124 results about "Akt signalling" patented technology

The invention relates to the technical field of biological medicines, in particular to rapamycin-induced extracellular vesicles and application thereof in preparation of a medicine for promoting wound repair. The rapamycin-induced extracellular vesicles can enhance the migration and tube forming ability of endothelial cells, so that angiogenesis is promoted; meanwhile, the proliferation and migration capabilities of macrophages can be inhibited, and the proportion of M1 type macrophages in a wound is reduced, so that the inflammatory response mediated by the macrophages is relieved; and the composition shows extraordinary effects in the aspect of accelerating wound repair. The biological activity of the extracellular vesicles induced by the rapamycin depends on the activation of a PI3K / Akt signal channel.

The invention discloses an application of an ALK / LTK inhibitor in preparation of a product for treating and / or preventing chronic lymphocytic leukemia. Cell tests prove that the ALK / LTK inhibitor can inhibit an AKT signal channel at the downstream of LTK, so that the cell cycle of tumor cells is stopped, cell apoptosis is promoted, and finally the inhibiting effect on CLL cell proliferation is achieved; in a mouse model, the ALK / LTK inhibitor is proved to be capable of remarkably prolonging the survival time of tumor-bearing mice; the invention provides more drug choices for clinical treatment of CLL.

The invention provides in-situ forming fluid bionic hydrogel as well as a preparation method and application thereof, and belongs to the technical field of biological medicines. The invention provides an injectable GelSSO / PDA (at) SDF fluid bionic niche, after in-situ photo-crosslinking, preferential and sustained release of PDA (at) SDF NPs initiates early signal amplification, which recruits EPCs and MSCs through an SDF-1 alpha / CXCR4 axis, promotes activation of the angiogenic vascular niche through an AKT signal, and repolarizes macrophages to a regenerated M2 phenotype. Subsequently, the gradual degradation of the bionic niche triggers the stable release of SSO, and the later signal is further amplified to form an osteogenic niche with transcriptional activity, thereby maintaining the MAPK / ERK-mediated MSCs osteogenic differentiation. The fluid bionic niche can form a niche conforming to defects through photopolymerization, the local immune imbalance and endogenous progenitor cell recruitment are corrected in the early stage, then formation of new vessels and lamellar bones is promoted, and finally vascularization regeneration of diabetic skull defects is achieved.

The invention provides an application of polyphyllin VII in preparation of an Akt signaling pathway inhibitor targeting GRB2, the invention reveals that PPVII is specifically combined with GRB2 protein and regulates and controls the function of the GRB2 protein for the first time, the Akt pathway inhibition effect is exerted, and the molecular mechanism of PPVII is specifically shown as follows: molecular docking and dynamic simulation confirms that PPVII and an SH3 structural domain of GRB2 form a stable compound, and the stable compound is used for inhibiting the Akt pathway of the GRB2. And the key amino acid binding sites are Ile65, Gln157, Tyr160 and Phe182. Cell thermal transfer experiments (CETSA) show that PPVII can significantly enhance the thermal stability of GRB2 protein, surface plasmon resonance (SPR) determines the direct binding affinity KD = 58.5 [mu] M, functional research proves that PPVII inhibits an Akt signal channel through a GRB2 dependency mode, the polyphyllin VII is used as a GRB2 targeted inhibitor, and by specifically binding with an SH3 structural domain of GRB2 and inhibiting a downstream Akt signal channel, the polyphyllin VII can be used for inhibiting the Akt signal channel in the GRB2 targeted inhibitor. And a new strategy and a candidate compound are provided for intervention of related diseases.

The invention belongs to the technical field of biological medicine and molecular biology, and provides application of GJB6 in preparation of an esophageal squamous cell carcinoma prognosis evaluation reagent and screening of drugs for targeted treatment of esophageal squamous cell carcinoma. The low expression of the GJB6 is applied to preparation of an esophageal squamous cell carcinoma prognosis evaluation reagent. GJB6 is low in expression in ESCC patients, and ESCC prognosis is poor. And the prognosis of patients with high expression of GJB6 is better. Overexpression of GJB6 inhibits ESCC cell proliferation, migration and invasion and in-vivo tumor enlargement. The GJB6 plays a role of a cancer suppressor gene in ESCC and inhibits cell proliferation, migration and invasion. The AKT signal channel is one of downstream channels for GJB6 to regulate the occurrence and development of ESCC. The AKT inhibitor effectively inhibits GJB6 low-expression ESCC malignant phenotypes, including enhancement of cell proliferation and migration invasion ability and in-vivo tumor enlargement. The AKT is a key therapeutic target of the GJB6 low expression type ESCC.

