124 results about "Caspase" patented technology

The invention belongs to the field of biological medicines, and particularly discloses application of a Ptprj agonist GJ103 in preparation of a medicine for treating acute kidney injury (AKI) induced by cisplatin. In-vivo and in-vitro experiments prove that the GJ103, by activating Ptprj, can significantly down-regulate expression of pro-apoptotic protein Bax and Cleved Caspase-3, up-regulate anti-apoptotic protein Bcl2 and reduce infiltration of inflammatory factors TNF-alpha and IL-6, so that apoptosis and inflammatory response of renal tubular epithelial cells are relieved. In in-vivo experiments, GJ103 (20-40mg / kg / day) can reduce serum creatinine and urea nitrogen levels of cis-platinum model mice and improve pathological injuries such as renal tubule dilatation; in in-vitro experiments, 20-40 [mu] M of GJ103 can inhibit apoptosis of renal tubular epithelial cells and reduce expression of renal injury markers NGAL and Kim-1. The pharmaceutical composition contains GJ103 and a pharmaceutical carrier, the preparation form can be a 4mg / mL injection (the purity is greater than or equal to 99.46%) or an oral preparation, and a new strategy is provided for clinical treatment of cisplatin renal toxicity.

The invention discloses design and synthesis of a series of brain-targeted ginsenoside Rg1 derivatives and application of the brain-targeted ginsenoside Rg1 derivatives in treatment of Alzheimer's disease. According to the invention, ginsenoside Rg1 and polyethylene glycol with a specific chain length are covalently linked to successfully construct the derivative capable of enhancing the penetrating power of the blood-brain barrier. The series of derivatives provided by the invention not only solve the problems of poor brain targeting and insufficient stability of natural Rg1, but also can inhibit neuroinflammation by regulating and controlling an NLRP3 / caspase-1 signal channel in an LPS-induced neuroinflammation model, and finally, the learning and memory ability is remarkably improved. The product is simple and convenient in preparation process and good in biological safety, and a new candidate compound is provided for developing a new generation of Alzheimer disease treatment medicines.

Abstract Described herein, in one aspect, are antigen presenting cells (APCs) comprising an exogenous nucleic acid encoding one or more candidate antigens, wherein the one or more candidate antigens are expressed and presented with MHC class I or MC class II molecules; a molecular reporter of Granzyme B (GzB) activity; and c) an exogenous inhibitor of caspase-activated deoxyribonuclease (CAD)-mediated DNA degradation, a CAD knockout, or a caspase knockout (e.g., caspase 3 knockout). Described herein, in another aspect, is a system for detection of recognized antigen presentation by an antigen presenting cell to a cytotoxic lymphocyte or NK cell. Abstract 2018 / 22761 oM - cell Target ml Target cell cell cell Target Target Target SUBSTITUTE SHEET (RULE 26) cell cell cell Target Target cell cell 1 / 28 my Isolate recognized cell Library of target cells target cells and displaying different Add T cells from sample sequence antigens antigens of interest. CTLs deliver cytotoxic granules to target cells displaying cognate antigen FIG. 1 PCT / US2018 / 036663 20 26 20 53 56 07 J ul 2 02 6 2 0 2 6 2 0 5 3 5 6 0 7 J u l 2 0 2 6 2 0 1 8 / 2 2 7 6 1 o M a n d m y 1 / 2 8 m y L i b r a r y o f t a r g e t c e l l s d i s p l a y i n g d i f f e r e n tA d d T c e l l s f r o m s a m p l e of interest. CTLs deliver c y t o t o x i c g r a n u l e s t o t a r g e t c e l l s d i s p l a y i n g c o g n a t e a n t i g e n P C T / U S 2 0 1 8 / 0 3 6 6 6 3

The application discloses application of a pyrimidinotriazine diketone derivative in preparation of a medicine for inhibiting activity of human protease caspase-1, and belongs to the technical field of medicines. In view of defects of existing caspase-1 inhibitors, the compound has the characteristics of high affinity binding to caspase-1 (K D = 8.11 μM; 8.78 μM) and strong inhibition on the activity (IC 50 = 11.90 nM-14.47 nM). The compound is used for preparation of a medicine for inhibiting the activity of caspase-1 and a medicine for treating inflammation-related diseases such as sepsis-related lung injury, acute respiratory distress syndrome or acute pancreatitis.

