26 results about "Protective drugs" patented technology

The present invention discloses a γ-arylbutenolide compound, a preparation method thereof, and an application thereof in the preparation of cardiovascular protective drugs. The above-mentioned structurally novel γ-arylbutenolide compound is isolated for the first time from the fermentation culture of the marine herbal soft coral symbiotic fungus Aspergillus sp. EGF7-0-1, and it is found for the first time that the above-mentioned compound has a protective effect on the cardiovascular system, providing a pharmacodynamic substance basis for the subsequent research on cardiovascular diseases.

The present application relates to a pharmaceutical composition comprising an NRF2 agonist and borneol, both of which synergize in a specific molar ratio range, enhance the overall anti-inflammatory and antioxidant biological activity of the drug, improve the oral bioavailability and target tissue distribution of the drug, inhibit the off-target side effects of the NRF2 agonist, and significantly improve the effectiveness and safety of the drug.

The invention discloses an application of gentiopicroside in preparation of a medicine for protecting liver ischemia-reperfusion injury, discusses the protection effect of gentiopicroside on mouse liver ischemia-reperfusion injury, and preliminarily reveals a ferroptosis related molecular mechanism. The invention discloses that gentiopicroside can play a role in protecting HIRI by inhibiting ferroptosis, oxidative stress and inflammatory response, further indicates that gentiopicroside can be further used for preparing a medicine for protecting liver ischemia-reperfusion injury, and meanwhile, the invention discloses the effect of ferroptosis in HIRI, discovers a new therapeutic target, and has a good application prospect. A new thought and a new direction are provided for treatment of liver diseases.

The present invention belongs to the field of biomedicine and specifically discloses the use of glycyrrhetinic acid or glycyrrhetinic acid liposomes in the preparation of a drug for protecting against abdominal aortic aneurysms. It reveals that glycyrrhetinic acid can effectively ameliorate the mortality of mice following aortic rupture caused by Ang II treatment, significantly improve the degradation of the aortic elastic fiber layer caused by Ang II treatment, and promote the polarization of lipopolysaccharide (LPS)-induced macrophages toward the M2 type. Intervention with glycyrrhetinic acid before Ang II treatment can alleviate the occurrence of Ang II-induced abdominal aortic aneurysms and improve the survival rate of mice, indicating that glycyrrhetinic acid can be used to prepare a drug for alleviating abdominal aortic aneurysms. Furthermore, the present invention improves the solubility and bioavailability of glycyrrhetinic acid by encapsulating it in liposomes. At the same time, after glycyrrhetinic acid is encapsulated using nanotechnology, its dosage can be effectively controlled, further improving and enhancing the therapeutic effect of glycyrrhetinic acid.

The invention relates to the technical field of biological medicine, in particular to application of nobiletin in prevention and treatment of ionizing radiation damage. The nobiletin provided by the invention is extracted from plants, is of a natural flavonoid structure, has high compatibility with endogenous metabolites of a human body, and has good biocompatibility. Animal experiments prove that when the medicine is administrated at the optimal effective dose (200mg / kg) and 12 hours before irradiation, no obvious toxic reaction is shown, the immunogenicity is low, the medicine is suitable for long-term or conventional radiation protection application, the common problems of adverse reaction and accumulated toxicity in synthesis of protective medicines are solved, and meanwhile, the medicine can be in the optimal action state when being exposed to radiation, so that the medicine can be applied to radiation protection for a long time. The survival time of irradiated mice is remarkably prolonged, acute radiation injury pathological symptoms such as intestinal edema and villus shortening are effectively improved, intestinal crypt regeneration and stem cell proliferation are promoted, and reliable radiation protection efficiency is shown.

The present invention relates to a sesquiterpenoid compound oxyphylleudne F separated from Alpinia oxyphylla seeds and its application, and a compound with a novel structure is found from Alpinia oxyphylla seeds, and the application of the new compound in the development of kidney protection drugs is realized. The technical solution is to separate and identify a new sesquiterpenoid compound oxyphylleudne F from the n-butanol part of Alpinia oxyphylla seeds, and find through experimental research that the compound can inhibit and attenuate the TGF-β-catenin induced by TGF-β-catenin in a dose-dependent manner. β 1 induces the expression of fibronectin, type I collagen and α The expression of SMA has anti-renal fibrosis activity and can be effectively used to prepare renal protective drugs. The preparation method has good reproducibility and the obtained compound has high purity, which is conducive to further pharmacological and clinical research on it, and has expanded the medicinal value of Alpinia oxyphylla, with huge economic and social benefits.

