41 results about "Imiquimod" patented technology

The present invention belongs to the field of traditional Chinese medicines, and particularly relates to Leixihaokang, a preparation method therefor, and use thereof. The Leixihaokang of the present invention is prepared from the following active pharmaceutical ingredients in parts by weight: 10 parts of Tripterygium glycosides and 0.1-1.3 parts of Artemisia annua extract. According to the present invention, animal experiments prove that the Leixihaokang can ameliorate renal damage in nephrotic syndrome caused by adriamycin, reduce the occurrence of proteinuria, and reduce the apoptosis of renal tissue cells. Meanwhile, the Leixihaokang of the present invention has a good inhibitory effect on renal, hepatic, splenic, and cardiac toxicity in the treatment process of nephrotic syndrome. According to the present invention, animal experiments also prove that the Leixihaokang can ameliorate skin injury in imiquimod-induced psoriasis, reduce inflammatory infiltration and alleviate skin damage. Meanwhile, the Leixihaokang has a certain degree of inhibitory effect on the hepatic and reproductive system toxicity in the treatment process of psoriasis.

The invention discloses an indoline derivative and application thereof. According to the invention, the regulation effect of the derivative on the chemotaxis and secretion functions of ILC3 is evaluated; it is found that the derivative has a promoting effect on chemotaxis of ILC3 to an inflammatory site and up-regulation of IL-22 expression, has very remarkable effects on mouse ulcerative colitis (UC) induced by DSS, mouse Crohn disease (CD) induced by TNBS, acute lung injury induced by lipopolysaccharide (LPS), mouse psoriasis induced by imiquimod and other diseases in vivo, and is superior to existing clinical treatment drugs. Good development and application prospects are realized.

The invention discloses an application of sarcandra glabra polysaccharide in preparation of a medicine for preventing and / or treating psoriasis and delaying relapse of psoriasis. The glabrous sarcandra herb polysaccharide can relieve inflammation caused by psoriasis, reduce expression of memory T cells at skin lesions of a psoriasis recurrence model mouse and relieve psoriasis symptoms of the recurrence model mouse. The invention finds that the glabrous sarcandra herb polysaccharide can obviously improve the skin injury degree of an imiquimod (imiquimod, IMQ) interval induced psoriasis recurrence model mouse, reduce the skin erythema, thickening and scale of the IMQ interval induced psoriasis recurrence model mouse, and reduce the expression of memory T cells at the skin injury part of the psoriasis recurrence model mouse, so that the glabrous sarcandra herb polysaccharide can be used for treating the psoriasis. The glabrous sarcandra herb polysaccharide has great application prospects in preparation of the medicine for preventing / treating the psoriasis, and especially can relieve recurrence symptoms of the psoriasis.

The invention belongs to the technical field of biology, and relates to application of isovaleric acid in treatment of psoriasis. In order to solve the problems that existing psoriasis treatment drugs (such as biological agents) have side effects, the curative effect is reduced, and relapse occurs after drug withdrawal, the invention provides a psoriasis treatment scheme taking isovaleric acid as an active component, and the imiquimod-induced psoriasis-like skin lesion can be remarkably relieved by locally smearing the isovaleric acid with the concentration of 2mM; the epidermis excessive proliferation and the expression of inflammatory factors such as IL-17A, IL-17F and CXCL1 are reduced. The isovaleric acid disclosed by the invention is a small molecule compound, is simple to prepare, convenient to administrate and high in safety, fills the application blank of the isovaleric acid in the field of psoriasis treatment, and provides a new effective way for psoriasis treatment.

The invention discloses a double-target inhibitor with anti-psoriasis activity, and the structural general formula of the double-target inhibitor is shown in the specification. The double-target inhibitor with anti-psoriasis activity provided by the invention has good efficacy on in-vitro anti-psoriasis related tests and in-vivo imiquimod induced mouse models; the compound B5e shows better anti-psoriasis activity than their parent drugs and combined administration of the parent drugs.

