Capsaicin(Synonyms: 辣椒素; (E)-Capsaicin)

Capsaicin (Synonyms: 辣椒素; (E)-Capsaicin) 纯度: 99.85%

Capsaicin ((E)-Capsaicin) 是辣椒中的活性成分,是一种 TRPV1 激动剂。Capsaicin 具有减轻疼痛、抗氧化、抗炎、神经保护和抗癌作用。

Capsaicin(Synonyms: 辣椒素; (E)-Capsaicin)

Capsaicin Chemical Structure

CAS No. : 404-86-4

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生物活性

Capsaicin ((E)-Capsaicin), an active component of chili peppers, is a TRPV1 agonist. Capsaicin has pain relief, antioxidant, anti-inflammatory, neuroprotection and anti-cancer effects[1][2].

IC50 & Target

EC50: 290 nM (hTRPV1, in HEK293 cell)[1]

体外研究
(In Vitro)

Capsaicin (50-300 µM; 24-72 hours) shows an augmented decrease in cell growth in a dose- and time-dependent manner. The observed IC50 value is around 150 µM[2].
Capsaicin (50-300 µM; 24-72 hours) shows increase in cytosolic cytochrome c, activation of caspase 3 and PARP (p85) levels, and decreases anti-apoptotic Bcl-2 protein and increases pro-apoptotic Bad/Bax expression[2].
Capsaicin increases the nuclear condensation, nuclear DNA fragmentation and sub-G1 DNA content[2].
Capsaicin suppresses the cell cycle progression at the G1/S phase in FaDu cells by decreasing the expression of the regulators of cyclin B1 and D1, as well as cyclin-dependent protein kinases cdk-1, cdk-2 and cdk-4[2].

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

Cell Viability Assay[2]

Cell Line: Human pharyngeal squamous carcinoma cells (FaDu) cells
Concentration: 50 µM, 100 µM, 200 µM, and 300 µM
Incubation Time: 24 hours, 48 hours and 72 hours
Result: Showed an augmented decrease in cell growth.

Apoptosis Analysis[2]

Cell Line: FaDu cells
Concentration: 50 µM, 100 µM and 200 µM
Incubation Time: 12 hours
Result: Increased the activity of caspase 3 in a time-dependent manner.

Western Blot Analysis[2]

Cell Line: FaDu cells
Concentration: 200 µM
Incubation Time: 24 hours
Result: The observed activation of caspase 3 and PARP (p85) levels.

体内研究
(In Vivo)

Capsaicin suppresses the development of lung carcinoma by amending the protein expressions of apoptotic regulators p53, Bcl-2, Bax and caspase-3[2].

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

Animal Model: Swiss albino mice (20-25 g; 8-10 weeks old) induced by Benzo(a)pyrene[3]
Dosage: 10 mg/kg
Administration: Intraperitoneal administration; once in a week; for 14 weeks
Result: Inhibited the development of mice lung carcinogenesis.

Clinical Trial

分子量

305.41

Formula

C18H27NO3

CAS 号

404-86-4

中文名称

辣椒素;辣椒碱

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶解性数据
In Vitro: 

Ethanol : 200 mg/mL (654.86 mM; Need ultrasonic)

DMSO : 100 mg/mL (327.43 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.2743 mL 16.3714 mL 32.7429 mL
5 mM 0.6549 mL 3.2743 mL 6.5486 mL
10 mM 0.3274 mL 1.6371 mL 3.2743 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 (protect from light)。-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% EtOH    90% corn oil

    Solubility: ≥ 20 mg/mL (65.49 mM); Clear solution

    此方案可获得 ≥ 20 mg/mL (65.49 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 200.0 mg/mL 的澄清 EtOH 储备液加到 900 μL玉米油中,混合均匀。

  • 2.

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

    Solubility: ≥ 2.5 mg/mL (8.19 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (8.19 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

  • 3.

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

    Solubility: ≥ 2.5 mg/mL (8.19 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (8.19 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
  • 4.

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

    Solubility: ≥ 2.5 mg/mL (8.19 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (8.19 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 MCE 网站选购。
参考文献
  • [1]. McNamara FN, et al. Effects of piperine, the pungent component of black pepper, at the human vanilloid receptor (TRPV1). Br J Pharmacol. 2005 Mar;144(6):781-90.

    [2]. Shin YH, et al. The Effect of Capsaicin on Salivary Gland Dysfunction. Molecules. 2016 Jun 25;21(7).

    [3]. Anandakumar P, et al. Capsaicin provokes apoptosis and restricts benzo(a)pyrene induced lung tumorigenesis in Swiss albino mice. Int Immunopharmacol. 2013 Jun 6;17(2):254-259.