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Curcumin (姜黃素)

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  • 型號

    HY-N0005

  • 品牌

    MCE

  • 廠商性質(zhì)

    代理商

  • 所在地

    杭州市

規(guī)格

100mg 450元 10000支可售

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CAS號 458-37-7 產(chǎn)地 國產(chǎn)
規(guī)格 100mg 級別 化工級
證書 ISO系列證書
Curcumin (Diferuloylmethane),是一種天然酚類化合物,是乙酰轉(zhuǎn)移酶 p300/CREB 結合蛋白 特異性抑制劑,抑制組蛋白/非組蛋白的乙?;徒M蛋白乙酰轉(zhuǎn)移酶依賴的染色質(zhì)轉(zhuǎn)錄。Curcumin 對 NF-κb 和 MAPKs 有抑制作用,并具有抗yan、抗氧化、抗增殖和抗血管生成等多種藥理作用。Curcumin 通過 Keap1 半胱an酸修飾誘導 Nrf2 蛋白的穩(wěn)定。

Curcumin  (Synonyms: 姜黃素; Diferuloylmethane; Natural Yellow 3; Turmeric yellow)

Curcumin (Diferuloylmethane),是一種天然酚類化合物,是乙酰轉(zhuǎn)移酶 p300/CREB 結合蛋白 特異性抑制劑,抑制組蛋白/非組蛋白的乙?;徒M蛋白乙酰轉(zhuǎn)移酶依賴的染色質(zhì)轉(zhuǎn)錄。Curcumin 對 NF-κb 和 MAPKs 有抑制作用,并具有抗yan、抗氧化、抗增殖和抗血管生成等多種藥理作用。Curcumin 通過 Keap1 半胱an酸修飾誘導 Nrf2 蛋白的穩(wěn)定。

生物活性

Curcumin (Diferuloylmethane), a natural phenolic compound, is a p300/CREB-binding protein-specific inhibitor of acetyltransferase, represses the acetylation of histone/nonhistone proteins and histone acetyltransferase-dependent chromatin transcription. Curcumin shows inhibitory effects on NF-κB and MAPKs, and has diverse pharmacologic effects including anti-inflammatory, antioxidant, antiproliferative and antiangiogenic activities. Curcumin induces stabilization of Nrf2 protein through Keap1 cysteine modification.


IC50 & Target

Keap1-Nrf2[1], Histone acetyltransferase[6]


體外研究(In Vitro)

Curcumin exerts its chemopreventive effects partly through the activation of nuclear factor (erythroid-2 related) factor 2 (Nrf2) and its antioxidant and phase II detoxifying enzymes[1]. Curcumin inhibits T47D cells growth, with IC50s of 25, 19 and 17.5 μM for 24, 48 and 72 h MTT assays respectively. IC50s of curcumin and silibinin mixture against T47D cells, are 17.5, 15, and 12 μM for 24, 48, and 72 h exposure times, respectively[2]. Curcumin (2.5-80 μM) induces apoptotic cell death in AGS and HT-29 cell lines, and the IC50 is 21.9±0.1, 40.7±0.5 μM, respectively, in both AGS and HT-29 cell lines. Curcumin-induced apoptosis requires caspase activities in AGS and HT-29 cells. Curcumin induces ER Ca2+ decline and mitochondrial Ca2+ overloading[3]. Curcumin induces the G2/M cell cycle arrest of LNCaP and PC-3 cells in a dose dependent manner. Curcumin upregulates the protein level of NF-kappaB inhibitor IkappaBalpha and downregulates protein levels of c-Jun and AR[5].


體內(nèi)研究(In Vivo)

Curcumin (10 mg/kg, p.o.) significantly prevents decrease in the percentage of sucrose consumption, as compared to the CMS-exposed rats. Curcumin treatment results in significant prevention of increase in TNF-α and IL-6 levels in stressed rats[4]. Curcumin decreases binding of p300/CREB-binding protein (CBP) at the brain-derived neurotrophic factor (BDNF) promoter at 20 mg/kg (i.p.), reduces binding of P300/CBP at the BDNF promoter at 40 mg/kg, and decreases binding all the four proteins of p300/CBP and H3K9ac/H4K5ac at the BDNF promoter at 60 mg/kg in chronic constriction injury (CCI) rats[6].


