58 results about "Statin" patented technology

The invention provides a culture medium for improving Klotho protein secreted by mesenchymal stem cells and application of the culture medium, and particularly, the culture medium comprises a basic culture medium, statins and a ROCK inhibitor. The culture medium can effectively improve the Klotho protein secretion level of the mesenchymal stem cells, does not affect the biological activity of the mesenchymal stem cells, and ensures the biological function integrity of the mesenchymal stem cells; meanwhile, operation is easy, cost is low, and good clinical application value is achieved.

The application discloses an inhibitor for inhibiting KRAS phase separation to play an anti-tumor role and application, and relates to the fields of tumor molecular biology and targeted therapy.The application aims at solving the problems of limited effect, strong drug resistance and limited application range of KRAS tumor treatment methods, and the inhibitor is a statin.The KRAS protein can form a liquid condensate in cells, and the application discloses the mechanism of the KRAS protein in promoting KRAS protein processing, transportation and downstream signal activation, and further provides a technical scheme for inhibiting tumor growth and enhancing the therapeutic effect of a KRAS inhibitor by inhibiting the formation of KRAS condensates, so as to provide a new target and intervention approach for tumor treatment.

This invention relates to the field of ovarian tissue in vitro culture technology, and discloses a formulation for activating and increasing follicles and its application. The formulation consists of a PI3K / Akt / mTOR pathway activator and / or a PTEN inhibitor SF1670. The PI3K / Akt / mTOR pathway activator is a 5-15 μM statin, and the PTEN inhibitor is a 20-50 μM SF1670. Using this formulation can achieve the follicle activation and increase effect of existing technologies, contributing to the development and selection of in vitro follicle activators in clinical practice. Furthermore, the use of this formulation opens up a new technological application area for statins.

A method of treating a wound may include topically administering a statin composition including a statin selected from atorvastatin, fluvastatin, lovastatin, pitavastatin, pravastatin, rosuvastatin, simvastatin, or combination thereof. The statin composition may be administered in an ointment, powder, or liquid format. The method may also include topically administering one or more antimicrobial drugs.

The present invention relates to a composition for preventing, alleviating or treating metabolic diseases, the composition comprising a rosuvastatin and ursodeoxycholic acid conjugate or a pharmaceutically acceptable salt thereof, in which the statin conjugates to an ursodeoxycholic acid transporter and has the effects of function inhibition, cholesterol level reduction, antilipid toxicity, body weight reduction, blood lipid reduction, fatty liver alleviation, inflammation alleviation, and kidney damage alleviation. The composition, in the form of a single formulation, has the characteristics of maintaining the therapeutic effects of rosuvastatin and ursodeoxycholic acid while reducing the side effects of existing statins, and thus can be widely used as a substitute for complex formulations in the treatment of metabolic diseases.

The invention belongs to the technical field of medicine. The invention particularly relates to application of statin combined with a KRAS inhibitor in preparation of a medicine for treating colorectal cancer. The invention provides a new effective strategy for treatment of the KRAS inhibitor drug-resistant colorectal cancer, namely a medication scheme of statin combined with the KRAS inhibitor, can significantly improve the treatment effect of the drug-resistant colorectal cancer, effectively inhibit the growth of tumor cells, inhibit the proliferation of tumors, and improve the treatment effect of the KRAS inhibitor drug-resistant colorectal cancer. The KRAS mutant colorectal cancer has an excellent treatment effect on the KRAS mutant colorectal cancer generating drug resistance to a first-line chemotherapy regimen, overcomes the clinical treatment difficulty caused by KRAS mutation, and has a very good application prospect.

The invention belongs to the technical field of chromatographic detection, and provides a simvastatin detection method and application thereof. According to the detection method disclosed by the invention, qualitative and quantitative detection of simvastatin in a sample can be realized by adopting a high performance liquid chromatography-tandem mass spectrometry mode. In the high performance liquid chromatography detection, the simvastatin possibly existing in the red yeast rice powder and the product thereof can be detected by combining a pentafluorophenyl propyl chromatographic column and a formic acid methanol mobile phase. The detection method provided by the invention can effectively distinguish the statins and simvastatin naturally existing in the red yeast rice powder, and can effectively avoid the false positive result of simvastatin detection; the method can also be applied to detection of various products including capsules, tablets, oral liquid and the like containing the red yeast rice powder, and various quality monitoring scenes can be considered.

