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The main objective of this placebo-controlled, triple-blind, balanced crossover study was to assess the acute effects of phenylcapsaicin (PC) intake (2.5 mg) on intraocular pressure (IOP), ocular perfusion pressure (OPP), and heart rate (HR) during a 30-min cycling task performed at 15% of the individual maximal power. Twenty-two healthy young adults performed the cycling task 45 min after ingesting PC or placebo. IOP was measured with a rebound tonometer before exercise, during cycling (every 6 min), and after 5 and 10 min of recovery. OPP was assessed before and after exercise. HR was monitored throughout the cycling task. We found an acute increase of IOP levels related to PC consumption while cycling (mean difference = 1.91 ± 2.24 mmHg; p =.007, η p 2 =.30), whereas no differences were observed for OPP levels between the PC and placebo conditions (mean difference = 1.33 ± 8.70 mmHg; p =.608). Mean HR values were higher after PC in comparison with placebo intake (mean difference = 3.11 ± 15.87 bpm, p =.019, η p 2 =.24), whereas maximum HR did not differ between both experimental conditions (p =.199). These findings suggest that PC intake before exercise should be avoided when reducing IOP levels is desired (e.g., glaucoma patients or those at risk). Future studies should determine the effects of different ergogenic aids on IOP and OPP levels with other exercise configurations and in the long term. [ABSTRACT FROM AUTHOR]

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. [ABSTRACT FROM AUTHOR]

Background/Objectives: Mesothelioma is an aggressive cancer with limited treatment options. Mesothelioma therapy often involves a multimodal approach including surgery, radiotherapy and chemotherapy. However, the prognosis for patients remains poor. Difficult diagnosis, late symptoms when the tumor is in an advanced stage and the onset of chemotherapy resistance make mesothelioma difficult to treat. For this reason, it is essential to discover new pharmacological approaches. Capsaicin (CAPS) is the active compound of chili peppers. Based on CAPS's anticancer properties on various tumor lines and its chemo-sensitizing action on resistant cells, in this study, we evaluated the effects of CAPS on mesothelioma cells to assess its potential use in mesothelioma therapy. Methods: To evaluate antiproliferative effects of CAPS, we performed MTS assays on various mesothelioma cells, representative of all major mesothelioma subtypes. Transwell migration and wound-healing assays were used to examine the effect of CAPS on mesothelioma cell migration. We also determined the effects of CAPS on oncogenic signaling pathways by assessing the levels of AKT and MAPK activation. Results: In this study, we show that CAPS significantly reduces proliferation of both parental and cisplatin-resistant mesothelioma cells. CAPS promotes S-phase cell cycle arrest and inhibits lateral motility and migration of mesothelioma cells. Accordingly, CAPS suppresses AKT and ERK1/2 activation in MSTO-211H and NCI-H2052 cells. Our results support an antitumor effect of CAPS on cisplatin-resistant mesothelioma cells, suggesting that it may reduce resistance to cisplatin. Conclusions: Our results could pave the way for further studies to evaluate the use of CAPS for mesothelioma treatment. [ABSTRACT FROM AUTHOR]

The salivary microbiota of Italian and sub-Saharan African individuals was investigated using Nanopore sequencing technology (ONT: Oxford Nanopore Technologies). We detected variations in community composition in relation to endogenous (ethnicity, sex, and diplotypic variants of the TRPV1 gene) and exogenous (sensitivity to capsaicin) factors. The results showed that Prevotella, Haemophilus, Neisseria, Streptococcus, Veillonella, and Rothia are the most abundant genera, in accordance with the literature. However, alpha diversity and frequency spectra differed significantly between DNA pools. The microbiota in African, male TRPV1 bb/ab diplotype and capsaicin low-sensitive DNA pools was more diverse than Italian, female TRPV1 aa diplotype and capsaicin high-sensitive DNA pools. Relative abundance differed at the phylum, genus, and species level. [ABSTRACT FROM AUTHOR]

Aging is associated with a decline in oral immune function, marked by reduced levels of antimicrobial peptides such as defensins. Capsaicin, a bioactive component found in chili peppers, has been theorized to modulate immune responses through specific receptor pathways. This study examined the effects of aging on oral defensin levels and the potential mitigating role of capsaicin, mediated by the immune response in oral tissues. We conducted a comparative analysis between young and aged mice, with or without capsaicin supplementation, for 3 months. The effect of capsaicin was also studied in vitro in senescence‐induced human oral keratinocytes. We found that aging did not reduce defensin levels uniformly but did so in some instances. Capsaicin treatment increased defensin levels in these cases, potentially through transient receptor potential cation channel subfamily V member 1 (TRPV1)‐mediated pathways in the oral cavity. Capsaicin supplementation may counteract age‐related declines in oral defensin levels, enabling the maintenance of oral immune function during aging. [ABSTRACT FROM AUTHOR]

Summary: Sensory thresholds of hotness and pungent odour were determined from 120 chilli users. Three groups of Light (L), Moderate (M), and Heavy (H) chilli users were categorised based on their chilli consumption habits and sensitivity to hotness standard solutions. After the screening test, the users participated in 12 Alternative Forced Choice (AFC)‐sets, for each of three stimuli (capsaicin and 1‐Penten‐3‐One (1P3O) odour and dried chilli powder). The dried chilli 3‐AFC sample's concentration range was calculated to equate the same range of standard capsaicin stimuli for hotness sensation measurements. Concentrations of the three stimuli tested were in a range of (0.08–16.80 dry basis g L−1) for standardised dried chilli powder, (0.10–20.16 mg L−1) for capsaicin, and (0.01–2.04 μL L−1) for 1P3O. Heavy chilli users group threshold, as anticipated, indicated the highest average recognition level of stimuli in terms of pungency odour perceived from dried chilli (5.88 g L−1) and 1P3O (1.34 μL L−1), as well as for hotness sensation from dried chilli (7.19 g L−1) and capsaicin (12.79 mg L−1) samples. The magnitudes of heavy user's thresholds were exponentially higher than that of light users. At the recognition thresholds of oral hotness perception, the level of capsaicin presented in dried chilli sample was found to be much lower than the concentration of standard capsaicin sample. It was concluded that pungent odours and other flavours in dried chilli, increase hotness perception as compared with capsaicin stimulus. We also confirmed that 1P3O contributes to chilli pungent odour. [ABSTRACT FROM AUTHOR]

Objective: This study was conducted to determine the effects of capsaicin (CAP) on productive performance, blood profile, intestinal morphology, carcass and meat quality of growingfinishing pigs. Methods: Two experimental diets were offered to 36 crossbred barrows: basal diet (0% CAP) and basal diet with CAP at 0.02%. Each experimental group consisted of 18 pigs, with six replications (three each). Results: Supplementation of CAP at 0.02% decreased average daily feed intake (p = 0.003) and feed cost/gain (p = 0.056), increased return on investment (p = 0.052) and increased gain:feed ratio (p = 0.037) during the growing period. There was no effect of CAP on the growth rate. The blood urea nitrogen and nitrogen (N) levels in faeces tended to decrease (p = 0.093 and p = 0.087), whereas the basophil level increased with CAP supplementation (p = 0.029). In addition, dietary CAP supplementation decreased crypt depth (p = 0.022) and tended to increase the villus height/crypt depth ratio in the segment of the jejunum (p = 0.084). Backfat (BF) thickness (p = 0.047) was reduced by supplementing CAP. Whereas the protein content increased with CAP supplementation (p = 0.021). Using CAP in the diet of growing pigs increased the pH at 6 h postmortem (p = 0.046) and tended to increase the springiness value (p = 0.078) of the meat. In terms of meat color, CAP supplementation increased the yellowness (p = 0.029). Conclusion: Supplemental CAP improves gut morphology and blood profiles, consequently promoting productive performance as well as carcass and meat quality. [ABSTRACT FROM AUTHOR]

