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This paper describes the preparation, characterization, and evaluation of honey/tripolyphosphate (TPP)/chitosan (HTCs) nanofibers loaded with capsaicin derived from the natural extract of hot pepper (Capsicum annuumL.) and loaded with gold nanoparticles (AuNPs) as biocompatible antimicrobial nanofibrous wound bandages in topical skin treatments. The capsaicin and AuNPs were packed within HTCs in HTCs-capsaicin, HTCs-AuNP, and HTCs-AuNPs/capsaicin nanofibrous mats. In vitro antibacterial testing against Pasteurella multocida, Klebsiella rhinoscleromatis,Staphylococcus pyogenes, and Vibrio vulnificus was conducted in comparison with difloxacin and chloramphenicol antibiotics. Cell viability and proliferation of the developed nanofibers were evaluated using an MTT assay. Finally, in vivo study of the wound-closure process was performed on New Zealand white rabbits. The results indicate that HTCs-capsaicin and HTCs-AuNPs are suitable in inhibiting bacterial growth compared with HTCs and HTCs-capsaicin/AuNP nanofibers and antibiotics (P < 0.01). The MTT assay demonstrates that the nanofibrous mats increased cell proliferation compared with the untreated control (P < 0.01). In vivo results show that the developed mats enhanced the wound-closure rate more effectively than the control samples. The novel nanofibrous wound dressings provide a relatively rapid and efficacious wound-healing ability, making the obtained nanofibers promising candidates for the development of improved bandage materials.

The aim of the present study was to determine the content of capsaicin and dihydrocapsaicin in Capsicum samples collected from city markets in Riyadh (Saudi Arabia), calculate their pungency in Scoville heat units (SHU) and evaluate the average daily intake of capsaicin for the population of Riyadh. The investigated samples consisted of hot chillies, red chillies, green chillies, green peppers, red peppers and yellow peppers. Extraction of capsaicinoids was done using ethanol as solvent, while high performance liquid chromatography (HPLC) was used for separation, identification and quantitation of the components. The limit of detection (LOD) of the method was 0.09 and 0.10 µg/g for capsaicin and dihydrocapsaicin, respectively, while the limit of quantification (LOQ) was 0.30 and 0.36 µg/g for capsaicin and dihydrocapsaicin, respectively. Hot chillies showed the highest concentration of capsaicin (4249.0 ± 190.3 µg/g) and the highest pungency level (67984.60 SHU), whereas green peppers had the lowest detected concentration (1.0 ± 0.9 µg/g); green peppers, red peppers and yellow peppers were non pungent. The mean consumption of peppers for Riyadh city population was determined to be 15.5 g/person/day while the daily capsaicin intake was 7.584 mg/person/day.

Sensing and responding to temperature is crucial in biology. The TRPV1 ion channel is a well-studied heat-sensing receptor that is also activated by vanilloid compounds, including capsaicin. Despite significant interest, the molecular underpinnings of thermosensing have remained elusive. The TRPV1 S1-S4 membrane domain couples chemical ligand binding to the pore domain during channel gating. Here we show that the S1-S4 domain also significantly contributes to thermosensing and couples to heat-activated gating. Evaluation of the isolated human TRPV1 S1-S4 domain by solution NMR, far-UV CD, and intrinsic fluorescence shows that this domain undergoes a non-denaturing temperature-dependent transition with a high thermosensitivity. Further NMR characterization of the temperature-dependent conformational changes suggests the contribution of the S1-S4 domain to thermosensing shares features with known coupling mechanisms between this domain with ligand and pH activation. Taken together, this study shows that the TRPV1 S1-S4 domain contributes to TRPV1 temperature-dependent activation. The TRPV1 ion channel is a heat-sensing receptor that is also activated by vanilloid compounds, but the molecular underpinnings of thermosensing have remained elusive. Here authors use in solution NMR on the isolated human TRPV1 S1-S4 domain and show that this domain undergoes a non-denaturing temperature-dependent transition with a high thermosensitivity.