The present invention concerns antibody-conjugate having general structure (2):wherein AB is an antibody capable of targeting Trop-2-expressing tumours and D is selected from the group consisting of taxanes, anthracyclines, camptothecins, epothilones, mytomycins, combretastatins, vinca alkaloids, maytansinoids, enediynes such as calicheamicins, duocarmycins, tubulysins, amatoxins, bleomycins, dolastatins and auristatins, pyrrolobenzodiazepine dimers, indolinobenzodiazepine dimers, radioisotopes, therapeutic proteins and peptides (or fragments thereof), kinase inhibitors, MEK inhibitors, KSP inhibitors, and analogues or prodrugs thereof. These antibody-conjugates exhibit an improved therapeutic index. The invention further concerns a process for preparing the antibody-conjugate according to the invention, a method for targeting Trop-2-expressing cells, medical uses of the antibody-conjugates according to the invention.

The invention discloses an efficient composite immobilized enzyme for preparing ethyl R (-)-4-cyano-3-hydroxybutyrate and a preparation method of the efficient composite immobilized enzyme, and relates to the technical field of biological catalysis. The composite immobilized enzyme comprises an active enzyme component, a Nicoordination modified mesoporous silica-chitosan composite carrier, and a sodium alginate auxiliary embedding-glutaraldehyde covalent cross-linking composite immobilization mode. The preparation method comprises the following steps: preparing a modified carrier, preparing an active enzyme mixed solution, carrying out an embedding-crosslinking reaction, collecting and drying. The compound immobilized enzyme can catalytically prepare ethyl R (-)-4-cyano-3-hydroxybutyrate, the substrate conversion rate is still kept at an extremely high level after the compound immobilized enzyme is repeatedly used for more than 15 times, and the compound immobilized enzyme is stable in enzyme activity, low in cost and suitable for industrial green production of statin drug intermediates.

Described herein are methods for reducing or preventing blood flow in a neurovascular blood vessel of a subject. The method involves injecting a composition composed of water, one or more polycationic polyelectrolytes and anionic counterions, one or more one polyanionic polyelectrolytes and cationic counterions, and a statin, an anti-cancer agent, or a combination thereof, wherein the composition has an ion concentration that is (i) sufficient to prevent association of the polycationic polyelectrolytes and the polyanionic polyelectrolytes in water and (ii) greater than the concentration of ions in the subject. Upon introduction of the composition into a subject, a solid is produced in situ. The injectable compositions have unique distal penetration properties, which make the injectable compositions described herein very useful as embolics for neurovascular blood vessels.

The invention belongs to the technical field of traditional Chinese medicines, and particularly relates to a traditional Chinese medicine composition for treating atherosclerosis and a preparation method thereof. The traditional Chinese medicine composition for treating atherosclerosis is prepared from the following raw materials in parts by weight: 20 to 40 parts of radix astragali seu hedysari, 7 to 10 parts of radix notoginseng, 10 to 20 parts of poria cocos, 5 to 15 parts of lotus leaves, 10 to 15 parts of raw fructus crataegi, 10 to 20 parts of radix salviae miltiorrhizae, 10 to 15 parts of radix angelicae sinensis and 2 to 10 parts of ramulus cinnamomi. The traditional Chinese medicine composition can intervene in the atherosclerosis process through multiple ways of adjusting the blood fat level, improving aorta pathological injury, inhibiting inflammatory response, increasing intestinal flora diversity and the like, and the comprehensive treatment effect of the traditional Chinese medicine composition is equivalent to that of clinical conventional medicine statins.

