137 results about "TRPV1" patented technology

The invention relates to a method for determining at least part of the cellular composition of at least one biological sample comprising leukocytes, wherein the proportion of at least one type of leukocyte is determined based on the identified methylation levels, in order to predict the relative distribution of that type of leukocyte in the sample. The invention further relates to the use of at least one artificial nucleic acid molecule for determining at least part of the cellular composition of a biological sample comprising leukocytes according to the above-mentioned method. In the context of the invention, the following CpG sites according to the invention with cell-type-specific methylation could be identified: cg22381196 (DHODH), cg12483340 (TMEM87A), cg06270401 (DYRK4), cg23054181 (FAM169BP), cg26076724 (RP11-146I2.2), cg12249234 (KSR1), cg04468741 (MICAL2), cg05074138 (CTLA4), cg05705140 (LINC01237), cg15564619 (SKI), cg11531557 (HMBOX1), cg02212339 (TRPV1), cg22488278 (ZFYVE28), cg02240030 (MAD1L1) and cg24408769 (JARID2).

The invention provides a polypeptide for inducing tumor cell immunogenic death, a bioactive solution and application of the polypeptide and the bioactive solution, and belongs to the technical field of biological medicine. Comprising an end-capping group, a phosphorylated gelling factor, a matrix metalloproteinase-2 response sequence and a transient receptor potential vanillic acid receptor 1 (TRPV1) agonist which are connected in sequence, the amino acid sequence of the phosphorylated gelling factor is GFFpY, and the response sequence of the matrix metalloproteinase-2 is PLGVR. The anti-tumor polypeptide provided by the invention can generate enzymatic in-situ self-assembly through the action of ALP and MMP-2 overexpressed outside tumor cells, and sequentially release pharmacophores outside and inside the cells to cause mitochondrial stress and endoplasmic reticulum stress and synergistically induce immunogenic death of the tumor cells.

The present invention provides a composition for inhibiting the TRPV1 pathway and reducing skin irritation, comprising camellia extract and purslane extract, the mass ratio of camellia extract to purslane extract being 0.01-10:0.01-10. The composition of the present invention for inhibiting the TRPV1 pathway and reducing skin irritation comprises camellia extract and purslane extract, which inhibit the TRPV1 pathway. Both exhibit a synergistic effect in increasing the irritation response threshold, reducing the skin sensitivity reaction, and relieving tingling, itching, and burning sensations of the skin due to TRPV1 channel activation.

A method of producing a population of mature human pluripotent stem cell-derived sensory neurons (hPSC-SNs) expressing a target gene associated with at least one of nociceptive pain, chronic pain, pruriception and a nociceptive- or pruriceptive- mediated condition, the method comprising introducing into a population of human pluripotent stem cells (hPSCs) a composition comprising at least one site-directed nuclease targeting a site within the target gene, and at least one nucleic acid comprising a nucleotide sequence encoding at least one screenable, selectable marker that is flanked by (i) a nucleotide sequence homologous with a region located upstream of the target site within the target gene and (ii) a nucleotide sequence homologous with a region located downstream of the target site within the target gene, wherein the target site is located downstream of the open reading frame of the target gene, and wherein the site-directed nuclease cleaves the target site of the target gene and the nucleic acid encoding the screenable, selectable marker is inserted at the target site; covering said population of hPSCs under an extracellular matrix comprising at least one neuronal differentiation driver to produce a sensory committed neural crest population; contacting said sensory committed neural crest population with at least one neuronal differentiation driver and at least one neurotrophic factor to produce a population of early sensory neurons (SNs); and contacting said population of early SNs with at least one neurotrophic factor to produce a population of mature hPSC-SNs expressing at least one of SN marker or one pan neuronal marker; isolating the cells expressing the at least one screenable, selectable marker, wherein said population of mature hPSC-SNs expressed said one target gene associated with nociceptive pain, chronic pain, pruriception a nociceptive- or pruriceptive- mediated condition, and wherein said population of mature hPSC-SNs responds to a nociceptive and pruriceptive stimulus.

The present disclosure relates to aqueous topical formulations comprising at least one TRPV1 antagonist and at least one specific plant extract. Also disclosed herein are methods of treating at least one symptom of menopause comprising topically administering an effective amount of the formulations disclosed.

Tobacco products comprising smokeless tobacco products and active ingredients, including those that antagonize nicotinic acetylcholine receptors, the TRPV1 channel, and / or the TRPA1 channel are disclosed. Nicotine replacement therapies comprising active ingredients, including those that antagonize nicotinic acetylcholine receptors, the TRPV1 channel, and / or the TRPA1 channel. The active ingredient may reduce or eliminate sensory irritation arising due to use of the product. Analgesic compositions comprising active ingredients. Methods of reducing taste and sensory irritation by employing an active ingredient.