Due to the fusion of culinary cultures, chili products have gained widespread popularity among consumers. Capsaicin, the primary compound responsible for the spiciness of chili products, serves as a pivotal parameter in assessing the quality of chili peppers. A three-dimensional (3D) cell-based electrochemical sensor was developed to detect capsaicin by monitoring the release of hydrogen peroxide (H2O2). The working electrode utilized in this study was a screen-printed carbon electrode (SPCE) that had been modified with AuPtNPs/ZIF-8-RGO. Encapsulation of HepG2 cells within a 4.0 wt% sodium alginate gel enabled their immobilization onto the working electrode, thus serving as the biometric element for signal recording via the amperometric i-t method. H2O2 kit assays showed that H2O2 release increased with increasing capsaicin concentration over a range of concentrations. With a detection limit of 0.848 μM, the developed biosensor effectively detected capsaicin at concentrations that varied from 10 μM to 120 μM. The sensor that was developed displayed exceptional sensitivity, stability, and reliability, offering a novel method for monitoring capsaicin level in food. [ABSTRACT FROM AUTHOR]

Introduction: The resolution of the skin's inflammatory response is only possible if its barrier function is restored. TRPV1 channel activation plays an important role during inflammation but the effect of this activation on the skin barrier under inflammatory conditions has not been clarified. We hypothesize that it could potentially aid the keratinocyte barrier by reducing inflammatory cytokine release and promoting tight junction development. Methods: To explore the role of TRPV1 activation in inflammation, we designed and optimized an in vitro model of keratinocytes with basal epidermal layer characteristics using HaCaT cells and TNFα to induce inflammation. Results: TNFα increased the gene expression of tight junction protein claudin 1 (CLDN1) by at least 2.60 ± 0.16-fold, in a concentration-dependent manner, over a 48 h period. The administration of a capsaicin pre-treatment reduced the CLDN1 expression to 1.51 ± 0.16-fold during the first 6 h after TNFα induction, whereas IL-8 cytokine release was reduced 0.64 ± 0.17-fold. After 48 h, CLDN1 protein levels increased by a factor of 6.57 ± 1.39 compared to cells only treated with TNFα. Discussion: These results suggest that activation of TRPV1 by capsaicin can potentiate the increase in CLDN1 expression and CLDN1 protein synthesis induced by TNFα in cultured keratinocytes, while reducing the release of IL-8. [ABSTRACT FROM AUTHOR]

Breast cancer continues to be one of the most commonly diagnosed cancers around the world. Despite the decrease in mortality, there has been a steady increase in its incidence. There is much evidence that naturally occurring phytochemicals could prove to be safer alternatives aimed at prevention and development of breast cancer. In the present review, we discuss important phytochemicals, namely capsaicin, alpha-santalol and diallyl trisulphide that are shown to have chemopreventive and anti-tumour properties against breast cancer development. We examined current knowledge of their bioavailability, safety and modulation of molecular mechanisms including their ability to induce apoptotic cell death, promote cell cycle arrest, and inhibit cellular proliferation in different breast cancer cell lines and in vivo models. This review emphasises the importance of these naturally occurring phytochemicals and their potential of becoming therapeutic options in the arsenal against breast cancer development provided further scientific and clinical validation. [ABSTRACT FROM AUTHOR]

There is an urgent need to study safe and biocompatible medicinal compounds which necessitates the discovery of new agents from simple natural starting materials. In this study, eight novel capsaicin derivatives have been synthesized by combination of oxadiazole containing fatty acids with vanillyl amide. All the compounds were characterized by spectral analysis and were examined for their cytotoxicity, antimicrobial, antioxidant and anti‐inflammatory properties. The antioxidant activity of the synthesized derivatives was evaluated by 1,1‐diphenyl‐2‐picryl‐hydrazyl (DPPH) and thiobarbituric acid reactive substances (TBARS) assays. All of the synthesized derivatives have exhibited significant antioxidant activity in comparison to butylated hydroxy toluene (BHT) which is used as a reference antioxidant. The novel capsaicin derivatives with nitro (8 e) and methoxy substituents (8 f, 8 g and 8 h) exhibited the most significant antioxidant activity compared with BHT. In cytotoxicity assay against three cell lines, the derivative with bromo substituent showed excellent activity against B16‐melanoma cancer cell line followed by nitro and methoxy analogs which showed promising activity against HepG2‐ hepato and DU145‐prostate cancer cell lines respectively. In addition, all the derivatives exhibited moderate broad spectrum antibacterial, antifungal and anti‐inflammatory activity. [ABSTRACT FROM AUTHOR]

Purpose of Review: Diabetic neuropathy is a common complication of diabetes mellitus (DM) and can affect up to 50% of DM patients during their lifetime. Patients typically present with numbness, tingling, pain, and loss of sensation in the extremities. Since there is no treatment targeting the underlying mechanism of neuropathy, strategies focus on preventative care and pain management. Recent Findings: Up to 69% of patients with diabetic neuropathy receive pharmacological treatment for neuropathic pain. The United States Food and Drug Administration (FDA) confirmed four drugs for painful diabetic neuropathy (PDN): pregabalin, duloxetine, tapentadol, and the 8% capsaicin patch. Nonpharmacological treatments such as spinal cord stimulation (SCS) and transcutaneous electrical nerve stimulation (TENS) both show promise in reducing pain in DM patients. Summary: Despite the high burden associated with PDN, effective management remains challenging. This update covers the background and management of diabetic neuropathy, including its epidemiology, pathogenesis, preventative care, and current therapeutic strategies. [ABSTRACT FROM AUTHOR]

Cancer is a global health challenge with rising incidence and mortality rates, posing significant concerns. The World Health Organization reports cancer as a leading cause of death worldwide, contributing to nearly one in six deaths. Cancer pathogenesis involves disruptions in cellular signaling pathways, resulting in uncontrolled cell growth and metastasis. Among emerging players in cancer biology, Transient Receptor Potential (TRP) channels, notably TRPV1, have garnered attention due to their altered expression in cancer cells and roles in tumorigenesis and progression. TRPV1, also known as the capsaicin receptor, is pivotal in cancer cell death and pain mediation, offering promise as a therapeutic target. Activation of TRPV1 triggers calcium influx and affects cell signaling linked to growth and death. Additionally, TRPV1 is implicated in cancer-induced pain and chemo-sensitivity, with upregulation observed in sensory neurons innervating oral cancers. Also, when capsaicin, a compound from chili peppers, interacts with TRPV1, it elicits a "hot" sensation and influences cancer processes through calcium influx. Understanding TRPV1's multifaceted roles in cancer may lead to novel therapeutic strategies for managing cancer-related symptoms and improving patient outcomes. The current review elucidates the comprehensive role of capsaicin in cancer therapy, particularly through the TRPV1 channel, highlighting its effects in various cells via different signaling pathways and discussing its limitations. [ABSTRACT FROM AUTHOR]

Purpose: Arthritis is the one of the leading causes of disability among a large group of population. It is a slowly progressive disorder that effects the joints to a stage where they are not considerably functional and mobile. Counter Anti-inflammatory agents are among the first choice of treatments that leads to reduction in swelling, inflammation and pain primarily. Method: The current study was aimed to develop topical gels loaded with microsponges of Capsaicin. The prepared microsponges were intended to release drug in the controlled manner thus effectively managing the red flags of arthritis. Microsponges technology is recognized as a novel technology of drug delivery that provides enhanced action for longer duration. In this study Boswellia Serrata a natural resin is also incorporated with capsaicin to study the possible effects of the two when given in combination. Capsaicin was procured in the purest form by AOS Products Private Limited which was then used to prepare microsponges and were further incorporated in the form of topical gels using various concentrations of Boswellia Serrata. Results: This research focuses on the possible positive effects of Capsaicin in the form of microsponges to manage the conditions of arthritis. The prepared formulations were optimized and were evaluated on the basis of experimental outcomes. DPPH model was used to calculate the Anti- inflammatory effect of using Capsaicin loaded microsponges in combination with Boswellia Serrata resin. Conclusion: The study concludes that for management of arthritis certain naturally available agents can show equivalent efficacy and results when compared to marketed available dosage forms. Moreover, the microsponge technology ensures controlled release that provides excellent therapeutic action for extended periods of time. [ABSTRACT FROM AUTHOR]

