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Capsiate is a key ingredient in the fruits of a nonpungent cultivar of Capsicum annuum . We investigated the effects of a C. annuum extract (CE) and a capsiate-rich fraction of CE (CR) on nuclear receptors involved in multiple signaling pathways, glucose uptake, and adipogenesis in comparison to pure capsiate (Ca). Similar to the effect of Ca (100 μM), CE (500 μg/mL) and CR (100 μg/mL) caused the activation of PPARα and PPARγ (>3-fold), while CR also activated LXR and NRF2 (>2 fold). CR (200 μg/mL) and Ca (100 μM) decreased lipid accumulation (22.6 ± 14.1 and 49.7 ± 7.3%, respectively) in adipocytes and increased glucose uptake (44.7 ± 6.2 and 30.1 ± 12.2%, respectively) in muscle cells and inhibited the adipogenic effect induced by rosiglitazone by 41.2 ± 5.6 and 13.9 ± 4.3%, respectively. This is the first report to reveal the agonistic action of CR and Ca on multiple nuclear receptors along with their enhanced glucose uptake and antiadipogenic effects. The results indicate the potential utility of the capsiate-rich fraction of C. annuum in alleviating the symptoms of metabolic syndrome and in preventing the undesired adipogenic effects of full PPARγ agonists such as rosiglitazone.

Capsaicinoids and capsinoids are bioactive compounds mostly found in peppers. Although preclinical studies have reported that these compounds can improve exercise performance due to transient receptor potential vanilloid subtype 1 (TRPV1)-mediated thermogenesis, sympathetic modulation, and releasing calcium, it is still unclear how they affect exercise performance in humans as ergogenic supplements. Conducted according to the Preferred Reporting Items for Systematic Reviews and Meta-Analyses reporting guide 2020, this systematic review examined the ergogenic effect of capsaicinoids and capsinoids on exercise performance in healthy adults. A total of 19 randomized placebo-controlled trials were included in the study. Studies were accessed by searching five databases (PubMed, Scopus, SPORTDiscus, Web of Science, and Cochrane Library). The quality of the studies was evaluated using the Cochrane risk-of-bias assessment tool. According to the study results, 10 studies examining the effect of capsaicinoid and capsinoid supplements on exercise performance reported positive effects. Also, the effect of capsaicinoids and capsinoids on exercise performance is more pronounced in resistance training. This difference, which varies according to the type of exercise, may be due to the correlation between capsaicin transient receptor potential vanilloid subtype 1 and insulin-like growth factor-1.

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.

Background: Sarcopenia is an aging-related loss of muscle mass and function, which induces numerous adverse outcomes. Capsaicin and capsiate, separately extracted from chilies and sweet peppers, have the potential to induce muscle hypertrophy via activation of transient receptor potential vanilloid 1. The present study aimed to investigate whether chili and sweet pepper consumption are related to sarcopenia in the elderly general population., Methods: A cross-sectional study with 2,451 participants was performed. Dietary chili and sweet pepper consumption were assessed using a validated self-administered food frequency questionnaire. Sarcopenia was defined according to the consensus of the Asian Working Group for Sarcopenia. Logistic regressions were performed to measure the effect of chili and sweet pepper consumption on sarcopenia., Results: The prevalence of sarcopenia was 16.1%. After adjustment for potential confounding variables, the odds ratios (95% confidence intervals) for sarcopenia across chili and sweet pepper consumption categories were 1.00 (reference) for almost never, 0.73 (0.55, 0.97) and 0.73 (0.56, 0.96) for ≤1 time/week, 0.60 (0.39, 0.90) and 0.66 (0.45, 0.95) for ≥2-3 times/week (both P for trend <0.01), respectively., Conclusion: The present study showed that higher consumption of chilies and sweet peppers was related to a lower risk of sarcopenia in older adults.

Apple latent spherical virus (ALSV) can infect a variety of crops, usually without inducing symptoms. Partial gene sequences can be introduced into ALSV vectors for the induction of virus-induced gene silencing (VIGS). These features are beneficial for the estimation of gene functions in plants, with relatively concise experimental manipulations. Given that the infectability of chili peppers (Capsicum spp.) by ALSV was unknown, an ALSV infectivity test was performed on the highly pungent Capsicum chinense cultivar 'Habanero'. The chili pepper plants were not infected after rub-inoculation with a crude homogenate of ALSV-infected Chenopodium quinoa leaves, whereas inoculating them with a concentrated ALSV virus preparation caused an infection. Inoculation with an ALSV RNA preparation by gold particle bombardment resulted in high infection rates (about 90%). The infection was systemic and the infected plants were symptomless. For the induction of VIGS, 201-nucleotide fragments of the putative aminotransferase (pAMT) gene were introduced into the ALSV vector. These ALSV vectors infected 80-90% of RNA-inoculated chili pepper seedlings. Expression of pAMT-mRNA was repressed in the placenta of immature fruit of infected plants. The silencing of pAMT in the infected plants caused a substantial decrease in capsaicin content and a concomitant moderate accumulation of the non-pungent bioactive metabolite capsiate in these plants. These results showed that ALSV could be used to study gene functions by VIGS and to enhance capsiate accumulation in chili pepper through genetic modification., (Copyright © 2019 Elsevier B.V. All rights reserved.)

