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.

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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

448.42

C₁₉H₂₈O₁₂

57420-46-9

固体

White to off-white

8-O-乙酰山栀苷甲酯

• Terpenoids
• Iridoids

• 植物
• 菊科
• 堆心菊属

• 植物
• 唇形科

Room temperature in continental US; may vary elsewhere.

DMSO 中的溶解度 : 100 mg/mL (223.01 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

* 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, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

• 方案 一

  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); 澄清溶液

  此方案可获得 ≥ 2.5 mg/mL（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；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水 定容至 1 mL。

  生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。

• 方案 二

  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); 澄清溶液

  此方案可获得 ≥ 2.5 mg/mL（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。

  20% SBE-β-CD in Saline 的配制（4°C，储存一周）：2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。

• 方案 三

  请依序添加每种溶剂： 10% DMSO    90% Corn Oil

  Solubility: ≥ 2.5 mg/mL (5.58 mM); 澄清溶液

  此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。

  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。

• [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.  [Content Brief]

  [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.  [Content Brief]

  [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.  [Content Brief]

  [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.  [Content Brief]

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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

• [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.  [Content Brief]

  [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.  [Content Brief]

  [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.  [Content Brief]

  [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.  [Content Brief]