The invention provides a diagnosis and treatment integrated nano platform as well as a preparation method and application thereof. According to the diagnosis and treatment integrated nano platform, an organic-inorganic nano hybrid is constructed through structure optimization and function integration, four modes of PTT, PDT, SDT and CDT are organically combined innovatively, and efficient synergistic treatment of GBM is achieved through real-time monitoring of photoacoustic imaging. First, a dOMV encapsulation strategy significantly improves the ability to penetrate through the blood brain barrier. Meanwhile, the IEICO-4F has a strong near-infrared absorption characteristic and has a synergistic effect with the high catalytic activity of the mesoporous platinum nanoparticles. Under the laser / ultrasonic excitation condition, the diagnosis and treatment integrated nano platform shows excellent photo-thermal conversion performance, the Fenton reaction rate can be increased, endogenous hydrogen peroxide can be continuously catalyzed to be decomposed to generate oxygen, and the tumor hypoxia state is effectively relieved. The series of reactions further enhance the generation of ROS, activate a Caspase-1 / GSDMD mediated pyroptosis pathway, finally achieve an efficient tumor inhibition effect, and successfully break through the limitation of a single treatment mode.

The present application belongs to the technical field of hair loss treatment, and particularly relates to a phototherapy and drug synergistic intervention system for androgenetic alopecia of human scalp. In the system, the drug is angelica extract with a concentration of 0.1-500 ug / mL; the phototherapy light source is a red light LED light source with a wavelength of 600-700 nm; the light irradiance is 2-100 mW / cm 2 ; the light dose is 2-20 J / cm 2 ; the irradiation mode is steady light or pulsed light; and the synergistic intervention mode is that the phototherapy and the drug application are performed synchronously or the phototherapy is performed within 0.5-2 hours after the drug application. Experiments show that the light-drug combined intervention significantly improves cell viability, ATP level, migration ability, IGF1 and VEGF secretion, reduces ROS and MDA levels, inhibits Caspase-3 activity, regulates BCL2 / BAX expression, activates Wnt, Hh and PI3K pathways, and inhibits BMP and TGF-beta pathways. The present application provides a treatment scheme with clear timing and standardization, and realizes safe, non-invasive and efficient hair loss treatment.

The invention discloses a preparation rich in polygonatum sibiricum polypeptide and application of the preparation in diabetes mellitus. The composition is prepared from rhizoma polygonati polypeptide, semeglutide, astaxanthin, an active agent and a ferroptosis mixture. Pharmacodynamic experiments show that in a diabetic mouse model, fasting blood glucose can be remarkably reduced, the serum insulin level can be increased, renal function indexes can be improved, and expression of NLRP3 inflammation pathway related proteins (NLRP3, Caspase-1 and IL-1beta) in pancreatic tissue can be remarkably inhibited. By integrating multiple mechanisms of blood glucose reduction, oxidation resistance, inflammation resistance, ferroptosis resistance and the like, multi-target collaborative intervention is realized, the pharmaceutical composition is remarkably superior to a single component in the aspects of blood glucose reduction, pancreas islet function protection and complication alleviation, and a new clinical strategy is provided for treatment of diabetes mellitus, especially type 1 diabetes mellitus.

