Barlerin(Synonyms: 8-O-Acetyl shanzhiside methyl ester)

天然产物 糖类和糖苷 Saccharides and Glycosides

Barlerin (Synonyms: 8-O-Acetyl shanzhiside methyl ester) 纯度: 99.0%

Barlerin (8-O-Acetyl shanzhiside methyl ester) 是从中国西藏民间药用植物中分离出的环孢菌素葡萄糖苷。Barlerin (8-O-Acetyl shanzhiside methyl ester) 可以抑制 NF-κB 活性。

Barlerin(Synonyms: 8-O-Acetyl shanzhiside methyl ester)

Barlerin Chemical Structure

CAS No. : 57420-46-9

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生物活性

Barlerin (8-O-Acetyl shanzhiside methyl ester) is an iridoid glucoside isolated from the leaves of Lamiophlomis rotata Kudo, a Chinese folk medicinal plant in Xi-zang. Barlerin (8-O-Acetyl shanzhiside methyl ester) could inhibt NF-κB.

IC50 & Target[1]

NF-κB

 

体外研究
(In Vitro)

Treatment of SH-SY5Y cells with Barlerin (8-O-Acetyl shanzhiside methyl ester) blocks TNF-α-induced nuclear transcription factor κB (NF-κB) activation and decreases high-mobility group box-1 (HMGB-1) expression. [1]. Treatment of H9c2 cells with Barlerin (8-O-Acetyl shanzhiside methyl ester) 9 μM blocks TNF-α-induced NF-κB phosphorylation by blocking High-mobility group box1 (HMGB1) expression[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

Barlerin (8-O-Acetyl shanzhiside methyl ester) 40 mg/kg demonstrates significant neuroprotective effect even after delayed administration at 4 hr after I/R. Barlerin 40 mg/kg attenuates the histopathological damage, decreases brain swelling, inhibits NF-κB activation and reduces HMGB-1 expression in ischaemic brain tissue[1]. Barlerin (8-O-Acetyl shanzhiside methyl ester) significantly promotes angiogenesis in the ischaemic brain and improves functional outcome after stroke. Barlerin also significantly increases vascularization compared with vehicle treatment. It increases the expression of VEGF, Ang1, phosphorylation of Tie2 and Akt VEGF[3]. Barlerin (8-O-Acetyl shanzhiside methyl ester) significantly shortens capillary blood clotting time and reduces blood loss volume, but does not influence mice activated partial thromboplastin time, prothrombin time or thrombin time. It significantly prolongs euglobulin clot lysis time in hyperfibrinolysis mice[4].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

448.42

Formula

C19H28O12

CAS 号

57420-46-9

中文名称

8-O-乙酰山栀苷甲酯

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
溶解性数据
In Vitro: 

DMSO : 100 mg/mL (223.01 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.2301 mL 11.1503 mL 22.3005 mL
5 mM 0.4460 mL 2.2301 mL 4.4601 mL
10 mM 0.2230 mL 1.1150 mL 2.2301 mL

*

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。-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: ≥ 2.5 mg/mL (5.58 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.58 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 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。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

  • 2.

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

    Solubility: ≥ 2.5 mg/mL (5.58 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.58 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 3.

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

    Solubility: ≥ 2.5 mg/mL (5.58 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.58 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 25.0 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 MCE 网站选购。
参考文献
  • [1]. Zhang L, et al. 8-O-acetyl shanzhiside methylester attenuates cerebral ischaemia/reperfusion injury through an anti-inflammatory mechanism in diabetic rats. Basic Clin Pharmacol Toxicol. 2014 Dec;115(6):481-7.

    [2]. Kang ZC, et al. Cardioprotection with 8-O-acetyl shanzhiside methylester on experimental myocardial ischemia injury. Eur J Pharm Sci. 2012 Aug 30;47(1):124-30.

    [3]. Jiang WL, et al. Effect of 8-O-acetyl shanzhiside methylester increases angiogenesis and improves functional recovery after stroke. Basic Clin Pharmacol Toxicol. 2011 Jan;108(1):21-7.

    [4]. Fan PC, et al. A new anti-fibrinolytic hemostatic compound 8-O-acetyl shanzhiside methylester extracted from Lamiophlomis rotata. J Ethnopharmacol. 2016 Jul 1;187:232-8.

Cell Assay
[2]

Prior to hypoxia, cells are pretreated with various concentrations (1, 3, 9 and 27μM) of Barlerin (8-O-Acetyl shanzhiside methyl ester) for 24 h. Cell viability are determined by MTT assay[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[3][4]

Rats: Barlerin (8-O-Acetyl shanzhiside methyl ester) is prepared in saline. Adult male rats are subjected to 1 hr of middle cerebral artery occlusion (MCAO) and reperfusion, and treated with or without different doses (5 and 10 mg/kg) of ND01, starting 24 hr after ischaemia and reperfusion (I/R) and by intravenous injection daily for 14 days. Neurological functional tests are performed and cerebral Evans blue extravasation is measured[3].

Mouse: Barlerin (8-O-Acetyl shanzhiside methyl ester) is prepared in saline. Male Balb/C mice (20 to 25g) are randomly divided into five groups (saline group, Hemocoagulase, 0.34 KU/kg, i.v. ASM-L, 100 mg/kg, i.v., ASM-M, 250 mg/kg, i.v., ASM-H, 500 mg/kg, i.v.). The drugs and vehicle are injected through vena caudal is 5 min before anesthetized with sodium pentobarbital (200 mg/kg, i.p.). Twenty minutes after injection, blood are drawn from heart. Activated partial thromboplastin time, prothrombin time, thrombin time and fibrinogen are assayed[4].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献
  • [1]. Zhang L, et al. 8-O-acetyl shanzhiside methylester attenuates cerebral ischaemia/reperfusion injury through an anti-inflammatory mechanism in diabetic rats. Basic Clin Pharmacol Toxicol. 2014 Dec;115(6):481-7.

    [2]. Kang ZC, et al. Cardioprotection with 8-O-acetyl shanzhiside methylester on experimental myocardial ischemia injury. Eur J Pharm Sci. 2012 Aug 30;47(1):124-30.

    [3]. Jiang WL, et al. Effect of 8-O-acetyl shanzhiside methylester increases angiogenesis and improves functional recovery after stroke. Basic Clin Pharmacol Toxicol. 2011 Jan;108(1):21-7.

    [4]. Fan PC, et al. A new anti-fibrinolytic hemostatic compound 8-O-acetyl shanzhiside methylester extracted from Lamiophlomis rotata. J Ethnopharmacol. 2016 Jul 1;187:232-8.

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