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44results about How to "Inhibit autophagy" patented technology
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Method for inhibiting autophagy of motor neurons
ActiveUS20140045765A1Inhibit autophagyBiocideNervous disorderPrimary motor neuronBULK ACTIVE INGREDIENT
A method for inhibiting the autophagy of motor neurons in a subject is provided. The method comprises administrating to the subject an effective amount of an active ingredient selected from the group consisting of a compound of formula (I), a pharmaceutically acceptable salt of the compound, a pharmaceutically acceptable ester of the compound and combinations thereof:wherein A is a C1-C5 alkyl optionally having one or more unsaturated bonds and optionally being substituted by one or more substituents selected from a group consisting of —OH, ═O and C1-C3 alkyl; X is H, —OH,Y is O or S and can optionally combine with A to form a five-membered ring; and R1 is H or a substituted or unsubstituted C1-C20 alkyl, wherein one or more —CH2— of the C1-C20 alkyl are optionally being replaced by —NH— or —O—.
Owner:CHINA MEDICAL UNIVERSITY(TW)
Cell autophagy inhibitor, preparation method thereof and application
ActiveCN107496901AInhibit autophagyWide variety of sourcesPowder deliveryOrganic active ingredientsKras mutationAutophagic death
The invention discloses a cell autophagy inhibitor taking rubiaceae-type cyclopeptides as effective components. The cell autophagy inhibitor is particularly used for inhibiting KRAS mutation, particularly KRAS dependent tumor cell protective autophagy, and promoting tumor cell apoptosis. The inhibitor is preferably a nano-micelle injection and can be applied to preparation of medicines for treating and preventing KRAS related cancers such as colon cancers, rectal cancers, lung cancers and pancreatic cancers. The cell autophagy inhibitor can effectively inhibit tumor cell protective autophagy, the rubiaceae-type cyclopeptides serving as the effective components are wide in source, the extraction process is mature, dosage forms and pharmacy modes are diversified, and the inhibitor can be applied to treatment and prevention of the KRAS related cancers and has a wide clinical application prospect.
Owner:CHINA PHARM UNIV +1
Application of DNA tetrahedron to induction of autophagy
PendingCN107961243AAutophagy inductionInhibit autophagyOrganic active ingredientsDrug compositionsSelf assembleA-DNA
The invention provides application of a DNA tetrahedron to induction of autophagy. The DNA tetrahedron is synthesized from four single DNA strands through self-assembling, wherein the sequences of thefour single DNA strands are shown in SEQ ID No. 1-4. The DNA tetrahedron can activate a PI3K / AKT / mTOR signaling pathway so as to conduct induction effect on autophagy. Specifically, the DNA tetrahedron can act on the upstream protein AKT of mTOR and conducts inhibition effect on the expression of the protein mTOR by activating the expression of AKT; meanwhile, DNA tetrahedron can negatively act on mTOR by up-regulating the expression of the upstream protein PI3K of mTOR so as to allow the expression of mTOR to be inhibited, so autophagy is further induced and biomolecules in cells are highlyrecycled for the cells, and thus, the proliferation and migration of cells are improved.
Owner:SICHUAN UNIV
Application of ligustilide as adjuvant drug of antitumor drugs
InactiveCN105748466AInhibit autophagyConducive to survivalOrganic active ingredientsAntineoplastic agentsAntitumor AAdjuvant Medication
The invention discloses an application of ligustilide as an adjuvant drug of antitumor drugs. The research found that ligustilide can directly inhibit autophagy and then can perform combined effects with the antitumor drugs such as tamoxifen, cis-platinum and the like, the antitumor effect is improved, and the drug resistance of tumor cells to the antitumor drugs can be improved.
