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Capsiate Sale

(Synonyms: 辣椒素酯) 目录号 : GC49433

A capsaicin analog with diverse biological activities

Capsiate Chemical Structure

Cas No.:205687-01-0

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10 mg
¥2,707.00
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25 mg
¥6,424.00
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50 mg
¥12,180.00
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产品描述

Capsiate is a non-pungent analog of capsaicin that has been found in C. annuum and has diverse biological activities.1,2,3,4 It inhibits Src in, as well as VEGF-induced proliferation of and tube formation by, human umbilical vein endothelial cells (HUVECs) when used at concentrations ranging from 5 to 25 µM.1 Capsiate activates transient receptor potential vanilloid 1 (TRPV1) in HEK293 cells expressing the human channel (EC50 = 290 nM) and induces licking and biting behaviors, markers of nociception, in mice.2 Topical application of capsiate reduces antigen-induced increases in ear thickness in a mouse model of passive cutaneous anaphylaxis and decreases epidermal thickness and eosinophil and mast cell infiltration in a mouse model of atopic dermatitis.3 Capsiate (10 mg/kg) decreases body weight gain and perirenal fat weight, as well as increases oxygen consumption, fat oxidation, and carbohydrate oxidation, in a mouse model of ad libitum feeding-induced weight gain.4

1.Pyun, B.-J., Choi, S., Lee, Y., et al.Capsiate, a nonpungent capsaicin-like compound, inhibits angiogenesis and vascular permeability via a direct inhibition of Src kinase activityCancer Res.68(1)227-235(2008) 2.Iida, Y., Kobata, T.M., Morita, A., et al.TRPV1 activation and induction of nociceptive response by a non-pungent capsaicin-like compound, capsiateNeuropharmacology44(7)958-967(2003) 3.Lee, J.J., Lee, Y.S., Lee, E.-J., et al.Capsiate inhibits DNFB-induced atopic dermatitis in NC/Nga mice through mast cell and CD4+ T-cell inactivationJ. Invest. Dermatol.135(8)1977-1985(2015) 4.Haramizu, S., Kawabata, F., Ohnuki, K., et al.Capsiate, a non-pungent capsaicin analog, reduces body fat without weight rebound like swimming exercise in miceBiomed. Res.32(4)279-284(2011)

Chemical Properties

Cas No. 205687-01-0 SDF
别名 辣椒素酯
Canonical SMILES CC(C)/C=C/CCCCC(OCC1=CC(OC)=C(C=C1)O)=O
分子式 C18H26O4 分子量 306.4
溶解度 DMF: 30 mg/ml,DMSO: 30 mg/ml,Ethanol: 30 mg/ml 储存条件 -20°C
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1 mM 3.2637 mL 16.3185 mL 32.6371 mL
5 mM 0.6527 mL 3.2637 mL 6.5274 mL
10 mM 0.3264 mL 1.6319 mL 3.2637 mL
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Research Update

The gut microbiota metabolite Capsiate promotes Gpx4 expression by activating TRPV1 to inhibit intestinal ischemia reperfusion-induced ferroptosis

Gut Microbes 2021 Jan-Dec;13(1):1-21.PMID:33779497DOI:10.1080/19490976.2021.1902719.

