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Spilanthol
Spilanthol (affinin) is a fatty acid amide isolated from ''Acmella oleracea''. It is believed to be responsible for the local anesthetic properties of the plant. Spilanthol permeates the human skin and the inside lining of the cheeks in the mouth (buccal mucosa), resulting in local as well as systemic pharmacological concentrations. In the skin and in the pancreas, spilanthol has also been shown to exert anti-inflammatory effects. The underlying mechanism involves inhibition of nitric oxide production due to reduced expression of inducible nitric oxide synthase enzyme (iNOS) in macrophages. Transcription factor array experiments revealed that spilanthol inhibits the activation of several transcription factors ( NFκB, ATF4, FOXO1, IRF1, ETS1, and AP-1) which may explain the effect of spilanthol on gene expression. The antihypertensive effect of spilanthol was blocked by CB1 antagonist rimonabant Rimonabant (also known as SR141716; trade names Acomplia, Zimulti) is an anorectic ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Acmella Oleracea
''Acmella oleracea'' is a species of flowering herb in the family Asteraceae. Common names include toothache plant, Szechuan buttons, paracress, jambu, buzz buttons, tingflowers and electric daisy. Its native distribution is unclear, but it is likely derived from a Brazilian ''Acmella'' species. A small, erect plant, it grows quickly and bears gold and red inflorescences. It is frost-sensitive but perennial in warmer climates. Its specific epithet (botany), specific epithet ''oleracea'' means "vegetable/herbal" in Latin and is a form of (). Culinary uses For culinary purposes, small amounts of shredded fresh leaves are said to add a unique flavour to salads. Cooked leaves lose their strong flavor and may be used as Leaf vegetable, leafy greens; additionally, they are edible in their raw form, along with the fruit. Young branches can be cooked and eaten without concern. In Madagascar, the plant is known as ''brèdes mafane'', and is a main ingredient in the national dish of the i ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Fatty Acid Amide
Fatty acid amides (FAAs) are amides formed from a fatty acid and an amine. In nature, many FAAs have ethanolamine as the amine component. Also known as ''N''-acylethanolamines, they contain the functionality RC(O)N(H)CH2CH2OH. A well known example is anandamide. Other fatty acid amides are fatty acid primary amides (FAPAs). They contain the functionality RC(O)NH2). Oleamide is an example of this class of FAPAs. Natural occurrences FAAs play a role in intracellular signalling. The signalling is controlled in part by fatty acid amide hydrolases, which convert the amide to the parent fatty acid. One example of signaling is induced by the binding of anandamide to the cannabinoid receptors. Aliphatic amides can be found in ''Zanthoxylum'' species found in Nigeria.The Nigerian Zanthoxylum; Chemical and biological values. S. K. Adesina, Afr. J. Trad. CAM, 2005, volume 2, issue 3, pages 282-301article See also * Fatty acid ester Fatty acid esters (FAEs) are a type of ester that ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Hydroxy Alpha Sanshool
Hydroxy can refer to: * In chemical nomenclature, the prefix "hydroxy-" shows the presence of a hydroxyl In chemistry, a hydroxy or hydroxyl group is a functional group with the chemical formula and composed of one oxygen atom covalently bonded to one hydrogen atom. In organic chemistry, alcohols and carboxylic acids contain one or more hydroxy ... functional group (−OH). * An abbreviation for the medication hydroxyzine, which is commonly sold under the brand names Atarax, Ucerax, Serecid, and Vistaril. * Hydroxy gas, a nickname for oxyhydrogen, a combination of hydrogen and oxygen gas produced from the electrolysis of water. {{disambiguation ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Capsazepine