The invention discloses an application of a hypoxia pretreated extracellular vesicle / miR-27b-3p in the treatment of ischemic stroke. The research proves that both the neuron-derived EV and H-EV can promote in-vivo and in-vitro MCAO repair. The two vesicles secreted by neuronal cells can significantly influence phenotypic change and apoptosis of astrocytes, wherein the effect of H-EV is more obvious than that of EV. Besides, the research result shows that H-EV secreted by neurons can regulate a PI3K / AKT signal channel by transmitting miR-27b-3p, so that astrocytes are promoted to be converted from the A1 phenotype to the A2 phenotype. The research of the invention provides a new therapeutic target and strategy for treating ischemic stroke.

The invention discloses application of 4-isopropyltoluene to improvement of depression-like behaviors of mice. An experiment adopts a chronic constraint stress method to construct a depression model, through behavioral detection such as a sucrose preference test, a tail suspension test and a novel inhibition ingestion test, and in combination with molecular biology means such as immunofluorescent staining and Western blot, the anti-depression effect and potential mechanism of 4-isopropyltoluene are systematically evaluated, and the anti-depression effect and potential mechanism of 4-isopropyltoluene are evaluated. Results show that 4-isopropyltoluene plays a significant anti-depression role by inhibiting neuroinflammation, enhancing glial cell support function and activating AKT signal pathway, and has the potential of being developed into a novel anti-depression candidate drug.

The application of phlorizin in the medicine for treating and / or preventing lupus nephritis, the molecular formula of phlorizin is C 21 H 24 O 10 , the application promotes the differentiation of regulatory T cells (Treg) by applying phlorizin to up-regulate the PI3K / Akt signal pathway, thereby reducing the symptoms of lupus nephritis, and provides an effective treatment method with less side effects. In the application, the traditional Chinese medicine monomer phlorizin can effectively promote the differentiation of Treg cells, and compared with compound traditional Chinese medicine, the use of single component has more advantages in drug efficacy control and efficacy evaluation. In addition, phlorizin is widely sourced, low in cost and non-toxic, and is very suitable for long-term treatment of lupus nephritis.

The invention discloses an application of isoquercitrin in preparation of a medicine for improving insulin resistance and diabetes-related liver diseases, and belongs to the technical field of medicines. According to the application, a high-glucose and high-fat diet and streptozotocin combined method is adopted to successfully construct a type 2 diabetes mouse model; experiments find that the isoquercitrin can effectively relieve the symptoms of weight loss and water intake increase of T2DM mice, significantly reduce the fasting blood-glucose level and improve abnormal glucose tolerance; the isoquercitrin can reduce the liver index of a T2DM mouse, relieve fatty degeneration of the liver and repair a liver cell structure; by activating a PI3K / AKT signal channel, the isoquercitrin up-regulates the expression levels of PI3K, p-AKT, p-GSK3 and GLUT4 and down-regulates the expressions of GSK3 and PEPCK at the same time, so that the insulin resistance of T2DM mice is effectively improved, the fatty degeneration of the liver is improved, and the isoquercitrin has a protection or repair effect on liver injury.

The present invention relates to the use of a Streptococcus sanguis extract in the preparation of a drug for the prevention and treatment of cancer, belonging to the field of pharmaceutical technology. To develop a new use of the Streptococcus sanguis extract (XLS) in cancer treatment, the present invention provides the use of a Streptococcus sanguis extract in the preparation of a drug for the prevention and treatment of cancer. The present invention demonstrates the inhibitory effect of the Streptococcus sanguis extract (XLS) on the ovarian cancer cell line SKOV3. CCK-8 assays demonstrate that the Streptococcus sanguis extract (XLS) can reduce SKOV3 cell viability and inhibit cell proliferation, invasion, and migration. Molecular biological experiments demonstrate that XLS inhibits activation of the PI3K / AKT signaling pathway by inhibiting AKT phosphorylation, thereby regulating the expression of apoptosis-related genes and inducing apoptosis in SKOV3 cells. Furthermore, XLS impairs tumor cell structure and function by disrupting mitochondrial membrane potential, increasing oxidative stress, and causing Ca2+ imbalance.