The invention discloses a lyophyllum decastes active polysaccharide, a preparation method thereof and application of the lyophyllum decastes active polysaccharide in preparation of drugs for improving drug-induced liver injury, and relates to the technical field of biological medicines. The preparation method comprises the following steps: with lyophyllum decastes sporocarp as a raw material, extracting by adopting a water extraction and alcohol precipitation method to obtain a lyophyllum decastes crude extract; performing deproteinization treatment on the lyophyllum decastes crude extract, and performing dialysis treatment to obtain lyophyllum decastes crude polysaccharide; and purifying the crude polysaccharide of the lyophyllum decastes through a DEAE-52 cellulose anion exchange chromatography column and a Superdex 16 / 600200pg molecular sieve gel filtration column respectively to obtain the active polysaccharide of the lyophyllum decastes. The lotus leaf lyophyllum decastes active polysaccharide provided by the invention has a good protection effect on drug-induced liver injury, can be used for preparing polysaccharide liver protection agent drugs, liver protection auxiliary materials and functional foods, and has important economic value and market value.

The application belongs to the technical field of medicine, and discloses application of 4-amino-1-benzylpiperidine in a drug for preventing and / or treating acute lung injury. The application carries out experimental research on the effect of 4-amino-1-benzylpiperidine in preventing and / or treating acute lung injury through in-vivo and in-vitro models, and the result shows that 4-amino-1-benzylpiperidine can significantly inhibit neutrophil chemotaxis, reduce the number of inflammatory cells and the release of inflammatory factors in bronchoalveolar lavage fluid of an animal with LPS-induced acute lung injury, and improve pathological damage of lung tissue, and can be used for preparing a protective drug for acute lung injury. The application provides a new use of 4-amino-1-benzylpiperidine in preparing a protective drug for acute lung injury, and provides a safe, effective and economical solution for treatment and prevention of acute lung injury.

The invention belongs to the technical field of medicines, and particularly discloses application of a compound 84-B10 in preparation of myocardial protection medicines. In order to solve the problems that in the prior art, effective therapeutic drugs are lacked for myocardial injury caused by sepsis and chemotherapeutic drugs (cis-platinum and adriamycin), and an existing cardiac protective agent possibly interferes with the chemotherapeutic effect, 84-B10 is used for preparing the myocardial protective drug, and the 84-B10 is particularly suitable for patients suffering from cardiac function injury caused by sepsis or chemotherapeutic drugs. Experiments show that the medicine can significantly improve the cardiac ejection fraction and shortening rate, reduce the levels of serum lactic dehydrogenase (LDH) and creatine kinase isoenzyme (CK-MB), and inhibit the expression of chemotactic factors (CCL5 and CXCL1) and inflammatory factors (IL-6 and IL-17A) in cardiac muscle tissues. Meanwhile, the medicine does not interfere with the killing effect of adriamycin on tumor cells, and the curative effect of chemotherapy is guaranteed. The medicine is simple in preparation process and high in stability, can realize efficient protection in a myocardial injury model, and has clinical application potential.

This invention relates to the field of biomedicine, specifically disclosing an amphiphilic prodrug for mitochondrial targeted therapy, its preparation method, and applications. The target-containing amphiphilic prodrug of this invention can self-assemble in water to form nanomicelles with an outer layer of hydrophilic short peptides and an inner layer of hydrophobic mitochondrial protective drugs. Because the hydrophilic short peptide SS-31 on the surface of the nanomicelles is positively charged, it can act as a cell-penetrating peptide to rapidly cross the cell membrane and even the blood-brain barrier in a non-toxic manner, and can also specifically and selectively enter the mitochondrial matrix, exerting an antioxidant effect by inhibiting cardiolipin oxidation. Therefore, these nanomicelles can rapidly target and accumulate in the mitochondrial region. Under the action of ROS, the small molecule linkers that specifically respond to reactive oxygen species break down and consume ROS. Through electron transfer, the mitochondrial protective drugs are released, synergistically acting on the mitochondria of damaged cells with SS-31, jointly exerting anti-inflammatory and anti-apoptotic effects.