Owner:SOUTHWEST UNIV
Application of berberine in preparation of drugs inhibiting adipocyte autophagy
InactiveCN103393679AInhibit autophagyOrganic active ingredientsMetabolism disorderWestern blotBerberine
Belonging to the field of medicine preparation, the invention in particular relates to application of berberine in preparation of drugs inhibiting subcutaneous adipose and visceral adipose cell autophagy. The invention takes high fat fed mice as experimental objects to test whether berberine inhibits autophagy of subcutaneous adipose and visceral adipose cells of the mice. Specifically, the process includes: feeding C57BL / 6 mice with high fat for 12 weeks, then dividing the mice into a high fat group and a berberine group, continuing the high fat diet and berberine gavage once a day for 4 weeks, using Western Blot to detect the change of autophagy related protein, and using Real-time PCR to detect the change of the corresponding mRNA level. Results show that: under high fat feeding, subcutaneous and visceral adipose tissue autophagy increases, and berberine could effectively inhibit subcutaneous adipose and visceral adipose autophagy of the high fat fed mice, thus providing the experimental data and theoretical basis for more reasonable application of berberine in treatment of obesity clinically.
Owner:RUIJIN HOSPITAL AFFILIATED TO SHANGHAI JIAO TONG UNIV SCHOOL OF MEDICINE
Nano-medicine, preparation method thereof and application of nano-medicine
ActiveCN110840860ARealize the combinationAchieving a sensitizing effectOrganic active ingredientsEnergy modified materialsCalcium biphosphateCalcium pidolate
The invention provides a nano-medicine, a preparation method thereof and an application of the nano-medicine. The nano-medicine comprises a calcium phosphate substrate, a chemotherapy medicine, a photo-thermal agent and an autophagy inhibitor, the chemotherapy medicine is sealed in the calcium phosphate substrate, the surface of the calcium phosphate substrate is modified by the photo-thermal agent, and the autophagy inhibitor is loaded into a pore of the photo-thermal agent. According to the nano-medicine, chemotherapy and thermotherapy are combined, calcium phosphate serves as a rigid substrate, the chemotherapy medicine and the photo-thermal agent are sealed in the rigid substrate of the calcium phosphate, the autophagy inhibitor of a cell is loaded on the rigid substrate, so that chemotherapy and thermotherapy effects can be improved by inhibiting autophagy, and tumor treatment effects are improved.
Owner:THE NAT CENT FOR NANOSCI & TECH NCNST OF CHINA
Pharmaceutical composition for treating digestive tract cancers
ActiveCN111110666AInhibit autophagyInhibition shiftOrganic active ingredientsAntineoplastic agentsDigestive tract cancerPharmaceutical drug
The present invention provides a pharmaceutical composition for treating digestive tract cancers, belongs to the technical field of drugs and an application of FTY720 or a combination of the FTY720 with JTE-013 in preparation of 5-fluorouracil (5-FU) drug resistance reversal agents. The provided pharmaceutical composition for treating the digestive tract cancers comprises 5-fluorouracil and at least one of the following 5-fluorouracil drug resistance reversal agents: FTY720 and JTE-013. The present invention also provides use of SphK2 and S1PR2 in screening drugs for reversing drug resistanceof fluorouracil compounds for the digestive tract cancers. The SphK2 up-regulates DPD expression-induced fluorouracil primary drug resistance and S1PR2 translocation-induced fluorouracil acquired drugresistance, and besides, the SphK2 and S1PR2 can be used as new molecular targets by designing targeted drugs to solve a drug resistance problem of the fluorouracil and derivatives thereof in cancertreatment processes.
Owner:CAPITAL UNIVERSITY OF MEDICAL SCIENCES
Application of 3, 4-broken cycloartane type triterpenoid compound in preparation of autophagy inhibitors and antitumor drugs
ActiveCN111481534AInhibition of ubiquitinationInhibition of protective autophagyOrganic active ingredientsAntineoplastic agentsReceptorTumor cells
The invention discloses new use of a 3, 4-broken cycloartane type triterpenoid compound. The compound is nigranoic acid or kadsuric acid, and is used in preparation of autophagy inhibitors and preparation of drugs for increasing the treatmnet sensitivity of anti-tumor drugs. The compound can be used for inhibiting ubiquitination modification of an autophagy receptor p62 and prevent activation of ap62 autophagy receptor function, and can inhibit the protective autophagy of tumor cells induced by anti-tumor drugs. The invention also provides an anti-tumor pharmaceutical composition, which comprises the 3, 4-broken cycloartane triterpenoid compound and an anti-tumor drug capable of easily causing tumor cell protective autophagy, can inhibit tumor cell growth and promote tumor cell death, andcan be used for treating cancers such as breast cancer and the like.