The invention relates to a composition with moisturizing, soothing and repairing effects and application thereof. The composition with the moisturizing, soothing and repairing effects comprises a pomelo fruit extract, a capparis spinosa fruit extract and hydroxyphenyl propionamide benzoic acid. Three active components, namely the pomelo fruit extract, the capparis spinosa fruit extract and the hydroxyphenyl propionamide benzoic acid, are creatively combined for use, wherein the pomelo fruit extract can inhibit release of inflammatory factors, reduce ultraviolet-induced DNA damage and inflammatory response, neutralize free radicals and reduce oxidative stress damage; wherein the capparis spinosa fruit extract can quickly moisturize, enhance cell viability and promote enhancement of a skin barrier; wherein hydroxyphenyl propionamide benzoic acid can block symptoms such as skin redness and swelling, pruritus and pain caused by the fact that histamine activates a TRPV1 pathway. The three components are matched with one another, have a synergistic effect in the aspects of moisturizing, relieving the skin and repairing the skin barrier, and have an excellent effect when being applied to cosmetics with related effects.

The invention discloses an antioxidant repairing composite composition containing a picea norvegensis leaf extract and a preparation method thereof, and relates to the field of skincare products, the picea norvegensis leaf extract, leontopodium alpinum and citrus fruit extract are used as main materials, and the picea norvegensis leaf extract and leontopodium alpinum can play a role in the whole pathway of Nrf2 and NF-kappa B, so that the antioxidant repairing composite composition has the advantages that the antioxidant repairing composite composition is free of toxic and side effects; and the citrus fruit extract can inhibit the activation of TRPV1 and relieve the discomfort of the sensitive skin, so that the composition not only can improve the skin barrier of the sensitive skin, but also can inhibit the activity of the TRPV1, and the TRPV1 can be activated only by breaking the barrier and damaging the barrier under the two actions, so that the skin barrier can be well repaired. And the vicious circle of barrier injury can be aggravated by the excessive activation of the TRPV1, so that the stabilization and repair of the skin are realized, and the emulsion provided by the invention has a relatively good DPPH clearance rate and relatively good oxidation resistance.

The invention relates to a method for establishing a PC12 cell model for evaluating the soothing effect of cosmetics. The method comprises the following steps: S1, determining model stimulation conditions; S11, detecting cell viability of a control group and cell viability of capsaicin groups with different concentrations by using a CCK-8 method; s12, observing the activation condition of the capsaicin on the TRPV1 channel of the PC12 cell by using a fluorescence microscope; s13, detecting the expression condition of the capsaicin to the TRPV1 of the PC12 cell by using an ELISA method; s14, detecting the expression condition of the capsaicin on the PC12 cell neuropeptide P substance by using an ELISA (enzyme-linked immuno sorbent assay) method; and S15, detecting the expression condition of capsaicin on IL-33 related to PC12 cell neuroinflammation by using an ELISA method. The invention also relates to evaluating the soothing efficacy of the cosmetic raw material. According to the method, the nerve-like cells are adopted to establish the cell model, the process that human skin is subjected to external stimulation and nerve reaction is excessive is effectively simulated, and the established in-vitro cell model can be used for evaluating the effectiveness of cosmetic raw materials / finished products in protecting or repairing skin nerve disorder and evaluating whether the cosmetic raw materials / finished products have soothing efficacy or not.

The invention discloses a compound and application thereof, and belongs to the technical field of medicinal chemistry. The structure of the compound is shown as a formula I. In the formula I, A ring is selected from C6-C12 aryl or C5-C6 cycloalkyl; r1 and R2 are independently selected from one or more of hydrogen, C1-C10 straight chain or branched chain alkyl, C3-C6 naphthenic base, C1-C10 alkoxy, substituted C1-C10 straight chain or branched chain alkyl, substituted C3-C6 naphthenic base, substituted C1-C10 alkoxy, amino, halogen, nitrile group and nitryl; m and n respectively represent the numbers of R1 and R2, m + n = 5, and m > = 1; l is selected from a thioformamido group, a formamido group, a sulfonyl group, a sulfonamido group, a sulfonylurea group, an ester group or a carbonyl group. The compound is unique and novel in structure, and has relatively strong inhibitory activity and excellent analgesic effect as a TRPV1 inhibitor. # imgabs0 #

Tobacco products comprising smokeless tobacco products and active ingredients, including those that antagonize nicotinic acetylcholine receptors, the TRPV1 channel, and / or the TRPA1 channel are disclosed. Nicotine replacement therapies comprising active ingredients, including those that antagonize nicotinic acetylcholine receptors, the TRPV1 channel, and / or the TRPA1 channel. The active ingredient may reduce or eliminate sensory irritation arising due to use of the product. Analgesic compositions comprising active ingredients. Methods of reducing taste and sensory irritation by employing an active ingredient.

