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 (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(jié)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(dǎo) 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 Number	Sponsor	Condition	Start Date	Phase
NCT01022632	Government Medical College, Bhavnagar\|Health and Family Welfare Department, Government of Gujarat, India\|Arjuna Natural Extracts Ltd.	Major Depressive Disorder	March 2009	Not Applicable
NCT00779493	Kaiser Permanente	Irritable Bowel Syndrome	November 2008	Phase 4
NCT03769766	University of Texas Southwestern Medical Center	Prostate Cancer	March 11, 2019	Phase 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(yùn)輸條件：Room temperature in continental US; may vary elsewhere.

儲存方式

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 mg	5 mg	10 mg

1 mM	2.7146 mL	13.5729 mL	27.1459 mL
5 mM	0.5429 mL	2.7146 mL	5.4292 mL
10 mM	0.2715 mL	1.3573 mL	2.7146 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(fù)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?jiān)?6 個月內(nèi)使用，-20°C 儲存時，請?jiān)?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(shí)驗(yàn)結(jié)果的可靠性，澄清的儲備液可以根據(jù)儲存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的工作液，建議您現(xiàn)用現(xiàn)配，當(dāng)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(xiàn)

[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