Clinical Trial


NCT NumberSponsorConditionStart DatePhase
NCT01022632Government Medical College, Bhavnagar|Health and Family Welfare Department, Government of Gujarat, India|Arjuna Natural Extracts Ltd.
Major Depressive Disorder
March 2009Not Applicable
NCT00779493Kaiser Permanente
Irritable Bowel Syndrome
November 2008Phase 4
NCT03769766University of Texas Southwestern Medical Center
Prostate Cancer
March 11, 2019Phase 3


分子量:368.38


性狀:Solid


Formula:

C21H20O6


CAS 號:458-37-7


中文名稱:姜黃素;酸性黃;姜黃色素


運輸條件:Room temperature in continental US; may vary elsewhere.


儲存方式

Powder-20°C3 years

4°C2 years
In solvent-80°C6 months

-20°C1 month


溶解性數(shù)據(jù)


In Vitro: 

DMSO : 120 mg/mL (325.75 mM; Need ultrasonic)

配制儲備液
濃度溶劑體積質(zhì)量1 mg5 mg10 mg
1 mM2.7146 mL13.5729 mL27.1459 mL
5 mM0.5429 mL2.7146 mL5.4292 mL
10 mM0.2715 mL1.3573 mL2.7146 mL
*

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。-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。

In Vivo:

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

  • 1.


    請依序添加每種溶劑: 1% (w/v) carboxymethylcellulose (CMC)

    Solubility: 25 mg/mL (67.86 mM); Suspension solution; Need ultrasonic


  • 2.


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

    Solubility: ≥ 3 mg/mL (8.14 mM); Clear solution


  • 3.


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

    Solubility: 3 mg/mL (8.14 mM); Suspended solution; Need ultrasonic

參考文獻

  • [1]. Gao S, et al. Curcumin attenuates arsenic-induced hepatic injuries and oxidative stress in experimental mice through activation of Nrf2 pathway, promotion of arsenic methylation and urinary excretion. Food Chem Toxicol. 2013 Jul 18. pii: S0278-6915(13)004  [Content Brief]

    [2]. Nasiri M, et al. Curcumin and Silibinin Inhibit Telomerase Expression in T47D Human Breast Cancer Cells. Asian Pac J Cancer Prev. 2013;14(6):3449-53.  [Content Brief]

    [3]. Cao A, et all. Curcumin induces apoptosis in human gastric carcinoma AGS cells and colon carcinoma HT-29 cells through mitochondrial dysfunction and endoplasmic reticulum stress. Apoptosis. 2013 Jul 24. [Epub ahead of print]  [Content Brief]

    [4]. Jiang H, et al. Antidepressant-like effects of curcumin in chronic mild stress of rats: Involvement of its anti-inflammatory action. Prog Neuropsychopharmacol Biol Psychiatry. 2013 Jul 20. pii: S0278-5846(13)00150-4.  [Content Brief]

    [5]. Guo H, et al. Curcumin induces cell cycle arrest and apoptosis of prostate cancer cells by regulating the expression of IkappaBalpha, c-Jun and androgen receptor. Pharmazie. 2013 Jun;68(6):431-4.  [Content Brief]

    [6]. Zhu X, et al. Curcumin alleviates neuropathic pain by inhibiting p300/CBP histone acetyltransferase activity-regulated expression of BDNF and cox-2 in a rat model. PLoS One. 2014 Mar 6;9(3):e91303.  [Content Brief]

    [7]. Balasubramanyam K, et al. Curcumin, a novel p300/CREB-binding protein-specific inhibitor of acetyltransferase, represses the acetylation of histone/nonhistone proteins and histone acetyltransferase-dependent chromatin transcription. J Biol Chem. 2004 Dec  [Content Brief]

    [8]. Jun Wan Shin, et al. Curcumin induces stabilization of Nrf2 protein through Keap1 cysteine modification. Biochem Pharmacol. 2020 Mar;173:113820.  [Content Brief]

注:產(chǎn)品僅用于科研

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