1. Anti-infection Metabolic Enzyme/Protease Immunology/Inflammation NF-κB Apoptosis PI3K/Akt/mTOR Vitamin D Related/Nuclear Receptor Cell Cycle/DNA Damage
  2. Bacterial Fungal Reactive Oxygen Species (ROS) Apoptosis MMP Interleukin Related PI3K Akt mTOR PPAR PGC-1α Pyroptosis
  3. (+)-Medioresinol

(+)-Medioresinol  (Synonyms: 梣皮树脂醇)

目录号: HY-N3307 纯度: 98.88%
COA 产品使用指南 技术支持

(+)-Medioresinol 是一种 Furofuran 型木脂素,具有抗真菌,抗菌作用。(+)-Medioresinol 与抗生素协同发挥抗菌和抗生物膜作用。(+)-Medioresinol 可诱导白色念珠菌中细胞内 ROS 积累和线粒体介导的凋亡 (apoptosis) 性死亡。(+)-Medioresinol 对 LPS (HY-D1056) 刺激的 IL-12p40 产生有抑制作用。(+)-Medioresinol 是一种 PGC-1α 激活剂,通过 PPARα-GOT1 轴防止缺血性中风中内皮细胞焦亡 (pyroptosis)。(+)-Medioresinol 可用于真菌 (fungal) 细菌 (bacterial) 感染、炎症、缺血性中风的研究。

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(+)-Medioresinol

(+)-Medioresinol Chemical Structure

CAS No. : 40957-99-1

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MCE 顾客使用本产品发表的 1 篇科研文献

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

(+)-Medioresinol is a furofuran-type lignan with antifungal and antibacterial properties. (+)-Medioresinol synergizes with antibiotics to exert antimicrobial and antibiofilm effects. (+)-Medioresinol induces intracellular ROS accumulation and mitochondrial-mediated apoptosis in Candida albicans. (+)-Medioresinol inhibits LPS (HY-D1056)-stimulated IL-12p40 production. (+)-Medioresinol is a PGC-1α activator that protects against endothelial cell pyroptosis in ischemic stroke via the PPARα-GOT1 axis. (+)-Medioresinol can be used in research on fungal and bacterial infection, inflammation, and ischemic stroke[1][2][3][4][5].

IC50 & Target[3]

IL-12

 

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
A549 IC50
> 30 μM
Compound: 8
Cytotoxicity against human A549 cells by SRB assay
Cytotoxicity against human A549 cells by SRB assay
[PMID: 26988298]
BMDC IC50
2 μM
Compound: 13
Antiinflammatory activity in C57BL/6 mouse BMDCs assessed as inhibition of LPS-stimulated IL-12p40 production treated 1 hr before LPS challenge measured 18 hrs post stimulation by ELISA
Antiinflammatory activity in C57BL/6 mouse BMDCs assessed as inhibition of LPS-stimulated IL-12p40 production treated 1 hr before LPS challenge measured 18 hrs post stimulation by ELISA
[PMID: 23484668]
BMDC IC50
20.87 μM
Compound: 13
Antiinflammatory activity in C57BL/6 mouse BMDCs assessed as inhibition of LPS-stimulated IL12 production treated 1 hr before LPS challenge measured 18 hrs post stimulation by ELISA
Antiinflammatory activity in C57BL/6 mouse BMDCs assessed as inhibition of LPS-stimulated IL12 production treated 1 hr before LPS challenge measured 18 hrs post stimulation by ELISA
[PMID: 23484668]
BMDC IC50
22.29 μM
Compound: 13
Antiinflammatory activity in C57BL/6 mouse BMDCs assessed as inhibition of LPS-stimulated TNF-alpha production treated 1 hr before LPS challenge measured 18 hrs post stimulation by ELISA
Antiinflammatory activity in C57BL/6 mouse BMDCs assessed as inhibition of LPS-stimulated TNF-alpha production treated 1 hr before LPS challenge measured 18 hrs post stimulation by ELISA
[PMID: 23484668]
BV-2 IC50
45.59 μM
Compound: 8
Anti-neuroinflammatory activity in LPS-activated mouse BV2 cells assessed as inhibition of NO production after 24 hrs by Griess assay
Anti-neuroinflammatory activity in LPS-activated mouse BV2 cells assessed as inhibition of NO production after 24 hrs by Griess assay
[PMID: 26988298]
RAW264.7 IC50
0.245 mM
Compound: 7
Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production after 24 hrs
Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production after 24 hrs
[PMID: 18986199]
SK-MEL-2 IC50
> 30 μM
Compound: 8
Cytotoxicity against human SK-MEL-2 cells by SRB assay
Cytotoxicity against human SK-MEL-2 cells by SRB assay
[PMID: 26988298]
SK-OV-3 IC50
> 30 μM
Compound: 8
Cytotoxicity against human SKOV3 cells by SRB assay
Cytotoxicity against human SKOV3 cells by SRB assay
[PMID: 26988298]
XF498 IC50
> 30 μM
Compound: 8
Cytotoxicity against human XF498 cells by SRB assay
Cytotoxicity against human XF498 cells by SRB assay
[PMID: 26988298]
体外研究
(In Vitro)