Type 2 diabetes mellitus (T2DM) is a metabolic disease. Diabetes increases the risk of benign prostatic hyperplasia (BPH). Capsaicin is extracted from chili peppers and possesses many pharmacological properties, including anti-diabetic, pain-relieving, and anti-cancer properties. This study aimed to investigate the effects of capsaicin on glucose metabolism and prostate growth in T2DM mice and uncover the related mechanisms. Mice model of diabetes was established by administering a high-fat diet and streptozotocin. Oral administration of capsaicin for 2 weeks inhibited prostate growth in testosterone propionate (TP)-treated mice. Furthermore, oral administration of capsaicin (5 mg/kg) for 2 weeks decreased fasting blood glucose, prostate weight, and prostate index in diabetic and TP-DM mice. Histopathological alterations were measured using hematoxylin & eosin (H&E) staining. The protein expression of 5α-reductase type II, androgen receptor (AR), and prostate-specific antigen (PSA) were upregulated in diabetic and TP-DM mice, but capsaicin reversed these effects. Capsaicin decreased the protein expression of p-AKT, insulin-like growth factor-1 (IGF-1), IGF-1R, and the receptor for advanced glycation end products (RAGE) in diabetic and TP-DM mice. Capsaicin also regulated epithelial-mesenchymal transition (EMT) and modulated the expression of fibrosis-related proteins, including E-cadherin, N-cadherin, vimentin, fibronectin, α-SMA, TGFBR2, TGF-β1, and p-Smad in TP-DM mice. In this study, capsaicin alleviated diabetic prostate growth by attenuating EMT. Mechanistically, capsaicin affected EMT by regulating RAGE/IGF-1/AKT, AR, and TGF-β/Smad signalling pathways. These results provide with new therapeutic approach for treating T2DM or T2DM-induced prostate growth. [ABSTRACT FROM AUTHOR]

Sweet bell pepper (SBP, Capsicum annuum L.) can be employed as a spice in many dishes and may also be eaten as a delicious fruit. These two nutritional attributes are owing to the strong, deep taste of many SBP phytochemicals. This fruit has many additional beneficial properties because it contains high concentrations of minerals and vitamins that distinguish it from other kinds of fruits. Almost every part of the SBP is thought to be an excellent source of bioactive substances that are health supporters, such as flavonoids, polyphenols, and various aromatic substances. The ability of SBP-phytochemicals to work as antioxidants, reducing the harmful effects of oxidative stress and consequently preventing many chronic illnesses, is one of their main biomedical characteristics. These phytochemicals have good antibacterial properties, mostly against gram-positive pathogenic microbes, in addition to their anti-carcinogenic and cardio-preventive effects. So, this review aims to highlight the nutritional qualities of SBP-derived phytochemicals and their illness-alleviated characteristics. Antioxidant, anti-inflammatory, antitumor, antidiabetic, and analgesic properties are some of the ones discussed. [ABSTRACT FROM AUTHOR]

In this present study, we have extracted the Capsaicinoids & characterized by HPLC method. Our aim is to isolate and identify the presence of capsaicin and Dihydrocapsaicin in the capsicum sample grown in a soil supplemented with bacterial culture of Rhodopseudomonas species. After growing the capsicum plants for six months (180 days), the sample from the pericarp, seed and placenta of the fruit were collected and bioactive compounds were extracted by methanol & estimated for the analysis of Capsaicin and Dihydrocapsaicin. In HPLC method, the level of Capsaicin and Dihydrocapsaicin in the Capsicum fruits were quantified and considered as the most reliable and rapid method available for qualitative and quantitative analysis of Capsaicinoids Chili has diverse uses, where it is used as a spice in food, medicinal preparations, as culinary supplement and also as ornamental plants. [ABSTRACT FROM AUTHOR]

Copyright of Journal of Food Safety & Quality is the property of Journal of Food Safety & Quality Editorial Department and its content may not be copied or emailed to multiple sites or posted to a listserv without the copyright holder's express written permission. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract. (Copyright applies to all Abstracts.)

Background: Capsaicin, a bioactive compound found in peppers, is recognized for its anti-inflammatory, antioxidant, and anti-lipidemic properties. This study aimed to evaluate the effects of capsaicin on atherosclerosis progression. Methods: Apolipoprotein E knockout mice and their C57BL/6 controls were utilized to assess blood lipid profile, inflammatory status, and atherosclerotic lesions. We also examined the influence of capsaicin on cholesterol influx and efflux, and the role of TRPV1 and PPARγ signaling pathways in bone marrow-derived macrophages. Results: Capsaicin treatment reduced weight gain, visceral adiposity, blood triglycerides, and total and non-HDL cholesterol. These improvements were associated with a reduction in atherosclerotic lesions in the aorta and carotid. Capsaicin also improved hepatic oxidative and inflammatory status. Systemic inflammation was also reduced, as indicated by reduced leukocyte rolling and adhesion on the mesenteric plexus. Capsaicin decreased foam cell formation by reducing cholesterol influx through scavenger receptor A and increasing cholesterol efflux via ATP-binding cassette transporter A1, an effect primarily linked to TRPV1 activation. Conclusions: These findings underscore the potential of capsaicin as a promising agent for atherosclerosis prevention, highlighting its comprehensive role in modulating lipid metabolism, foam cell formation, and inflammatory responses. [ABSTRACT FROM AUTHOR]

The incidence of liver disease continues to rise, encompassing a spectrum from simple steatosis or non-alcoholic fatty liver disease (NAFLD) to non-alcoholic steatohepatitis (NASH), cirrhosis and liver cancer. Dietary habits in individuals with liver disease may significantly impact the treatment and prevention of these conditions. This article examines the role of chili peppers, a common dietary component, in this context, focusing on capsaicin, the active ingredient in chili peppers. Capsaicin is an agonist of the transient receptor potential vanilloid subfamily 1 (TRPV1) and has been shown to exert protective effects on liver diseases, including liver injury, NAFLD, liver fibrosis and liver cancer. These protective effects are attributed to capsaicin's anti-oxidant, anti-inflammatory, anti-steatosis and anti-fibrosis effects. This article reviewed the different molecular mechanisms of the protective effect of capsaicin on liver diseases. [ABSTRACT FROM AUTHOR]

Introduction: The a6 subunit-containing GABAA receptors (a6GABAARs) are highly expressed in the trigeminal ganglia (TG), the sensory hub of the trigeminovascular system (TGVS). Hypo-GABAergic transmission in the TG was reported to contribute to migraine-related behavioral and histopathological phenotypes. Previously, we found that Compound 6, an a6GABAAR-selective positive allosteric modulator (PAM), significantly alleviated TGVS activationinduced peripheral and central sensitization in a capsaicin-induced migrainemimicking model. Methods: Here, we tested whether the deuterated analogues of Compound 6, namely DK-1-56-1 and RV-I-29, known to have longer half-lives than the parent compound, can exert a similar therapeutic effect in the same model. The activation of TGVS was triggered by intra-cisternal (i.c.) instillation of capsaicin in male Wistar rats. Centrally, i.c. capsaicin increased the quantity of c-Fosimmunoreactive (c-Fos-ir) neurons in the trigeminal cervical complex (TCC). Peripherally, it increased the calcitonin gene-related peptide immunoreactivity (CGRP-ir) in TG, and caused CGRP release, leading to CGRP depletion in the dura mater. Results: DK-I-56-1 and RV-I-29, administered intraperitoneally (i.p.), significantly ameliorated the TCC neuronal activation, TG CGRP-ir elevation, and dural CGRP depletion induced by capsaicin, with DK-I-56-1 demonstrating better efficacy. The therapeutic effects of 3 mg/kg DK-I-56-1 are comparable to that of 30 mg/kg topiramate. Notably, i.p. administered furosemide, a blood-brain-barrier impermeable a6GABAAR-selective antagonist, prevented the effects of DK-I-56-1 and RV-I-29. Lastly, orally administered DK-I-56-1 has a similar pharmacological effect. Discussion: These results suggest that DK-I-56-1 is a promising candidate for novel migraine pharmacotherapy, through positively modulating TG a6GABAARs to inhibit TGVS activation, with relatively favourable pharmacokinetic properties. [ABSTRACT FROM AUTHOR]

