25 results about "Tissue distribution" patented technology

The invention belongs to the technical field of biological medicines, and discloses a cationic polymer targeted nano material modified siRNA (small interfering ribonucleic acid) nano-drug and application thereof. The siRNA nano-drug disclosed by the invention has the capability of effectively penetrating through the blood brain barrier and improving the brain tissue distribution of the siRNA drug.

The invention discloses a lipophilic modified nucleic acid medicine composition and application thereof, the lipophilic modification is saturated or unsaturated C4-C30 alkyl, the composition comprises an absorption enhancer, and the method is that the lipophilic modified nucleic acid medicine is delivered to the brain through the nasal mucosa. Nucleic acid drugs are transmitted into the olfactory bulb region through a neural pathway, namely, cross-olfactory mucosa, bypass BBB and directly enter the brain, the drug concentration content of the olfactory bulb is far higher than that of other tissues of the brain, and the tissues except the olfactory bulb are uniformly distributed, so that the olfactory bulb can be used as a drug reservoir and gradually and slowly spread to the other tissues of the brain; the long-time drug effect can be maintained by one-time drug administration, so that the drug administration frequency can be reduced. Compared with intrathecal injection, by adopting the composition disclosed by the invention for nasal administration and using 1 / 2 of intrathecal administration dosage, the same intrathecal steady-state distribution as intrathecal distribution can be achieved, so that the method disclosed by the invention is safer, noninvasive and efficient.

The application discloses a kind of recombinant fusion protein and its application in preparation anti-gastric cancer angiogenesis drug, it is related to biological medicine technical field.The amino acid sequence of the recombinant fusion protein is as shown in SEQ ID NO.1.The amino acid sequence of gastric cancer vascular targeting peptide CNTGSPYEC is recombined with the strong vascular inhibitor Endostatin gene to construct recombinant fusion protein, using the selective distribution ability of targeting peptide, can carry anti-vascular drug Endostatin more specifically enriched in gastric cancer vascular endothelial cells, to improve anti-vascular effect and antitumor effect, simultaneously because Endostatin is reduced in normal vascular and tissue distribution, can reduce corresponding toxic side effect, it has important significance to improve gastric cancer anti-vascular treatment present situation.

The invention belongs to the technical field of medicine analysis, and particularly relates to a method for analyzing serum migration components and heart tissue distribution components of a Danshen-Shanzha herb pair (DSHP) based on a myocardial infarction disease model. The invention discloses a method for analyzing DSHP serum migration components and heart tissue distribution components in an MI model by adopting an ultra-high performance liquid chromatography-quadrupole time-of-flight mass spectrometry technology, according to the method, 22 prototype components of DSHP extracts are successfully identified in a rat body, and 10 of the prototype components are serum and heart tissue co-distribution components. The invention establishes a systematic analysis method for the medicinal components of DSHP in a pathological state, can realize comprehensive detection of DSHP serum migration components and heart tissue distribution components, and also can provide key technical support for clarification of medicinal material basis, reveal of action mechanism and establishment of quality control standard.

The invention provides a method for quantitatively detecting plant polysaccharide in a biological sample, the biological sample is plasma of a rat or tissue of the rat, the content of characteristic monosaccharide in the biological sample is quantitatively detected, and then the content of the plant polysaccharide in the biological sample is calculated according to the proportion of the characteristic monosaccharide in the plant polysaccharide. The characteristic monosaccharide comprises rhamnose and arabinose. The method provided by the invention avoids interference and structural damage introduced by an exogenous marker, and has high specificity and high sensitivity (LLOQ signal-to-noise ratio gt; 10: 1), high accuracy (the accuracy is 85-115%) and high precision (RSDlt; compared with an FITC (fluorescein isothiocyanate) labeling method, the method is proved to be successfully applied to quantitative analysis of target characteristic monosaccharide content in blood plasma and tissues of rats for intravenous injection of plant polysaccharide, and is successfully applied to in-vivo pharmacokinetics and tissue distribution research of hedysarum polybotrys polysaccharide. A key methodological tool is provided for explaining the in-vivo process and the pharmacological mechanism.

The invention discloses a screening method and application of activity and effective components of Duliang soft capsules for treating Parkinson's disease, and relates to the technical field of medicines. The method comprises the following steps: firstly, measuring the contents of nine chemical components of the Duliang soft capsule by using a high performance liquid chromatography; the method comprises the following steps: constructing an in-vitro Parkinson's disease model by utilizing MPTP to induce SH-SY5Y cell injury, determining proper modeling and administration concentrations, and screening out components with neuroprotective effects such as SENA and ISO; the research on pharmacokinetics and tissue distribution of the six chemical components in the Duliang soft capsule finds that the components are low in metabolism and distribution speed in a rat body, can penetrate through a blood brain barrier and are widely distributed in various tissues; six components contained in DL are proved to have a remarkable curative effect on PD, and the action mechanism of the six components is related to regulation and control of mitochondrial Bcl-2 and Bax cell apoptosis pathways. The screening method is comprehensive and systematic, provides an active ingredient basis for treatment of Parkinson's disease by the Duliang soft capsule, is beneficial to deep research on the treatment mechanism of the Duliang soft capsule, and promotes research and development of novel anti-Parkinson's disease drugs.

