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  1. MAPK/ERK Pathway Apoptosis Autophagy
  2. JNK Apoptosis Autophagy
  3. Juglanin

Juglanin 是一種可以從粗萹蓄中分離得到的黃酮類化合物。Juglanin 是一種 JNK 的激活劑,具有抗炎,抗氧化和抗腫瘤活性。Juglanin 能誘導人乳腺癌細胞的凋亡 (apoptosis) 和自噬 (autophagy)。

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Juglanin Chemical Structure

Juglanin Chemical Structure

CAS No. : 5041-67-8

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查看 JNK 亞型特異性產(chǎn)品:

  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻

生物活性

Juglanin, a occurring flavonoid that can be isolated from crude Polygonum aviculare, is a JNK acticator, with anti-inflammatory, anti-oxidant and anti-tumor activities. Juglanin can induce apoptosis and autophagy on human breast cancer cells[1][2].

IC50 & Target[1]

JNK

 

細胞效力
(Cellular Effect)
Cell Line Type Value Description References
C3H 10T1/2 IC50
> 100 μM
Compound: 8
Cytotoxicity against mouse C3H10T1/2 cells after 24 hrs by FMCA method
Cytotoxicity against mouse C3H10T1/2 cells after 24 hrs by FMCA method
[PMID: 21190854]
DU-145 IC50
2.4 μM
Compound: 8
Cytotoxicity against human DU145 cells after 24 hrs by FMCA method
Cytotoxicity against human DU145 cells after 24 hrs by FMCA method
[PMID: 21190854]
HaCaT IC50
2 μM
Compound: 8
Inhibition of human HH/Gli1-mediated transcriptional activity in tetracycline-treated human HaCaT cells treated after 12 hrs of tetracycline addition by luciferase reporter gene assay
Inhibition of human HH/Gli1-mediated transcriptional activity in tetracycline-treated human HaCaT cells treated after 12 hrs of tetracycline addition by luciferase reporter gene assay
[PMID: 21190854]
PANC-1 IC50
1.8 μM
Compound: 8
Cytotoxicity against human PANC1 cells after 24 hrs by FMCA method
Cytotoxicity against human PANC1 cells after 24 hrs by FMCA method
[PMID: 21190854]
體外研究
(In Vitro)

Juglanin(0-40 μM,24-48 h)以劑量和時間依賴的方式抑制乳腺癌癥細胞的增殖,并對正常細胞表現(xiàn)出較少的細胞毒性[1]。
Juglanin (0-10 μM, 24 h) 誘導 MCF-7/SKBR3 細胞 G2/M 期阻滯和 Caspase 依賴性凋亡[1]。
Juglanin (10 μM, 24 h) 促進 MCF-7/SKBR3 細胞中 ROS 生成,增強 JNK 活化[1]。
Juglanin (40-160 μM, 24 h) 可抑制脂多糖 (HY-D1056) 處理的 AST 細胞中的炎癥,并減輕神經(jīng)炎癥[2]。
Juglanin (40 μM, 24 h) 抑制 TGF-β1 培養(yǎng)的 MRC-5 細胞中 Sting 的表達[3]

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

Cell Viability Assay[3]

Cell Line: MCR-5 cell
Concentration: 0-40 μM
Incubation Time: 0-72 h
Result: Reduced the cell viability of MCR-5 after 24 h exposure at 160 μM.
Reduced the cell viability of MCR-5 after 72 h exposure at 40 μM.

Western Blot Analysis[1]

Cell Line: MCF-7, SKBR3
Concentration: 0-10 μM
Incubation Time: 24 h
Result: Increased the expressions of phosphorylated Chk2, Chk2, phosphorylated Cdc25C, phosphorylated Cdc2, p27, cyclin D, Bad, Bax and decreased the levels of Cdc25C, Cdc2, Bcl-2.
Activated caspases and led to Casapse-9, Casapse-8 and Caspase-3 cleavage.
Increased the level of JNK phosphorylation.

