1. MAPK/ERK Pathway Autophagy Apoptosis NF-κB Metabolic Enzyme/Protease Immunology/Inflammation
  2. p38 MAPK Autophagy Apoptosis Reactive Oxygen Species (ROS) NF-κB Bcl-2 Family
  3. Hesperetin

Hesperetin  (Synonyms: 橙皮素)

目录号: HY-N0168 纯度: 99.12%
COA 产品使用指南 技术支持

Hesperetin 是一种天然黄烷酮,存在于柑橘类水果中,是一种强效且具有口服活性的广谱人类 UGT 活性抑制剂。Hesperetin 通过激活 p38 MAPK 诱导细胞凋亡。Hesperetin 具有多种生物活性,包括抗氧化、抗炎和抗癌。Hesperetin 可诱导细胞周期停滞于 G2/M 期。Hesperetin 可以降低 Bcl-2 并增强 BaxM。Hesperetin 通过抑制 NF-κB 受体诱导细胞凋亡(apoptosis)。

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Hesperetin

Hesperetin Chemical Structure

CAS No. : 520-33-2

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥410
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25 mg ¥373
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50 mg ¥500
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100 mg ¥779
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500 mg ¥1558
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1 g   询价  
5 g   询价  

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Customer Review

Other Forms of Hesperetin:

    Hesperetin purchased from MCE. Usage Cited in: Nutr Cancer. 2020;72(3):538-545.  [Abstract]

    Hesperetin induced G2/M arrest in GBM cell. Cells are treated with vehicle or various doses of hesperetin for 24 h. Whole cell lysates are immunoblotted with indicated antibodies. The protein levels of p21, CDK1, and cyclin B1 are measured by western blotting.

    Hesperetin purchased from MCE. Usage Cited in: Nutr Cancer. 2020;72(3):538-545.  [Abstract]

    The expression of Bax and Bcl-2 was examined by western blotting. GAPDH was served as a loading control.

    Hesperetin purchased from MCE. Usage Cited in: Nutr Cancer. 2020;72(3):538-545.  [Abstract]

    U-251 cells are cultured with indicated concentration of Hesperetin for 24 h. Then the cells are stained with DAPI and observed under a fluorescence microscope.

    Hesperetin purchased from MCE. Usage Cited in: Nutr Cancer. 2020;72(3):538-545.  [Abstract]

    p38 MAPK activation is involved in Hesperetin-induced apoptosis. The phosphorylation of p38 MAPK, JNK, and ERK in U-21 cells treated with hesperetin is analyzed by western blotting.
    • 生物活性

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Hesperetin is a natural flavanone that can be found in citrus, and acts as a potent and orally active broad-spectrum inhibitor against human UGT activity. Hesperetin induces apoptosis via p38 MAPK activation. Hesperetin displays a range of bioactivities including antioxidant, anti-inflammatory, and anti-cancer. Hesperetin is found to induce cell-cycle arrest at G2/M phase. Hesperetin can reduce Bcl-2 and enhance BaxM. Hesperetin induces apoptosis through inhibiting NF-κB receptor[1][2][3][4].