The invention provides medical application of a licochalcone B derivative CTG12 in preparation of an NLRP3 inflammasome inhibitor, and belongs to the technical field of biological medicine. The invention provides application of a licochalcone B derivative CTG12 in preparation of an NLRP3 inflammasome inhibitor. The invention also discloses application of the compound in preparation of drugs for preventing or treating diseases related to abnormal activation of NLRP3 inflammasomes. The synthesized compound CTG12 has the remarkable activity of inhibiting caspase-1 generated by BMDM cells, the effect is improved by about eight times compared with licochalcone B, and the compound CTG12 has the broad-spectrum and specific inhibiting effect and can effectively inhibit activation of NLRP3 inflammasomes.

The invention discloses application of TPN171H, an active fragment thereof or a derivative thereof in preparation of a medicine for treating spinal cord injury. The TPN171H shows an excellent treatment effect in spinal cord injury treatment, the levels of apoptosis factors BAX and Caspase-3 cleaved can be remarkably reduced, the level of Bcl-2 is improved, the content of a neuron marker MAP-2 is also remarkably increased, and the number of Tunel bodies and the cavitation-like structure are remarkably reduced. The intervention of the TPN171H also can reduce MNSS, and prompts that the TPN171H has the functions of promoting the spinal cord movement and coordination of the rat with spinal cord injury and improving the sensory system of the rat with spinal cord injury.

The present application belongs to the technical field of coordination chemistry and biomedical science, and provides a multifunctional iridium (III) complex, a preparation method and application thereof. The multifunctional iridium (III) complex (Mito-Ir) is composed of an iridium (III) complex cation and a coordination anion shown in the following formula. Mito-Ir can efficiently target mitochondria, and also has the abilities of phosphorescence imaging, type I and type II active oxygen generation, and photocatalytic oxidation of nicotinamide adenine dinucleotide. Under light irradiation, Mito-Ir triggers severe mitochondrial dysfunction through the above synergistic effect, and then specifically activates the caspase-3 / GSDME signaling pathway, and significantly induces pyroptosis; this pyroptosis-based cell death mechanism can effectively overcome the apoptosis tolerance of tumor cells, and is accompanied by the release of a large amount of inflammatory factors and damage-associated molecular patterns, stimulates immunogenic cell death, and activates the body's anti-tumor immune response.

The present disclosure relates generally to alkyne containing pharmaceutical agents, and in particular, to phenylethynyl-thiophene based compounds. More particularly, the present disclosure provides a class of compounds that can inhibit and / or attenuate apoptosis via caspase 3 for the treatment of various degenerative disorders. Additionally, the present disclosure relates to methods for treating specific degenerative disorders such as amyotrophic lateral sclerosis (ALS), Huntington's disease, epilepsy, spinal cord injury, complication due to diabetes, multiple sclerosis (MS), muscular dystrophy (MD), Parkinson's disease (PD), irritable bowel syndrome (IBS) and Alzheimer's disease (AD) in a patient comprising administering to the patient an effective amount of a present compound.

The present application relates to the field of biological medicine, in particular to a kind of muscone in the application of viral inhibitor.The viral inhibitor of the present application is used to inhibit the replication of Japanese encephalitis virus and / or porcine epidemic diarrhea virus.The present application finds that muscone has no cytotoxicity, and does not directly inactivate virus, but produces antiviral effect on Japanese encephalitis virus by inhibiting NLRP3 / Caspase-1, Caspase-9 / Caspase-3 / Bax / BCL-2, JNK / ERK / P38 and other signal pathways, and inhibits porcine epidemic diarrhea virus invasion into cells by reducing caveolin level.The antiviral effect is remarkable, the mechanism of action is clear, the selectivity is high, and the safety is better.

The invention relates to a caspase-1 responsive fluorescent probe based on FRET (Fluorescence Resonance Energy Transfer), a preparation method, application and a product, and belongs to the technical field of FRET fluorescent probes. The technical problem to be solved is to provide the FRET fluorescent probe capable of simultaneously carrying out in-vitro caspase-1 enzyme detection and in-vivo caspase-1 activity detection, and the specific technical scheme is that the FRET fluorescent probe with a chemical structure shown in a formula I is provided. The FRET fluorescent probe provided by the invention has short reaction time, is suitable for caspase-1 activity detection and pyroptosis imaging under a fluorescence confocal microscope, and can realize multi-scale imaging of pyroptosis in cell spheres and animal bodies.