Western Blot Analysis[2]

Cell Line: Lipopolysaccharides (LPS, HY-D1056)-treated AST cells
Concentration: 40-160 μM
Incubation Time: 24 h
Result: Decreased the expression of TLR4, MyD88, CD14, p-IKKα, p-IκBα, p-NF-κB, GFAP, BDNF, Aβ and p-Tau induced by LPS (HY-D1056).
Increased the level of SYP, PSD-25 and SNAP-25.
體內(nèi)研究
(In Vivo)

Juglanin(10-20 mg/kg, 腹腔注射, 每天一次, 7天)在腫瘤移植小鼠模型中抑制人乳腺癌癥異種移植物的生長[1]。
Juglanin (10-30 mg/kg, 腹腔注射, 每周五次) 通過抑制 C57BL6 雄性小鼠中 TLR4/NF-κB ,改善神經(jīng)炎癥相關(guān)的記憶障礙和神經(jīng)退行性變[2]。
Juglanin (80 mg/kg, 灌胃, 每天一次, 21 天) 可以通過抑制 C57BL/6 雄性小鼠的纖維化來保護博來霉素 (BLM,HY-108345) 引起的肺部損傷[3]。

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

Animal Model: Tumor-transplanted mouse model [1]
Dosage: 10-20 mg/kg
Administration: Intraperitoneal injection (i.p.), daily, 7 days
Result: Increased levels of cleaved Caspase-9 and Caspase-3, LC3BI, LC3BII and phosphorylated JNK.
Increased dead cells and apoptosis proportion in juglanin-treated tumor tissues.
Increase in mean areas that stained positively cleaved Caspase-3 in juglanin-treated tumor tissues.
Animal Model: C57BL6 male mice[2]
Dosage: 10-30 mg/kg
Administration: Intraperitoneal injection (i.p.), 5 times weekly
Result: Increased number of platform crossings and expanded time in target quadrant.
Decreased the expression level of α-synuclein, pro-inflammatory cytokines (IL-1β, TNF-α, IL-18 and COX-2), TLR-4, MyD88, CD14, Aβ, phosphorylation of Tau, Ibal and neurotrophic factor (BDNF).
Reversed LPS-triggered effect on synaptic markers, up-regulating the expression of SYP, PSD-95 and SNAP-25.
Restored TH levels in the hippocampus of mice in a dose-dependent manner.
Decreased p-IKKα, p-IκBα and p-NF-κB levels combinated with LPS.
Decreased the GFAP-positive cells.
Animal Model: C57BL/6 male mice[3]
Dosage: 80 mg/kg
Administration: i.g., daily, 1-21 days
Result: Improved the survial rate of the BLM (HY-108345)-treated mice.
Decreased the expression of BALF, CXCL1, IL-6, TNF-α, MPO activity, TGF-β1, and its down-streaming proteins (fibronectin/MMP-9/α-SMA/collagen I) Reduced the number of total cells, neutrophils and macrophages in BALF.
分子量

418.35

Formula

C20H18O10

CAS 號
性狀

固體

顏色

White to yellow

結(jié)構(gòu)分類
初始來源
運輸條件

Room temperature in continental US; may vary elsewhere.

儲存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性數(shù)據(jù)
細胞實驗: 

DMSO 中的溶解度 : 100 mg/mL (239.03 mM; 超聲助溶; 吸濕的 DMSO 對產(chǎn)品的溶解度有顯著影響,請使用新開封的 DMSO)

配制儲備液
濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
1 mM 2.3903 mL 11.9517 mL 23.9034 mL
5 mM 0.4781 mL 2.3903 mL 4.7807 mL
查看完整儲備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液;一旦配成溶液,請分裝保存,避免反復凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C儲存時,請在6個月內(nèi)使用,-20°C儲存時,請在1個月內(nèi)使用。

  • 摩爾計算器

  • 稀釋計算器

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

質(zhì)量
=
濃度
×
體積
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

濃度 (start)

C1

×
體積 (start)

V1

=
濃度 (final)

C2

×
體積 (final)

V2

動物實驗:

請根據(jù)您的 實驗動物和給藥方式 選擇適當?shù)娜芙夥桨浮?

