    
Solid

Formula    
C47H80O17

CAS 号    
155683-00-4

中文名称    
三七皂甙 Ft1

结构分类    
TerpenoidsTriterpenes
来源    
PlantsAraliaceaePanax notoginseng
运输条件    
Room temperature in continental US; may vary elsewhere.

储存方式    
4°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

溶解性数据    
In Vitro: 
DMSO : 6.67 mg/mL (7.27 mM; Need ultrasonic)

配制储备液    
浓度溶剂体积质量    1 mg    5 mg    10 mg
1 mM    1.0904 mL    5.4518 mL    10.9036 mL
5 mM    0.2181 mL    1.0904 mL    2.1807 mL
10 mM    ---    ---    ---
*
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (stored under nitrogen)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:
请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 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: ≥ 0.67 mg/mL (0.73 mM); Clear solution

2.
请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in saline)

Solubility: ≥ 0.67 mg/mL (0.73 mM); Clear solution

3.
请依序添加每种溶剂： 10% DMSO    90% corn oil

Solubility: ≥ 0.67 mg/mL (0.73 mM); Clear solution
 

参考文献

[1]. Shen K, et al. Notoginsenoside Ft1 promotes angiogenesis via HIF-1α mediated VEGF secretion and the regulation of PI3K/AKT and Raf/MEK/ERK signaling pathways. Biochem Pharmacol. 2012 Sep 15;84(6):784-92.  [Content Brief] [2]. Gao B, et al. Platelet P2Y?? receptors are involved in the haemostatic effect of notoginsenoside Ft1, a saponin isolated from Panax notoginseng. Br J Pharmacol. 2014 Jan;171(1):214-23.  [Content Brief] [3]. Shen K, et al. Notoginsenoside Ft1 activates both glucocorticoid and estrogen receptors to induce endothelium-dependent, nitric oxide-mediated relaxations in rat mesenteric arteries. Biochem Pharmacol. 2014 Mar 1;88(1):66-74.  [Content Brief] [4]. Gao B, et al. p38 MAPK and ERK1/2 pathways are involved in the pro-apoptotic effect of notoginsenoside Ft1 on human neuroblastoma SH-SY5Y cells. Life Sci. 2014 Jul 17;108(2):63-70.  [Content Brief]