Owner:KUNMING INST OF ZOOLOGY CHINESE ACAD OF SCI +1
Use of novel autophagy inhibitors to treat autophagy related human diseases
ActiveUS20160375029A1Inhibit autophagyInhibiting endosomal traffickingOrganic active ingredientsAntiparasitic agentsMalariaCancer research
Owner:VERSITECH LTD
Detection method for influences of micro RNA-138-5p on human pancreatic cancer cell apoptosis under hypoxia
InactiveCN108531587APromote apoptosisAvoid survivalMicrobiological testing/measurementMaterial analysisWestern blotAutophagy
The invention belongs to the technical field of medicinal preparations with organic and effective components, and discloses a detection method for influences of micro RNA-138-5p on human pancreatic cancer cell apoptosis under hypoxia. After up-regulation of miR-138-5p mimics, autophagy-associated protein of western blot detection experimental groups is inhibited; pancreas tumor cell autophagic vacuoles of confocal microscopy examination experimental groups are increased. The apoptotic cell percentage plus the necrotic cell percentage and differences between the groups have remarkable significance, and expression of apoptosis-associated protein of the western blot detection experimental groups is regulated up. MiR-138-5p and SIRT1 3'UTR regions are complementarily combined to inhibit reduction of SIRT1 expression. The miR-138-5p plays an important role in autophagy fluxes under hypoxia of pancreatic cancer cells, expression of SIRT1 is regulated through direct targeting to inhibit hypoxia-induced autophagy, and apoptosis of the panc-1 pancreatic cancer cells is promoted at the same time.
Owner:THE AFFILIATED HOSPITAL OF GUIZHOU MEDICAL UNIV
Application of brown algae oligosaccharide
ActiveCN113440532ADecreased urine concentrationImprove pathological changesOrganic active ingredientsUrinary disorderInflammatory factorsDisease
Owner:HAITANG (JIANGSU) BIOTECHNOLOGY CO LTD
Application of tanshinone I in preparation of tumor cell autophagy inducer drugs
ActiveCN111000851AInduce autophagyGrowth inhibitionOrganic active ingredientsAntineoplastic agentsCancer cellCervical ca
The invention discloses application of tanshinone I in preparation of tumor cell autophagy inducer drugs. Compared with the prior art, the invention for the first time finds that tanshinone I can induce autophagy of tumor cells and has a remarkable treatment effect on cervical cancer, breast cancer or liver cancer, especially cervical cancer. Research proves that tanshinone I can inhibit cancer cell growth, inhibit cancer cell mitochondrial injury and autophagy, and induce the expression of tumor cell autophagy molecules and cutting of autophagy molecule LC3.
Owner:YANGZHOU UNIV
Application of SGLT2 inhibitor to preparation of product for improving sensitivity of antitumor drug
ActiveCN112439067AInhibit autophagyGood treatment effectOrganic active ingredientsAntineoplastic agentsEfficacyTherapeutic effect
The invention discloses an application of an SGLT2 inhibitor to preparation of a product for improving sensitivity of an antitumor drug. The inventor finds that the SGLT2 inhibitor Canagliflozin can inhibit the autophagy phenomenon of stress protection generated by tumor cells during chemotherapeutic drug treatment by inhibiting the expression and functions of P-glycoprotein in the tumor cells, sothat the sensitivity of the tumor cells to chemotherapeutic drugs is improved, and the treatment effect of the drug is enhanced. The inhibitor of the type can exist in the form of liquid, dry powderor extract, can be made into capsules, tablets, injections, pills, granules, powder and other various dosage forms with health-care or medicinal effects together with various conventional auxiliary materials, and can be combined with other chemotherapeutic drugs to be used for treating malignant tumors.