    细胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    BJ EC50
    > 10 μM
    Compound: 3
    Cytotoxicity against human BJ cells assessed as viable cells after 72 hrs by calcein AM assay
    Cytotoxicity against human BJ cells assessed as viable cells after 72 hrs by calcein AM assay
    [PMID: 20192247]
    Caco-2 IC50
    66.67 μM
    Compound: 28
    Cytotoxicity in human Caco2 cells after 72 hrs by MTT assay
    Cytotoxicity in human Caco2 cells after 72 hrs by MTT assay
    [PMID: 28793973]
    CCRF-CEM EC50
    > 10 μM
    Compound: 3
    Cytotoxicity against human CEM cells assessed as viable cells after 72 hrs by calcein AM assay
    Cytotoxicity against human CEM cells assessed as viable cells after 72 hrs by calcein AM assay
    [PMID: 20192247]
    HCT-116 GI50
    36.1 μM
    Compound: Hesperetin
    Anticlonogenic activity in human HCT116 cells after 6 days by crystal violet staining based assay
    Anticlonogenic activity in human HCT116 cells after 6 days by crystal violet staining based assay
    [PMID: 27840137]
    HeLa EC50
    > 10 μM
    Compound: 3
    Cytotoxicity against human HeLa cells assessed as viable cells after 72 hrs by calcein AM assay
    Cytotoxicity against human HeLa cells assessed as viable cells after 72 hrs by calcein AM assay
    [PMID: 20192247]
    MCF7 EC50
    > 10 μM
    Compound: 3
    Cytotoxicity against human MCF7 cells assessed as viable cells after 72 hrs by calcein AM assay
    Cytotoxicity against human MCF7 cells assessed as viable cells after 72 hrs by calcein AM assay
    [PMID: 20192247]
    Monocyte IC50
    2.1 μM
    Compound: hesperetin
    Inhibition of procoagulant activity in monocyte from human blood assessed as counteraction of IL1-induced tissue factor expression after 18 hrs
    Inhibition of procoagulant activity in monocyte from human blood assessed as counteraction of IL1-induced tissue factor expression after 18 hrs
    [PMID: 8882428]
    PC-3 IC50
    40 μM
    Compound: Hesperetin
    Antiproliferative activity against human PC3 cells after 48 hrs by MTT assay
    Antiproliferative activity against human PC3 cells after 48 hrs by MTT assay
    [PMID: 31398616]
    PC-3 IC50
    90 μM
    Compound: Hesperetin
    Antiproliferative activity against human PC3 cells after 24 hrs by MTT assay
    Antiproliferative activity against human PC3 cells after 24 hrs by MTT assay
    [PMID: 31398616]
    RAW264.7 CC50
    > 100 μM
    Compound: 16
    Cytotoxicity against mouse RAW264.7 cells assessed as reduction in cell viability measured after 24 hrs by MTT assay
    Cytotoxicity against mouse RAW264.7 cells assessed as reduction in cell viability measured after 24 hrs by MTT assay
    [PMID: 33667099]
    RAW264.7 IC50
    31.2 μM
    Compound: 16
    Inhibition of LPS induced NO production in mouse RAW264.7 cells measured after 24 hrs by Griess reagent based assay
    Inhibition of LPS induced NO production in mouse RAW264.7 cells measured after 24 hrs by Griess reagent based assay
    [PMID: 33667099]
    RAW264.7 IC50
    48.59 μM
    Compound: 1; Hes
    Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced NO production preincubated for 2 hrs followed by LPS stimulation and measured after 24 hrs by Griess method
    Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced NO production preincubated for 2 hrs followed by LPS stimulation and measured after 24 hrs by Griess method
    [PMID: 33493826]
    RPMI-8226 EC50
    > 10 μM
    Compound: 3
    Cytotoxicity against human RPMI8226 cells assessed as viable cells after 72 hrs by calcein AM assay
    Cytotoxicity against human RPMI8226 cells assessed as viable cells after 72 hrs by calcein AM assay
    [PMID: 20192247]
    THP-1 EC50
    > 10 μM
    Compound: 3
    Cytotoxicity against human THP1 cells after 72 hrs by erythosin B staining method
    Cytotoxicity against human THP1 cells after 72 hrs by erythosin B staining method
    [PMID: 20192247]
    U-266 EC50
    > 10 μM
    Compound: 3
    Cytotoxicity against human U266 cells assessed as viable cells after 72 hrs by calcein AM assay
    Cytotoxicity against human U266 cells assessed as viable cells after 72 hrs by calcein AM assay
    [PMID: 20192247]
    Vero IC50
    8.3 μM
    Compound: Hesperetin
    Inhibition of SARS coronavirus 3C-like protease cis-cleavage activity transfected in african green monkey Vero cells by luciferase reporter gene assay
    Inhibition of SARS coronavirus 3C-like protease cis-cleavage activity transfected in african green monkey Vero cells by luciferase reporter gene assay
    [PMID: 23647823]
    体外研究
    (In Vitro)