(+)-Medioresinol (18 小时) 对粪肠球菌 ATCC 19434、金黄色葡萄球菌 ATCC 25923、痤疮丙酸杆菌 ATCC 6919、大肠杆菌 O-157 ATCC 43895、大肠杆菌 ATCC 25922 和铜绿假单胞菌 ATCC 27853 具有抗菌活性,MIC 分别为 2.5、5、5、5、2.5、20 µg/mL[1]
(+)-Medioresinol 与 Cefotaxime (HY-A0088A) 和 Chloramphenicol (HY-B0239) 联合使用对大肠杆菌具有增强的抗菌作用,与 Ampicillin (HY-B0522) 和 Cefotaxime 联合使用可抑制金黄色葡萄球菌的形成[1]
(+)-Medioresinol (MIC/FIC x 1、x 4、x 10) 与 Ampicillin、Cefotaxime、Chloramphenicol 联合使用可抑制屎肠球菌 ATCC 19434、金黄色葡萄球菌 ATCC 25923、痤疮丙酸杆菌 ATCC 6919、大肠杆菌 O-157 ATCC 43895、大肠杆菌 ATCC 25922、丙酸杆菌、铜绿假单胞菌 ATCC 27853 的生物膜形成[1]
(+)-Medioresinol 对白色念珠菌、近平滑念珠菌、贝氏木霉和糠秕毛细管菌具有抗真菌活性,MIC 为 3.125-6.25 µg/mL[2]
(+)-Medioresinol (3.125 μg/mL, 2-4 小时) 在白色念珠菌细胞中将细胞阻滞于 G0/G1 期,增加细胞内 ROS 水平的积累,诱导细胞内 MMP 去极化[2]
(+)-Medioresinol (3.125 μg/mL,2-4 小时) 在白色念珠菌细胞中可诱导线粒体释放细胞色素 c、激活半胱天冬酶以及造成 DNA 和细胞核损伤,增加磷脂酰丝氨酸外化和侧向散射 (SSC),降低前向散射 (FSC) [2]
(+)-Medioresinol (Compound 13) 在 LPS 刺激的 BMDCs 中对 IL-12p40 表现出显著的抑制活性, IC50 为 2 μM[3]
(+)-Medioresinol (60-120 μM,24 小时) 可抵消 H9c2 细胞因氧糖缺乏 (OGD) 引起的活力下降和 NT-proBNP 水平升高[4]
(+)-Medioresinol (60-120 μM,24 小时) 可降低 OGD H9c2 细胞中的 ROS、TNF-α 和 IL-1β 水平,并升高 PI3K、p-AKT 和 p-mTOR 水平[4]
(+)-Medioresinol (5-20 μM,3-15 小时) 可减少 LDH 的分泌,促进 PGC-1α 的表达以及 ZO-1 和 Occludin 的蛋白表达,激活 PGC-1α 保护 bEnd.3 细胞中缺血性脑损伤[5]
(+)-Medioresinol (20 μM,15 小时) 可通过调节氧糖剥夺 (OGD) 引起的 bEnd.3 细胞中苯丙氨酸代谢以及 PGC-1α 介导的 PAH 和 GOT1 表达来抑制内皮细胞焦亡,从而保护 BBB 的完整性[5]

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

Cell Cycle Analysis[2]

Cell Line: C. albicans cells
Concentration: 3.125 μg/mL
Incubation Time: 4 h
Result: Arrested cells in G0/G1 phase.

Apoptosis Analysis[2]

Cell Line: C. albicans cells
Concentration: 3.125 μg/mL
Incubation Time: 2 h
Result: Induced ROS accumulation related to apoptosis.
Reduced the fluorescence of FL-2 and slightly increased the fluorescence of FL-1, induced depolarization of mitochondrial membrane potential.
Reduced the relative level of Cyt c in mitochondria and increased the relative level of Cyt c in the cytoplasm.
Induced metacaspase activation, increased phosphatidylserine externalization, decreased FSC, increased SSC.
Induced DNA and nuclear damage.

Western Blot Analysis[4]

Cell Line: OGD H9c2 cells
Concentration: 120 μM
Incubation Time: 24 h
Result: Increased PI3K, p-AKT, and p-mTOR levels.

Western Blot Analysis[5]

Cell Line: bEnd.3 cells
Concentration: 5, 10, 20 μM
Incubation Time: 3, 15 h
Result: Promoted the protein expression of ZO-1 and Occludin.
Reduced the expressions of pyroptosis-associated proteins (NLRP3, ASC, cleaved caspase-1, IL-1β and GSDMD-NT).
Increased the expression of PAH and GOT1.

Immunofluorescence[5]

Cell Line: bEnd.3 cells
Concentration: 20 μM
Incubation Time: 15 h
Result: Reduced OGD induced mtROS expression, reversed OGD-induced mitochondrial membrane potential reduction, reduced infarct volume and NLRP3+CD31+ cells number in the peri-infarct cortex at 48 h after surgery.

