Resveratrol(Synonyms: 白藜芦醇; trans-Resveratrol; SRT501)

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Resveratrol (Synonyms: 白藜芦醇; trans-Resveratrol; SRT501) 纯度: 99.70%

Resveratrol (trans-Resveratrol; SRT501) 是一种天然多酚,具有抗氧化,抗炎,保护心脏和抗癌的特性。 它的靶点广泛,如 mTORJAKβ-amyloidAdenylyl cyclaseIKKβDNA polymerase。Resveratrol 也是一种特异性的 SIRT1 活化剂。Resveratrol 是有效的孕烷 X 受体 (PXR) 抑制剂。Resveratrol 是一种 Nrf2 激活剂,在小鼠模型中可以改善衰老相关的进行性肾损伤。Resveratrol 作用于内皮细胞促进 NO 产生。

Resveratrol(Synonyms: 白藜芦醇; trans-Resveratrol;  SRT501)

Resveratrol Chemical Structure

CAS No. : 501-36-0

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生物活性

Resveratrol (trans-Resveratrol; SRT501), a natural polyphenolic phytoalexin that possesses anti-oxidant, anti-inflammatory, cardioprotective, and anti-cancer properties. Resveratrol (SRT 501) has a wide spectrum of targets including mTOR, JAK, β-amyloid, Adenylyl cyclase, IKKβ, DNA polymerase. Resveratrol also is a specific SIRT1 activator[1][2][3][4]. Resveratrol is a potent pregnane X receptor (PXR) inhibitor[5]. Resveratrol is an Nrf2 activator, ameliorates aging-related progressive renal injury in mice model[6]. Resveratrol increases production of NO in endothelial cells[7].

IC50 & Target[1]

Adenylyl cyclase

0.8 nM (IC50)

IKKβ

1 μM (IC50)

DNA polymerase α

3.3 μM (IC50)

DNA polymerase δ

5 μM (IC50)

Autophagy

 

Mitophagy

 

Sirtuin

 

体外研究
(In Vitro)

Resveratrol (trans-Resveratrol; SRT501) is one of the numerous polyphenolic compounds found in several vegetal sources In the vast majority of cases, Resveratrol displays inhibitory/activatory effects in the micromolar range, which is potentially attainable pharmacologically, although targets with affinities in the nanomolar range have also been reported[1].
MCF-7 cells are plated in DME-F12 medium supplemented with 5% FBS in the presence of increasing concentrations of Resveratrol. Control cells are treated with the same volume of vehicle only (0.1% ethanol). Resveratrol inhibits the growth of MCF-7 cells in a dose-dependent fashion. Addition of 10 μM Resveratrol results in an 82% inhibition of MCF-7 cell growth after 6 days while at 1 μM, only a 10% inhibition is observed. The cells treated with 10 μM Resveratrol have a doubling time of 60 hr whereas control cells doubled every 30 hr. Trypan blue exclusion assay shows that at concentrations of 10 μM or lower, Resveratrol does not affect cell viability (90% viable cells) whereas at 100 μM, only 50% of the cells are viable after 6 days of Resveratrol treatment. Moreover, MCF-7 cells do not undergo apoptosis after incubation with Resveratrol at concentration of 10 μM as determined by ApoAlert Annexin V Apoptosis kit[2].
Resveratrol increases the production of nitric oxide (NO) in endothelial cells by upregulating the expression of endothelial NO synthase (eNOS), stimulating eNOS enzymatic activity, and preventing eNOS uncoupling[7].

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 average tumor volume is reduced by treatment with Resveratrol (trans-Resveratrol; SRT501) at a dose of 50 mg/kg body weight (195.5±124.8 mm3; P<0.05) or 100 mg/kg body weight (81.7±70.5 mm3; P<0.001) compare with the vehicle-treated animals (315±94 mm3). There is a good correlation between the tumor volume and the tumor mass[3].

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.

Clinical Trial

分子量

228.24

Formula

C14H12O3

CAS 号

501-36-0

中文名称

白藜芦醇;虎杖甙元;茋三酚;芪三酚

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 (438.14 mM; Need ultrasonic)

Ethanol : 50 mg/mL (219.07 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 4.3814 mL 21.9068 mL 43.8135 mL
5 mM 0.8763 mL 4.3814 mL 8.7627 mL
10 mM 0.4381 mL 2.1907 mL 4.3814 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: 0.5% CMC-Na/saline water

    Solubility: 16.67 mg/mL (73.04 mM); Suspended solution; Need ultrasonic

  • 2.

    请依序添加每种溶剂: 50% PEG300    50% saline

    Solubility: 12.5 mg/mL (54.77 mM); Suspended solution; Need ultrasonic

  • 3.

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

    Solubility: 5 mg/mL (21.91 mM); Clear solution; Need ultrasonic

    此方案可获得 5 mg/mL (21.91 mM) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 50.0 mg/mL 的澄清 EtOH 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

  • 4.

    请依序添加每种溶剂: 10% EtOH    90% (20% SBE-β-CD in saline)

    Solubility: 5 mg/mL (21.91 mM); Clear solution; Need ultrasonic

    此方案可获得 5 mg/mL (21.91 mM) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 50.0 mg/mL 的澄清 EtOH 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 5.