Background: Lipid droplet (LD) is a metabolically active organelle, which changes dynamically with the metabolic state and energy requirements of cells. Proteins that either insert into the LD phospholipid monolayer or are present in the cytoplasm, playing a crucial role in lipid homeostasis and signaling regulation, are known as LD-associated proteins. Methods: The keywords "lipid droplets" and "metabolic diseases" were used to obtain literature on LD metabolism and pathological mechanism. After searching databases including Scopus, OVID, Web of Science, and PubMed from 2013 to 2024 using terms like "lipid droplets", "lipid droplet-associated proteins", "fatty liver disease", "diabetes", "diabetic kidney disease", "obesity", "atherosclerosis", "hyperlipidemia", "natural drug monomers" and "natural compounds", the most common natural compounds were identified in about 954 articles. Eventually, a total of 91 studies of 10 natural compounds reporting in vitro or in vivo studies were refined and summarized. Results: The most frequently used natural compounds include Berberine, Mangostin, Capsaicin, Caffeine, Genistein, Epigallocatechin-3-gallate, Chlorogenic acid, Betaine, Ginsenoside, Resveratrol. These natural compounds interact with LD-associated proteins and help ameliorate abnormal LDs in various metabolic diseases. Conclusion: Natural compounds involved in the regulation of LDs and LD-associated proteins hold promise for treating metabolic diseases. Further research into these interactions may lead to new therapeutic applications. [ABSTRACT FROM AUTHOR]

Although there are numerous available immunomodulators, those of natural origin would be preferable based on their safety profile and effectiveness. The research and clinical interest in immunomodulators have increased in the last decades, especially in the immunomodulatory properties of plant-based therapies. Innovative technologies and extensive study on immunomodulatory natural products, botanicals, extracts, and active moieties with immunomodulatory potential could provide us with valuable entities to develop as novel immunomodulatory medicines to enhance current chemotherapies. This review focuses on plant-based immunomodulatory drugs that are currently in clinical studies. However, further studies in this area are of utmost importance to obtain complete information about the positive effects of medicinal plants and their chemical components and molecules as an alternative to combatting various diseases and/or prevention. [ABSTRACT FROM AUTHOR]

Amphiphilic block copolymers, made of biocompatible polycaprolactone (PCL) and polyethylene glycol (PEG), due to their ability to self‐assemble in water into nanoscopic micelles, have been largely exploited for drug delivery systems (DDS). This study introduces a novel approach by synthesizing a fluorescein isothiocyanate FITC‐labelled PCL‐PEG‐PCL triblock copolymer, with the aim to develop a drug delivery system for natural bioactive. As a proof of concept, the FITC‐labelled PCL‐PEG‐PCL copolymer is applied for the preparation of micelles encapsulating into the core capsaicin (CP), a pungent alkaloid found in chili peppers with diverse therapeutic applications. Challenges associated with CP′s solubility, bioavailability, and stability are addressed using this DDS. Comprehensive characterization of FITC‐labelled copolymer is conducted using a range of analytical techniques, including nuclear magnetic resonance (NMR), dynamic light scattering (DLS), high‐performance liquid chromatography (HPLC), Fourier‐transform infrared spectroscopy (FTIR), fluorescence, and confocal laser scanning microscopy (CLSM). Key properties such as critical micelle concentration, CP loading, and release behavior are thoroughly investigated and compared with the characteristics of the unlabeled parent copolymer. This research pioneers the investigation of PCL‐PEG‐PCL triblock copolymers for CP delivery, along with the use of FITC‐labelled variants, opening new avenues for research in drug delivery and nanomedicine. [ABSTRACT FROM AUTHOR]

Intracerebral hemorrhage (ICH) induces a complex sequence of apoptotic cascades and inflammatory responses, leading to neurological impairment. Transient receptor potential vanilloid 1 (TRPV1), a nonselective cation channel with high calcium permeability, has been implicated in neuronal apoptosis and inflammatory responses. This study used a mouse ICH model and neuronal cultures to examine whether TRPV1 activation exacerbates brain damage and neurological deficits by promoting neuronal apoptosis and neuroinflammation. ICH was induced by injecting collagenase in both wild‐type (WT) C57BL/6 mice and TRPV1−/− mice. Capsaicin (CAP; a TRPV1 agonist) or capsazepine (a TRPV1 antagonist) was administered by intracerebroventricular injection 30 min before ICH induction in WT mice. The effects of genetic deletion or pharmacological inhibition of TRPV1 using CAP or capsazepine on motor deficits, histological damage, apoptotic responses, blood–brain barrier (BBB) permeability, and neuroinflammatory reactions were explored. The antiapoptotic mechanisms and calcium influx induced by TRPV1 inactivation were investigated in cultured hemin‐stimulated neurons. TRPV1 expression was upregulated in the hemorrhagic brain, and TRPV1 was expressed in neurons, microglia, and astrocytes after ICH. Genetic deletion of TRPV1 significantly attenuated motor deficits and brain atrophy for up to 28 days. Deletion of TRPV1 also reduced brain damage, neurodegeneration, microglial activation, cytokine expression, and cell apoptosis at 1 day post‐ICH. Similarly, the administration of CAP ameliorated brain damage, neurodegeneration, brain edema, BBB permeability, and cytokine expression at 1 day post‐ICH. In primary neuronal cultures, pharmacological inactivation of TRPV1 by CAP attenuated neuronal vulnerability to hemin‐induced injury, suppressed apoptosis, and preserved mitochondrial integrity in vitro. Mechanistically, CAP reduced hemin‐stimulated calcium influx and prevented the phosphorylation of CaMKII in cultured neurons, which was associated with reduced activation of P38 and c‐Jun NH2‐terminal kinase mitogen‐activated protein kinase signaling. Our results suggest that TRPV1 inhibition may be a potential therapy for ICH by suppressing mitochondria‐related neuronal apoptosis. [ABSTRACT FROM AUTHOR]

Chili peppers are globally cultivated for their rich bioactive compound profile. This study investigates the impact of two biostimulants, Humix® and Energen, on Capsicum chinense 'Habanero Orange' and Capsicum annuum 'Kristian', focusing on quantitative and qualitative parameters. Conducted over two years with three annual harvests, the research assesses the effects of biostimulant application on yield, fresh fruit number, fruit weight, drying ratio, capsaicin, dihydrocapsaicin, and ascorbic acid content (via HPLC-DAD analysis), as well as carotenoid levels (via spectrophotometric analysis). Biostimulant application significantly increased (p ≤ 0.05) total yields and capsaicin levels. Harvest timing also influenced dihydrocapsaicin and capsaicin levels, with the third harvest showing the highest values (p ≤ 0.001). The effects on ascorbic acid and carotenoids were variable and depended on genotype, harvest, and treatment. Thus, our study provides insights into the dynamic responses of Capsicum species to biostimulants under variable climatic conditions, contributing new knowledge to agricultural practices and the scientific understanding of biostimulant effects in Capsicum production. [ABSTRACT FROM AUTHOR]

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Copyright of Shipin Kexue/ Food Science is the property of Food Science Editorial Department and its content may not be copied or emailed to multiple sites or posted to a listserv without the copyright holder's express written permission. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract. (Copyright applies to all Abstracts.)