The invention discloses application of RMTE in preparation of a medicine for preventing and controlling grass carp reovirus. The hemorrhagic disease caused by the grass carp reovirus (GCRV) is a key bottleneck restricting healthy development of the grass carp breeding industry, and the current vaccine for treating the grass carp reovirus (GCRV) has the problems of unstable immune protection effect, low protection rate for crossing of strains of different genotypes and the like, so that the research and development process of antiviral drugs is slow. The invention discloses an influence and a potential mechanism of a rhodamine B-ethyl sulfide condensation compound (RMTE) on GCRV (Growth Factor Receptor Virus) infection. Results show that the RMTE can significantly inhibit expression of VP6 and VP7 genes in GCRV infected cells, can effectively relieve expression inhibition of GCRV on GPX4, Caspase and p53 genes and promote expression of the three genes, and prove that the RMTE has a significant inhibition effect on GCRV infection and plays an antiviral effect through multiple ways. Research results provide new potential drugs and theoretical basis for prevention and control of GCRV.

The invention discloses a new application of Renqingchangjue and an extract of Renqingchangjue. Specifically, the invention provides a new application of Tibetan medicine Renqingchangjue and an extract in preparation of a medicine for treating chronic atrophic gastritis, and systematically clarifies an exact molecular mechanism of the Tibetan medicine Renqingchangjue for treating CAG. The core of the invention is to reveal the core signal axis of Renqingchangjue by inhibiting TNF / NF-kB / Caspase-3 for the first time, so that the Renqingchangjue synergistically exerts the effects of resisting inflammation, resisting apoptosis and promoting mucosa repair, and provides a new intervention target and scientific basis for reversing gastric mucosa gland atrophy. The invention not only provides a modern pharmacological basis for the clinical curative effect of the Renqingchangjue, but also provides a brand new technical scheme and a protection basis for developing a medicine or a medicine composition which is based on the clear pathway target and is used for treating the chronic atrophic gastritis.

This invention discloses the application of a "Super Brain-Boosting Capsule," belonging to the field of pharmaceutical technology. The Super Brain-Boosting Capsule is used in the preparation of drugs for treating Alzheimer's disease. The capsule enhances the mitochondrial membrane potential of Glu-treated HT22 cells by inhibiting ferroptosis. At the transcriptional level, the capsule activates the expression of key Nrf2 / HO-1 / GPX4 signaling molecules NRF2, HO-1, GPX4, SLC7A11, ACSL4, FTH1, and FPN1, while reversing the expression of Bcl-2, Caspase-3, and Caspase-9 to inhibit apoptosis in AD cells. This invention reveals that the Super Brain-Boosting Capsule, based on the Nrf2 / HO-1 / GPX4 pathway, inhibits Glu-induced ferroptosis in HT22 cells, which can treat Alzheimer's disease. This invention provides experimental evidence and direction for the further development of the Super Brain-Boosting Capsule in the prevention and treatment of Alzheimer's disease and other neurodegenerative diseases.

The present application provides chemical compounds useful, for example, in inhibiting gasdermin pore formation in a CA cell, inhibiting inflammasome-mediated death of a cell (pyroptosis); inhibiting cytokine secretion from a cell, inhibiting an inflammatory caspase in a cell, and / or covalently reacting with a cysteine of a gasdermin protein in a cell. These compounds are also useful in treating or preventing diseases or conditions in which inflammasome activation is implicated in pathogenesis. One example of such disease or condition is sepsis.

