2. Metabolic Enzyme/Protease Membrane Transporter/Ion Channel Apoptosis Neuronal Signaling MAPK/ERK Pathway Immunology/Inflammation NF-κB Anti-infection
  3. Glutathione S-transferase P-glycoprotein Apoptosis iGluR CaMK p38 MAPK Reactive Oxygen Species (ROS) Bacterial
  4. Coniferyl ferulate

Coniferyl ferulate  (Synonyms: 阿魏酸松柏酯)

目录号: HY-N1916 纯度: 98.73%
COA 产品使用指南 技术支持

Coniferyl ferulate 是一种口服有效的酚酸类化合物。Coniferyl ferulate 是谷胱甘肽 S-转移酶 (GST) 的强效抑制剂 (IC50 = 0.3 μM)，可下调 P-gp 表达，诱导 B-MD-C1 (ADR+/+) 细胞凋亡 (apoptosis)，逆转多药耐药性。Coniferyl ferulate 可阻断 NMDAR/NR2B-CaMKII-MAPKs 信号通路，抑制 ROS 产生和线粒体凋亡，同时重塑肠道微生物群和微生物代谢，改善小鼠结肠炎症、减轻小鼠的抑郁症状。Coniferyl ferulate 能够通过靶向 Mgst2 来减轻二甲苯对造血干细胞和祖细胞的毒性。Coniferyl ferulate 对革兰氏阳性菌枯草芽孢杆菌和金黄色葡萄球菌具有抗菌活性。

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Coniferyl ferulate

Coniferyl ferulate Chemical Structure

CAS No. : 63644-62-2

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Coniferyl ferulate 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Coniferyl ferulate is an orally active phenolic acid compound. Coniferyl ferulate is a potent inhibitor of glutathione S-transferase (GST) (IC50 = 0.3 μM), which downregulates P-gp expression, induces apoptosis in B-MD-C1 (ADR+/+) cells, and reverses multidrug resistance. Coniferyl ferulate blocks the NMDAR/NR2B-CaMKII-MAPKs signaling pathway, inhibits ROS production and mitochondrial apoptosis, while reshapes the intestinal microbiota and microbial metabolism, ameliorates colonic inflammation and alleviates depressive symptoms in mice. Coniferyl ferulate can alleviate the toxicity of xylene to hematopoietic stem and progenitor cells by targeting Mgst2. Coniferyl ferulate exhibits antibacterial activity against the Gram-positive Bacillus subtilis and Staphylococcus aureus[1][2][3][4][5].

IC50 & Target[2]

CaMK II

 

NMDA Receptor

 

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
MDA-MB-231 IC50
19.8 μM
Compound: 40; coniferyl ferulate
Antimigratory activity against human MDA-MB-231 cells expressing c-MET assessed as inhibition of HGF-induced cell migration incubated for 24 hrs by Giemsa staining based wound healing assay
Antimigratory activity against human MDA-MB-231 cells expressing c-MET assessed as inhibition of HGF-induced cell migration incubated for 24 hrs by Giemsa staining based wound healing assay
[PMID: 27258622]
MDA-MB-231 IC50
22.3 μM
Compound: 40; coniferyl ferulate
Antiproliferative activity against human MDA-MB-231 cells expressing c-MET assessed as inhibition of HGF-induced cell growth incubated for 72 hrs by MTT assay
Antiproliferative activity against human MDA-MB-231 cells expressing c-MET assessed as inhibition of HGF-induced cell growth incubated for 72 hrs by MTT assay
[PMID: 27258622]
MDA-MB-468 IC50
25.6 μM
Compound: 40; coniferyl ferulate
Antiproliferative activity against human MDA-MB-468 cells expressing c-MET assessed as inhibition of HGF-induced cell growth incubated for 72 hrs by MTT assay
Antiproliferative activity against human MDA-MB-468 cells expressing c-MET assessed as inhibition of HGF-induced cell growth incubated for 72 hrs by MTT assay
[PMID: 27258622]
体外研究
(In Vitro)

Coniferyl ferulate (5-20 μM, 48 h) 在 B-MD-C1 (ADR+/+) 细胞中诱导凋亡，并阻滞细胞周期于 G1 期[1]。
Coniferyl ferulate (5-20 μM, 48 h) 抑制 Doxorubicin (HY-15142A) 引起的 MDR1/P-gp 上调，并使 B-MD-C1 (ADR+/+) 细胞中 P-gp 的表达接近正常水平[1]。
Coniferyl ferulate (0.2-20 μM, 28 h) 过阻断 NMDA-CaMKII-MAPKs 信号级联、降低 ROS 水平和增强 SOD 活性，保护 PC12 细胞免受 Glutamate (HY-14608) 诱导的细胞活力下降和凋亡，减轻细胞膜损伤[2]。

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

Coniferyl ferulate 相关抗体:

Apoptosis Analysis[1]

Cell Line: B-MD-C1(ADR+/+) cells
Concentration: 5, 10 and 20 μM
Incubation Time: 48 h
Result: Induced apoptosis.

Cell Cycle Analysis[1]

Cell Line: B-MD-C1(ADR+/+) cells
Concentration: 5, 10 and 20 μM
Incubation Time: 48 h
Result: Markedly increased the proportion of cells in G1-phase, decreased the proportion of cells in S-phase.

RT-PCR[1]

Cell Line: B-MD-C1(ADR+/+) cells
Concentration: 5, 10 and 20 μM
Incubation Time: 48 h
Result: Dose-dependently inhibited Doxorubicin-induced MDR1 overexpression.
Brought the expression of P-gp close to the basal level.