Capsazepine is a synthetic antagonist of capsaicin. It is used as a biochemical tool in the study of TRPV ion channels. Pharmacology Capsazepine blocks the painful sensation of heat caused by capsaicin (the active ingredient of chilli pepper) which activates the TRPV1 ion channel. Capsazepine is therefore considered to be a TRPV1 antagonist. The TRPV1 channel functions as a pain and temperature sensor in mammalians. Capsazepine blocks the activation of TRPV1 channels by other chemicals, but not by other painful stimuli such as heat. Depending on the pharmacological assay, the IC50 is in the nanomolar to low micromolar range. In addition to its effects on TRPV1 channels, it was also shown to activate the noxious chemical sensor TRPA1 channel, inhibit the cold activated TRPM8 channel, voltage-activated calcium channels and nicotinic acetylcholine receptors. It mainly serves as a tool to study the TRPV1 ion channel. Development Capsazepine was discovered by a research group worki ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Rimonabant
Rimonabant (also known as SR141716; trade names Acomplia, Zimulti) is an anorectic antiobesity drug approved in Europe in 2006 but was withdrawn worldwide in 2008 due to serious psychiatric side effects; it was never approved in the United States. Rimonabant is an inverse agonist for the cannabinoid receptor CB1 and was first-in-class for clinical development. History Rimonabant is a selective CB1 receptor blocker and was discovered and developed by Sanofi-Aventis. On 21 June 2006, the European Commission approved the sale of rimonabant in the then-25-member European Union as a prescription drug for use in conjunction with diet and exercise for patients with a body mass index (BMI) greater than 30 kg/m2, or patients with a BMI greater than 27 kg/m2 with associated risk factors, such as type 2 diabetes or dyslipidaemia. FroEMA index page It was first in its class to be approved anywhere in the world. Rimonabant was submitted to the Food and Drug Administration ( ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
AP-1 Transcription Factor
Activator protein 1 (AP-1) is a transcription factor that regulates gene expression in response to a variety of stimuli, including cytokines, growth factors, stress, and bacterial and viral infections. AP-1 controls a number of cellular processes including differentiation, proliferation, and apoptosis. The structure of AP-1 is a heterodimer composed of proteins belonging to the c-Fos, c-Jun, ATF and JDP families. History AP-1 was first discovered as a TPA-activated transcription factor that bound to a cis-regulatory element of the human metallothionein IIa ( hMTIIa) promoter and SV40. The AP-1 binding site was identified as the 12-O-Tetradecanoylphorbol-13-acetate ( TPA) response element (TRE) with the consensus sequence 5’-TGA G/C TCA-3’. The AP-1 subunit Jun was identified as a novel oncoprotein of avian sarcoma virus, and Fos-associated p39 protein was identified as the transcript of the cellular Jun gene. Fos was first isolated as the cellular hom ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
ETS1
Protein C-ets-1 is a protein that in humans is encoded by the ''ETS1'' gene. The protein encoded by this gene belongs to the ETS family of transcription factors. Function There are 28 ETS genes in humans and 27 in mice. They bind the DNA via their winged-helix-turn-helix DNA binding motif known as the Ets domain that specifically recognizes DNA sequences that contain a GGAA/T core element. However, Ets proteins differ significantly in their preference for the sequence flanking the GGAA/T core motif. For instance, the consensus sequence for Ets1 is PuCC/a-GGAA/T-GCPy. On the other hand, many natural Ets1-responsive GGAA/T elements differ from this consensus sequence. The later suggests that several other transcription factors may facilitate Ets1 binding to unfavorable DNA sequences. ChIP-Seq studies have shown that Ets1 can bind both AGGAAG and CGGAAG motifs. Ets1 binds to DNA as a monomer. Phosphorylation of serine residues of the C-terminal domain (in the nucleotide sequence ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
IRF1
Interferon regulatory factor 1 is a protein that in humans is encoded by the ''IRF1'' gene. Function Interferon regulatory factor 1 was the first member of the interferon regulatory transcription factor (IRF) family identified. Initially described as a transcription factor able to activate expression of the cytokine Interferon beta, IRF-1 was subsequently shown to function as a transcriptional activator or repressor of a variety of target genes. IRF-1 regulates expression of target genes by binding to an interferon stimulated response element (ISRE) in their promoters. The IRF-1 protein binds to the ISRE via an N-terminal helix-turn-helix DNA binding domain, which is highly conserved among all IRF proteins. Beyond its function as a transcription factor, IRF-1 has also been shown to trans-activate the tumour suppressor protein p53 through the recruitment of its co-factor p300. IRF-1 has been shown to play roles in the immune response, regulating apoptosis, DNA damage and tu ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