Owner:SHENZHEN GRADUATE SCHOOL TSINGHUA UNIV
Application of ICTF (trifluoro-icaritin) to preparation of drug for activating Akt signals and inhibiting autophagy
ActiveCN109381456AAvoid damageInhibit autophagyOrganic active ingredientsCardiovascular disorderVascular diseaseMyocardial cell
The invention discloses an application of ICTF (trifluoro-icaritin) to preparation of a drug for activating Akt signals and inhibiting autophagy. When ICTF is applied to a drug for treating cardiovascular diseases, it is proved that ICTF can relieve ischemia reperfusion-induced EGG damage, reduce myocardial oxidative stress of ischemia reperfusion injury, inhibit autophagy and apoptosis of myocardial cells, improve activation of the Akt signals and reduce levels of autophagy markers Beclin-1 and LC3-II. The drug for treating the cardiovascular diseases has development prospect and is especially used for treating myocardial ischemia (myocardial infarction) reperfusion injury.
Owner:GANNAN MEDICAL UNIV
Application of tizoxanide and nitazoxanide in preparation of autophagy inducer
InactiveCN109999045AInhibit autophagyAutophagy inductionOrganic active ingredientsDrug compositionsDiseaseMedicine
The invention discloses novel medical application of tizoxanide and / or nitazoxanide and a pharmaceutically acceptable salt thereof, namely application of tizoxanide and / or nitazoxanide in the preparation of an autophagy inducer and application of drugs for treating and inhibiting diseases related to mTOR expression. According to the application, the tizoxanide and / or nitazoxanide and the pharmaceutically acceptable salt thereof can achieve related medicine effects by reducing PI3K and AKT protein phosphorylation and reducing ERK protein phosphorylation, the autophagy inhibition function in cells is reduced accordingly, and the cells are induced to achieve autophagy.
Owner:SHANGHAI VETERINARY RES INST CHINESE ACAD OF AGRI SCI
Medicine for treating erectile dysfunction and application thereof
ActiveCN114209837AInhibit autophagyPrevent fibrosisOrganic active ingredientsSexual disorderSexual impotenceFibroblast
The invention discloses a medicine for treating erectile dysfunction and application thereof. The medicine for treating the erectile dysfunction comprises an inhibitor of a Wnt signal channel. The invention finds that the Wnt signal channel is a key channel activated by the fibroblast for the first time, and proves that the inhibitor using the Wnt signal channel can obviously inhibit the expression of collagen in the fibroblast derived from the cavernosum so as to inhibit the fibrosis of the penis cavernosum; therefore, the inhibitor of the Wnt signal channel has the potential of serving as the medicine for treating the erectile dysfunction, and a new thought is provided for developing the medicine for treating the erectile dysfunction.
Owner:THE FIFTH AFFILIATED HOSPITAL SUN YAT SEN UNIV
Combined medicine for treating malignant tumors
PendingCN112220917ATumor targetingSlow autophagyOrganic active ingredientsCarbon-sulfur lyasesChemotherapy effectsPharmaceutical drug
The invention provides a combined medicine for treating malignant tumors. The combined medicine contains unit preparations with different specifications and is used for simultaneously or respectivelysupplying genetically engineered bacteria and chloroquine diphosphate salt. The combined medicine disclosed by the invention can be used for effectively treating cancers, and the effect is obviously superior to that of single use of the genetically engineered bacteria and the chloroquine diphosphate salt, so that the genetically engineered bacteria and the chloroquine diphosphate salt have an obvious synergistic effect after cooperating for use, have strong anti-tumor activity and small side effects, and provide a new treatment direction for patients who lose operation indications clinically,cannot be operated and have poor radiotherapy and chemotherapy effects.