The present invention relates to the technical field of plant compositions, and in particular to a plant anti-allergic, antipruritic and analgesic composition and its application. The present application discloses a plant anti-allergic, antipruritic and analgesic composition, which comprises the following raw materials by weight percentage: gentiana cyanus extract: 0.5%-5%, kava root extract: 1%-10%, prickly pear cactus leaf extract: 0.5%-5%, Centella asiatica extract: 1%-10%, and the balance is water. The present application provides a plant anti-allergic, antipruritic and analgesic composition, which achieves the effects of anti-inflammatory, anti-allergic, antipruritic and analgesic by inhibiting NO generation, inhibiting histamine pathways and inhibiting TRPV1 ion channels.

The invention provides a compound for regulating and controlling a TRPV1 ion channel. The structural formula of the compound is as shown in formula I. The invention also provides application of the compound in preparation of a medicine for regulating and controlling the TRPV1 ion channel. The invention provides a pharmaceutical composition with an anti-inflammatory effect, the pharmaceutical composition comprises the compound, and pharmaceutically acceptable auxiliary materials or auxiliary components are added to prepare a pharmaceutically common preparation. Compared with azobenzene, the compound has the advantages that the illumination wavelength is increased, the illumination wavelength is 660 nm, a TRPV1 targeted photosensitizer is used, a channel is activated by using a low-energy near-infrared light'precise key ', depth, safety and reversibility are considered, and the anti-inflammatory effect of the compound is obvious.

A method of producing a population of mature human pluripotent stem cell-derived sensory neurons (hPSC-SNs) expressing a target gene associated with at least one of nociceptive pain, chronic pain, pruriception and a nociceptive- or pruriceptive- mediated condition, the method comprising introducing into a population of human pluripotent stem cells (hPSCs) a composition comprising at least one site-directed nuclease targeting a site within the target gene, and at least one nucleic acid comprising a nucleotide sequence encoding at least one screenable, selectable marker that is flanked by (i) a nucleotide sequence homologous with a region located upstream of the target site within the target gene and (ii) a nucleotide sequence homologous with a region located downstream of the target site within the target gene, wherein the target site is located downstream of the open reading frame of the target gene, and wherein the site-directed nuclease cleaves the target site of the target gene and the nucleic acid encoding the screenable, selectable marker is inserted at the target site; covering said population of hPSCs under an extracellular matrix comprising at least one neuronal differentiation driver to produce a sensory committed neural crest population; contacting said sensory committed neural crest population with at least one neuronal differentiation driver and at least one neurotrophic factor to produce a population of early sensory neurons (SNs); and contacting said population of early SNs with at least one neurotrophic factor to produce a population of mature hPSC-SNs expressing at least one of SN marker or one pan neuronal marker; isolating the cells expressing the at least one screenable, selectable marker, wherein said population of mature hPSC-SNs expressed said one target gene associated with nociceptive pain, chronic pain, pruriception a nociceptive- or pruriceptive- mediated condition, and wherein said population of mature hPSC-SNs responds to a nociceptive and pruriceptive stimulus.

The present application discloses a compound of formula (I), compositions comprising said compound, and a method of using said compound as a cannabinoid receptor ligand in the treatment or prevention of diseases associated with a cannabinoid receptor, such as, CB1, CB2, 5HT1A, 5HT2A, GPR18, GPR119, TRPV1, TPRV2, PPARγ or a μ-opioid receptor.

Formula I below: [Formula 1] The present invention provides compounds of formula Ia, Ib, III, IV or V as defined herein, and their use in modulating the activity of voltage-gated potassium channels and / or TRPV1 channels and treating conditions associated with the activity of these channels, such as conditions associated with neuronal vortex excitation.

Compounds represented by Formula I: (I) wherein A, B, W, V, Z, Ra, Rb, n and m are as defined in the instant specification, or by Formula la, lb, III, IV or V, as defined in the instant specification, and uses thereof in modulating an activity of a voltage-dependent potassium channel and / or a TRPV1 channel and in treating a medical condition associated with an activity of these channels, such as medical conditions associated with neuronal hyper-excitability, are provided.