The invention belongs to the field of medicines, and particularly relates to a quinonoid diterpenoid compound, a preparation method thereof and application of the quinonoid diterpenoid compound in treating psoriasis. The synthetic raw materials are easy to obtain, the steps are simple, the reaction is easy to control, and the method has important reference and practical values for preparing quinonoid diterpenoid compounds on a large scale. The prepared compound 5 (LZY-15) has remarkable AhR agonist activity. The drug effect of the compound 5 (LZY-15) on skin inflammation psoriasis is explored through animal experiments, and the compound 5 (LZY-15) can obviously relieve squamation and skin thickening of psoriasis-like skin lesion local parts induced by imiquimod and improve the pathological score of psoriasis; the contents of leucocytes, monocytes and neutrophils in peripheral blood of mice can be obviously reduced, and the inflammation level of the mice is reduced; in addition, the traditional Chinese medicine composition can also obviously improve cuticle pathological changes such as hyperkeratinization and incomplete keratinization, epidermal pathological changes such as spinous skin thickening and granular layer disappearance, and changes such as corium papillary extension caused by imiquimod induction.

The invention discloses an application of a CD177 targeted membrane modified liposome in preparation of a medicine for preventing and / or treating systemic lupus erythematosus. The structure of the CD177 targeting membrane modified lipidosome is divided into three layers, and comprises a lipidosome loaded with a PADI4 inhibitor, a targeting recognition layer formed by coupling CD177 targeting peptide on the surface of the lipidosome, and a bionic functional layer formed by coating a natural neutrophile granulocyte membrane on the outermost layer. In an imiquimod (IMQ)-induced lupus model, the medicine treatment shows strong disease remission capability: 1) improving the whole body phenotype: obviously reducing the swollen spleen and lymph node of lupus mice; 2) repairing kidney functions: significantly relieving glomerulonephritis, and reducing inflammatory cell infiltration and IgG and complement C3 deposition in glomerulus, and 3) significantly reducing the level of proinflammatory cytokines in serum and the titer of a lupus marker anti-dsDNA antibody.

The application belongs to the technical field of animal model construction, and particularly relates to a construction method of a stress-aggravated psoriasis mouse model and application. The construction method comprises the following steps: (1) shaving the back of the mouse, placing the mouse in a 50-milliliter breathable centrifuge tube, and limiting the activity for four hours; (2) taking out the mouse, and waiting for the back skin to dry; (3) uniformly applying imiquimod cream to the back of the mouse, and placing the mouse back into the cage; and (4) repeating the above steps every day until the stress-aggravated psoriasis mouse model is successfully constructed. The construction method can quickly and simply construct the stress-aggravated psoriasis mouse model for subsequent research.

The application discloses a Bifidobacterium breve capable of relieving psoriasis and an application thereof, and belongs to the technical field of microorganisms. The application screens a Bifidobacterium breve CCFM683, and the Bifidobacterium breve CCFM683 has the effect of relieving psoriasis caused by imiquimod, which is specifically embodied in the following aspects: (1) significantly reducing the weight loss of psoriasis mice; (2) significantly improving the pathological characteristics such as scales, thickening and redness of the skin of psoriasis-like mice; (3) regulating the level of skin immune factors of psoriasis-like mice; and (4) significantly inhibiting the proliferation of keratinocytes of the skin of psoriasis mice. The Bifidobacterium breve CCFM683 has great application prospect in the preparation of food or medicine for preventing and / or treating psoriasis.

The invention discloses a piperine-based pseudo-natural dimer amide alkaloid compound 1 and a piperine-based pseudo-natural dimer amide alkaloid compound 2 as well as a preparation method and medical application thereof. Dimerization of piperine is realized through a visible light catalytic reaction system Ir (ppy) 3 / 465nm LED, and optically pure enantiomers 1a / 1b and 2a / 2b are obtained through acetonitrile-water system preparative HPLC separation and purification in combination with a chiral chromatographic resolution technology. HRESIMS, multi-dimensional NMR and X-single crystal diffraction confirm that the structure of the compound has a unique cyclohexene skeleton and a bis-piperidyl structure. A biological activity research shows that the target compound has a remarkable inhibition effect on LPS-induced RAW264.7 macrophage NO release, the compound 1 shows an excellent curative effect in an imiquimod-induced psoriasis mouse model, and the effect of the compound 1 is superior to that of a positive drug benvitimod. The invention provides a green and efficient photocatalytic synthesis method, and the obtained compound provides candidate molecules for developing multi-target anti-psoriasis drugs.