The application discloses a preparation method of high-proportion open-loop statin red koji for regulating blood fat and blood vessel plaques, and belongs to the technical field of microbial fermentation and functional food / medicine. The method takes Monascus purpureus CGMCC No. 18110 as a starting strain, and high-proportion open-loop monacolin K red koji powder is prepared by a core process of compound metabolic regulation substrate preparation + phased variable-temperature gradient oxygen supply fermentation and combined with precise post-processing technology. The total monacolin K content in the obtained red koji powder is greater than or equal to 8 mg / g, the open-loop monacolin K proportion is greater than or equal to 85%, and the citrinin content is less than or equal to 50 ppb. The red koji disclosed by the application can significantly inhibit HMG-CoA reductase activity, realize efficient blood fat regulation, and stabilize, resolve and repair blood vessel endothelium through multi-target synergistic effect, and can be widely applied to the preparation of functional food, medicinal preparations and special medical use formula food. The process has the advantages of high product proportion, high safety, strong process stability and controllable cost, solves the technical pain points of low open-loop rate, large liver and kidney burden and insufficient safety of existing red koji products, and has good industrialization prospect and market value.

The present disclosure provides pharmaceutic compositions for oral delivery comprising an antisense oligonucleotide (e.g., CIVI 008) and an oral delivery agent such as 5-CNAC. In some aspects, the disclosure provides a capsule comprising a dry blend of CIVI 008 and 5-CNAC, and optionally a statin.

The application provides a method for improving 2-deoxy-D-ribose-5-phosphate aldolase (DERA) activity through immobilization. The method can significantly activate the aldolase activity of DERA, and is simple, mild, simple and easy to operate, and can be applied to preparation of chiral side chains of statins.

This invention relates to a method for treating patients with heterozygous familial hypercholesterolemia (heFH), comprising administering a pharmaceutical composition containing a PCSK9 inhibitor to a patient with heterozygous familial hypercholesterolemia. In some embodiments, the PCSK9 inhibitor is an anti-PCSK9 antibody, such as the exemplary antibody referred to herein as mAb316P. The method of the present invention can be used to treat patients with heterozygous familial hypercholesterolemia whose cholesterol is poorly controlled with the maximum tolerated dose of statins, with or without other lipid-lowering therapy.

The invention relates to the technical field of biological detection, in particular to polypeptide, a kit and a method for detecting mouse statin. The invention provides a specific synthetic polypeptide with an amino acid sequence as shown in SEQ ID NO: 1, and the synthetic polypeptide is used as a substance with clear chemical definition and replaces natural protein which is complex in structure and difficult to preserve in a traditional double-antibody sandwich method, so that inherent inter-batch difference and quality fluctuation of a biological source standard substance are eliminated from the source. Based on the core reagent, the competitive ELISA detection system constructed by the invention achieves the technical effects of strong specificity, high accuracy and good repeatability, and meanwhile, as the synthetic polypeptide can realize low-cost and high-throughput chemical synthesis, the development period of the whole detection scheme is greatly shortened, and the economical efficiency is remarkably improved.

The present disclosure provides pharmaceutic compositions for oral delivery comprising an antisense oligonucleotide (e.g., CIVI 008) and an oral delivery agent such as 5-CNAC. In some aspects, the disclosure provides a capsule comprising a dry blend of CIVI 008 and 5-CNAC, and optionally a statin.

The present invention describes a cholesterol synthesis inhibitor alone or in association with at least another anticancer agent for use in the treatment of cancers characterized by aberrant expression of hERG1. Further the present invention describes also a kit for a simultaneous, separate or sequential use in the treatment of cancers characterized by aberrant expression of hERG1, said kit comprising a cholesterol lowering agent and at least an anticancer agent, preferably a cholesterol synthesis inhibitor, an anti-hERG1 / β1 integrin complex bispecific antibody and / or chemotherapy agent.

This disclosure provides medicaments and methods for treating envenomation using small molecule inhibitors of secretory phospholipase A2 (sPLA2). The sPLA2 inhibitor AZD2716 and related compounds can be used as monotherapy. Alternatively, the sPLA2 inhibitor varespladib and / or methyl varespladib can be used in combination with a statin. When a subject has been envenomed (for example, by a snake bite or bee sting), the medicaments can be administered to prevent lethal effects or tissues damage cause by the venom: for example, acute kidney injury, mast cell degranulation, or cerebral edema. The medicaments may be contained in an automatic injection device or an injection pen to deliver an effective dose as soon as possible following envenomation.