This application provides a barrier-repairing composition and its use. The composition comprises panthenol, niacinamide, folic acid, and cobalamin in a mass ratio of 3-7:1-5:0.0005-0.1:0.00005-0.01. This application also provides uses of the composition and products containing the same. The composition utilizes panthenol, niacinamide, folic acid, and cobalamin in combination, where the components complement and enhance each other, achieving a synergistic effect in upregulating BMAL2 gene expression. This enhances the DNA damage repair capacity of skin fibroblasts and potentially promotes barrier repair. Furthermore, the composition provided herein can significantly reduce the expression of capsaicin receptor 1 (TRPV1) and increase the expression of involucrin, PIEZO1, and TNXB, reducing skin discomfort and enhancing skin barrier function. Furthermore, the composition provided herein can reduce the expression of inflammatory factors, demonstrating its anti-inflammatory effect.

The application discloses a composition with soothing anti-inflammatory anti-wrinkle firming efficacy and a preparation method thereof, and the composition comprises a TRPV1 inhibitor, an extract of Glycyrrhiza inflata Bat., palmitoyl tripeptide-1 and palmitoyl tetrapeptide-7. The four raw materials are compounded to have a synergistic effect, reduce the release of pro-inflammatory mediators and inhibit the high reactivity of nerve fibers to achieve soothing anti-inflammatory and anti-irritation; promote the generation of self collagen and sodium hyaluronate, reduce the oxidative stress response to achieve the anti-wrinkle firming efficacy and delay skin aging. The composition has comprehensive effects in soothing, anti-inflammatory, anti-irritation, anti-oxidation, anti-wrinkle and firming, reduces the generation of inflammation and delays skin aging, relieves the burning and stinging sensation of the skin at the same time, and meets the requirements of safety and high efficiency pursued by sensitive skin groups.

The present application relates to the technical field of asiatic acid, and particularly relates to an asiatic acid derivative and a preparation method.The asiatic acid derivative provided by the present application has R which is a straight chain or a branched chain with 1-24 carbon atoms, or a saturated or unsaturated monohydric alcohol alkyl formed by removing a hydroxyl group.The R group of the asiatic acid derivative of the present application has higher water solubility and oil solubility, especially oil solubility, so that the asiatic acid derivative has obviously enhanced liposolubility compared with asiatic acid, is easily dissolved in natural oil, alkane and other ester solvents, and has obviously enhanced biological activity, so that the asiatic acid derivative of the present application has high availability, improves the inhibition effect of the asiatic acid derivative on EDNRA and TRPV1, and further improves the anti-tumor effect, and the asiatic acid derivative has no safety risk.

The invention relates to a TRPV1 / URAT1 dual inhibitor containing a naphthalene ring and a 2, 2-difluorobenzodioxole structure and an application of the TRPV1 / URAT1 dual inhibitor. The invention relates to a TRPV1 / URAT1 dual inhibitor containing a naphthalene ring and a 2, 2-difluorobenzodioxole structure, and the structural formula of the TRPV1 / URAT1 dual inhibitor is as follows: # imgabs0 #. The compound is unique and novel in structure, a preparation method of the compound is researched and provided, the compound has high inhibitory activity as a TRPV1 / URAT1 dual inhibitor, IC50 to TRPV1 is smaller than or equal to 100 nM, IC50 to URAT1 is smaller than or equal to 1 mu M, and inhibitory activity IC50 to an hERG channel is larger than 30 mu M; the traditional Chinese medicine composition has an excellent treatment effect on hyperuricemia, gout, inflammatory pain and the like, also has a better analgesic effect, and can be used as an analgesic medicine, a medicine for treating gout or hyperuricemia and the like.

The present invention relates to antibodies that bind to TRPV1. The present invention also relates to certain epitopes of the protein TRPV1. The present invention also relates to immunoconjugates and compositions comprising such antibodies. The present invention also provides methods of producing such antibodies. The present invention further provides the use of such antibodies for therapeutic purposes, for example in the treatment of pain.

Disclosed herein is a novel pharmaceutical composition for treating pain, wherein the pharmaceutical composition targets a transient receptor potential vanilloid 1 (TRPV1) receptor and acts as an antagonist.

The application belongs to the technical field of genetic engineering, and relates to a gene editing method for enhancing low-temperature tolerance of fish by targeting a trpv1 gene and application. The application precisely edits a fish trpv1 gene by using CRISPR-Cas9 technology, blocks negative signal transduction induced by low temperature, and releases the inhibition on related metabolic pathways. The application provides a brand-new molecular target for improvement of low-temperature tolerance of fish and cold-resistant breeding of aquatic products, and has important application value.