Copyright of Tianjin Medical Journal is the property of Tianjin Medical Journal and its content may not be copied or emailed to multiple sites or posted to a listserv without the copyright holder's express written permission. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract. (Copyright applies to all Abstracts.)

Background: Serving as a reservoir, the gastric fundus can expand significantly, with an initial receptive and a following adaptive relaxation, controlled by extrinsic and intrinsic reflex circuits, respectively. We hypothesize that mechanosensitive enteric neurons (MEN) are involved in the adaptive relaxation, which is initiated when a particular gastric volume and a certain stretch of the stomach wall is reached. To investigate whether the responsiveness of MEN in the gastric fundus is dependent on tissue stretch, we performed mechanical stimulations in stretched versus ganglia "at rest". Methods: Responses of myenteric neurons in the guinea pig gastric fundus were recorded with membrane potential imaging using Di‐8‐ANEPPS. MEN were identified by small‐volume intraganglionic injection in ganglia stretched to different degrees using a self‐constructed stretching tool. Immunohistochemical staining identified the neurochemical phenotype of MEN. Hexamethonium and capsaicin were added to test their effect on recruited MEN. Key Results: In stretched compared to "at rest" ganglia, significantly more MEN were activated. The change in the ganglionic area correlated significantly with the number of additional recruited MEN. The additional recruitment of MEN was independent from nicotinic transmission and the ratio of active MEN in stretched ganglia shifted towards a nitrergic phenotype. Conclusion and Inferences: The higher number of active MEN with increasing stretch of the ganglia and their greater share of nitrergic phenotype might indicate their contribution to the adaptive relaxation. Further experiments are necessary to address the receptors involved in mechanotransduction. [ABSTRACT FROM AUTHOR]

Diabetic neuropathic pain (DNP) is a diabetic complication that causes severe pain and deeply impacts the quality of the sufferer’s daily life. Currently, contemporary clinical treatments for DNP generally exhibit a deficiency in effectiveness. Electroacupuncture (EA) is recognized as a highly effective and safe treatment for DNP with few side effects. Regrettably, the processes via which EA alleviates DNP are still poorly characterized. Transient receptor potential vanilloid 1 (TRPV1) and phosphorylated calcium/calmodulin-dependent protein kinase II (p-CaMKII) are overexpressed on spinal cord dorsal horn (SCDH) in DNP rats, and co-localization is observed between them. Capsazepine, a TRPV1 antagonist, effectively reduced nociceptive hypersensitivity and downregulated the overexpression of phosphorylated CaMKIIα in rats with DNP. Conversely, the CaMKII inhibitor KN-93 did not have any impact on TRPV1. EA alleviated heightened sensitivity to pain caused by nociceptive stimuli and downregulated the level of TRPV1, p-CaMKIIα, and phosphorylated cyclic adenosine monophosphate response element-binding protein (p-CREB) in DNP rats. Intrathecal injection of capsaicin, on the other hand, reversed the above effects of EA. These findings indicated that the CaMKII/CREB pathway on SCDH is located downstream of TRPV1 and is affected by TRPV1. EA alleviates DNP through the TRPV1-mediated CaMKII/CREB pathway. [ABSTRACT FROM AUTHOR]

Copyright of Feed Industry is the property of Liaoning Provincial Institute of Agricultural Mechanization and its content may not be copied or emailed to multiple sites or posted to a listserv without the copyright holder's express written permission. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract. (Copyright applies to all Abstracts.)

Capsaicin, carotenoids, and phenolic compounds from cumari-do-Pará peppers (Capsicum chinense Jacq.) harvested from two different locations in Pará, Brazil, and at different ripening stages were extracted by employing green methodologies as an alternative to organic solvents. Edible vegetable oils from soybeans (Glycine max), Brazilian nuts (Bertholettia excelsa H.B.), and palm olein were used in combination with ultrasonic-assisted extraction (UAE). The proximate composition of the pepper extracts and vitamin C were determined through AOAC methods, total phenolics and carotenoids were assessed by UV/Vis spectrophotometry, and capsaicin by high-performance liquid chromatography. Antioxidant cumari-do-Pará extract activities were evaluated by the ABTS radical scavenging and β-carotene/linoleic acid assays. The vegetable oils were suitable for extracting and preserving bioactive pepper compounds, especially mature ones harvested from Igarapé-Açu. Bioactive compound content and antioxidant activity varied with harvesting location and ripening stage. Soybean oil was the most effective in extracting bioactive pepper compounds, particularly carotenoids, with 69% recovery. Soybean oil extracts enriched in capsaicin, carotenoids, and phenolics obtained from cumari-do-Pará can be used as spices in foodstuffs and/or as additives in pharmaceutical and nutraceutical formulations. Edible vegetable oils combined with UAE are promising for bioactive compound extraction, representing an environmentally friendly, safe, low-cost, versatile, and fast alternative. [ABSTRACT FROM AUTHOR]

Summary: Capsaicin is the main pungent compound in red pepper responsible for its dual attributes of culinary utility and bioactive efficacy. This review aims to systematically review the preparation methods, pungency, and bioactivities of capsaicin. Capsaicin can be extracted by maceration, microwave, near‐infrared extraction, supercritical fluid, and ultrasound‐assisted extraction methods. Also, it can be synthesised through chemical, biosynthetic, and in vitro cell methods. Capsaicin can elicit a pungent sensation via activation of TRPV1 receptor. Furthermore, it has been reported to display various bioactivities, such as hypoglycaemic, hypolipidemic, analgesic, anti‐cancer, anti‐inflammatory, and intestinal health‐protecting activities via several signalling pathways. Overall, this review can provide a theoretical reference for understanding the preparation, pungent sensation, and bioactivities of capsaicin. [ABSTRACT FROM AUTHOR]

Transient Receptor Potential Vanilloid 1 (TRPV1) is a protein that functions as a non-selective channel receptor that is widely expressed in skin tissue, including keratinocytes, peripheral sensory nerve fibers, and immune cells. Several structural features of TRPV1 are involved in heat-induced activation, where stimulation of TRPV1 elicits a burning sensation, reflecting the receptor's important role in pain. A TRPV1-mediated signalling pathway that functions as an endogenous pain resolution mechanism by inducing nuclear translocation of β-arrestin2 to minimize desensitization of μ-opioid receptors (MOR). TRPV1 agonists can reduce pain primarily by interfering with pain nerve conduction. Several TRPV1 antagonist drug candidates have failed in clinical trials because by interfering with the detection of the above-mentioned stimuli, they triggered serious side effects such as hyperthermia and painful impaired heat detection. In the case of agonists, systemic administration causes more severe side effects such as respiratory damage. Therefore, only topical preparations with limited effectiveness have been developed. The TRPV1 agonist capsaicin is currently the only one approved for the treatment of muscle, bone, neuropathic pain and migraine, and is only available as a low-concentration cream or as a transdermal patch. [ABSTRACT FROM AUTHOR]