The application relates to the field of biological medicine, and discloses ascorbyl palmitate nanoliposomes capable of inducing tumor cell oncosis, a preparation method and application thereof. The nanoliposomes are constructed by inserting ascorbyl palmitate as a lipid component into a phospholipid bilayer, and are prepared by a film dispersion method from lecithin, cholesterol, pegylated phospholipid and ascorbyl palmitate. The average particle size of the nanoliposomes is 80-150 nm, the encapsulation rate is high, and the stability is good. The nanoliposomes can be administered through a tail vein, utilize the specific hydrolysis of matrix metalloproteinase MMP-2 which is highly expressed by tumor cells to hydrolyze ascorbyl palmitate, release palmitic acid and ascorbic acid, thereby inducing Caspase-independent oncosis of tumor cells, effectively overcoming apoptosis-related drug resistance, and reversing a tumor immunosuppressive microenvironment. The nanoliposomes avoid the cumulative toxicity of metal-type inducers, and provide a new safe and effective option for reversing chemotherapy resistance.

The application relates to the technical field of pharmaceutical chemistry, and discloses a sulfuryl hydrazone compound, a preparation method thereof and anti-tumor application. The compound is synthesized from isatin derivatives and sulfuryl hydrazine through two-step nucleophilic substitution-elimination reaction, has a chemical structure as shown in formula (I), and is characterized by 1H NMR, 13C NMR and HRMS. The sulfuryl hydrazone compound has significant inhibitory activity on A549 (lung cancer), HepG2 (liver cancer) and Hela (cervical cancer) three human cancer cell strains, the value of some compounds is as low as 0.03 micromole / L, the compound can induce cell apoptosis by mediating ROS generation in tumor cells, inhibiting the NF-kappa B signal pathway and activating Caspase-3 activity, and can effectively inhibit cancer cell migration and colony formation. The compound has a mild synthesis process, simple operation and wide substrate applicability, can be used as a potential anti-tumor active ingredient, can be used for preparing drugs for resisting lung cancer, liver cancer, cervical cancer and other tumors, and can provide new candidate compounds and technical support for cancer treatment.

The invention discloses an application of a pyroptosis pathway inhibitor in protection of plateau brain impact lung injury, the pyroptosis pathway inhibitor is applied to preparation of a medicine for preventing and / or treating lung injury caused by plateau brain impact injury, the pyroptosis pathway inhibitor acts on a Caspase-1 / GSDMD signal pathway, the inhibitor comprises a Caspase-1 inhibitor, an ASC inhibitor or a GSDMD-D inhibitor, and the inhibitor comprises a Caspase-1 inhibitor, an ASC inhibitor or a GSDMD-D inhibitor. The medicine is used for improving lung function impairment caused by plateau brain impact injury. The lung function indexes comprise at least one of the maximum inspiration flow rate, the maximum expiration flow rate, the respiratory rate and the accumulated volume, and the medicine is used for relieving lung tissue pathological injury caused by the plateau brain impact injury; the pathological injury comprises at least one of pulmonary alveolar wall thickening, inflammatory cell infiltration, pulmonary alveolar cavity internal hemorrhage and pulmonary alveolar rupture and fusion into pulmonary bulla. The invention provides a new target spot and strategy for clinical prevention and treatment of the secondary lung injury of the plateau craniocerebral impact injury.

The invention discloses an application of butyric acid or a derivative thereof in preparation of a zearalenone reproductive toxicity resisting preparation. Also disclosed is an antitoxic feed composition comprising a specific base ration and a butyric acid derivative. In-vivo and in-vitro tests and molecular mechanism researches prove that butyric acid and derivatives thereof (such as tributyrin and sodium butyrate) can effectively relieve zearalenone (ZEN)-induced animal ovary injury. The action mechanism of the traditional Chinese medicine composition is that follicular atresia is reduced, the balance of reproductive hormones (such as GnRH, E2, AMH and P4) is recovered, and clinical symptoms caused by ZEN poisoning such as vulva swelling and the like are relieved by activating a BMPs / SMAD signal channel, especially up-regulating SMAD4 protein expression and inhibiting oxidative stress (ROS) and Caspase-3 mediated granular cell apoptosis.