Capsaicin, the pungent ingredient of the hot chili pepper, is known to act on the transient receptor potential cation channel vanilloid subfamily member 1 (TRPV1). TRPV1 is involved in somatic and visceral peripheral inflammation, in the modulation of nociceptive inputs to spinal cord and brain stem centers, as well as the integration of diverse painful stimuli. In this review, we first describe the chemical and pharmacological properties of capsaicin and its derivatives in relation to their analgesic properties. We then consider the biochemical and functional characteristics of TRPV1, focusing on its distribution and biological effects within the somatosensory and viscerosensory nociceptive systems. Finally, we discuss the use of capsaicin as an agonist of TRPV1 to model acute inflammation in slices and other ex vivo preparations.

Carbonic anhydrase (CA, EC 4.2.1.1) is a zinc containing metalloenzyme that catalyzes the rapid and reversible conversion of carbon dioxide (CO2) and water (H2O) into a proton (H+) and bicarbonate (HCO3–) ion. On the other hand, capsaicin is the main component in hot chili peppers and is used extensively used in spices, food additives and drugs; it is responsible for their spicy flavor and pungent taste. There are sixteen known CA isoforms in humans. Human CA isoenzymes I, and II (hCA I and hCA II) are ubiquitous cytosolic isoforms. In this study, the inhibition properties of capsaicin against the slow cytosolic isoform hCA I, and the ubiquitous and dominant rapid cytosolic isozymes hCA II were studied. Both CA isozymes were inhibited by capsaicin in the micromolar range. This naturally bioactive compound has a Ki of 696.15 µM against hCA I, and of 208.37 µM against hCA II.

The Capsicum genus, native to the Americas and cultivated worldwide for culinary and medicinal purposes, includes five domesticated species with diverse fruit characteristics, pungency, and phytochemical profiles. However, the influence of casual urban backyard growing conditions on these traits remains unknown. In this study, we first assessed morphological production traits of 11 popular pepper cultivars over two growing seasons to establish a consistent baseline for cultivar performance. Next, we evaluated capsaicinoid and phenolic profiles of 47 pepper cultivars, which contribute to their pungency and antioxidant properties. Capsaicinoid profiles revealed species-specific ratios of capsaicin, dihydrocapsaicin, and nordihydrocapsaicin, with C. annuum and C. baccatum displaying an average 64:30:6 profile, C. chinense and C. frutescens showing a capsaicin-dominant 73:25:2 profile, and C. pubescens expressing a distinct dihydrocapsaicin-dominant 34:60:6 profile. Antioxidant activity positively correlated with capsaicinoid content (ABTS: R2 = 0.8264, p < 0.0001; FRAP: R2 = 0.8117, p < 0.0001), with C. chinense (Carolina Reaper) exhibiting the highest activity (FRAP = 111.8 µM TE/g). In LPS-activated macrophages, all cultivars suppressed nitric oxide production both at the enzymatic (66–89%, p < 0.001) and gene expression levels (4.2 to 5.3-fold reduction, p < 0.05). Interleukin IL-1β expression was upregulated (3.8 to 12.9-fold, p < 0.001), while no significant effects were noted on Cox-2, IL-6, and MCP-1 mRNA levels. These results provide novel insights into the molecular and biochemical adaptations of peppers grown in urban environments and underscore the importance of optimizing cultivation conditions to maximize their bioactive potential and health benefits.

Capsaicin, the major pungent alkaloid in Capsicum species, has been reported to exhibit cytotoxic activity through various mechanisms. In this study, capsaicin and 37 structurally related vanillylamide and ester analogs were synthesized and evaluated for cytotoxic activity and tumor cell/non-tumor cell selectivity in vitro and compared with a Capsicum baccatum (Aji mochero) extract. Seven analogs with superior potency and selectivity compared to capsaicin were identified. Notably, vanillylamides with a C16–C18 chain exhibited IC50 values five-fold lower than capsaicin (15–84 µM), with selectivity indices up to 35. The extract obtained from the dried chili fruit, known to hold capsaicin as its primary component, however, exhibited significantly lower cytotoxic activity against tumor cells than pure capsaicin. These data demonstrate that even minor modifications to the acyl chain (as exemplified for the nonivamide analogs) can enhance the cytotoxicity and selectivity of these derivatives and that isolated compounds are able to offer even greater efficacy than whole-fruit extracts.