This application relates to the field of molecular biology, and in particular to a screening method for TRPV1 agonists and its application. The provided screening method includes: obtaining transcriptome gene sequences from the coral *Dipsastraea rotumana* for functional annotation analysis, followed by classification to obtain transcriptome data; performing sequence alignment and phylogenetic tree construction on the transcriptome data to identify polypeptide sequences highly homologous to existing TRPV1 agonists; performing three-dimensional modeling of the polypeptide sequences to obtain the polypeptide 3D structure; and sequentially performing molecular docking and molecular dynamics analysis on the polypeptide 3D structure and the TRPV1-3D structure to screen for TRPV1 agonists. This method is highly efficient and low-cost, with high efficiency and accuracy; it facilitates the application of TRPV1 agonists in the preparation of products for treating neuroinflammation, providing new ideas and solutions for the treatment of neurodegenerative diseases.

The invention discloses a capsaicin stimulation inhibitor for cosmetics and a preparation method and application thereof.The preparation method of the capsaicin stimulation inhibitor for cosmetics comprises the following steps that A, medicinal materials are soaked in an extraction solvent with the weight being 15-20 times that of the medicinal materials for 2-16 h, and a soaking solution is obtained; the extraction solvent is an aqueous alkali solution with the concentration of 0.2 mol / L-0. 8mol / L, and the medicinal materials are at least one of calendula officinalis, purslane and radix scrophulariae; b, extracting the soak solution for 1-3 hours under the condition of 95-105 DEG C; the capsaicin stimulation inhibitor for cosmetics prepared by the preparation method disclosed by the invention can obviously inhibit secretion of keratinocyte IL-1alpha and expression of TRPV-1 protein caused by capsaicin stimulation, and the combination of every two inhibitors has a certain synergistic effect; therefore, the compound can be applied to inhibition of TRPV1 expression induced by capsaicin, inhibition of IL-1alpha secretion induced by capsaicin and preparation of skin external preparations.

The invention relates to a novel TRPV1 channel blocker developed by high-throughput screening of marine natural products, and hexa-epoxyanthrone separated from marine bacteria. In particular, these chrexanthophycins are potent TRPV1 inhibitors, which are potent as analgesic agents. The present application also relates to a method of treating pain, comprising applying an analgesic comprising these chrexanthophycins to a pain site of a patient.

Novel peptides and nucleotides encoding the peptides, and compositions containing the peptides and / or nucleotides are disclosed. Also disclosed are uses of the peptides, nucleotides, and compositions. N-terminus and / or a C-terminus of the peptides may be capped. The peptides, nucleotides, and compositions are suitable for treating pain or a transient receptor potential cation channel subfamily V member 1 (TRPV1)-mediated disease.

The application discloses a sciaenops ocellatus TRPV1 inhibiting peptide, a preparation method and application, belongs to the polypeptide field, and the amino acid sequence of the sciaenops ocellatus TRPV1 inhibiting peptide is RLF.The sciaenops ocellatus TRPV1 inhibiting peptide, the preparation method and the application take the skin of sciaenops ocellatus as starting raw material, and the amino acid sequence of the sciaenops ocellatus TRPV1 inhibiting peptide is successfully obtained through a specific process.Experiment verification shows that the prepared sciaenops ocellatus TRPV1 inhibiting peptide shows excellent inhibiting effect on TRPV1.The inhibiting peptide can be used for preparing a TRPV1 antagonist, the antagonist can play an anti-inflammatory regulation role through multiple channels, and can effectively down-regulate skin microvascular hyperreactivity.

This invention belongs to the field of biomedical technology, specifically relating to a peptide targeting TRPV1 and its applications. A peptide targeting TRPV1 has the amino acid sequence shown in SEQ ID NO.1. The peptide also includes a mutant obtained by amino acid scanning mutation based on the sequence shown in SEQ ID NO.1. The amino acid sequence of the mutant is shown in any one of SEQ ID NO.2-16. This peptide is used to prepare formulations that block or inhibit TRPV1 activity. This invention provides a peptide targeting TRPV1 and its applications. Through a strategy combining artificial intelligence screening and structural prediction, SEQ ID NO.1 was successfully identified and its mechanism of action was elucidated. Experimental results show that SEQ ID NO.1 and its mutants exhibit excellent analgesic activity and good safety both in vitro and in vivo, demonstrating significant clinical application potential.