Background: Capsaicin‐containing red pepper sauce suspension augments esophageal contraction amplitude on conventional manometry. This study used high‐resolution manometry (HRM) to investigate if capsaicin infusion modulates segmental esophageal smooth muscle peristalsis in healthy adults. Methods: Sixteen healthy volunteers (mean age 37 years, 14 male) underwent HRM for the evaluation of primary peristalsis and secondary peristalsis using slow and rapid air distensions. Both primary and secondary peristalsis were assessed following infusions of capsaicin‐containing red pepper sauce and saline. Key Results: Capsaicin infusion significantly increased heartburn symptoms compared to saline infusion (p < 0.001), and significantly decreased threshold volumes of secondary peristalsis during rapid air distensions (p = 0.02). The frequency of secondary peristalsis during rapid air distensions was significantly increased by capsaicin infusion (p = 0.03). Neither capsaicin infusion (p = 0.06) nor saline infusion (p = 0.27) altered threshold volume during slow air distensions. Capsaicin infusion significantly increased distal contractile integral (DCI) of primary peristalsis (p = 0.04), particularly in the proximal smooth muscle segment (p = 0.048). It enhanced secondary peristalsis during rapid air distensions (p = 0.003) but not during slow air distension (p = 0.23). Saline infusion significantly increased DCI of secondary peristalsis during rapid air distension (p = 0.01). Conclusions and Inferences: Augmentation of distension‐induced secondary peristalsis can be modulated by activation of capsaicin‐sensitive afferents similar to mechanosensitive afferents. Capsaicin‐induced augmentation of primary peristalsis isolates to the cholinergic‐mediated proximal smooth muscle segment, which warrants study in ineffective esophageal motility to determine therapeutic potential. [ABSTRACT FROM AUTHOR]

Recent research in rodents suggests that oxidative stress, inflammation, and apoptosis in the testes caused by high-fat diets (HFD) are a cause of male infertility. To investigate the therapeutic efficacy of the combination of hydroxycitric acid and capsaicin (HCC) against male reproductive disorders, we developed an HFD-induced obese rat model. Rats received HFD supplementation for 21 weeks, which induced obesity. From week 16, HCC (100 mg/kg body weight) was administered to investigate its potential to treat testicular toxicity. According to the results of the current study, treatment of obese rats with HCC improved their sperm quality, increased the production of testosterone, follicle-stimulating hormone, and luteinizing hormone and significantly increased the activities of steroidogenic enzymes and corresponding mRNA levels. In addition, HCC decreased lipid peroxidation and nitric oxide levels in both spermatozoa and testes while increasing the expression of mRNA for the antioxidant enzymes superoxide dismutase, catalase, and glutathione peroxidase in the testes, which in turn reduced oxidative stress in the testes. Moreover, after HCC treatment, testicular tissues showed a remarkable decrease in mRNA levels responsible for inflammation (TNF-α, IL-6, NF-κB) and apoptosis (Bax and Bcl-2). Our results suggest that HCC may alleviate obesity-induced male reproductive dysfunction by attenuating oxidative stress, inflammation, and apoptosis in the testes of HFD-induced obese male rats. [ABSTRACT FROM AUTHOR]

Conventional treatment strategies suffer from a lack of solubility, low bioavailability at the target site, a lack of target specificity, and indiscriminate drug distribution, all of which lead to drug resistance. Therefore, the present study aimed to deliver capsaicin into breast cancer cells through folic acid-conjugated capsaicin-loaded carboxylic acid-functionalised multiwalled carbon nanotubes (FA-CAP-COOHMWCNTs). FA-CAP-COOHMWCNTs was formulated and characterized by FTIR (Fourier transform infrared spectroscopy), SEM (Scanning electron microscopy), HR-TEM (High-resolution transmission electron microscopy), and XRD (X-ray diffraction) analysis. In silico studies demonstrated that the active molecule, capsaicin can strongly bind onto C-SRC kinase receptor to suppress cancer progression. The in vitro cellular viability of MCF-7 breast cancer cells after 24h treatment with 100 µg × mL− 1 of FA-CAP-COOHMWCNTs was found to be 29.27 ± 2.59% and IC50 value was observed to be 22.71 µg × mL− 1. Subsequently, in vivo anticancer activity of FA-CAP-COOHMWCNTs was performed against 7,12-dimethylbenz(a) anthracene (DMBA)-induced breast cancer in female Wistar rats. After 21 days of treatment with FA-CAP-COOHMWCNTs, breast cancer-induced rats showed a significant reduction in mammary tumor size, and elevated levels of antioxidant enzymes in serum/breast tissue. The most powerful antioxidant effects were seen in the medium dose (5 mg × kg− 1) of FA-CAP-COOHMWCNTs, which also caused tumors to shrink significantly, almost as much as the standard drug (doxorubicin). Histopathological studies also showed near-normal architecture of breast tissue. Altogether, it can be interpreted that FA-CAP-COOHMWCNTs have antiproliferative efficacy against breast tumor progression in breast cancer-induced rats. [ABSTRACT FROM AUTHOR]

BACKGROUND: Myoglobin (Mb) in duck meat is commonly over‐oxidized when heated at high temperatures, which may worsen the color of the meat. Enhancing the oxidative stability of Mb is essential for improving the color of duck meat. Capsaicin and dihydrocapsaicin (CA‐DI) in chili exhibit antioxidant properties. This study investigated the effects of CA‐DI on the structure and oxidative damage of Mb by fluorescence spectroscopy, differential scanning calorimetry analysis and particle size in duck meat during heat treatment. RESULTS: When the ratio of CA‐DI to Mb was 10:1 g kg−1 and heat‐treated for 36 min, oxymyoglobin significantly increased, and metmyoglobin significantly decreased compared with the control group (P < 0.05). In parallel, the carbonyl content of Mb in the CA‐DI group decreased by 43.40 ± 0.10%, the sulfhydryl content increased by 188 ± 0.21%, and the free radical scavenging activity of Mb was significantly enhanced (P < 0.05). Moreover, the addition of CA‐DI resulted in a significant decrease in the particle size of the Mb surface (P < 0.05). When the ratio of CA‐DI to Mb was 10:1 g kg−1, CA‐DI enhanced the thermal stability and significantly increased the thermal denaturation temperature of Mb. The molecular docking results indicated that hydrophobic interactions and hydrogen bonds were involved in the binding of CA‐DI to Mb. CONCLUSION: CA‐DI could combine with Mb and improve the oxidation stability of Mb in duck meat. This suggested that CA‐DI could be a potential natural antioxidant that improves the color of meat products. © 2024 Society of Chemical Industry. [ABSTRACT FROM AUTHOR]

Tongue squamous cell carcinoma (TSCC) is one of the most common malignant tumors among oral cancers, and its treatment is based on radio-chemotherapy and surgery, which always produces more serious side effects and sequelae. Traditional medicine can compensate for the shortcomings of modern medical treatments and play a better therapeutic role. Currently, active ingredients derived from plants are attracting the attention of researchers and clinical professionals. We examined capsaicin (CAP), an active ingredient isolated from Capsicum annuum (family Solanaceae), and explored the effect of CAP combined with cisplatin (DDP) on epithelial-mesenchymal transition (EMT) and TSCC cells migration. Our results demonstrated that Transforming growth factor-β1(TGF-β1) induced EMT and promoted cell migration in TSCC cells. CAP combined with DDP inhibits non-TGF-β1-induced or TGF-β1-induced EMT and migration. Mechanistically, the inhibition of non-TGF-β1-induced EMT and migration by CAP combined with DDP was mediated by the AMPK/mTOR pathway, whereas TGF-β1-induced EMT and migration were regulated by the Claudin-1/PI3K/AKT/mTOR pathway. A nude lung metastasis mouse model was established for in vivo validation. These results support our hypothesis that the combination of CAP and DDP inhibits TSCC metastasis. These data set the stage for further studies aimed at validating CAP as an effective active ingredient for enhancing chemotherapy efficacy and reducing the dosage and toxicity of chemotherapeutic drugs, ultimately paving the way for translational research and clinical trials for TSCC eradication. [ABSTRACT FROM AUTHOR]