Capsaicin, a natural bioactive compound, has attracted wide interest for its potential health benefits. However, its rapid metabolism and strong irritancy upon oral administration have greatly limited its further application. To address these issues, this study developed a nanoparticle delivery system using corn Zein and Brassica rapa L. polysaccharide (BP) as carriers, with capsaicin (CAP) as the core. The optimized formulation (BP:Zein = 1:2, Zein:CAP = 2.5:1, mg/mg) produced stable, uniform spherical nanoparticles with an average particle size of 203.05 nm, a polydispersity index (PDI) of 0.138, a zeta potential of −44.9 mV, an encapsulation efficiency of 54.03%, and a drug loading capacity of 184.57 μg/mg. Fourier transform infrared spectroscopy (FTIR), fluorescence spectroscopy (FS), X-Ray diffraction, scanning electron microscope (SEM), and transmission electron microscopy (TEM) analyses confirmed that CAP was successfully encapsulated, forming nanoparticles through hydrogen bonding and hydrophobic interactions between CAP and Zein. The obtained nanoparticles displayed regular spherical morphology and uniform size distribution. Compared with single-layer Zein–CAP nanoparticles, BP–Zein–Capsaicin (BZC) nanoparticles exhibited markedly improved stability under different pH, ionic strength, and storage conditions. In vitro simulated digestion showed a sustained-release profile, with 36.76% of CAP released after 4 h. The anti-inflammatory experiment showed that both the nanoparticle and free capsaicin groups significantly inhibited xylene-induced acute ear edema in mice, with the medium- and high-dose nanoparticle groups exhibiting stronger anti-inflammatory effects than the free capsaicin group. These findings suggest that the nanoparticle delivery system effectively enhances the anti-inflammatory activity of capsaicin, possibly by improving its stability, achieving sustained release, and enhancing its bioavailability in vivo. Overall, capsaicin-loaded Brassica rapa L. polysaccharide–Zein nanoparticles combine small particle size, high drug loading, and excellent stability, providing a promising strategy for functional food development and targeted bioactive delivery.

Background: Medicinal plants have proven their value as a source of molecules with therapeutic potential, and recent studies have shown that capsaicin has profound anticancer effects in several types of human cancers. However, its clinical use is handicapped due to its poor pharmacokinetics. This study aims to enhance capsaicin’s pharmacokinetic properties by loading the molecule into nanoliposomes model and testing its anticancer activity. Methods: Nanoliposomes were prepared using the thin-film method, and characteristics were examined followed by qualitative and quantitative analyses of encapsulation efficiency and drug loading using HPLC at different lipid/capsaicin ratios. Cell viability assay (MTT) was used to determine IC50. Results: Capsaicin-loaded nanoliposomes showed optimum characteristics of morphology, particle size, zeta potential, and stability. In vitro anticancer activity of capsaicin and capsaicin-loaded nanoliposomes were compared against MCF7, MDA-MB-231, K562, PANC1, and A375 cell lines. Capsaicin-loaded nanoliposomes showed significant improvement in anticancer activity against cancers cell lines studied (p < 0.001), with increased selectivity against cancer cells compared to capsaicin. Conclusion: The encapsulated capsaicin nanoliposomes produced an improvement in pharmacokinetics properties, enhancing the anticancer activity and selectivity compared with capsaicin. This model seems to offer a potential for developing capsaicin formulations for the prevention and treatment of cancer.

Capsaicin, the major active constituent of chilli, is an agonist on transient receptor potential vanilloid channel 1 (TRPV1). TRPV1 is present on many metabolically active tissues, making it a potentially relevant target for metabolic interventions. Insulin resistance and obesity, being the major components of metabolic syndrome, increase the risk for the development of cardiovascular disease, type 2 diabetes, and non-alcoholic fatty liver disease. In vitro and pre-clinical studies have established the effectiveness of low-dose dietary capsaicin in attenuating metabolic disorders. These responses of capsaicin are mediated through activation of TRPV1, which can then modulate processes such as browning of adipocytes, and activation of metabolic modulators including AMP-activated protein kinase (AMPK), peroxisome proliferator-activated receptor α (PPARα), uncoupling protein 1 (UCP1), and glucagon-like peptide 1 (GLP-1). Modulation of these pathways by capsaicin can increase fat oxidation, improve insulin sensitivity, decrease body fat, and improve heart and liver function. Identifying suitable ways of administering capsaicin at an effective dose would warrant its clinical use through the activation of TRPV1. This review highlights the mechanistic options to improve metabolic syndrome with capsaicin.