The invention discloses an application of a novel peptide UPCP in preparation of a medicine for treating and / or preventing psoriasis. Belongs to the technical field of biological medicine. The application discloses the treatment effect of the novel peptide UPCP on psoriasis for the first time, and researches find that the novel peptide UPCP can effectively relieve symptoms of a psoriasis model induced by LSP, TNF alpha and M2 in an in-vitro cell experiment, significantly down-regulate the expression level of psoriasis cell markers, significantly reduce the transcriptional level of psoriasis-related inflammatory factors, and improve the psoriasis treatment effect. The condition of excessive proliferation of HaCaT cells is effectively reduced. In in-vivo experiments, psoriasis symptoms such as skin desquamation, hyperplasia, erythema, thickening and splenomegaly of an imiquimod-induced psoriasis mouse model can be effectively relieved, the effect of treating psoriasis is achieved, and a new theoretical basis and intervention means are provided for clinical treatment of psoriasis.

The application discloses a method for establishing a psoriasis animal model. The method for establishing the psoriasis animal model is realized by injecting cytokines and applying imiquimod cream externally. The model is characterized by the severity of skin lesions, histopathological changes of skin lesions, expression of CD4 + and CD8 + T cells in immunohistochemistry of skin lesions, and the level of serum inflammatory factors, and conforms to the characteristics of psoriasis. Compared with the model induced by imiquimod cream alone, the model has the advantages of faster occurrence and development of psoriasis, more obvious characteristics of the model, higher stability of the model, longer maintenance time of the model, more diversified mechanisms of the model, and reduced systemic immune response. The model established by the application is simple and easy to operate, and can be widely popularized and applied, and provides an experimental tool for the research and development of the pathogenesis and drugs of psoriasis.

The invention discloses a composite hydrogel with a redox bidirectional regulation function and a preparation method and application thereof, and belongs to the field of biomedical materials.According to the composite hydrogel, polyvinyl alcohol and carboxymethyl chitosan serve as gel matrixes, crosslinking of the two matrixes is achieved through genipin by means of the action of hydrogen bonds and amido bonds, and the composite hydrogel with the redox bidirectional regulation function is obtained. The hydrogel network is loaded with chlorella capable of removing active oxygen components and Ag (at) ZnO capable of generating the active oxygen components. According to the hydrogel, the ROS level can be indirectly regulated and controlled by regulating and controlling the illumination condition, so that potential balance between oxidative stress resistance and ROS accumulation is realized. The hydrogel is locally fed to an imiquimod-induced psoriasis mouse model, a good anti-psoriasis treatment effect is obtained, and it is proved that the hydrogel can effectively resist local skin lesion of psoriasis in a multifunctional, non-irritant and non-invasive mode.

The invention discloses a compound with anti-psoriasis activity and double-target inhibition, and the structural general formula of the compound is shown in the specification. The compound with anti-psoriasis activity and double-target inhibition provided by the invention has good efficacy on in-vitro anti-psoriasis related tests and in-vivo imiquimod induced mouse models; the compound H7e shows better anti-psoriasis activity than their parent drugs and combined administration of the parent drugs.

The invention discloses an application of total glucosides of paeony in treatment of psoriasis in combination with Jikukiespecially and calcipotriol, and relates to the technical field of medical treatment, a psoriasis-like mouse model induced by imiquimod is established, and the synergistic treatment effect of a triple therapy of total glucosides of paeony, Jikukiespecially and calcipotriol is verified; the application comprises the step of jointly applying the three medicines according to a specific dosage. The triple therapy can improve erythema, scale and infiltration symptoms of psoriasis-like skin lesion, effectively reduce the area and severity index score of psoriasis, and inhibit the protein and mRNA expression level of key proinflammatory cytokines in skin lesion tissues; compared with a single drug or a combination of two drugs, the triple therapy provided by the invention shows a better treatment effect, and a new and effective drug combination scheme is provided for clinical treatment of psoriasis.