ATF4
Activating transcription factor 4 (tax-responsive enhancer element B67), also known as ATF4, is a protein that in humans is encoded by the ''ATF4'' gene. Function This gene encodes a transcription factor that was originally identified as a widely expressed mammalian DNA binding protein that could bind a tax-responsive enhancer element in the LTR of HTLV-1. The encoded protein was also isolated and characterized as the cAMP-response element binding protein 2 ( CREB-2). The protein encoded by this gene belongs to a family of DNA-binding proteins that includes the AP-1 family of transcription factors, cAMP-response element binding proteins ( CREBs) and CREB-like proteins. These transcription factors share a leucine zipper region that is involved in protein–protein interactions, located C-terminal to a stretch of basic amino acids that functions as a DNA-binding domain. Two alternative transcripts encoding the same protein have been described. Two pseudogenes are located on ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Forkhead Box Protein O1
Forkhead box protein O1 (FOXO1), also known as forkhead in rhabdomyosarcoma (FKHR), is a protein that in humans is encoded by the ''FOXO1'' gene. FOXO1 is a transcription factor that plays important roles in regulation of gluconeogenesis and glycogenolysis by insulin signaling, and is also central to the decision for a preadipocyte to commit to adipogenesis. It is primarily regulated through phosphorylation on multiple residues; its transcriptional activity is dependent on its phosphorylation state. Function Adipogenesis FOXO1 negatively regulates adipogenesis. Presently, the exact mechanism by which this is accomplished is not entirely understood. In the currently accepted model, FOXO1 negatively regulates adipogenesis by binding to the promoter sites of PPARG and preventing its transcription. Rising levels of PPARG are required to initiate adipogenesis; by preventing its transcription, FOXO1 is preventing the onset of adipogenesis. During stimulation by insulin, FOXO1 is e ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
NF-κB
Nuclear factor kappa-light-chain-enhancer of activated B cells (NF-κB) is a family of transcription factor protein complexes that controls transcription (genetics), transcription of DNA, cytokine production and cell survival. NF-κB is found in almost all animal cell types and is involved in cellular responses to stimuli such as stress, cytokines, free radicals, heavy metals, ultraviolet irradiation, oxidized LDL, and bacterial or viral antigens. NF-κB plays a key role in regulating the immune response to infection. Incorrect regulation of NF-κB has been linked to cancer, inflammatory and autoimmune diseases, septic shock, viral infection, and improper immune development. NF-κB has also been implicated in processes of synaptic plasticity and memory. Discovery NF-κB was discovered by Ranjan Sen in the lab of Nobel laureate David Baltimore via its interaction with an 11-base pair sequence in the immunoglobulin light-chain Enhancer (genetics), enhancer in B cells. Later work ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Macrophage
Macrophages (; abbreviated MPhi, φ, MΦ or MP) are a type of white blood cell of the innate immune system that engulf and digest pathogens, such as cancer cells, microbes, cellular debris and foreign substances, which do not have proteins that are specific to healthy body cells on their surface. This self-protection method can be contrasted with that employed by Natural killer cell, Natural Killer cells. This process of engulfment and digestion is called phagocytosis; it acts to defend the host against infection and injury. Macrophages are found in essentially all tissues, where they patrol for potential pathogens by amoeboid movement. They take various forms (with various names) throughout the body (e.g., histiocytes, Kupffer cells, alveolar macrophages, microglia, and others), but all are part of the mononuclear phagocyte system. Besides phagocytosis, they play a critical role in nonspecific defense (innate immunity) and also help initiate specific defense mechanisms (adapti ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