A highly sensitive, selective method has been developed and validated for determination of capsiate and dihydrocapsiate for the first time using HPLC-ESI/MS(QTOF). For both capsinoids, LODs and LOQs were 0.02 and 0.05 µmol/l, respectively. The intra- and interday repeatability values (RSD %) were 0.26-0.41% for retention time, and 2.25-2.11% for peak area. Recoveries were up to 98% and 97% for capsiate and dihydrocapsiate, respectively. This method was successfully applied to quantify capsiate and dihydrocapsiate in eight pepper fruit accessions. Capsinoids were found in the range of 1.21-544.59 μg/g DW for capsiate and of 0.61-81.95 μg/g DW for dihydrocapsiate. In the 'Tabasco' accession, capsiate and dihydrocapsiate were quantified for the first time, ranging from 3.09 to 58.76 and 1.80 to 6.94 μg/g DW, respectively. Additionally, the ESI-MS/MS(QTOF) analysis has allowed the tentative identification of two other minor capsinoids by exact mass and fragmentation pattern, in the 'Bhut Jolokia' accession., (Copyright © 2018 Elsevier Ltd. All rights reserved.)

Chili peppers exhibit antiobesity, anticancer, antidiabetic, and pain- and itch-relieving effects on animals and humans; these effects are due to capsaicin, which is the main pungent and biologically active component of pepper. Capsiate, a nonpungent capsaicin analogue, is similar to capsaicin in terms of structure and biological activity. In this study, we investigated whether capsaicin and capsiate exhibit the same hypoglycemic effects on rats with type 1 diabetes (T1D). Experimental rats were categorized into four groups: control, model, capsaicin, and capsiate groups. The two treatment groups were treated orally with 6 mg/kg bw capsaicin and capsiate daily for 28 days. Treatment with capsaicin and capsiate increased body weight, increased glycogen content, and inhibited intestinal absorption of sugar in T1D rats. Particularly, insulin levels were increased from 14.9 ± 0.76 mIU/L (model group) to 22.4 ± 1.39 mIU/L (capsaicin group), but the capsiate group (16.7 ± 0.79 mIU/L) was increased by only 12.2%. Analysis of the related genes suggested that the transient receptor potential vanilloid 1 (TRPV1) receptor was activated by capsaicin. Liver X receptor and pancreatic duodenum homeobox 1 controlled the glycometabolism balance by regulating the expression levels of glucose kinase, glucose transport protein 2 (GLUT2), phosphoenolpyruvate carboxykinase, and glucose-6-phosphatase, leading to reduced blood glucose levels in T1D rats. Meanwhile, the hypoglycemic effect was enhanced by the down-regulated expression of sodium glucose cotransporter 1, GLUT2, and GLUT5 in the intestine. The results showed that the spicy characteristics of capsaicin might be the root of its ability to decrease blood glucose.

Capsiate is a non-pungent analogue of capsaicin. Consumed worldwide, capsiate hitherto remains unexplored despite its proven track record as a food ingredient and recent use for its therapeutic profile. Though possessing a much better safety profile and an equivalent therapeutic potential, the molecule has not been extensively explored in scientific research pertaining to either food or therapeutic sciences. This comprehensive review summarizes the studies demonstrating the therapeutic potential of capsiate in various pathological conditions. The mechanistic pathways for these pharmacological activities are also deliberated upon. Discussed also are various patents that have been filed for various innovative uses of capsiate. The molecule has been successfully explored in treatment of obesity, metabolic disorders, cancer, cardiovascular disorders and gastro-intestinal disorders. It, however, faces the challenge of low aqueous solubility and stability. The lack of popularity of this immensely useful therapeutic nutraceutical probably accrues from these two factors. Designing an effective dosage form with complete absence of water is a challenge in itself. The capsules available in the market for its anti-obesity effect are also oily in nature. The challenge further intensifies when topical delivery across the mucous membrane of skin is targeted. The approaches that may be used for exploration of this drug in conditions like weight management, cancer, pain, diabetes, dysphagia, skin diseases and muscle atrophy include solid lipid nanoparticles, polymer nanoparticles, dendrimers, non-aqueous nanoemulsions and even liquid/solid self-nanoemulsifying drug delivery systems that may be reconstituted at the time of injection. • Conventional and modern methods for isolation of capsiate. • Chemical and enzymatic strategies for synthesis of capsiate. • Therapeutic benefits of capsiate due to activation of TRPV1 receptors. • Patents on the isolation, formulation development and pharmacological actions of capsiate. [ABSTRACT FROM AUTHOR]

Various methods to synthesize capsinoids (the nonpungent analogs of capsaicinoids) from precursor molecules have been reported. Capsinoids are also naturally present, at typically low concentrations, in the fruit of many Capsicum species and genotypes. However, they are also present in the fruit of select genotypes at high concentrations. The fruit of high-capsiate genotypes represents a commercial source of these compounds. To date, no method has been published that efficiently extracts and purifies capsinoids from Capsicum fruit in a rapid and simple bulk process. This study evaluated the efficacy of various organic solvents for the extraction of capsinoids from dried Capsicum annuum fruit. Among the organic solvents evaluated, pentane appeared to provide a good combination of both recovery and purity. A subsequent liquid/liquid extraction step, utilizing pentane and acetonitrile, resulted in 26.3% (wt/wt) capsiate and 19.4% (wt/wt) dihydrocapsiate for a combined capsinoids yield of 45.7% (wt/wt). A third step, involving a rapid hp20ss chromatography column using a water/acetonitrile gradient, resulted in a combined capsinoids yield of 96.6% (wt/wt). [ABSTRACT FROM AUTHOR]