The invention discloses a traditional Chinese medicine combined pill for treating thrombus and carotid plaque and a preparation method, and belongs to the technical field of traditional Chinese medicines. The traditional Chinese medicine combined pill is composed of a monarch drug, a ministerial drug, an adjuvant drug and a conductant drug in parts by weight, the monarch drug comprises safflower, ligusticum wallichii and the like, the ministerial drug comprises notopterygium root, rhizoma atractylodis and the like, the adjuvant drug comprises radix paeoniae alba, radix puerariae and the like, and the conductant drug is ginkgo leaf. The preparation method comprises the following steps: weighing the medicinal materials, cleaning and airing, crushing and sieving, mixing and briquetting, and pelleting and drying. The pill follows the syndrome differentiation and treatment and holism concept of traditional Chinese medicine, the cure and rehabilitation rate reaches about 98% by reducing phlegm, clearing damp, promoting blood circulation, removing blood stasis, softening hardness, dissipating binds, activating meridians to stop pain and conditioning viscera to improve qi and blood circulation after being taken for 1-3 months, aspirin and statins medicines and operations can be replaced, side effects and operation risks are avoided, the clinical medicine vacancy is filled, and the pill is worthy of popularization and application. The medicine is suitable for treating thrombus, carotid plaque and related symptoms.

The invention discloses a benzisoselenazolone-statin bonding molecule as well as a preparation method and application of the benzisoselenazolone-statin bonding molecule. The bonding molecule is formed by chemically bonding a statin pharmacophore (3, 5-dihydroxyvaleric acid or a lactone structure thereof) and an ebbeselenium pharmacophore (benzisoselenazolone). The invention provides a plurality of synthesis paths including'first connection and then cyclization 'and'first parent nucleus construction and then coupling', and a plurality of specific compounds such as IA-6, IB-6, IIA-7, IIIB-5 and the like are efficiently prepared. In-vitro activity experiments show that the compounds can significantly reduce the content of triglyceride (TG) in hepatic cells induced by oleic acid and palmitic acid at the cellular level, the cytotoxicity is low, and the activity of part of the compounds is equivalent to that of atorvastatin. The invention provides a brand-new lead compound for developing a novel NASH treatment medicine with lipid-lowering and antioxidant / anti-inflammatory dual activities.

The invention discloses an application of a benzo-aza derivative in preparation of a medicine for preventing or treating atherosclerosis, the benzo-aza derivative is a compound with a chemical structure as shown in a formula I, or a pharmaceutically acceptable salt, a precursor or a metabolite of the compound, and in the formula I, X is halogen or H. The traditional Chinese medicine composition has the technical effects that the plaque stabilizing effect is obvious, the plaque composition is improved, the necrosis core area in the plaque is reduced, the total plaque load can be effectively reduced, the lesion progress is delayed / reversed, the dependence on lipid reduction is avoided, the treatment blank is filled, a brand new plaque stabilizing treatment strategy is provided, and the clinical problem of residual cardiovascular risks is expected to be solved. The safety is good, the organ specificity is high, and the whole body toxicity is low. The invention provides a new treatment normal form, new use of old medicines and large clinical transformation potential, and can be used as a supplement and enhancement of a basic therapy (such as statin lipid reduction) to form a combined treatment scheme of lipid reduction and spot stabilization, thereby realizing multi-channel cooperative control of atherosclerosis.

Complement is an arm of the innate immune system that plays an important role in defending the body against infectious agents. Although compositions that inhibit complement are known, there remains a need for compositions that can acutely inhibit complement. Methods and compositions comprising PEGylated compstatin analog for inhibiting complement are described.