Chronic low-grade inflammation (CLGI) is associated with obesity and is one of its pathogenetic mechanisms. Lipopolysaccharide (LPS), a component of Gram-negative bacterial cell walls, is the principal cause of CLGI. Studies have found that capsaicin significantly reduces the relative abundance of LPS-producing bacteria. In the present study, TRPV1-knockout (TRPV1−/−) C57BL/6J mice and the intestinal epithelial cell line Caco-2 (TRPV1−/−) were used as models to determine the effect of capsaicin on CLGI and elucidate the mechanism by which it mediates weight loss in vivo and in vitro. We found that the intragastric administration of capsaicin significantly blunted increases in body weight, food intake, blood lipid, and blood glucose in TRPV1−/− mice fed a high-fat diet, suggesting an anti-obesity effect of capsaicin. Capsaicin reduced LPS levels in the intestine by reducing the relative abundance of Proteobacteria such as Helicobacter, Desulfovibrio, and Sutterella. Toll-like receptor 4 (TLR4) levels decreased following decreases in LPS levels. Then, the local inflammation of the intestine was reduced by reducing the expression of tumor necrosis factor (TNF)-α and interleukin (IL)-6 mediated by TLR4. Attenuating local intestinal inflammation led to the increased expression of tight junction proteins zonula occludens 1 (ZO-1) and occludin and the restoration of the intestinal barrier function. Capsaicin increased the expression of ZO-1 and occludin at the transcriptional and translational levels, thereby increasing trans-endothelial electrical resistance and restoring intestinal barrier function. The restoration of intestinal barrier function decreases intestinal permeability, which reduces the concentration of LPS entering the circulation, and reduced endotoxemia leads to decreased serum concentrations of inflammatory cytokines such as TNF-α and IL-6, thereby attenuating CLGI. This study sheds light on the anti-obesity effect of capsaicin and its mechanism by reducing CLGI, increasing our understanding of the anti-obesity effects of capsaicin. It has been confirmed that capsaicin can stimulate the expression of intestinal transmembrane protein ZO-1 and cytoplasmic protein occludin, increase the trans-epithelial electrical resistance value, and repair intestinal barrier function. [ABSTRACT FROM AUTHOR]

Clodronate (Clod), a first-generation bisphosphonate, acts as a natural analgesic inhibiting vesicular storage of the nociception mediator ATP by vesicular nucleotide transporter (VNUT). Epidermal keratinocytes participate in cutaneous nociception, accumulating ATP within vesicles, which are released following different stimulations. Under stress conditions, keratinocytes produce microvesicles (MVs) by shedding from plasma membrane evagination. MV secretion has been identified as a novel and universal mode of intercellular communication between cells. The aim of this project was to evaluate if two nociceptive stimuli, Capsaicin and Potassium Hydroxide (KOH), could stimulate MV shedding from human keratinocytes, if these MVs could contain ATP, and if Clod could inhibit this phenomenon. In our cellular model, the HaCaT keratinocyte monolayer, both Capsaicin and KOH stimulated MV release after 3 h incubation, and the released MVs contained ATP. Moreover, Clod (5 µM) was able to reduce Caps-induced MV release and abolish the one KOH induced, while the Dansylcadaverine, an endocytosis inhibitor of Clod uptake, partially failed to block the bisphosphonate activity. Based on these new data and given the role of the activation of ATP release by keratinocytes as a vehicle for nociception and pain, the "old" bisphosphonate Clodronate could provide the pharmacological basis to develop new local analgesic drugs. [ABSTRACT FROM AUTHOR]

As a fruit and vegetable crop, the ornamental pepper is not just highly ornamental but also rich in nutritional value. The quality of ornamental pepper fruits is given in their contents of capsaicin, vitamin C (VC), flavonoids and total phenols. The study concentrated on the accumulation of capsaicin and dihydrocapsaicin in different tissues of 18 peppers during fruit growth and development. The results showed that the pericarp and placenta contained significantly higher levels of capsaicin than dihydrocapsaicin. Additionally, the placenta contained significantly higher levels of both capsaicin and dihydrocapsaicin compared to the pericarp. The content of capsaicin was in the range of 0–6.7915 mg·g−1, the range of dihydrocapsaicin content was 0–5.329 mg·g−1. Interestingly, we found that the pericarp is rich in VC (5.4506 mg·g−1) and the placenta is high in flavonoids (4.8203 mg·g−1) and total phenols (119.63 mg·g−1). The capsaicin is the most important component using the correlation analysis and principal component analysis. The qPCR results substantiated that the expression of genes in the placenta was significantly higher than that in the pericarp and that the expression of genes in green ripening stage was higher than that in red ripening stage. This study could be utilized to select the best ripening stages and tissues to harvest peppers according to the use of the pepper and to the needs of producers. It not only provides a reference for quality improvement and processing for consumers and market but also provides a theoretical basis for high-quality pepper breeding. [ABSTRACT FROM AUTHOR]

Objective: Adipose tissue stores lipids necessary for the maintenance of nutritional homeostasis. It is also an endocrine organ that reacts to changes in inflammation and energy status. Capsaicin, the principal bioactive compound in red pepper, has garnered significant attention for its reported anti-obesity, anti-diabetic, anti-oxidant, and anti-inflammatory properties. In this study, we aimed to elucidate the influence and most efficacious dose of capsaicin on the expression of lipid metabolism-related inflammatory proteins and the inhibition of adipocyte cell differentiation. Materials and Methods: Cell viability analysis was performed using CCK-8, cell differentiation was assessed using Oil Red O, and gene expression levels of peroxisome proliferator-activated receptor gamma (PPARγ), CCAAT/enhancer binding protein alpha (C/EBPa), adiponectin, leptin, cyclooxygenase-2 (COX-2), interleukin-6 (IL-6), nuclear factor kappa B1 (NF-κB1), tumor necrosis factor-alpha (TNF-a), sirtuin-1 (SIRT-1), transient receptor potential vanilloid receptor 1 (TRPV1), and uncoupling protein 2 (UCP2) were evaluated using quantitative real time polymerase chain reaction (qRT-PCR). Statistical analyses were conducted using GraphPad Prism 5. One-way ANOVA was performed to compare quantitative data between the groups. Results: Capsaicin suppressed preadipocyte-to-adipocyte differentiation and mitigated the release of pro-inflammatory cytokines, particularly at low concentrations. Capsaicin effectively suppressed adiponectin levels at all concentrations but decreased leptin levels at lower concentrations (0.5 µM and 1 µM). Capsaicin stimulated the expressions of SIRT1 and TRPV-1 in adipocytes. According to our findings, the most effective capsaicin dose for the regulation of SIRT1 and TRPV-1 expressions appears to be 20 µM. Conclusion: Capsaicin's effect on proteins regulating adipogenesis is not dose-related, but its inhibitory effect on adiposity-dependent inflammation was more pronounced at low concentrations. [ABSTRACT FROM AUTHOR]