以下溶解方案都請先按照 In Vitro 方式配制澄清的儲備液,再依次添加助溶劑:
——為保證實驗結(jié)果的可靠性,澄清的儲備液可以根據(jù)儲存條件,適當保存;體內(nèi)實驗的工作液,建議您現(xiàn)用現(xiàn)配,當天使用;
以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比;如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象,可以通過加熱和/或超聲的方式助溶

  • 方案 一

    請依序添加每種溶劑: 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (5.98 mM); 澄清溶液

    此方案可獲得 ≥ 2.5 mg/mL(飽和度未知)的澄清溶液。

    1 mL 工作液為例,取 100 μL 25.0 mg/mL 的澄清 DMSO 儲備液加到 400 μL PEG300 中,混合均勻;再向上述體系中加入 50 μL Tween-80,混合均勻;然后再繼續(xù)加入 450 μL 生理鹽水 定容至 1 mL。

    生理鹽水的配制:將 0.9 g 氯化鈉,溶解于 ddH?O 并定容至 100 mL,可以得到澄清透明的生理鹽水溶液。
  • 方案 二

    請依序添加每種溶劑: 10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (5.98 mM); 澄清溶液

    此方案可獲得 ≥ 2.5 mg/mL(飽和度未知)的澄清溶液。

    1 mL 工作液為例,取 100 μL 25.0 mg/mL 的澄清 DMSO 儲備液加到 900 μL 20% 的 SBE-β-CD 生理鹽水水溶液 中,混合均勻。

    2 g SBE-β-CD(磺丁基醚 β-環(huán)糊精)粉末定容于 10 mL 的生理鹽水中,完全溶解至澄清透明。
動物溶解方案計算器
請輸入動物實驗的基本信息:

給藥劑量

mg/kg

動物的平均體重

g

每只動物的給藥體積

μL

動物數(shù)量

由于實驗過程有損耗,建議您多配一只動物的量
請輸入您的動物體內(nèi)配方組成:
%
DMSO +
+
%
Tween-80 +
%
Saline
如果您的動物是免疫缺陷鼠或者體弱鼠,建議 DMSO 中的在最后工作液體系中的占比盡量不超過 2%。
方案所需 助溶劑 包括:DMSO ,均可在 MCE 網(wǎng)站選購。 ,Tween 80,均可在 MCE 網(wǎng)站選購。
計算結(jié)果
工作液所需濃度 : mg/mL
儲備液配制方法 : mg 藥物溶于 μL  DMSO(母液濃度為 mg/mL)。

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

您所需的儲備液濃度超過該產(chǎn)品的實測溶解度,以下方案僅供參考,如有需要,請與 MCE 中國技術(shù)支持聯(lián)系。
動物實驗體內(nèi)工作液的配制方法 : 取 μL DMSO 儲備液,加入 μL 。 μL ,混合均勻至澄清,再加 μL Tween 80,混合均勻至澄清,再加 μL 生理鹽水
連續(xù)給藥周期超過半月以上,請謹慎選擇該方案。
請確保第一步儲備液溶解至澄清狀態(tài),從左到右依次添加助溶劑。您可采用超聲加熱 (超聲清洗儀,建議頻次 20-40 kHz),渦旋吹打等方式輔助溶解。
純度 & 產(chǎn)品資料

純度: 99.90%

參考文獻

完整儲備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液;一旦配成溶液,請分裝保存,避免反復凍融造成的產(chǎn)品失效
儲備液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C儲存時,請在6個月內(nèi)使用,-20°C儲存時,請在1個月內(nèi)使用。

可選溶劑 濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.3903 mL 11.9517 mL 23.9034 mL 59.7586 mL
5 mM 0.4781 mL 2.3903 mL 4.7807 mL 11.9517 mL
10 mM 0.2390 mL 1.1952 mL 2.3903 mL 5.9759 mL
15 mM 0.1594 mL 0.7968 mL 1.5936 mL 3.9839 mL
20 mM 0.1195 mL 0.5976 mL 1.1952 mL 2.9879 mL
25 mM 0.0956 mL 0.4781 mL 0.9561 mL 2.3903 mL
30 mM 0.0797 mL 0.3984 mL 0.7968 mL 1.9920 mL
40 mM 0.0598 mL 0.2988 mL 0.5976 mL 1.4940 mL
50 mM 0.0478 mL 0.2390 mL 0.4781 mL 1.1952 mL
60 mM 0.0398 mL 0.1992 mL 0.3984 mL 0.9960 mL
80 mM 0.0299 mL 0.1494 mL 0.2988 mL 0.7470 mL
100 mM 0.0239 mL 0.1195 mL 0.2390 mL 0.5976 mL
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  • 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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產(chǎn)品名稱:
Juglanin
目錄號:
HY-N3442
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