This invention discloses a polypeptide and its applications, belonging to the field of biomedical technology. The amino acid sequence of the polypeptide is shown in SEQ ID NO: 1. The polypeptide is prepared by conventional chemical solid-phase synthesis or recombinant expression. In vitro, the polypeptide significantly inhibits the inflammatory response of HaCaT cells induced by M5, exhibiting good anti-inflammatory activity. In vivo experiments show that the polypeptide can effectively improve imiquimod-induced psoriasis-like symptoms in mice. The degree of epidermal acanthosis was significantly reduced in the polypeptide-treated group, and the number and infiltration of T cells in the lesion site were significantly decreased, indicating that the polypeptide can improve the histopathological characteristics of psoriasis by inhibiting epidermal acanthosis and reducing T cell infiltration. Furthermore, the polypeptide has good safety and application potential, providing a new candidate molecule for the clinical treatment and development of novel drugs for psoriasis.

Compounds can specifically activate TLR7. The compounds are useful because they can stimulate innate immunity. The compounds can be used in the treatment of conditions including cancer, viral infections and skin lesions. The compounds can optionally be formulated for enhanced penetration following topical administration, the composition preferably initiating a local specific inflammatory cytokine response while limiting undesirable erythema and other inflammatory reactions. Pharmaceutical compositions contain the compound and preferably an additional compound such as imiquimod and / or resiquimod (R848). A composition contains the compound and a compound can be used as a medicament. Other aspects, embodiments, advantages and applications will become clear from the further description herein.

The present invention relates to compounds capable of specifically activating TLR7. The compounds of the present invention are useful because they can stimulate innate immunity. The compounds of the present invention can be used to treat diseases including cancer, viral infections, and skin lesions. The compounds can optionally be formulated for enhanced penetration after topical administration, and the compositions preferably initiate a localized, specific inflammatory cytokine response while limiting undesirable erythema and other inflammatory responses. The present invention also relates to pharmaceutical compositions comprising the compounds of the present invention and, preferably, additional compounds such as imiquimod and / or resiquimod (R848). The present invention also relates to compositions comprising the compounds of the present invention and to compounds for use as pharmaceuticals. Other aspects, embodiments, advantages, and uses of the present invention will become apparent from the further description herein.

This invention discloses a method for constructing and applying a mouse model of systemic lupus erythematosus (SLE). The SLE mouse model constructed by this invention utilizes intraperitoneal injection of pristane combined with topical application of imiquimod cream. Specifically, C57 BL / 6J mice are injected intraperitoneally with pristane, followed by continuous application of an appropriate dose of imiquimod to a single ear. The SLE mouse model provided by this invention effectively simulates the immune response induced by pristane and imiquimod in mice. This model can be used to explore the pathogenesis, pathophysiology, immunology, and therapeutic drug development of SLE, and is of great significance for accelerating the translation of scientific research into clinical practice.

The invention discloses an indoline derivative and application thereof. According to the invention, the regulation effect of the derivative on the chemotaxis and secretion functions of ILC3 is evaluated; it is found that the derivative has a promoting effect on chemotaxis of ILC3 to an inflammatory site and up-regulation of IL-22 expression, has very remarkable effects on mouse ulcerative colitis (UC) induced by DSS, mouse Crohn disease (CD) induced by TNBS, acute lung injury induced by lipopolysaccharide (LPS), mouse psoriasis induced by imiquimod and other diseases in vivo, and is superior to existing clinical treatment drugs. Good development and application prospects are realized.

The utility model relates to the field of biological medicine, in particular to an adjustable wart-removing warm patch. An adjustable wart removing warm patch comprises a shell, a limiting ring, a fixing ring and the like, the limiting ring is fixedly connected to the upper side of the outer side wall of the shell, a cavity is formed in the middle of the shell and used for being filled with heating materials, the fixing ring is fixedly connected to the lower side of the outer side wall of the shell, and annular pressure-sensitive adhesive is fixedly connected to the bottom of the fixing ring. The middle part of the annular pressure-sensitive adhesive is fixedly connected with a sealing plate, and the bottoms of the annular pressure-sensitive adhesive and the sealing plate are jointly and fixedly connected with protective isolation paper. The wart-removing warm patch is flexible and adjustable in manufacturing size, integrates the functions of spontaneous heating, temperature measurement and temperature adjustment, is simple, convenient and rapid to operate, does not need to depend on large medical equipment, is small in size and convenient to carry, has great market popularization potential, is easy and worry-free in the using process, can be used in cooperation with immunoregulation drugs such as imiquimod cream, effectively promotes deep penetration of the drugs, and improves the wart-removing effect of the wart-removing warm patch. The wart treatment effect is obviously improved.