This invention provides the application of a traditional Chinese medicine composition in the preparation of cardiovascular protective drugs after percutaneous coronary intervention (PCI) for myocardial infarction, specifically acute ST-segment elevation myocardial infarction (STEMI), with a TCM syndrome of "heart yang deficiency." The composition comprises raw Cornus officinalis, dried ginger, ginseng, Astragalus membranaceus, Atractylodes macrocephala, Alisma plantago-aquatica, Poria cocos, and Aconitum carmichaelii. The cardiovascular protective effects of this composition include improving cardiac function, inhibiting postoperative oxidative stress, reducing NT-proBNP, and decreasing the risk of cardiovascular events within one year post-surgery. It can be prepared as a decoction, oral liquid, or other dosage forms, and can be used in combination with conventional Western medicine treatments for synergistic effects. The composition of this invention is scientifically formulated, targets multiple points of action, and effectively addresses the problem of limited cardiovascular protection methods after PCI in STEMI patients, significantly improving patient prognosis and demonstrating good clinical application value.

The invention belongs to the technical field of medicine synthesis, and particularly relates to a 1, 2, 4-triazole compound as well as a preparation method and application thereof. The 1, 2, 4-triazole compound provided by the invention has a structure as shown in a formula I: # imgabs0 # test results show that the 1, 2, 4-triazole compound provided by the invention not only has a better selective inhibition effect on HDAC6 protein, but also can inhibit proliferation of gastric adenocarcinoma cells, has a protection effect on myocardial cells, and can be used for preparing a medicine for treating gastric adenocarcinoma cells. The compound can be developed and applied as an HDAC6 inhibitor, an anti-gastric cancer drug or a myocardial protection drug. Therefore, the skeleton type of the compound in an HDAC6 inhibitor is enriched, and meanwhile, a new direction and data support are provided for developing an anti-tumor drug which is low in myocardial injury risk and has HDAC6 selectivity.

The present invention relates to a nucleic acid molecule or a composition comprising said molecule for use as an anti-inflammatory and / or anticoagulant and / or organ protective drug. The present invention also relates to the use of said nucleic acid molecule or said composition for the manufacture of a medicament for the prevention, treatment, regression, cure and / or delay of a disease or condition in which inflammation and / or coagulation and / or organ impairment or failure occurs in an individual. Finally, the present invention further relates to a method for alleviating one or more symptoms and / or parameters and / or improving a disease or condition in which inflammation and / or coagulation and / or organ impairment or failure occurs in an individual, the method comprising administering to said individual said nucleic acid molecule or said composition.

The invention discloses a polaprezinc gastric floating tablet which sequentially comprises a tablet core layer, a shell layer and an outermost layer from inside to outside, and the tablet core layer comprises polaprezinc, a sustained-release material A, a coloring agent and a lubricating agent A; the shell layer composition comprises a sustained-release material B, a retardant and a lubricant B; the outermost layer comprises polaprezinc, a disintegrating agent, an adhesive, a filling agent and a lubricating agent C. The medicinal gastric floating tablet prepared by the formula and the method disclosed by the invention can effectively prolong the acting time of the medicine in the stomach, only needs to be taken once a day, and can be effectively used as a gastric mucosa protection medicine for assisting in treating gastric ulcer.

According to the laminaria proteoglycan purified extract and the preparation method and application thereof, in the preparation process of the purified extract, an ultrasonic-assisted water extraction method and anion exchange chromatography are adopted for purification, the extraction efficiency is high, the purification effect is good, laminaria proteoglycan effective ingredients in laminaria can be effectively enriched, and the content of laminaria proteoglycan in laminaria is increased. The obtained extract is high in purity and high in activity, high-value utilization of kelp resources is achieved, kelp proteoglycan is used as a whole for extraction, purification and activity research, and the synergistic effect of kelp proteoglycan is fully exerted. In the invention, a caenorhabditis elegans model, a zebra fish model and a human renal epithelial cell (HK-2) model verify that the laminarin purified extract has a remarkable protective effect on the body injury caused by the microplastics, and a new candidate medicine and a scientific basis are provided for developing the microplastic injury protection medicine.