The invention belongs to the field of molecular biology, particularly relates to the field of tumor treatment, and particularly relates to application of a TRK inhibitor LYS-8 in preparation of a medicine for treating malignant tumors, particularly pancreatic cancer. LYS-8 is a small molecule TRK inhibitor with a novel structure, and research finds that LYS-8 can significantly inhibit TRK kinase activity and down-regulate downstream PI3K-AKT and other signal channels. Experimental results show that the inhibition effect of LYS-8 in pancreatic cancer cells is obviously superior to that of colorectal cancer cells, and the IC50 value of LYS-8 is lower; in an animal model, the tumor inhibition rate of LYS-8 on pancreatic cancer reaches about 70%, and the inhibition rate on colorectal cancer is about 56%, which is obviously superior to that of a colorectal cancer model. The invention reveals that LYS-8 has an unexpected curative effect advantage on pancreatic cancer, and a new drug choice is provided for targeted therapy of pancreatic cancer.

The invention discloses a copper ion-kaempferol nano-composite and application thereof in treatment of inflammatory bowel disease, the obtained nano-composite has very strong stability and active oxygen scavenging ability, and has excellent oxidation resistance and anti-inflammatory ability, and the specific performance is as follows: the surface is negatively charged, and the nano-composite can specifically target the diseased region of intestinal inflammation, so that the copper ion-kaempferol nano-composite can be applied to treatment of inflammatory bowel disease. The intestinal mucosal barrier injury is effectively repaired, the imbalance state of intestinal flora is adjusted, and the intestinal inflammation microenvironment is remarkably improved; the antioxidant and anti-inflammatory capacities of cells can be enhanced by regulating and controlling a PI3K-Akt signal channel and a nuclear factor kappa B (NF-kappa B) signal channel; the compound shows an excellent treatment effect in mouse models of typical inflammatory bowel diseases such as ulcerative colitis and Crohn's disease and related complications of bowel diseases. The invention provides a new way for constructing a multi-target and multi-layer treatment platform for the inflammatory bowel disease of a natural product.

The invention belongs to the technical field of biological medicine, and particularly relates to application of LRRFIP1 serving as a bilberry extract to improvement of a target spot of insulin resistance of gestational diabetes mellitus. The insulin resistance of gestational diabetes mellitus is improved by specifically regulating and controlling a PI3K-AKT signal channel and a GLUT4 glucose transporter function in skeletal muscle based on the bilberry extract. The bilberry extract used in the invention is a natural plant source, is high in safety, and is suitable for pregnancy. PI3K-AKT signal channels can be activated at the same time, and insulin resistance and lipid metabolism disorder can be synergistically improved. The action mechanism is systematically illuminated through technical means such as proteomics, network pharmacology, molecular docking and the like. Glucose tolerance, insulin sensitivity and blood fat level of GDM rats can be remarkably improved, and no remarkable side effect exists.

The invention relates to the field of biological medicine, in particular to a benzofuran [2, 3-b] quinoline derivative as well as a preparation method and application thereof in resisting renal fibrosis. The structure of the benzofuran [2, 3-b] quinoline derivative, the optical isomer thereof or the pharmaceutical salt thereof is shown as a formula (I): # imgabs0 #, wherein R1 is selected from C1-C8 alkoxy, halogen, a 3-8 membered aliphatic heterocyclic ring, a substituted 3-8 membered aliphatic heterocyclic ring and-NR3R4; r2 is selected from = O, hydroxyl and hydrogen; the substituent group of the substituted 3-8-membered aliphatic heterocyclic ring is selected from C1-C8 alkyl, C1-C8 alkyl ester group, = O and 3-8-membered aliphatic ring. A plurality of derivatives with novel structures are synthesized, the derivatives have the potential of becoming anti-renal fibrosis drugs, renal fibrosis is relieved by dual regulation and control of TGF-beta1 / Smad2 / Smad3 and PI3K / AKT signal pathways, and a new strategy and thought are provided for treatment of CKD.