The invention relates to a composite nano aluminum phosphate adjuvant as well as a preparation method and application thereof, and belongs to the technical field of vaccine adjuvants. The gel is prepared from the following raw materials: ethylene glycol chitosan GCS with the molecular weight of 1-30 kDa and an aluminum phosphate adjuvant AP in a weight ratio of n: 1, wherein n is equal to 0.1-7. The invention has the advantages of excellent dispersibility and stability, high-pressure sterilization and freeze-drying treatment tolerance, and can be stored at normal temperature for more than 15 months. Animal experiments show that compared with a traditional aluminum phosphate adjuvant, the nano aluminum adjuvant disclosed by the invention can induce body fluid and cell immune response which is stronger in effect, safer and more balanced, can be used as a novel adjuvant platform to carry adjuvants such as ZMF59, C-di-AMP or Imiquimod, further improves the immune effect, and is suitable for being applied to vaccines needing Th1 / Th2 immune balance or strong cell immunity.

The invention discloses a copper-based nano-enzyme as well as a preparation method and application thereof. The copper-based nano-enzyme is obtained through a self-assembly reaction of trimesic acid, a Cu < 2 + > source and polyvinylpyrrolidone. The copper-based nano enzyme has inherent CAT, SOD, OXD and POD similar enzyme activity; through cascade of multiple enzymes, the copper-based nano enzyme generates active oxygen, relieves oxygen deficit, consumes an endogenous antioxidant / copper chelating pool, and finally triggers enhanced copper-induced apoptosis; after the copper-based nano-enzyme permeates through the skin and is taken by keratinocyte, active oxygen can be generated in an explosive mode, the mitochondrial function is destroyed, and copper death characterized by iron-sulfur cluster protein loss and lipoic acylation mitochondrial enzyme aggregation is triggered. Moreover, in-vivo results show that the copper-based nano-enzyme can obviously relieve mouse psoriasis-like phenotype induced by imiquimod, systematic or organ toxicity is not detected, and the clinical potential of the copper-based multiple enzyme mode is highlighted.

The invention belongs to the technical field of traditional Chinese medicines, and particularly relates to a skin-reaching detoxification formula as well as a preparation method and application thereof. The skin-reaching detoxifying formula is prepared from the following raw materials in parts by mass: 10 to 15 parts of fructus mume, 5 to 10 parts of vinegar-processed rhizoma curcumae, 10 to 20 parts of herba sarcandrae, 10 to 20 parts of radix rehmanniae recen, 10 to 15 parts of cortex moutan, 10 to 20 parts of cornu bubali, 5 to 10 parts of rhizoma pinellinae praeparata, 3 to 5 parts of rhizoma coptidis, 5 to 10 parts of radix scutellariae, 5 to 10 parts of rhizoma zingiberis, 5 to 10 parts of sun-dried ginseng, 5 to 10 parts of cassia twig, 10 to 20 parts of poria cocos, 10 to 15 parts of spina gleditsiae and 10 to 20 parts of fructus forsythiae. Animal experiments show that the skin-reaching detoxifying formula disclosed by the invention has a relatively good treatment effect on an imiquimod-induced psoriasis mouse model and a relapse psoriasis mouse model. Therefore, the traditional Chinese medicine composition disclosed by the invention has a good treatment effect on initial psoriasis and recurrent psoriasis.