Use of vitamin D in the preparation of a protective drug for avoiding chemotherapy-induced ovarian injury, pertaining to the field of biotechnology. It has been discovered for the first time that in experiments involving intraperitoneal injection of calcitriol (the active form of vitamin D) and retinoic acid into newborn mice, both calcitriol and retinoic acid, when used individually, can partially reverse the DNA damage caused by the chemotherapeutic drugs cyclophosphamide and doxorubicin, and significantly reduce the number of primordial follicle apoptosis induced by chemotherapeutic drugs (including cyclophosphamide and doxorubicin); the combined drug use (calcitriol + retinoic acid) has a better effect. This discovery expands the application of vitamins in the female reproductive system, provides new ideas for preventing damage to ovarian follicle development caused by chemotherapeutic drugs and for the in vivo protection of fertility, and is also of great significance for safeguarding the quality of life of female patients after chemotherapy.

The invention belongs to the field of small molecule drugs, and discloses a new application of a natural small molecule compound coumarin 478 (MIC) in prevention and treatment of doxorubicin-induced cardiotoxicity (DIC). The clinical application of doxorubicin is limited by dose-dependent cardiotoxicity, and the existing protective drug dextrolecomycin has the defects of bone marrow suppression, curative effect interference and the like. In-vitro screening finds that MIC can reduce myocardial cell mitochondrial oxidative stress (figure 1-2) in a dose-dependent manner under the concentration of 0.5-10 [mu] M, improve energy metabolism and inhibit apoptosis; animal experiments prove that MIC can restore heart functions (EF (upward)) and relieve fibrosis and myocardial hypertrophy (figure 4). Mechanism research shows that MIC plays a role through specific up-regulation of myocardial cell uncoupling protein UCP3 expression (Figure 5). The key advantage is that the combination of MIC and adriamycin does not affect the antitumor activity (figure 3), and can reduce the risk of myelosuppression. The invention provides a safe and effective new strategy for DIC prevention and treatment, and is especially suitable for tumor patients needing long-term adriamycin treatment.

The invention provides a new application of Rab5a in preparation of a medicine for protecting the heart. The invention finds that Rab5a provides a new therapeutic target for hypertension heart injury, Rab5a overexpression can improve cardiac hypofunction and pathological change caused by hypertension, and a new choice is provided for clinical treatment of heart disease.

The invention relates to the technical field of biological medicine, and particularly discloses application of KYNA in preparation of a medicine for preventing intestinal injury caused by ionizing radiation, and the intestinal injury caused by ionizing radiation comprises radioactive substances capable of causing ionization of substances or intestinal injury caused by irradiation of rays emitted by linear accelerator equipment. The protection of the intestinal injury caused by the ionizing radiation comprises prolonging the survival time of the mouse irradiated by the ionizing radiation and protecting the intestinal tissue structure of the mouse irradiated by the ionizing radiation. The medicine taking KYNA as the active component for preventing intestinal injury caused by ionizing radiation provided by the invention has the advantages of low price, small toxic and side effects, remarkable curative effect, convenience and safety in medication and the like.

This invention discloses a microchannel-based bioresorbable polylactic acid (PLA) scaffold and its preparation method. The scaffold comprises a tubular mesh body made of PLA-based bioresorbable material, with at least a portion of the scaffold struts forming a continuous hollow microchannel network, which serves as a structural reservoir for therapeutic drugs. The scaffold preparation method is as follows: a three-dimensional tubular template is constructed using sacrificial template fibers; PLA solution is impregnated / drained into the three-dimensional tubular template and solidified into a composite preform; the composite preform undergoes reinforcement, shaping, and curing treatment; subsequently, the template is dissolved and removed to form the microchannel network; then, a drug solution is perfused into the microchannel network using pressure-driven infusion, followed by drying and curing to complete the loading. Compared to surface coating drug loading methods, this invention can achieve protective drug loading and controlled release while maintaining mechanical support, making it suitable for interventional treatments in cardiovascular, peripheral vascular, and non-vascular lumens.