The invention discloses an additive for resisting cow ovarian aging and its application. The additive is made of a composition of anthocyanidins, glycyrrhizic acid and wolfberry glycopeptide. When the composition is used in clinical veterinary treatment of cow ovarian aging, the role of primary cow ovarian granulosa cells is clarified through transcription, which is mainly involved in regulating programmed cell death, Ras protein signal transduction, tissue development, cell serine, tryptophan kinase activity, MAPK signaling pathway, PI3K-AKT signaling pathway, and laser confocal results show that the composition can significantly reduce the production of mitochondrial reactive oxygen; at the same time, the therapeutic effect on the persistent corpus luteum of the main cow is achieved by improving the intestinal flora structure, and more specifically, the colony is significantly changed upstream at the genus and species level; B-ultrasound results reveal that for a persistent corpus luteum cow, more large follicles can be detected on the ovaries after one month of gavage with the additive composition.

The present disclosure relates to the technical field of use of chidamide in drug preparation, particularly to use of chidamide in preparing a drug for treating renal fibrosis. The present disclosure proves that the chidamide can significantly improve the fibrosis of TGF-β stimulated HK2 cells. The chidamide significantly improves the renal fibrosis of UUO mice and ameliorates the renal fibrosis through a PI3K / Akt signaling pathway, so that the present disclosure has wide clinical application prospects.

This invention discloses butylphthalide nanoparticles, comprising: a layered double hydroxide and butylphthalide, wherein the butylphthalide is loaded onto the layered double hydroxide. This invention also discloses a method for preparing the above-mentioned butylphthalide nanoparticles, comprising the following steps: mixing the layered double hydroxide, butylphthalide, and water, adsorbing, separating the solid and liquid phases, and drying to obtain butylphthalide nanoparticles. This invention further discloses the application of the above-mentioned butylphthalide nanoparticles in the preparation of drugs for treating acute renal ischemia-reperfusion injury. This invention also discloses a drug for treating acute renal ischemia-reperfusion injury, comprising: the above-mentioned butylphthalide nanoparticles and pharmaceutically acceptable excipients. The butylphthalide nanoparticles of this invention have high drug loading capacity, good stability, and can target and activate the PI3K-AKT signaling pathway, effectively inhibit HK-2 cell apoptosis and oxidative stress, restore mitochondrial function, and improve renal ischemia-reperfusion injury.

The invention discloses an application of a sesquiterpene lactone compound in preparation of a medicine for enhancing a radiation therapy effect, and belongs to the technical field of biomedicine.The elephantopus tomentosus monomer EM-2 in a formula (I) enhances G2 / M phase retardation caused by ionizing radiation by inhibiting a signal channel caused by the ionizing radiation, so that the sensitivity of the radiation therapy is remarkably improved. Experimental results show that the compound combined with radiotherapy can reduce the expression of a cell proliferation marker Ki67, reverse ionizing radiation induced p-AKT activation, and further enhance the anti-tumor effect of radiotherapy. The compound has a good proliferation inhibition effect on cervical cancer cells, and has low toxicity on normal human skin fibroblast HSF cells. On the other hand, EM-2 can be combined with AKT protein in a targeted mode to inhibit a PI3K / AKT signal transduction pathway activated by radiotherapy, meanwhile, protective autophagy activated after radiotherapy is inhibited, and the sensitivity of ionizing radiation to cervical cancer cells is improved.

The invention belongs to the technical field of biological medicine, and provides a human umbilical cord mesenchymal stem cell preparation and application thereof, the preparation comprises human umbilical cord mesenchymal stem cells, ginsenoside Rg3 and a medicinal carrier; the medicinal carrier is a phosphate buffer solution; according to the application, 1 * 10 < 6 > HUCMSCs pretreated by Rg3 are subjected to caudal vein injection on a T2DM mouse model induced by high fat diet combined with STZ, the curative effect and mechanism are verified by combining OGTT, IPITT, serum biochemical detection, HE / PAS tissue staining, q-PCR and other technologies, and finally the purposes of improving glycometabolism of the T2DM mouse, repairing liver / kidney / pancreas target organ injuries, protecting pancreas islet beta cell functions, reducing pancreas islet beta cell functions, reducing pancreas islet beta cell functions, reducing pancreas islet beta cell functions, reducing pancreas islet beta cell functions and the like are achieved. And a theoretical basis is provided for accurate intervention of T2DM by activating an IGF-1R / PI3K-AKT signal channel and regulating and controlling the expression of a glycometabolism-related gene.

