Tetrahydrocurcumin(Synonyms: 四氢姜黄素; HZIV 81-2)

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Tetrahydrocurcumin (Synonyms: 四氢姜黄素; HZIV 81-2) 纯度: ≥95.0%

Tetrahydrocurcumin 在姜黄 (Curcuma longa) 中发现的一种姜黄素,是由 Curcumin 还原产生的。Tetrahydrocurcumin 抑制 CYP2C9CYP3A4

Tetrahydrocurcumin(Synonyms: 四氢姜黄素; HZIV 81-2)

Tetrahydrocurcumin Chemical Structure

CAS No. : 36062-04-1

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生物活性

Tetrahydrocurcumin is a Curcuminoid found in turmeric (Curcuma longa) that is produced by the reduction of Curcumin. Tetrahydrocurcumin inhibit CYP2C9 and CYP3A4.

IC50 & Target[1]

CYP2C9

 

CYP3A4

 

Autophagy

 

Human Endogenous Metabolite

 

体外研究
(In Vitro)

Tetrahydrocurcumin (THC) has a number of attractive properties not shared with Curcumin that may make it superior. Tetrahydrocurcumin inhibited lipoxygenase as low as 1 μM. Tetrahydrocurcumin is tested for its ability to inhibit CYP2C9, CYP3A4, CYP1A2 and CYP2D6. Tetrahydrocurcumin yields dose-dependent inhibition of CYP2C9, and to a lesser extent, CYP3A4. Tetrahydrocurcumin exhibits maximum inhibition of CYP2C9 and CYP3A4 at 50 to 100 μM. Tetrahydrocurcumin does not show a consistent dose-response inhibition of CYP1A2 or CYP2D6 over the range of concentrations tested. In some cases, the percent inhibition exceeds 100%. The effect of Tetrahydrocurcumin on cancer cell viability is measured. Sup-T1 cells, T-cell lymphoblastic lymphoma cells, are treated with Tetrahydrocurcumin to determine its ability to induce growth inhibition using an MTS assay, and the corresponding IC50 values are in the mid-to-high micromolar range[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

The serum Tetrahydrocurcumin (THC) concentration versus time curve shows that more than one absorption and distribution phase is present. Initially, a rapid absorption phase with an average Tmax of 6.8 μg/mL at 1 h is observed, followed by a short elimination phase. This is followed by two redistributions with two smaller Tetrahydrocurcumin maxima at 6 and 24 h. Both redistribution phases has similar maxima of about 1 μg/mL. The total amount of Tetrahydrocurcumin excrets unchanged in urine was up to 8 μg at 24 h[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

372.41

Formula

C21H24O6

CAS 号

36062-04-1

中文名称

四氢姜黄素

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
In Vitro: 

DMSO : 100 mg/mL (268.52 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.6852 mL 13.4261 mL 26.8521 mL
5 mM 0.5370 mL 2.6852 mL 5.3704 mL
10 mM 0.2685 mL 1.3426 mL 2.6852 mL

*

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。

In Vivo:

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

  • 1.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (6.71 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.71 mM,饱和度未知) 的澄清溶液。

    以 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;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (6.71 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.71 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    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。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献
  • [1]. Novaes JT, et al. Disposition, Metabolism and Histone Deacetylase and Acetyltransferase Inhibition Activity of Tetrahydrocurcumin and Other Curcuminoids. Pharmaceutics. 2017 Oct 12;9(4). pii: E45.

Cell Assay
[1]

Sup-T1 cells are cultured in RPMI 1640 supplemented with 10% FBS and 1% Penicillin/Streptomycin at 37°C and 5% CO22. 2×105 cells/mL are seeded in each well and Tetrahydrocurcumin, Curcumin and Calebin-A, at 0.1, 0.5, 1.0, 5.0, 10.0, 50.0 and 100.0 μM dissolved in DMSO, are added to their respective wells and incubated for 24, 48 and 72 h. The MTS reagent is added and incubated for 4 h. Absorbance is recorded at 490 nm in Synergy HT multi-well plate reader and Gen5 data analysis software[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

Rats[1]
Surgically-modified, exposed jugular vein-catheterized, adult male CD Sprague-Dawley rats (250–300 g) ared used. Each rat is placed in a separate metabolic cage and fasted for 12 h prior to dosing with free access to water. On the day of experiment, the animals (N=3) receive a single dose of Tetrahydrocurcumin by oral gavage (500 mg/kg) in a volume not exceeding 1 mL. Animals have free access to water pre- and post-dosing, and food is provided 2 hours post-dosing. A series of blood samples (0.3 mL) are collected at 0, 15 and 30 min, and 1, 2, 4, 6, 12, 24, 48 and 72 h post-dose. At 72 h after administration, the animals are euthanized and exsanguinated. Immediately after each blood collection time point (except the terminal point), the cannula is flushed with 0.3 mL of 0.9% saline to replenish the collected blood volume. The dead volume of the cannula is replaced with sterile heparin/50% dextrose catheter lock solution to maintain the patency of the cannula as advised in the technical sheet supplied with the animals from Charles River. Following centrifugation of blood samples at 15,000 rpm for 5 min, serum is collected and placed into 2 mL tubes at -20°C until further analysis. Urine samples are collected at 0, 2, 6, 12, 24, 48 and 72 h post-dose and placed in 15 mL tubes. The exact urine volume of each sample is recorded then stored at -20°C until further analysis[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献
  • [1]. Novaes JT, et al. Disposition, Metabolism and Histone Deacetylase and Acetyltransferase Inhibition Activity of Tetrahydrocurcumin and Other Curcuminoids. Pharmaceutics. 2017 Oct 12;9(4). pii: E45.

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