Owner:GUANGZHOU SINOGEN PHARMA CO LTD
Method for inhibiting autophagy of motor neurons
ActiveUS8729026B2Inhibit autophagyOrganic active ingredientsNervous disorderPrimary motor neuronAutophagic death
A method for inhibiting the autophagy of motor neurons in a subject is provided. The method comprises administrating to the subject an effective amount of an active ingredient selected from the group consisting of a compound of formula (I), a pharmaceutically acceptable salt of the compound, a pharmaceutically acceptable ester of the compound and combinations thereof:wherein A is a C1-C5 alkyl optionally having one or more unsaturated bonds and optionally being substituted by one or more substituents selected from a group consisting of —OH, ═O and C1-C3 alkyl; X is H, —OH,Y is O or S and can optionally combine with A to form a five-membered ring; and R1 is H or a substituted or unsubstituted C1-C20 alkyl, wherein one or more —CH2— of the C1-C20 alkyl are optionally being replaced by —NH— or —O—.
Owner:CHINA MEDICAL UNIVERSITY(TW)
Application of seneciphylline in preparation of antitumor medicines
InactiveCN108096245AInhibit autophagyOrganic active ingredientsAntineoplastic agentsAutophagic deathBiological activation
The invention discloses an application of seneciphylline in preparation of antitumor medicines. The seneciphylline can inhibit HeLa cell proliferation and induce HeLa cell autophagy in a dose dependent and a time dependent manner. In addition, the seneciphylline inducing the HeLa cell autophagy is depended on activation of MEK / ERK1 / 2 pathway. The invention provides a novel treatment medicine of treating human cervical cancer.
Owner:LONGYAN UNIV
Autophagy inhibitors
ActiveUS11229680B2Inhibit autophagyPeptide/protein ingredientsAntibody mimetics/scaffoldsDiseaseATG8
Owner:THE HONG KONG UNIV OF SCI & TECH
Cell autophagy inhibitor and its preparation method and application
ActiveCN107496901BInhibit autophagyWide variety of sourcesPowder deliveryOrganic active ingredientsCyclic peptideKras mutation
The invention discloses a cell autophagy inhibitor with Rubiaceae type cyclic peptide as an active ingredient, especially for inhibiting KRAS mutation, especially KRAS-dependent tumor cell protective autophagy, and promoting tumor cell apoptosis; The inhibitor is preferably a nano-micelle injection, which can be applied to the preparation of drugs for treating and preventing KRAS-related cancers, including colon cancer, rectal cancer, lung cancer and pancreatic cancer. The autophagy inhibitor described in the present invention can effectively inhibit the protective autophagy of tumor cells. Its active ingredient Rubiaceae type cyclic peptide has a wide range of sources, its extraction process is mature, and its dosage forms and medication methods are diversified. It can be applied to the treatment of KRAS-related cancers. Treatment and prevention have broad clinical application prospects.
Owner:CHINA PHARM UNIV +1
Use of ligustilide as an auxiliary drug for antineoplastic drugs
InactiveCN105748466BInhibit autophagyConducive to survivalOrganic active ingredientsAntineoplastic agentsAutophagic deathCis-platinum
The invention discloses an application of ligustilide as an adjuvant drug of antitumor drugs. The research found that ligustilide can directly inhibit autophagy and then can perform combined effects with the antitumor drugs such as tamoxifen, cis-platinum and the like, the antitumor effect is improved, and the drug resistance of tumor cells to the antitumor drugs can be improved.
Owner:SOUTHWEST UNIV
Application of curcumin analogue CD35 to preparation of medicine for treating breast cancer
InactiveCN107184568AInhibition of energy metabolismInhibit transferKetone active ingredientsAntineoplastic agentsSide effectStructural formula
The invention relates to application of a curcumin analogue CD35 to preparation of a medicine for treating breast cancer. A chemical formula of the curcumin analogue CD35 is 1-(4-hydroxy-3-methoxyphenyl)-5-(2-nitrophenyl)-1,4-pentadiene-3-one, and a structural formula is shown in the description; the curcumin analogue CD35 is used for down-regulating the expression of YAP proteins in a Hippo path to inhibit the autophagy of breast cancer cells, so as to inhibit the energy metabolism of the breast cancer cells. The curcumin analogue CD35 provided by the invention has remarkable advantages of improving the targeting ability of the medicine for treating the breast cancer and reducing the toxic and side effects of the medicine.