The invention discloses a liver-soothing sleep-aiding traditional Chinese medicine composition for stimulating a PI3K / Akt signal channel and a preparation method and application thereof, and the traditional Chinese medicine composition is prepared from the following raw materials in parts by weight: 5-20 parts of radix bupleuri, 10-30 parts of spina date seed, 10-25 parts of poria with hostwood, 10-25 parts of tuber fleeceflower stem, 5-20 parts of radix paeoniae alba, 3-15 parts of radix curcumae and 5-20 parts of cortex albiziae. The traditional Chinese medicine composition is based on a traditional Chinese medicine formula for regulating liver and regulating qi, nourishing blood and tranquilizing, accords with the compatibility of monarch, minister, assistant and guide, and has the effects of soothing liver-qi stagnation, helping sleep and tranquilizing by combining the medicines.

The present application relates to the technical field of biological medicine, and particularly relates to a composition for protecting cochlear spiral ganglion neurons and application thereof. The composition comprises Panax notoginseng saponins (PNS) and Polygonatum sibiricum polysaccharide (PSP). Research shows that the composition can significantly improve the survival rate of neurons, promote neurite growth, reduce the level of reactive oxygen species, inhibit cell apoptosis, and promote autophagy by regulating the PI3K / AKT signaling pathway, thereby effectively resisting ototoxicity damage induced by aminoglycoside antibiotics. The present application further provides the use of the composition in the preparation of a drug for preventing or treating sensorineural hearing loss.

The present application relates to the technical field of RPS4X, and particularly relates to siRNA targeting RPS4X gene, LAMB3-PI3K-AKT signal pathway inhibitor, ovarian cancer drug and application. The siRNA targets and interferes with RPS4X gene expression. The siRNA and the LAMB3-PI3K-AKT signal pathway inhibitor are used on in-vitro ovarian cancer cells and in-vivo ovarian cancer tissues, and both have the effect of inhibiting proliferation, migration and invasion. The various siRNAs targeting RPS4X gene and the LAMB3-PI3K-AKT signal pathway inhibitors provided in the embodiments have the effects of promoting apoptosis of ovarian cancer cells and tissues and inhibiting tumor angiogenesis, have obvious ovarian cancer prevention and treatment effects, and have the application prospect of developing as ovarian cancer drugs.

The invention relates to the technical field of immunology and biomedicine, in particular to application of CD23 as a target spot to preparation of a medicine for treating IL-17 mediated diseases. By enhancing the expression or function of CD23, an IL-7R alpha-mediated mTORC2-AKT signal channel is activated, the expression of Bcl-2 is promoted, and the apoptosis of NKT17 cells is inhibited, so that the steady state and function of the NKT17 cells are maintained. Experimental results show that the deletion of CD23 causes the reduction of NKT17 cells, the expression of p-AKT (Ser473) and Bcl-2 is reduced, and the signal activity can be recovered by the supplementation of exogenous IL-7. The dependency of the signal path is further verified by using an mTORC2 inhibitor. An airway hyperreactivity model experiment shows that the lung airway hyperreactivity of a CD23-deficient mouse can be reduced, the IL-17 level is reduced, and the inflammatory response is relieved.

The application relates to the field of biological medicine, and particularly relates to application of kaempferol-3-O-acacia di-saccharide-7-O-rhamnose glycoside in preparation of a medicine for preventing and / or treating diseases related to glycolipid metabolism disorder. The compound or a pharmaceutically acceptable salt, ester, solvate or prodrug thereof can be used for treating diseases such as type 2 diabetes, insulin resistance, hyperglycemia, hyperlipidemia and non-alcoholic fatty liver disease. The compound can significantly reduce intracellular glucose, triglyceride and total cholesterol levels, and can play a role by activating an AKT signal pathway, so as to improve glycolipid metabolism disorder and has potential clinical application value.