The application discloses application of a petroleum ether extract of a root of a roadside green plant in preparation of a drug for treating colorectal cancer by regulating a PI3K / AKT / MDM2 / p53 pathway. In the application, the petroleum ether extract of the root of the roadside green plant for treating colorectal cancer is obtained by petroleum ether reflux extraction of the root of the roadside green plant. Pharmacological experiments show that the petroleum ether extract of the root of the roadside green plant treats colorectal cancer by regulating the PI3K / AKT / MDM2 / p53 signal pathway through down-regulating p-PI3K / PI3K and p-AKT / AKT ratio, up-regulating p-MDM2 and down-regulating p53 level; the extract has an anti-malignant proliferation effect, induces G1 phase arrest by targeting CDK2, up-regulating p21, down-regulating Cyclin E1-CDK2 and Cyclin D1-CDK4; the extract induces HCT-116 cell apoptosis through a mitochondrial pathway by up-regulating Bax / Bcl-2, reducing ΔΨm, releasing Cyt C, activating Caspase-9 / 3 and cleaving PARP; the extract inhibits migration and invasion of HCT-116 cells by targeting MMP9, down-regulating MMP-2, MMP-9 and N-cadherin expression and up-regulating E-cadherin expression. In addition, the extract inhibits growth of a transplanted tumor in a nude mouse transplanted tumor model by inducing apoptosis of transplanted tumor cells.

The application relates to an anti-apoptosis baculovirus expression vector, which realizes a broad-spectrum anti-apoptosis effect by expressing siRNA targeting a Sf-caspase-1 and Tn-caspase-1 common sequence of Spodoptera frugiperda and Trichoplusia ni insect cells through the vector. The baculovirus vector contains a specific DNA sequence, the DNA sequence contains an siRNA sequence targeting the Sf-caspase-1 and Tn-caspase-1 common sequence transcribed by an RNA polymerase III promoter; the recombinant virus of the vector can express double-stranded small RNA in a host cell, silences the caspase-1 encoded by the host cell through an RNA interference pathway, thereby inhibiting the apoptosis of the host cell, and significantly improving the expression level of an exogenous protein. The application can be used for industrialized production of protein preparations and vaccines.

The invention discloses a sensor for detecting cytochrome c and caspase in a single cell as well as a preparation method and application of the sensor. The sensor comprises a theta-type nanotube with two channels, wherein a cytochrome c aptamer and a caspase recognition peptide are respectively fixed on the two channels; one end of the theta-shaped nanotube is a tip, is provided with a theta-shaped nanopore and is used for puncturing into a single cell for sampling. Different detection molecules are respectively fixed in two channels of the theta-type nanotube, and synchronous, high-sensitivity and high-selectivity detection of two key apoptosis markers in a single cell is realized by utilizing the change of charge density on the inner wall of the channel when a target exists. The sensor has good reversibility, stability and reproducibility, can be used for monitoring dynamic changes of cyt c release and caspase-3 activation in a cell apoptosis process in real time, reveals spatial-temporal heterogeneity of an apoptosis mechanism, and provides a powerful tool for cell apoptosis research, disease diagnosis and treatment evaluation.

The invention relates to the field of biological medicine, in particular to application of muscone in preparation of a virus inhibitor. The virus inhibitor is used for inhibiting replication of Japanese encephalitis virus and / or porcine epidemic diarrhea virus. It is found that muscone has no cytotoxicity, does not directly inactivate viruses, generates an antiviral effect on Japanese encephalitis viruses by inhibiting signal channels such as NLRP3 / Caspase-1, Caspase-9 / Caspase-3 / Bax / BCL-2, JNK / ERK / P38 and the like, and inhibits porcine epidemic diarrhea viruses from invading cells by reducing the level of litter protein. The antiviral effect is obvious, the action mechanism is clear, the selectivity is high, and the safety is better.