Reducing fertilizer pollution is an important direction for modern ecological agriculture. Commonly, excessive nitrogen is applied to pepper. Capsaicin is one of the most important economic qualities of spicy peppers, but the effect of nitrogen on capsaicin is still inconsistent. This study aims to elucidate the impact of nitrogen fertilizer on capsaicin accumulation and to provide guidance on fertilizer application on highly spicy chili peppers. The experiment was conducted with five nitrogen fertilizer concentrations: N1 (urea 750 kg ha−1), N2 (urea 562.5 kg ha−1), N3 (urea 375 kg ha−1), N4 (urea 187.5 kg ha−1), and N0 (no nitrogen fertilizer). Nitrogen treatment was applied to two varieties with different spiciness levels from the seedling stage. The fruits in different layers of pepper plants were sampled on the 20th, 35th, and 50th day after anthesis, and the fruits' size, content of capsaicin, capsaicin precursors, capsaicin competitors, as well as capsaicin-related enzyme activities and gene expression level were analyzed. The results indicate that, when applying N2 and N3, both chili pepper varieties exhibited higher fruit length, diameter, weight, and yield values. There were increased contents of total phenol, flavonoids, and tannins in both fruit varieties with N2 application. Moreover, the placenta weights of the bottom, middle, and top layers of the fruits on the 35th day were improved by 40.14%, 26.80%, and 55.91% for 'Honglong 23' and 55.10%, 37.04%, and 75.56% for 'Hongxi' compared with N0. At the same time, under N2 treatment, the phenylalanine ammonia-lyase (PAL) enzyme activity of capsaicin synthase significantly increased. In contrast, the capsaicin-degrading enzyme activities of peroxidase (POD) and polyphenol oxidase (PPO) decreased notably. The expression levels of capsaicin-synthetic genes such as phenylalanine cleavage enzyme gene (PAL), acyltransferase gene (AT3), 4-Coumaroyl coenzyme A ligase gene (4CL), cinnamate 4-hydroxylase gene (C4H), caffeoyl coenzyme A-3-oxo-methyltransferase gene (COMT), paminotransferase gene (PAMT), and hydroxycinnamyltransferase gene (HCT) were up-regulated in N2 fruits, which led to a significant increase in capsaicin content compared with the other four nitrogen amounts. A further reduction in nitrogen application to N3 and N4 resulted in a decrease in the precursor substance's total phenol content and PAL activity and an increase in the competitive substance's flavonoid, lignin, POD, and PPO enzyme activities. At the same time, the expression levels of capsaicinoid synthetic genes were downregulated in the N3 and N4 treatments, leading to a low content of total capsaicinoids. The capsaicinoid content showed a trend of 35th day > 50th day > 20th day for both varieties. Additionally, the contents of total capsaicinoids, total phenols, flavonoids, and lignins, as well as PAL enzyme activity, and the expression levels of PAL, AT3, 4CL, C4H, COMT, PAMT, and HCT exhibited characteristics of bottom layers > middle layers > top layers. The activities of POD and PPO gradually increased from the bottom to the top layers. The N2 (562.5 kg ha−1) treatment resulted in increases in placenta mass, maximum capsaicinoid precursor substance of total phenol content, and synthase enzyme activity, as well as decreases in capsaicinoid competing substances and degradative enzyme activity, so there were more substances available for capsaicin synthesis. Combined with the higher fruit weight and capsaicinoid content in the N2 treatment, N2 was considered a suitable nitrogen fertilizer dosage for highly spicy chili pepper cultivation. [ABSTRACT FROM AUTHOR]

Copyright of Die Dermatologie is the property of Springer Nature and its content may not be copied or emailed to multiple sites or posted to a listserv without the copyright holder's express written permission. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract. (Copyright applies to all Abstracts.)

The study objectives are to investigate the ability of capsaicin to revert the toxic effects in glutamate and lipopolysaccharide (LPS)-induced neurotoxicity in Neuro2a (N2a) cells as well as thwarting cognitive impairments, mitochondrial deficits, and oxidative insults induced by 3-nitropropanoic acid (3-NP) in a rodent model of Huntington's disease. In-vitro study with N2a cells was performed through MTT and LDH assay and their biochemical examinations were also performed. 3-NP-administered mice (n = 6) were treated with capsaicin (5, 10, and 20 mg/kg) through the per-oral (p.o.) route for 7 consecutive days. Physiological and behavioral studies were performed in drug-treated mice. After behavioral studies, biochemical parameters were performed for cytokines levels, various oxidative stress parameters, and mitochondrial enzyme complex activities with mitochondrial permeability. N2a cells treated with capsaicin demonstrated neuroprotective effects and reduced neurotoxicity. Based on experimental observation, in an in-vitro study, the effective dose of CAP was 50 µM. Moreover, a 100 µM dose of capsaicin had toxic effects on neuronal cells (N2a cells). On the other hand, the effective dose of 3-NP was 20 mg/kg, (p.o.) in animals (in-vivo). All tested doses of capsaicin upturned the cognitive impairment and motor in-coordination effects induced by 3-NP. 3-NP-injected mice demonstrated substantially increased pro-inflammatory cytokine concentrations, defective mitochondrial complex activity, and augmented oxidative insult. However, capsaicin at different doses reduced oxidative damage and cytokines levels and improved mitochondrial complex activity along with mitochondrial permeability. Furthermore, capsaicin (10 and 20 mg/kg) improved the TNF-α concentration. These findings suggested because of the anti-inflammatory and antioxidant effect, capsaicin can be considered a novel treatment for the management of neurodegenerative disorders by reverting the antioxidant enzyme activity, pro-inflammatory cytokines concentration, and mitochondrial functions. [ABSTRACT FROM AUTHOR]

It is widely accepted that milk provides the greatest relief from capsaicin burn, an effect typically attributed to its fat content and temperature. Previously, Lawless et al. reported partitioning lipophilic capsaicin in fat reduces burn, whereas Green showed lower temperature reduces burn. Recent research shows that dairy and nondairy proteins also reduce capsaicin burn, suggesting that multiple factors reduce oral burn from chilies. Here, we investigated the effectiveness of palate cleansers with varied viscosities, temperatures, and sugar, fat, and protein content. Specifically, we tested ice cream, Italian ice, yogurt, lassi, cold water (4°C), and warm water (37°C). Participants rinsed with a 5 ppm capsaicin solution, followed by a palate cleanser, before rating burn intensity continuously for 2 min on a general Labeled Magnitude Scale. Inspection of the time–intensity (TI) curves revealed all palate cleansers performed better than warm water. Italian ice performed on par with cold water, which did better than yogurt. Pairwise comparisons showed that ice cream and lassi had significantly lower burn ratings at some time points relative to warm or cold water. We extracted scaffolding parameters for each TI curve, finding that ice cream and lassi had the lowest areas‐under‐the‐curve and the greatest percent decrease from their maxima, with ice cream performing slightly better in both parameters. These data support the view that it is not just one characteristic of a product, but rather a combination of product factors that reduce oral burn, including fat content, protein content, and temperature. More research is required to determine the relative weight of these factors in combination, given the multiple mechanisms underlying burn reduction. [ABSTRACT FROM AUTHOR]

Copyright of Science & Technology of Food Industry is the property of Science & Technology of Food Industry Editorial Office and its content may not be copied or emailed to multiple sites or posted to a listserv without the copyright holder's express written permission. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract. (Copyright applies to all Abstracts.)

Cisplatin is commonly used for the chemotherapy of tongue squamous cell carcinoma (TSCC); however, adverse side effects and drug resistance impact its therapeutic efficacy. Capsaicin is an active ingredient in chili peppers that exerts antitumor effects, whether it exerts antitumor effects on cisplatin‐resistant cells remains unknown. Therefore, in this study, we investigated the effect of capsaicin on cisplatin resistance in TSCC cells and explored the underlying mechanisms. A cisplatin‐resistant TSCC cell line was established by treated with increasing cisplatin concentrations. Combined treatment with cisplatin and capsaicin decreased the glucose consumption and lactate dehydrogenase activity and increased the adenosine triphosphate production both in vitro and in vivo, suggesting the inhibition of the Warburg effect. Moreover, this combined treatment induced cell apoptosis and significantly upregulated the levels of proapoptotic proteins, such as Bax, cleaved caspase‐3, ‐7, and ‐9, and apoptosis‐inducing factor. In contrast, levels of the antiapoptotic protein, Bcl‐2, were downregulated. Additionally, LKB1 and AMPK activities were stimulated, whereas those of AKT and mTOR were suppressed. Notably, AMPK knockdown abolished the inhibitory effects of capsaicin and cisplatin on the AKT/mTOR signaling pathway and Warburg effect. Overall, combined treatment with capsaicin and cisplatin reversed cisplatin resistance by inhibiting the Warburg effect and facilitating mitochondrial‐dependent apoptosis via the AMPK/AKT/mTOR axis. Our findings suggest combination therapy with capsaicin and cisplatin as a potentially novel strategy and highlight capsaicin as a promising adjuvant drug for TSCC treatment. [ABSTRACT FROM AUTHOR]