The invention belongs to the field of medicines for treating rheumatoid arthritis, discloses application of Klotho in preparation of medicines for treating rheumatoid arthritis, and particularly relates to application of Klotho in improvement of the inflammatory state of rheumatoid arthritis by regulating a PI3K-AKT signal channel. Klotho can effectively improve clinical inflammation indexes of RA (rheumatoid arthritis). The Klotho can improve the inflammatory state of the RA by adjusting a PI3K-AKT signal channel. Animal experiments prove that Klotho can be applied to treatment of rheumatoid arthritis diseases.

The invention provides an application of CLCA2 or a carrier for overexpressing the CLCA2 or a lentivirus for overexpressing the CLCA2 in preparation of a medicine for treating triple negative breast cancer. The invention firstly points out that the CLCA2 is a regulatory factor for promoting the apoptosis of triple negative breast cancer cells, and compared with a wild mouse, the mouse overexpressing the CLCA2 shows that the tumor progression of the triple negative breast cancer is obviously inhibited. It is proposed for the first time that the drug target CLCA2 can regulate and control cell apoptosis of the triple-negative breast cancer, the sensitivity of platinum chemotherapeutic drugs (carboplatin) of the triple-negative breast cancer is enhanced by inhibiting a PI3K-AKT signal channel, and a new regulatory factor is provided for improvement of a cell apoptosis signal channel.

The invention relates to a Csi-Bantam inhibitor and application of the Csi-Bantam inhibitor in preparation of a medicine for treating hepatic fibrosis, and belongs to the technical field of biological manufacturing. The invention finds that a Csi-Bantam simulant can be combined with a 3 '-UTR region of a Trim35 gene, and a PI3K / Akt signal channel of the Csi-Bantam is blocked by inhibiting the function of the Csi-Bantam, so that hepatic stellate cells (activated hepatic stellate cells are core driver cells of hepatic fibrosis, and the activated hepatic stellate cells are core driver cells of hepatic fibrosis) can be obviously inhibited; ) and excessive secretion of extracellular matrixes such as type I and type III collagenous fibers, so that the hepatic fibrosis process is effectively improved. The invention discloses the new application of the Csi-Bantam inhibitor in preparation of the medicine for treating hepatic fibrosis for the first time. The discovery provides a brand new thought for targeted therapy of hepatic fibrosis, and has important clinical transformation value for treatment of hepatic fibrosis caused by parasitic infection and other factors.

This invention relates to the application of cucurbitacin Q1 in the preparation of drugs for treating gliomas, belonging to the field of biomedical technology. The cucurbitacin Q1 of this invention has a significant inhibitory effect on glioma cell activity. It can inhibit the protein expression of JAK1, JAK2, and STAT4 by regulating the JAK-STAT signaling pathway, and block the phosphorylation activation of STAT3 protein, thus weakening downstream signal transduction in this pathway. Simultaneously, it can also exert an anti-tumor effect by regulating the phosphorylation level of related proteins in the PI3K-AKT signaling pathway. The cucurbitacin Q1 of this invention not only significantly inhibits the proliferation, invasion, and migration of glioma cells, but also significantly increases the apoptosis rate of glioma cells.

The invention discloses an application of a traditional Chinese medicine compound decoction in treatment of non-small cell lung cancer in the technical field of medicines, effective components of the traditional Chinese medicine compound decoction can inhibit proliferation and migration of non-small cell lung cancer cells, induce cell apoptosis and S-phase arrest of a cell cycle, inhibit activation of an IL-6 / AKT signal channel, inhibit apoptosis of the cells and inhibit apoptosis of the cells. Meanwhile, Ki-67 protein expression can be down-regulated to inhibit cell proliferation, the response not only can directly inhibit tumor cell proliferation and promote apoptosis in curative effect, but also can obviously enhance the sensitivity of the existing chemotherapeutic drugs, and has a unique protective effect of preventing or reducing liver and kidney toxicity caused by chemotherapy, so that the synergistic treatment purpose of reducing toxicity and improving efficiency is achieved.

The invention discloses an application method of ginsenoside Rg3 for relieving broiler chicken immune stress, and relates to the technical field of broiler chicken immune stress intervention. The invention reveals that ginsenoside Rg3 drives the polarization conversion of macrophages from M1 type to M2 type by regulating MAPK and mTOR / PI3K / AKT signal channels for the first time, and alleviates the immune stress of broiler chickens.