Ferroptosis, a new type of cell death has been found to aggravate intestinal ischemia/reperfusion (I/R) injury. However, little is known about the changes of gut microbiota and metabolites in intestinal I/R and the role of gut microbiota metabolites on ferroptosis-induced intestinal I/R injury. This study aimed to establish a mouse intestinal I/R model and ileum organoid hypoxia/reoxygenation (H/R) model to explore the changes of the gut microbiota and metabolites during intestinal I/R and protective ability of Capsiate (CAT) against ferroptosis-dependent intestinal I/R injury. Intestinal I/R induced disturbance of gut microbiota and significant changes in metabolites. We found that CAT is a metabolite of the gut microbiota and that CAT levels in the preoperative stool of patients undergoing cardiopulmonary bypass were negatively correlated with intestinal I/R injury. Furthermore, CAT reduced ferroptosis-dependent intestinal I/R injury in vivo and in vitro. However, the protective effects of CAT against ferroptosis-dependent intestinal I/R injury were abolished by RSL3, an inhibitor of glutathione peroxidase 4 (Gpx4), which is a negative regulator of ferroptosis. We also found that the ability of CAT to promote Gpx4 expression and inhibit ferroptosis-dependent intestinal I/R injury was abrogated by JNJ-17203212, an antagonist of transient receptor potential cation channel subfamily V member 1 (TRPV1). This study suggests that the gut microbiota metabolite CAT enhances Gpx4 expression and inhibits ferroptosis by activating TRPV1 in intestinal I/R injury, providing a potential avenue for the management of intestinal I/R injury.

Effects of Capsaicin and Capsiate on Endurance Performance: A Meta-Analysis

Nutrients 2022 Oct 28;14(21):4531.PMID:36364793DOI:10.3390/nu14214531.

Several studies have explored the effects of capsaicin and Capsiate on endurance performance, with conflicting findings. This systematic review aimed to perform a meta-analysis examining the effects of capsaicin and Capsiate vs. placebo on endurance performance in humans. Seven databases were searched to find eligible studies. The effects of capsaicin and Capsiate on aerobic endurance (e.g., time-trials or time-to-exhaustion tests), muscular endurance (e.g., repetitions performed to muscular failure), and rating of perceived exertion (RPE) were examined in a random-effects meta-analysis. Fourteen studies (n = 183) were included in the review. Most studies provided capsaicin or Capsiate in the dose of 12 mg, 45 min before exercise. In the meta-analysis for aerobic endurance, there was no significant difference between the placebo and capsaicin/Capsiate conditions (Cohen's d: 0.04; 95% confidence interval: -0.16, 0.25; p = 0.69). In subgroup meta-analyses, there were no significant differences between the placebo and capsaicin/Capsiate conditions when analyzing only studies that used time-trials (p = 0.20) or time-to-exhaustion tests (p = 0.80). In the meta-analysis for muscular endurance, a significant ergogenic effect of capsaicin/Capsiate was found (Cohen's d: 0.27; 95% confidence interval: 0.10, 0.43; p = 0.002). When analyzing set-specific effects, an ergogenic effect of capsaicin/Capsiate was found in set 1, set 2, and set 3 (Cohen's d: 0.21-29). Capsaicin/Capsiate ingestion reduced RPE following muscular endurance (p = 0.03) but not aerobic endurance tests (p = 0.58). In summary, capsaicin/Capsiate supplementation acutely enhances muscular endurance, while the effects on aerobic endurance are less clear.

Improvement of Lipid and Glucose Metabolism by Capsiate in Palmitic Acid-Treated HepG2 Cells via Activation of the AMPK/SIRT1 Signaling Pathway

J Agric Food Chem 2018 Jul 5;66(26):6772-6781.PMID:29886733DOI:10.1021/acs.jafc.8b01831.