This application discloses succinimide derivatives in the field of organic chemistry, with the general structural formula shown in Formula V. During preparation, compound I reacts with compound II to yield compound III; compound III reacts with compound IV in the presence of a condensing agent to yield succinimide derivative V. The succinimide derivatives of this application can be used in the preparation of sedative, tranquilizing, nootropic, anticonvulsant, antiepileptic, antineuralgia, anti-anxiety, antidepressant, antidementia, and / or brain injury protective drugs.

The invention belongs to the technical field of biological medicines, and particularly relates to application of silibinin in preparation of a low-dose radiation-induced immune system injury protection medicine. The invention provides an application of silybin in preparation of a medicine for preventing immune system injury caused by low-dose radiation, the low-dose radiation comprises low-dose radiation treatment through 60 Co gamma, and the low dose is 0.1-2Gy. The silibinin can significantly promote RAW264.7 cell proliferation after low-dose radiation, significantly reduce the expression level of ROS in cells and the mRNA level of inflammatory factors IL-6, IL-1beta and TNF-alpha, has a alleviation trend to mouse spleen inflammatory cell infiltration caused by low-dose radiation, and inhibits reduction of the number of spleen immune cells. Silybin has a protection effect on immune system injury caused by low-dose radiation, and cell injury caused by radiation can be reduced by regulating and controlling a cGAS signal channel, so that the radiation protection effect is achieved.

The application belongs to the field of pharmaceutical chemistry and particularly relates to application of specific pyrrolidone chalcone compounds in preparation of therapeutic drugs for diseases related to myocardial injury, the pyrrolidone chalcone compounds can have good protective effect on oxidative stress and high glucose induced myocardial cell injury, they can effectively eliminate generation of active oxygen in oxidative stress injury by activating Nrf2 / HO-1 antioxidant signal pathway, and have good protective effect on myocardial cell injury.

The invention discloses a sesquiterpene lactone derivative as well as preparation and application thereof in dialysis blood vessel protection. The sesquiterpene lactone derivative disclosed by the invention has a structure as shown in a formula (I), is mainly prepared from sesquiterpene lactone and amino acid through reaction, and can be used for preparing an internal arteriovenous fistula protection medicine for renal dialysis. Expression of PCNA and TLR4 in VSMCs can be effectively inhibited, proliferation of VSMCs in an AVF model is further inhibited, venous stenosis and thrombosis caused by neointimal hyperplasia are reduced, the incidence rate of AVF dysfunction is reduced, and the application prospect in preparation of internal arteriovenous fistula protection drugs for renal dialysis is good. # imgabs0 #

This invention discloses a pyrrolidine alkaloid compound, its preparation method, and its applications, belonging to the field of biotechnology. This invention originates from marine fungi. Trichoderma harzianum A novel pyrrolidine alkaloid compound was extracted and isolated from the fermentation culture of ZN-4. Cell experiments showed that the pyrrolidine alkaloid compound provided by this invention has good cardiomyocyte protective activity and low cytotoxicity, and has development prospects in the preparation of cardiomyocyte protective drugs or functional foods.

The application provides a laminarin proteoglycan purified extract and a preparation method and application thereof. In the preparation process of the purified extract, ultrasonic-assisted water extraction and anion exchange chromatography are used for purification, the extraction efficiency is high, the purification effect is good, the effective components of laminarin proteoglycan in laminaria can be effectively enriched, the obtained extract has high purity and strong activity, the high-value utilization of laminaria resources is realized, the laminarin proteoglycan is extracted and purified as a whole and activity research is conducted, and the synergistic effect is fully exerted. In the application, through the Caenorhabditis elegans model, the zebra fish model and the human kidney epithelial cell (HK-2) model, it is verified that the laminarin proteoglycan purified extract has a significant protection effect on the damage of the organism caused by microplastics, and a new candidate drug and scientific basis are provided for the development of a microplastic damage protection drug.