    Hesperetin (Compound HET) (100 μM) 对 10 种受试 rhUGT 异构体表现出强或中度抑制作用[2]
    Hesperetin (100-800 μM,24-48 小时) 以时间和浓度依赖性方式显著降低 U-251 和 U-87 细胞的活力[4]
    Hesperetin (200-400 μM,24 小时) 以剂量依赖性方式显著增加 U-251 细胞的凋亡细胞比例[4]

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

    Immunofluorescence[4]

    Cell Line: U-251 cell line
    Concentration: 200 and 400 μM
    Incubation Time: 24 h
    Result: Resulted in significant accumulation of cell populations at the G2/M phase, with a concomitant decrease of cell populations in G1 phase and a slightly elevated population in S phase.

    Cell Viability Assay[4]

    Cell Line: U-251 and U-87 cells
    Concentration: 100, 200, 400, 600, and 800 μM
    Incubation Time: 24 and 48 h
    Result: Significantly reduced the viabilities of U-251 and U-87 cells in a time- and concentration-dependent manner with IC50s of 468.33 μM and 441.87 μM.
    体内研究
    (In Vivo)

    Hesperetin (Compound Hp) (40 mg/kg,口服,21 天) 可使镉暴露大鼠的乙酰胆碱酯酶活性恢复到接近正常水平[3]

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

    Animal Model: Cd-exposed male albino Wistar rats (180-210 g)[3]
    Dosage: 40 mg/kg
    Administration: Oral gavage (p.o.)
    Result: Significantly reversed the activities of AChE to near normal.
    Decreased the levels of LPO products in brain.
    Significantly increased the levels of antioxidants in brain.
    Significantly increased the activities of ATPases enzymes in brain.
    Decreased the levels of Bax, cytochrome c, caspase 3 and 9 and increased the levels of Bcl2 markers.
    Significantly restores the activities of mitochondrial enzyme complex I, II, III and IV.
    Restored the levels of NO and OH-.
    Restored the enzyme activities in cererbrum.
    Reduced the tail length, tail moment, and tail intensity.
    Clinical Trial
    分子量

    302.28

    Formula

    C16H14O6

    CAS 号
    性状

    固体

    颜色

    White to off-white

    中文名称

    橙皮素

    结构分类
    初始来源
    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
    细胞实验: 

    DMSO 中的溶解度 : 125 mg/mL (413.52 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 3.3082 mL 16.5410 mL 33.0819 mL
    5 mM 0.6616 mL 3.3082 mL 6.6164 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。-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: ≥ 2.5 mg/mL (8.27 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。

      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 (8.27 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。

      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。

    以下溶解方案,请直接配制工作液。建议现用现配,在短期内尽快用完。 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: 0.5% CMC/saline water

      Solubility: 20 mg/mL (66.16 mM); 悬浊液; 超声助溶

    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)。
    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: 99.12%

    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。-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 3.3082 mL 16.5410 mL 33.0819 mL 82.7048 mL
    5 mM 0.6616 mL 3.3082 mL 6.6164 mL 16.5410 mL
    10 mM 0.3308 mL 1.6541 mL 3.3082 mL 8.2705 mL
    15 mM 0.2205 mL 1.1027 mL 2.2055 mL 5.5137 mL
    20 mM 0.1654 mL 0.8270 mL 1.6541 mL 4.1352 mL
    25 mM 0.1323 mL 0.6616 mL 1.3233 mL 3.3082 mL
    30 mM 0.1103 mL 0.5514 mL 1.1027 mL 2.7568 mL
    40 mM 0.0827 mL 0.4135 mL 0.8270 mL 2.0676 mL
    50 mM 0.0662 mL 0.3308 mL 0.6616 mL 1.6541 mL
    60 mM 0.0551 mL 0.2757 mL 0.5514 mL 1.3784 mL
    80 mM 0.0414 mL 0.2068 mL 0.4135 mL 1.0338 mL
    100 mM 0.0331 mL 0.1654 mL 0.3308 mL 0.8270 mL
    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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