Protein phosphatase 5 (PP5) is a serine / threonine protein phosphatase involved in the maturation and activation of numerous signaling pathways essential for cancer growth. PP5 activity is essential for the survival of clear cell renal cell carcinoma (ccRCC), however the mechanism remains unclear. Data demonstrates that PP5 interacts with caspase-8, FADD, and RIPK1, components of extrinsic apoptotic pathway Complex II. Specifically, PP5 dephosphorylates and inactivates the death effector proteins RIPK1 and FADD, preserving Complex II integrity and regulating extrinsic apoptosis. Protein phosphatases are considered to be ‘undruggable,’ however we have developed a specific inhibitor of PP5 (P-053) that prevents substrate binding to the active site. Encouragingly, PP5 inhibition using P-53 in VHL-null ccRCC robustly induces extrinsic apoptosis. Taken together, the data suggests that PP5 promotes ccRCC survival by suppressing extrinsic apoptosis, and small molecule inhibition of PP5 presents a viable therapeutic strategy for ccRCC.

To provide a cell death-inducing agent capable of inducing cell death of cancer cells based on a new mechanism, a pharmaceutical composition for treating or preventing cancer comprising the cell death-inducing agent, and a cancer cell-detecting agent for detecting cancer cells to which the cell death-inducing agent can be applied.SOLUTION: An agent for inducing apoptosis of cancer cells expressing IFI16, ASC, and Caspase-1, the agent comprising a polynucleotide having at least one repeat unit in a repeat sequence of telomeric DNA.SELECTED DRAWING: None

The application discloses a composition for treating radiation enteropathy and application thereof, and belongs to the technical field of biological medicine, and solves the problem that there is no effective treatment drug for radiation enteropathy at present. The composition comprises puerarin, baicalein, berberine and glycyrrhetinic acid. The composition for treating radiation enteropathy can regulate Wnt / beta-catenin, NF-kappa B and Caspase-9 / 3 signal pathways and the like, promote the proliferation of intestinal cells after radiation damage, reduce the inflammation level of intestinal tissues after radiation, reduce the apoptosis of intestinal cells after radiation and the like, improve the radiation damage of intestinal epithelial cells, play an anti-radiation enteropathy role, and has a remarkable effect on treating radiation enteropathy.

The invention relates to a diterpenoid compound in callicarpa uniflora, a preparation method and application, the structure of the compound is shown as a formula (1), the compound belongs to the field of natural medicinal chemistry, and the invention aims to protect the application of the compound in preparation of an NLRP3 inflammasome inhibitor for treating inflammation. The invention has the following outstanding beneficial effects: 1, so far, there is no report on a pharmaceutical composition with the formula (1) as an effective component in the prior art, and there is no report on the compound and the pharmaceutical composition thereof in preparation of anti-inflammatory drugs for treatment of inflammation; and 2, the compound obtained by research in the invention inhibits the expression levels of Caspase-1 and IL-1beta in a dose-dependent manner, and inhibits shearing maturation of GSDMD at the same time, which shows that the compound has a significant inhibition effect on NLRP3 inflammasome-mediated inflammatory reaction. According to the invention, the medicinal value of the clerodane diterpenoid compound in the callicarpa uniflora is expanded.

The invention belongs to the technical field of medicines, and particularly relates to application of hibiscus (the hibiscus is a plant hibiscus flower and an extract and an active monomer thereof) in preparation of medicines for treating stomach diseases (atrophic gastritis, gastric mucosal lesion and gastric cancer). The invention discloses application of hibiscus syriacus in treatment of gastric diseases. The application comprises at least one of chronic atrophic gastritis treatment, gastric mucosa protection and gastric cancer prevention. In-vitro experiments show that the shrub althea flower extract, shrub althea flower polyphenol, syringic acid (I), protocatechuic acid (II), kaempferol (III) and kaempferol-7-O-beta-D-glucoside (IV) have obvious antioxidant activity and gastric mucosa protection activity, can obviously reduce the ROS content in ethanol-induced GES-1 cells and the expression of apoptosis marker protein Caspase-3 / Bax, and have a wide application prospect.