Capsiate, a nonpungent ingredient of CH-19 Sweet, exhibits anti-obesity effects on animals and humans. This study investigated the effects and molecular mechanism of Capsiate on lipid and glucose metabolism in PA-treated HepG2 cells. Results showed that compared with the PA-alone group, 100 μM Capsiate inhibited lipid accumulation, decreased TG (0.0562 ± 0.0142 vs 0.0381 ± 0.0055 mmol/g of protein; P = 0.024) and TC (0.1087 ± 0.0037 vs 0.0359 ± 0.0059 mmol/g of protein; P = 0.000) levels, and increased the HDL-C level (0.0189 ± 0.0067 vs 0.1050 ± 0.0106 mmol/g of protein; P = 0.000) and glycogen content (0.0065 ± 0.0007 vs 0.0146 ± 0.0008 mg/106 cells; P = 0.000) of PA-treated HepG2 cells; 100 μM Capsiate also upregulated the level of CD36 ( P = 0.000), phosphorylation of ACC ( P = 0.034), and expression of CPT1 ( P = 0.013) in PA-treated HepG2 cells, leading to an enhancement of lipid metabolism. Meanwhile, 100 μM Capsiate upregulated the levels of GLUT1, GLUT4, GK, and phosphorylation of GS ( P = 0.001, 0.029, 0.000, and 0.045, respectively) and downregulated the PEPCK level ( P = 0.001) to improve glucose metabolism in PA-treated HepG2 cells. Furthermore, the levels of phosphorylation of AMPK and expression of SIRT1 in HepG2 cells were increased by a 100 μM Capsiate treatment ( P = 0.001 and 0.000, respectively), while the FGF21 level was decreased ( P = 0.003). Most of these effects were reversed by pretreatment with compound C, a selective AMPK inhibitor. Thus, Capsiate might improve lipid and glucose metabolism in HepG2 cells by activating the AMPK/SIRT1 signaling pathway.

Sweet pepper and its principle constituent Capsiate: functional properties and health benefits

Crit Rev Food Sci Nutr 2022;62(26):7370-7394.PMID:33951968DOI:10.1080/10408398.2021.1913989.

Capsiate is a non-pungent analogue of capsaicin. It belongs to the family of capsinoids which are esters of vanillyl alcohol with fatty acids while capsaicin belongs to the family of capsaicinoids that are amides of vanillylamine with a variety of branched-chain fatty acids. While capsaicin is extensively reported for plethora of pharmacological actions, Capsiate remains much less explored. Extracted from various species of Capsicum plant, the molecule has also been chemically synthesized via a number of synthetic and enzymatic routes. Based on its action on transient receptor potential vanilloid subfamily member 1 receptors, recent research has focused on its potential roles in treatment of obesity, metabolic disorders, cancer, cardiovascular disorders and gastro-intestinal disorders. Its toxicity profile has been reported to be much safe. The molecule, however, faces the challenge of low aqueous solubility and stability. It has been commercialized for its use as a weight loss supplement. However, the therapeutic potential of the compound which is much beyond boosting metabolism remains unexplored hitherto. This comprehensive review summarizes the studies demonstrating the therapeutic potential of Capsiate in various pathological conditions. Discussed also are potential future directions for formulation strategies to develop efficient, safe and cost-effective dosage forms of Capsiate to explore its role in various disease conditions. The databases investigated include Cochrane library, Medline, Embase, Pubmed and in-house databases. The search terms were "Capsiate," "capsinoids," "thermogenesis," and their combinations. The articles were screened for relevance by going through their abstract. All the articles pertaining to physicochemical, physiological, pharmacological and therapeutic effects of Capsiate have been included in the manuscript.

Capsiate treatment in liver surgeries may compromise its recovery

Acta Cir Bras 2018 May;33(5):439-445.PMID:29924209DOI:10.1590/s0102-865020180050000006.

Purpose: To investigate the effects of Capsiate treatment on hepatic hyperplasia in partially hepatectomized rats. Methods: The animals were divided into a Capsiate group (CPH), a Capsiate Post-Partial Hepatectomy group (CPPH) and a Partial Hepatectomy Control group (PH). CPH and CPPH animals received 60 mg/kg/day Capsiate for 30 days. Next, the rats underwent partial hepatectomy. CPPH animals continued to receive treatment for 48 h after partial hepatectomy. Liver tissue and intracardiac blood samples were obtained 24 or 48 h after PH. Results: Capsiate treatment interfered with hepatic parameters, reducing the number of mitoses and apoptosis and increasing blood ALT and alkaline phosphatase concentrations. Conclusion: Capsiate treatment preceding hepatic surgery may compromise the initial period of postoperative recovery.