Cell Viability Assay[2]

Cell Line: Glutamate-damaged PC12 cells
Concentration: 0.2, 2, 20 μM
Incubation Time: After 4 hours of pre-treatment, with Glutamate for another 24 hours
Result: Concentration-dependently protected the decline in cell viability induced by Glutamate.
Significantly alleviated the damage to the cell membrane caused by Glutamate.

Apoptosis Analysis[2]

Cell Line: Glutamate-damaged PC12 cells
Concentration: 0.2, 2, 20 μM
Incubation Time: After 4 hours of pre-treatment, with Glutamate for another 24 hours
Result: Reduced nuclear shrinkage and PI-positive cells.

Apoptosis Analysis[2]

Cell Line: Glutamate-damaged PC12 cells
Concentration: 0.2, 2, 20 μM
Incubation Time: After 4 hours of pre-treatment, with Glutamate for another 24 hours
Result: Decreased the level of p-NR2B, p-CaMKII, p-JNK and p-p38.
increased the Bcl-2/Bax ratio and decreased the release of cytochrome C and activation of Caspase-3.
体内研究
(In Vivo)

Coniferyl ferulate (25-100 mg/kg, i.g., 每天一次共 13-14 天) 在小鼠行为测试中具有抗抑郁作用[2]。
Coniferyl ferulate (50 mg/kg, i.g., 每天一次共 4 周) 可减轻慢性不可预测温和应激 (CUMS) 诱导的类抑郁和类焦虑行为，并显著改善小鼠结肠炎症[3]。
Coniferyl ferulate (50 mg/kg, i.g., 每天一次共 25 天) 通过抑制 Mgst2 减轻二甲苯引起的小鼠造血干细胞和祖细胞毒性[4]。

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

Animal Model: Behavioral test (tail suspension and forced-swimming test) established in male ICR mice (18-22 g)[2]
Dosage: 25, 50 and 100 mg/kg
Administration: Intragastric administration (i.g.), once daily, for 13 and 14 days
Result: Obviously decreased the immobility time in tail suspension test (TST) and forced swimming test (FST).
Animal Model: CUMS model established in in 8-week-old male C57BL/6 SPF mice (20 g)[3]
Dosage: 50 mg/kg
Administration: Intragastric administration (i.g.), once daily, for 4 weeks
Result: Improved depressive in sucrose preference test (SPT), open field test (OFT), FTS and TST and anxiety-like behaviors in elevated plus-maze test (EPM).
Restored the reduction of intestinal microvilli and alleviated mitochondrial swelling.
Lowered the levels of IL-6, IL-1β, and TNF-α.
Restructured the gut microbiome, and microbial metabolism.
Animal Model: Xylene-induced hematotoxicity model established in male C57BL/6 SPF mice (8 weeks old, 20 g)
Dosage: 50 mg/kg
Administration: Intragastric administration (i.g.), once daily, for 25 days
Result: Significantly reversed the White blood cell count (WBC) reduction induced by xylene.
Restored the proportion of bone marrow LSK cells to the normal level.
Reduced the level of ROS in mitochondria and restored the mitochondrial membrane potential inhibited by xylene.
Acted directly on the Mgst2 target site (KD=8.0861 kcal/mol).
分子量

356.37

Formula

C20H20O6
CAS 号
性状

固体

颜色

White to off-white

中文名称

阿魏酸松柏酯
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 : 100 mg/mL (280.61 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)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.8061 mL 14.0304 mL 28.0607 mL
5 mM 0.5612 mL 2.8061 mL 5.6121 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    90% (20% SBE-β-CD in Saline)

    Solubility: 2.5 mg/mL (7.02 mM); 悬浊液; 超声助溶

    此方案可获得 2.5 mg/mL的均匀悬浊液，悬浊液可用于口服和腹腔注射。

    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。

    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 二

    请依序添加每种溶剂： 10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (7.02 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。

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

只
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

纯度: 98.73%

COA (282 KB) HNMR (255 KB) LCMS (98 KB)

产品使用指南 (1538 KB)
参考文献

Coniferyl ferulate 相关分类

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 2.8061 mL 14.0304 mL 28.0607 mL 70.1518 mL
5 mM 0.5612 mL 2.8061 mL 5.6121 mL 14.0304 mL
10 mM 0.2806 mL 1.4030 mL 2.8061 mL 7.0152 mL
15 mM 0.1871 mL 0.9354 mL 1.8707 mL 4.6768 mL
20 mM 0.1403 mL 0.7015 mL 1.4030 mL 3.5076 mL
25 mM 0.1122 mL 0.5612 mL 1.1224 mL 2.8061 mL
30 mM 0.0935 mL 0.4677 mL 0.9354 mL 2.3384 mL
40 mM 0.0702 mL 0.3508 mL 0.7015 mL 1.7538 mL
50 mM 0.0561 mL 0.2806 mL 0.5612 mL 1.4030 mL
60 mM 0.0468 mL 0.2338 mL 0.4677 mL 1.1692 mL
80 mM 0.0351 mL 0.1754 mL 0.3508 mL 0.8769 mL
100 mM 0.0281 mL 0.1403 mL 0.2806 mL 0.7015 mL
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Keywords:

Coniferyl ferulate63644-62-2阿魏酸松柏酯Glutathione S-transferaseP-glycoproteinApoptosisiGluRCaMKp38 MAPKReactive Oxygen Species (ROS)BacterialGlutathione transferasesGSTsP-gpPgpMultidrug resistance protein 1MDR1ATP-binding cassette sub-family B member 1ABCB1Cluster of differentiation 243CD243Ionotropic glutamate receptorsCalmodulin-dependent protein kinasesCalmodulin-dependent kinasesXiaoyaosanAnti-depressionOxidative stressNMDARCaMKIIInhibitorinhibitorinhibit

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