The application discloses a traditional Chinese medicine composition with lipid-lowering efficacy, Quling Huatu granules and a preparation method thereof, and belongs to the technical field of Chinese patent medicines. The traditional Chinese medicine composition comprises the following components in parts by weight: 5-10 parts of red yeast rice, 10-30 parts of poria cocos, 5-15 parts of atractylodes, 5-15 parts of dried ginger and 5-15 parts of costus. The atractylodes, the poria cocos and the costus in the application can dispel cold, invigorate the spleen, warm the middle and harmonize the stomach, so that the qi of the spleen and stomach runs smoothly. Meanwhile, the Quling Huatu granules contain statin components, can inhibit the synthesis of excessive cholesterol in the body, increase the synthesis of low-density protein receptors, reduce the blood cholesterol and low-density protein cholesterol levels, prevent the further development of cardiovascular diseases, and also do not cause problems such as liver and kidney function damage and gastrointestinal discomfort.

The application belongs to the technical field of medicine, and particularly relates to the use of icariin in the preparation of lipid-lowering drugs with muscle protection. In view of the adverse reactions such as myalgia and myositis caused by the existing statins in the lipid-lowering process, the muscle protection effect of icariin in the lipid-lowering process is evaluated by constructing a high-fat cell model and a high-fat Caenorhabditis elegans model. It is found through research that icariin can significantly reduce the content of triglyceride, total cholesterol and lipid droplet accumulation in high-fat cells, reduce the content of triglyceride and lipid droplet accumulation in high-fat C. elegans, and prolong the lifespan of high-fat C. elegans. Further research shows that icariin can improve the muscle state of high-fat C. elegans while lowering lipid, and the specific performance is the enhancement of the movement ability of C. elegans and the maintenance of the structural integrity of body wall muscle fibers. The application discloses the unique advantage of icariin in the lipid-lowering process, that is, the muscle protection effect, and can solve the adverse reactions such as myalgia and myositis caused by the existing statins, and has an important clinical application prospect.

The invention belongs to the crossing field of bioengineering and pharmaceutical technology, and particularly relates to a heterologous expression technology of 2-deoxyribose-5-phosphate aldolase derived from rhodococcus ruber SD3 and optimization of aldol condensation reaction conditions of substrates acetaldehyde and chloroacetaldehyde catalyzed by the aldolase. The enzyme can catalyze a substrate to specifically synthesize a statin drug key intermediate (3R, 5S)-6-chloro-2, 4, 6-trideoxy pyranoside, the conversion rate can reach 44.45%, and a new biological catalysis approach and technical support are provided for efficient and green production of statin drugs. The rhodococcus ruber SD3 is preserved in the China Center for Type Culture Collection, and the preservation number of the rhodococcus ruber SD3 is CCTCC NO: M 2012035.

The invention discloses application of a statin compound in preparation of an alpha + beta 4 type BK channel agonist, and belongs to the technical field of biological medicine. Specifically, by researching the influence of the statin compound on an ion channel, it is considered that the statin compound possibly has high activation activity on a BK alpha beta 4 channel. Through comparison of activation effects of the compounds on different BK channel subtypes, high selectivity of the compounds on BK alpha beta 4 channels is found, and compared with channels such as BK alpha and BK alpha beta 1, the activation effect of the compounds on the BK alpha beta 4 channels is improved by several times or even hundreds of times. Therefore, an alpha + beta 4 type BK channel agonist, namely a statin drug, is obtained, so that a new strategy for activating a specific BK channel is provided, and a new basis is provided for adjustment of a current statin medication scheme.

The application provides an anti-TROP2 antibody-drug conjugate or a stereoisomer or a pharmaceutically acceptable salt thereof, wherein the heavy chain of the anti-TROP2 antibody comprises at least one non-natural amino acid residue as shown in formula (I). The application also provides a preparation method and uses of the antibody-drug conjugate. The anti-TROP2 antibody and auristatin toxin are conjugated at a specific site in the application, so that a brand new antibody-drug conjugate is obtained, which has very excellent biological activity and is obviously superior to existing similar products, and the preparation process is simple and easy to control.

The present invention provides an antibody-linker-drug conjugate, wherein the antibody is a salcetuzumab and the drug is an aurestatin analogue or a pharmaceutically acceptable salt thereof. The present invention also provides a method of preparing the antibody-linker-conjugate of the present invention.