The present invention relates to compounds that can specifically activate TLR7. The compounds of the present invention are useful as they can stimulate innate immunity. The compounds of the invention may be used to treat conditions including cancer, viral infections, and skin lesions. These compounds may optionally be formulated to enhance penetration following topical administration, which compositions preferably elicit topically specific inflammatory cytokine responses while limiting undesirable erythema and other inflammatory responses. The invention also relates to pharmaceutical compositions comprising a compound of the invention and preferably further compounds such as imiquimod and / or requinimod (R848). The invention also relates to a composition comprising the compounds of the invention and to compounds for use as medicaments. Other aspects, embodiments, advantages, and applications of the invention will become clear from further description herein.

The present invention discloses the use of decorin or its encoding gene as a target in the preparation of a psoriasis treatment drug. Through a series of experiments, the present invention demonstrates that DCN can effectively protect against imiquimod-induced psoriatic skin inflammation in mice, improve skin scaling, erythema, thickening, and abnormal epidermal differentiation, enhance the skin's barrier function, reduce the infiltration of inflammatory cells, and exert a certain anti-inflammatory effect. The experimental studies of the present invention have confirmed that DCN has significant efficacy in psoriasis models, is safe, highly effective, and has no side effects, and has a simple production process, showing the potential for medical transformation. This will also help expand the potential application value of DCN in various other inflammatory skin diseases.

The invention relates to an imidazopyrimidine compound for treating allergic conjunctivitis by targeting a TLR7 receptor pathway and a preparation method and application thereof, the imidazopyrimidine compound or a pharmaceutically acceptable salt thereof has a structure as shown in formula (I): (I) wherein R1 is phenyl, phenyl monosubstituted or polysubstituted by R4 or pyridyl monosubstituted or polysubstituted by R4; r2 is a C1-6 alkyl group or a C1-6 alkoxy group and a C1-6 alkyl group; and R3 is phenyl, phenyl which is monosubstituted or polysubstituted by R5, five-membered heteroaryl or pyridyl which is monosubstituted or polysubstituted by R5. Compared with imiquimod, the compound disclosed by the invention has stronger agonistic activity on a TLR7 agonist, can inhibit'excessive activation of Th2 immune cells' and'inflammation activation of epithelial conjunctival cells', breaks through the limitation of traditional treatment by'targeted root and accurate regulation ', and has the potential of treating allergic conjunctivitis.

The invention discloses a three-dimensional printing photo-thermal immune scaffold for postoperative treatment and repair of skin melanoma and a preparation method of the three-dimensional printing photo-thermal immune scaffold. The preparation method comprises the following steps: S1, preparing manganese silicate nanospheres loaded with an immunologic adjuvant; and S2, mixing the composite nanoparticles obtained in the step S1 with a photo-crosslinking hydrogel precursor solution, a calcium ion source and a photoinitiator to obtain an internal phase slurry, and preparing a sodium alginate aqueous solution as an external phase slurry. According to the invention, a photo-thermal therapeutic agent (manganese silicate), an immunologic adjuvant (imiquimod) and a tissue regeneration promoting factor (manganese and silicon ions) are integrated on a three-dimensional scaffold platform for the first time, and through a precise preparation method, space-time synergy and function integration of local ablation-system immunity-tissue repair are realized.

This invention relates to the field of traditional Chinese medicine extracts and drug preparation technology, and discloses a *Hypericum perforatum* extract composition, its preparation method, and its application, including the application of an ethanol extract of *Hypericum perforatum* or components isolated from its ethanol extract in the preparation of drugs for the prevention and / or treatment of psoriasis. In vitro and in vivo experiments have demonstrated that *Hypericum perforatum* extract can significantly improve imiquimod (IMQ)-induced psoriasis-like skin lesions (erythema, scaling, and skin thickening) in mice and reduce PASI scores. Its mechanism of action differs from single-target biological agents; instead, it simultaneously regulates the IL-23 / IL-17 inflammatory axis, corrects Th17 / Treg immune imbalance, and inhibits abnormal activation of the NF-κB signaling pathway, demonstrating the advantages of multi-component, multi-target synergistic effects of natural drugs. Furthermore, *Hypericum perforatum* is a unique plant resource in my country with a wide distribution. Compared to expensive biological agents, this invention has a significant cost advantage and is expected to be developed into a more affordable and accessible anti-psoriasis drug.