RT-PCR[5]

Cell Line: bEnd.3 cells
Concentration: 20 μM
Incubation Time: 4 h
Result: Increased PGC-1α mRNA expression, while has no effect on the mRNA expression of PGC-1β and PPRC.
体内研究
(In Vivo)

(+)-Medioresinol (1-10 mg/kg,静脉注射,缺血后 2 小时和 24 小时) 在雄性 ICR 小鼠模型中通过抑制脑微血管内皮细胞焦亡和保护 BBB 完整性,发挥对脑缺血的保护作用[5]
(+)-Medioresinol (1-10 mg/kg,静脉注射,缺血后 2 小时和 24 小时) 可促进 tMCAO 小鼠模型中缺血小鼠的长期功能恢复[5]

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

Animal Model: Male ICR mice (25-30 g, 8-10 weeks old) model[1]
Dosage: 1 mg/kg or 10 mg/kg
Administration: i.v., at 2 h and 24 h after ischemia
Result: Reduced infarct volume tested by TTC staining, decreased brain swelling volume and brain water content, decreased the area of IgG extravasation, reversed the reduction of ZO-1 and Occludin, attenuated ischemia-caused decrease in the protein expression of Occludin in cerebral microvascular endothelial cells.
Decreased protein expression level of pyroptosis-associated markers, NLRP3+ CD31+ cells in peri-infarct cortex, the ASC expression in cerebral microvascular endothelial cells.
Animal Model: Focal cerebral ischemia procedure (tMCAO) male ICR mice (25-30 g, 8-10 weeks old) model[1]
Dosage: 1 mg/kg or 10 mg/kg
Administration: i.v., at 2 h and 24 h after ischemia
Result: Decreased infarct sizes and mortality, increased the time in Rotarod test, and decreased the number of right turns and the scores of mNSS.
分子量

388.41

Formula

C21H24O7

CAS 号
性状

固体

颜色

White to off-white

中文名称

梣皮树脂醇

结构分类
初始来源
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶解性数据
细胞实验: 

DMSO 中的溶解度 : 50 mg/mL (128.73 mM; 超声助溶 (<60°C); 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.5746 mL 12.8730 mL 25.7460 mL
5 mM 0.5149 mL 2.5746 mL 5.1492 mL
查看完整储备液配制表

* 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 (protect from light)。-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。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物实验:

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

  • 方案 一

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 1.25 mg/mL (3.22 mM); 澄清溶液

    此方案可获得 ≥ 1.25 mg/mL(饱和度未知)的澄清溶液。

    1 mL 工作液为例,取 100 μL 12.5 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: ≥ 1.25 mg/mL (3.22 mM); 澄清溶液

    此方案可获得 ≥ 1.25 mg/mL(饱和度未知)的澄清溶液。

    1 mL 工作液为例,取 100 μL 12.5 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。

    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。
动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
请输入您的动物体内配方组成:
%
DMSO +
+
%
Tween-80 +
%
Saline
如果您的动物是免疫缺陷鼠或者体弱鼠,建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
方案所需 助溶剂 包括:DMSO ,均可在 MCE 网站选购。 Tween 80,均可在 MCE 网站选购。
计算结果
工作液所需浓度 : mg/mL
储备液配制方法 : mg 药物溶于 μL  DMSO(母液浓度为 mg/mL)。

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

您所需的储备液浓度超过该产品的实测溶解度,以下方案仅供参考,如有需要,请与 MCE 中国技术支持联系。
动物实验体内工作液的配制方法 : 取 μL DMSO 储备液,加入 μL  μL ,混合均匀至澄清,再加 μL Tween 80,混合均匀至澄清,再加 μL 生理盐水
连续给药周期超过半月以上,请谨慎选择该方案。
请确保第一步储备液溶解至澄清状态,从左到右依次添加助溶剂。您可采用超声加热 (超声清洗仪,建议频次 20-40 kHz),涡旋吹打等方式辅助溶解。
纯度 & 产品资料
参考文献

完整储备液配制表

* 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 (protect from light)。-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。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.5746 mL 12.8730 mL 25.7460 mL 64.3650 mL
5 mM 0.5149 mL 2.5746 mL 5.1492 mL 12.8730 mL
10 mM 0.2575 mL 1.2873 mL 2.5746 mL 6.4365 mL
15 mM 0.1716 mL 0.8582 mL 1.7164 mL 4.2910 mL
20 mM 0.1287 mL 0.6436 mL 1.2873 mL 3.2182 mL
25 mM 0.1030 mL 0.5149 mL 1.0298 mL 2.5746 mL
30 mM 0.0858 mL 0.4291 mL 0.8582 mL 2.1455 mL
40 mM 0.0644 mL 0.3218 mL 0.6436 mL 1.6091 mL
50 mM 0.0515 mL 0.2575 mL 0.5149 mL 1.2873 mL
60 mM 0.0429 mL 0.2145 mL 0.4291 mL 1.0727 mL
80 mM 0.0322 mL 0.1609 mL 0.3218 mL 0.8046 mL
100 mM 0.0257 mL 0.1287 mL 0.2575 mL 0.6436 mL
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