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

    Solubility: ≥ 5 mg/mL (21.91 mM); Clear solution

    此方案可获得 ≥ 5 mg/mL (21.91 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 50.0 mg/mL 的澄清 EtOH 储备液加到 900 μL玉米油中,混合均匀。

  • 6.

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

    Solubility: ≥ 2.5 mg/mL (10.95 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (10.95 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

  • 7.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (10.95 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (10.95 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 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 8.

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

    Solubility: ≥ 2.5 mg/mL (10.95 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (10.95 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。

  • 9.

    请依序添加每种溶剂: 5% DMSO    40% PEG300    5% Tween-80    50% saline

    Solubility: ≥ 2.5 mg/mL (10.95 mM); Clear solution

  • 10.

    请依序添加每种溶剂: 5% DMSO    95% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (10.95 mM); Clear solution

*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]. Pirola L, et al. Resveratrol: one molecule, many targets. IUBMB Life. 2008 May;60(5):323-32.

    [2]. Lu R, et al. Resveratrol, a natural product derived from grape, exhibits antiestrogenic activity and inhibits the growth of human breast cancer cells. J Cell Physiol. 1999 Jun;179(3):297-304.

    [3]. Lee MH, et al. Resveratrol suppresses growth of human ovarian cancer cells in culture and in a murine xenograft model: eukaryotic elongation factor 1A2 as a potential target. Cancer Res. 2009 Sep 15;69(18):7449-58.

    [4]. Du LL, et al. Activation of sirtuin 1 attenuates cerebral ventricular streptozotocin-induced tau hyperphosphorylation and cognitive injuries in rat hippocampi. Age (Dordr). 2014 Apr;36(2):613-23.

    [5]. Smutny T, et al. Resveratrol as an inhibitor of pregnane X receptor (PXR): another lesson in PXR antagonism. J Pharmacol Sci. 2014;126(2):177-8.

    [6]. Eun Nim Kim,et al. Resveratrol, an Nrf2 activator, ameliorates aging-related progressive renal injury. Aging (Albany NY). 2018 Jan; 10(1): 83–99.

    [7]. Huige Li, et al. Resveratrol and Vascular Function. Int J Mol Sci. 2019 Apr 30;20(9):2155.

Cell Assay
[2]

To determine the effect of Resveratrol on cell growth, MCF-7 cells are plated in 6-well plates at 105 cells per well in 2 mL of DME-F12 medium supplemented with 5% FBS in the presence or absence of increasing concentrations of Resveratrol. The cell number is measured every 2 days till day 6 with a hemocytometer after detaching the cells with trypsin-EDTA[2].

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
[3]

Mice[3]
Female BALB/c (nu/nu) mice, 6 weeks old, are used. PA-1 cells (1×107 in 200 μL PBS) are injected s.c. on the right hind flank. Tumor volume (length×width×depth×0.52) is measured three times a week. After 10 days of implantation, two groups (n=10) are given Resveratrol (dissolved in 5% ethanol and 25% polyethyleneglycol 400 in distilled water) i.p. at a daily dose of 50 or 100 mg/kg body weight for consecutive 4 weeks, whereas the other group receive the vehicle only. Body weights are recorded everyday. Animals are given bromodeoxyuridine (BrdUrd; 10 mg/kg body weight, i.p.) 2 h before sacrifice. Xenograft tumors are weighed and frozen in liquid nitrogen or fixed in 10% formalin and embedded in paraffin. The BrdUrd-labeled cells in paraffin-embedded tissues are detected employing a monoclonal anti-BrdUrd antibody.

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]. Pirola L, et al. Resveratrol: one molecule, many targets. IUBMB Life. 2008 May;60(5):323-32.

    [2]. Lu R, et al. Resveratrol, a natural product derived from grape, exhibits antiestrogenic activity and inhibits the growth of human breast cancer cells. J Cell Physiol. 1999 Jun;179(3):297-304.

    [3]. Lee MH, et al. Resveratrol suppresses growth of human ovarian cancer cells in culture and in a murine xenograft model: eukaryotic elongation factor 1A2 as a potential target. Cancer Res. 2009 Sep 15;69(18):7449-58.

    [4]. Du LL, et al. Activation of sirtuin 1 attenuates cerebral ventricular streptozotocin-induced tau hyperphosphorylation and cognitive injuries in rat hippocampi. Age (Dordr). 2014 Apr;36(2):613-23.

    [5]. Smutny T, et al. Resveratrol as an inhibitor of pregnane X receptor (PXR): another lesson in PXR antagonism. J Pharmacol Sci. 2014;126(2):177-8.

    [6]. Eun Nim Kim,et al. Resveratrol, an Nrf2 activator, ameliorates aging-related progressive renal injury. Aging (Albany NY). 2018 Jan; 10(1): 83–99.

    [7]. Huige Li, et al. Resveratrol and Vascular Function. Int J Mol Sci. 2019 Apr 30;20(9):2155.

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