| Description | Capsaicin ((E)-Capsaicin) is a natural product extracted from Capsicum annuum, and is a TRPV1 agonist (EC50=0.29 μM). Capsaicin has antitumor, anti-inflammatory, antioxidant and neuroprotective activities. |
| In vitro | 方法：人咽鳞癌细胞 FaDu 用 Capsaicin (50-300 µM) 处理 24-72 h，使用 MTT Assay 检测细胞活力。结果：随着 Capsaicin 剂量的增加，用显示出细胞生长的增强下降。存活细胞的百分比随着培养时间的增加而降低。IC50 值约为 150 µM。[1]方法：人口腔表皮癌细胞 KB 用 Capsaicin (150-250 µM) 处理 24-48 h，使用 Hoechst 染色检测细胞凋亡情况。结果：Capsaicin 诱导 KB 细胞凋亡。[2] |
| In vivo | 方法：为研究对体温调节和运动活动的影响，将 Capsaicin (10-20 mg/kg，saline+3% ethanol+10% Tween 80) 单次灌胃给药给 WT 和 TRPV1 KO 的 C57BL/6J 小鼠。结果：口服 Capsaicin 会导致 TRPV1 依赖性急性低温和 TRPV1 非依赖性运动活动的长期增加，此外还会激活控制体温调节和代谢的脑回路。[3]方法：为检测神经保护活性，将 Capsaicin (5-20 mg/kg) 口服给药给给予东莨菪碱的小鼠，每天一次，持续七天。结果：Capsaicin 通过恢复线粒体功能、抗氧化作用和调节促炎细胞因子发挥经验神经保护作用。连续七天的 10 mg/kg 剂量的 Capsaicin 是最有效的剂量。[4] |
| Cell experiments | Capsaicin is dissolved in DMSO and stored, and then diluted with appropriate medium before use[3]. FaDu cells are plated at a density of 1×105 cells/well on 24-well plate. After overnight growth, the cells are treated with various concentrations of Capsaicin (0 μM, 50 μM, 100 μM, 150 μM, 200 μM, 250 μM, 300 μM, and 350 μM) for 24, 48 and 72 hours, with medium replacement every 24 hours. At the end of treatment, 30 μL of the tetrazolium compound MTT, and 270 μL of fresh medium are added. After further incubation for 4 hours at 37°C, 200 μL of 0.1 N HCl in 10% SDS is added into each well to dissolve the tetrazolium crystals. Finally, the absorbance at a wavelength of 540 nm is recorded using an ELISA plate reader[3]. |
| Target activity | TRPV1 (HEK293 cells):0.29 μM(EC50) |
| Synonyms | Qutenza, 8-Methyl-N-vanillyl-trans-6-nonenamide, 天然辣椒素, Vanilloid, 辣椒素, (E)-Capsaicin, Zostrix |
| molecular weight | 305.41 |
| Molecular formula | C18H27NO3 |
| CAS | 404-86-4 |
| Storage | keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 50 mg/mL (163.71 mM) |
| References | 1. Le TD, et al. Capsaicin-induced apoptosis of FaDu human pharyngeal squamous carcinoma cells. Yonsei Med J. 2012 Jul 1;53(4):834-4doi: 10.3349/ymj.2012.53.4.834. Erratum in: Yonsei Med J. 2012 Nov 1;53(6):1228. 2. Lin CH, et al. Capsaicin induces cell cycle arrest and apoptosis in human KB cancer cells. BMC Complement Altern Med. 2013 Feb 25;13:46. 3. Inagaki H, et al. Oral gavage of capsaicin causes TRPV1-dependent acute hypothermia and TRPV1-independent long-lasting increase of locomotor activity in the mouse. Physiol Behav. 2019 Jul 1;206:213-224. 4. Tyagi S, et al. Neuropharmacological Study on Capsaicin in Scopolamine-injected Mice. Curr Alzheimer Res. 2023;20(9):660-676. 5. Kagawa Y, et al. Investigation of capsaicin-induced superficial punctate keratopathy model due to reduced tear secretion in rats. Curr Eye Res. 2013 Jul;38(7):729-35. 6. Wang J, et al. Anti-inflammatory and retinal protective effects of capsaicin on ischaemia-induced injuries through the release of endogenous somatostatin. Clin Exp Pharmacol Physiol. 2017 Jul;44(7):803-814. 7. Xia J, Gu L, Guo Y, et al. Gut Microbiota Mediates the Preventive Effects of Dietary Capsaicin Against Depression-Like Behavior Induced by Lipopolysaccharide in Mice[J]. Frontiers in Cellular and Infection Microbiology. 2021, 11. 8. Tang K, Zhang X, Guo Y. Identification of the dietary supplement capsaicin as an inhibitor of Lassa virus entry[J]. Acta Pharmaceutica Sinica B. 2020. |