Owner:WENZHOU MEDICAL UNIV
Application of Abemaciclib in preparation of medicine for treating NAFLD
PendingCN111973597AImprove lipid degenerationReduce contentOrganic active ingredientsDigestive systemAbemaciclibHepg2 cells
The invention discloses an application of Abemaciclib in preparation of a medicine for treating NAFLD. After the Abemaciclib is administered to a C57BL / 6 mouse by intragastric administration for 2 weeks, histopathology and serum biochemical results show that the Abemaciclib can improve the liver lipidemia of the mouse and reduce the contents of serum ALT, AST and liver triglyceride. In-vitro experiment results show that the Abemaciclib can resist oxidative stress damage of cells through SESN2 and other mediated anti-oxidative stress pathways. In addition, our studies found that Abemaciclib caninduce HepG2 cells to form intracytoplasmic vacuoles similar to autophagy, presuming that Abemaciclib may improve NASH by inducing autophagy and inhibiting liver fibrosis.
Owner:CHINA PHARM UNIV
Vascular endothelial cell PINK1 acetylation inhibitor and application thereof
InactiveCN109200040AInhibit autophagyOrganic active ingredientsMetabolism disorderAcute hyperglycaemiaVascular endothelium
The invention discloses a pharmaceutical composition capable of inhibiting acetylation of PINK1 of vascular endothelial cells, which is characterized in that astaxanthin is contained and also discloses the use of the pharmaceutical composition in the preparation of medicaments for preventing and / or treating cardiovascular diseases including, but not limited to, atherosclerosis, coronary heart disease, angina pectoris, cerebral thrombosis, hypertension, hyperglycemia, hyperlipidemia, myocardial infarction, ischemic cor pulmonale and the like.
Owner:NINGBO UNIV
Platinum-copper alloy/chloride ion transporter composite tumor treatment preparation and preparation method and application thereof
ActiveCN113350522AAchieve killEfficient killingPowder deliveryMaterial nanotechnologyPlatinumCation Pump
The invention relates to a platinum-copper alloy / chloride ion transporter composite tumor treatment preparation and a preparation method and application thereof. The preparation method comprises the step that a chloride ion transporter is loaded to the surfaces of platinum-copper alloy nanoparticles through the electrostatic interaction. The preparation has the advantages of being good in controllability, small in side effect and the like, and the efficient tumor treatment effect can be achieved.
Owner:ZHEJIANG UNIV HANGZHOU GLOBAL SCI & TECH INNOVATION CENT
A pharmaceutical composition for preventing and treating cyclosporin A chronic nephrotoxicity
ActiveCN104825587BReduce vitalityInhibit apoptosisUrinary disorderPlant ingredientsCyclosporine nephrotoxicityActive ingredient
Owner:GUANGZHOU UNIVERSITY OF CHINESE MEDICINE
Application of 3,4 cleavage cyclic altine triterpenoids in the preparation of autophagy inhibitors and antitumor drugs
ActiveCN111481534BInhibition of ubiquitinationInhibition of protective autophagyOrganic active ingredientsAntineoplastic agentsReceptorTumor cells
The present invention discloses new uses of 3,4-fragmented cyclic altine-type triterpenoids, the compounds are black schisandrin or southern schisandra, including for preparing autophagy inhibitor, preparing for increasing antitumor drug treatment A sensitive drug, the compound can inhibit the ubiquitination modification of autophagy receptor p62, prevent the activation of p62 autophagy receptor function, and can inhibit the protective autophagy of tumor cells induced by anti-tumor drugs, and the present invention also provides An anti-tumor drug composition, including 3,4-fragmented cyclic altine-type triterpenoids and anti-tumor drugs that easily induce tumor cell protective autophagy, can inhibit tumor cell growth and promote tumor cell death, and can be used for Treatment of cancers such as breast cancer.
Owner:KUNMING INST OF ZOOLOGY CHINESE ACAD OF SCI +1
Medicinal use of a kind of lycorine and bortezomib composition
ActiveCN105079776BIncreased sensitivityInhibition of proliferative abilityDipeptide ingredientsBoron compound active ingredientsLycopeneCombined use
Owner:CENT SOUTH UNIV
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