Spicing it up with fluorine : Enantiomers of α‐fluorinated capsaicin 2 , have been prepared by organocatalytic electrophilic fluorination and have been used as probes for the binding conformation of capsaicin to the TRPV1 pain receptor. No enantiomeric bias is observed, thus suggesting an extended binding conformation along the molecular axis.
Research concerning the benefits derived from dietary polyphenols, a significant class within the family of phytonutrients, has increased considerably in the last decade. Prior to the late 1990s, the nutritional spotlight focused on the antioxidant capabilities of carotenoids, vitamins, and minerals. More recently, however, research has emerged in strong support of the antioxidant capacity of polyphenols and their role in the prevention and/or treatment of certain cancers, diabetes, cardiovascular diseases, and inflammation. Polyphenols are categorized according to the nature of their carbon skeleton, ranging from basic phenolic molecules to highly complex compounds, such as flavonoids, the most common and widely studied of all phenolic compounds. The most prevalent phenolic acids include ellagic acid, gallic acid, tannic acid, and capsaicin. 相似文献
Oral cancer is a major global health problem with high incidence and low survival rates. The oral cavity contains biofilms as dental plaques that harbour both Gram-negative and Gram-positive bacterial antigens, lipopolysaccharide (LPS) and lipoteichoic acid (LTA), respectively. LPS and LTA are known to stimulate cancer cell growth, and the bioactive phytochemical capsaicin has been reported to reverse this effect. Here, we tested the efficacy of oral cancer chemotherapy treatment with capsaicin in the presence of LPS, LTA or the combination of both antigens. LPS and LTA were administered to Cal 27 oral cancer cells prior to and/or concurrently with capsaicin, and the treatment efficacy was evaluated by measuring cell proliferation and apoptotic cell death. We found that while capsaicin inhibits oral cancer cell proliferation and metabolism (MT Glo assay) and increases cell death (Trypan blue exclusion assay and Caspase 3/7 expression), its anti-cancer effect was significantly reduced on cells that are either primed or exposed to the bacterial antigens. Capsaicin treatment significantly increased oral cancer cells’ suppressor of cytokine signalling 3 gene expression. This increase was reversed in the presence of bacterial antigens during treatment. Our data establish a rationale for clinical consideration of bacterial antigens that may interfere with the treatment efficacy of oral cancer. 相似文献
AbstractThis study examines the performance of a parabolic greenhouse-type solar dryer used for drying of cayenne pepper (Capsicum annuum) in Nan (northern Thailand). The dryer has a base area of 6.0?m × 8.2?m and a height of 3.25?m with the loading capacity of 100–200?kg for fruit or vegetables. It has a parabolic roof structure covered with polycarbonate sheets and is placed on a concrete floor. It is ventilated by three DC fans powered by a 50-Watt solar cell module. The produce is placed on trays with wire mesh base and located on steel supports. Among the advantages of this type of dryer is that the product is protected from rain, dust and insects. The pepper samples consisted of whole pods or cut pods. The drying experiments were carried out in the solar dryer and in an electrical (convective) tray dryer. The study was focusing on drying kinetics and on the effects of the drying treatments on one of the main quality attributes namely the capsaicin content in the dried products. 相似文献
Although the pharmacological activity of capsaicin has been explained by its specific binding to transient receptor potential vanilloid type 1, the amphiphilic structure of capsaicin may enable it to act on lipid bilayers. From a mechanistic point of view, we investigated whether capsaicin and its antagonist capsazepine interact with biomimetic membranes, and how capsazepine influences the membrane effect of capsaicin. Liposomal phospholipid membranes and neuro-mimetic membranes were prepared with 1,2-dipalmitoylphosphatidylcholine and with 1-palmitoyl-2-oleoylphosphatidylcholine and sphingomyelin plus cholesterol, respectively. These membrane preparations were subjected to reactions with capsaicin and capsazepine at 0.5–250 μM, followed by measuring fluorescence polarization to determine the membrane interactivity to modify the fluidity of membranes. Both compounds acted on 1,2-dipalmitoylphosphatidylcholine bilayers and changed membrane fluidity. Capsaicin concentration-dependently interacted with neuro-mimetic membranes to increase their fluidity at low micromolar concentrations, whereas capsazepine inversely decreased the membrane fluidity. When used in combination, capsazepine inhibited the effect of capsaicin on neuro-mimetic membranes. In addition to the direct action on transmembrane ion channels, capsaicin and capsazepine share membrane interactivity, but capsazepine is likely to competitively antagonize capsaicin’s interaction with neuro-mimetic membranes at pharmacokinetically-relevant concentrations. The structure-specific membrane interactivity may be partly responsible for the analgesic effect of capsaicin. 相似文献