The invention provides composite particles for regulating and controlling bioavailability and tissue distribution of resveratrol and piperine and a preparation method of the composite particles, and belongs to the technical field of nutritional active ingredient delivery systems. According to the resveratrol-zein-lecithin-piperine-konjac glucomannan composite particle and the preparation method thereof, firstly, a particle core is formed through an anti-solvent coprecipitation method, then a piperine solution and a konjac glucomannan solution are sequentially injected, and the resveratrol-zein-lecithin-piperine-konjac glucomannan composite particle of a core-shell structure is formed through layer-by-layer assembly. Compared with a free form, the composite particle has the advantages that the physical and chemical stability of the resveratrol and the piperine is remarkably improved, the residence time of the resveratrol and the piperine in intestinal tracts is prolonged, and the oral bioavailability and the liver tissue enrichment capacity of the resveratrol and the piperine are effectively enhanced. The composite particle provided by the invention is clear in structure, the preparation method is simple and convenient to operate, and the composite particle has a good application prospect in functional food and drug development.

The invention belongs to the technical field of biological medicine, and relates to an intelligent cantharidin drug delivery system. According to the present invention, the cantharidin is delivered through the polymer hybrid carrier having the accurate pH response function, such that the efficient delivery of the cantharidin is achieved, the tissue distribution and the drug release performance of the cantharidin are significantly improved, especially the system can have the good lysosome escape function, and the anti-breast cancer treatment effect and the safety of the cantharidin are significantly improved.

The application discloses a use of a combination of juglone and solanum aviculare in preparation of a medicine for inducing tumor cell ferroptosis. The juglone and the solanum aviculare form a quinone-amine free radical (ESR g≈2.004) under a tumor microenvironment, and induce ferroptosis by synergistically inhibiting GPX4 and DHODH. 50 =15.8 μM, CI=0.58 (strong synergy), and the inhibition rate is 78%. The tumor / normal tissue distribution ratio is greater than 5:1. The combination can be used for treating triple-negative breast cancer.

The invention belongs to the technical field of metabonomics, and particularly relates to a detection method of rheum tanguticum tissue specific metabolites and a comprehensive development and utilization method of rheum tanguticum, the detection method comprises the following steps: grinding roots, stems, leaves and seeds of rheum tanguticum to obtain powder samples of each tissue; mixing the powder sample with the extracting solution, extracting by adopting an ultrasonic-assisted method, and standing, centrifuging and filtering the obtained extract to obtain supernate; and carrying out liquid chromatography-tandem mass spectrometry analysis on the supernate, collecting data, and screening differential metabolites in combination with multivariate statistics and metabolic pathway enrichment analysis. According to the invention, a non-targeted metabonomics technology is adopted, composition differences of metabolites in various tissues of rheum tanguticum are systematically analyzed, and tissue-specific marker metabolites are screened out. The tissue distribution rule of the secondary metabolite on the metabolome level is disclosed, and a scientific basis is provided for medicine part selection, non-medicine tissue utilization, molecular breeding and the like.

The application discloses a kind of four sulfur bond bridging dimer prodrugs and its self-assembly nanoparticles and application, belong to medical technology field.The four sulfur bond bridging dimer prodrug and its self-assembly nanoparticles are designed and synthesized, the ideal four sulfur bond is obtained by screening four sulfur bond chemical stability, and it is applied to the construction of prodrug self-assembly nanoparticles, and then the various applications in drug delivery are realized.The influence of different kinds of four sulfur bond and four sulfur bond compared with three sulfur bond and disulfide bond on the stability of prodrug self-assembly nanoparticles, drug release, pharmacokinetics and tissue distribution, and the influence of the ultimate antitumor effect in vivo and in vitro is explored, and the mechanism and effect of four sulfur bond bridging prodrug self-assembly nanoparticles drug combined with reducing substance are explored, to provide a variety of choices for developing high-efficiency low-toxicity prodrug self-assembly nanoparticles, promote the application of prodrug self-assembly nanoparticles in tumor treatment, meet the urgent needs of high-end cancer chemotherapy preparations in clinic.

A method for determining a tissue distribution phenotype of an animal or a human subject for an exogenous agent, such as a drug. The method includes administering the exogenous agent to the subject, and at one or more time points after administration, determining an amount of the exogenous agent in the interstitial fluid of a tissue of the subject. The amount of exogenous agent may be determined by an electrochemical aptamer-based sensor. The determined amount is used on its own or in conjunction with another value to determine a tissue distribution phenotype of the subject for the exogenous agent.

The use of a class of prodrugs of 2-PMPA that alter tissue distribution of 2-PMPA to non-prostate tissues is disclosed. The presently disclosed prodrugs preferentially distribute to healthy tissues including the kidney, lacrimal glands, and salivary glands, which represent sites of off-target binding and toxicity for PSMA-targeted prostate cancer imaging agents and therapies. Accordingly, the 2-PMPA prodrugs can be used to pretreat, bind to, and shield the kidney and salivary glands from PSMA-targeted cytotoxic or radiotherapy.

The invention provides an ALK5 PROTAC compound and application thereof, and belongs to the field of medicinal chemistry and biological medicine. A series of PROTAC small molecule compounds for targeted degradation of ALK5 protein are prepared, and the structures of the PROTAC small molecule compounds are as shown in a formula I in the specification. The compounds can be degraded through an ALK5 ubiquitination-proteasome pathway, and the bioavailability gt is injected in the intraperitoneal cavity; and the tissue distribution is good. The ALK5 PROTAC compound provided by the invention provides a new accurate intervention means for treating ALK5 mediated fibrosis diseases and tumors.

Disclosed in the present invention is a thyroid hormone receptor β (THR-β) agonist. The present invention provides a compound as represented by formula I, or a stereoisomer or pharmaceutically acceptable salt thereof. Compared with VK-2809, the compound provided in the present invention has significantly superior agonistic activity against THR-β than VK-2809, or in terms of in vivo organ / tissue distribution, has a liver / heart distribution ratio or plasma / heart distribution ratio superior to that of VK-2809.

The present application relates to the technical field of medicine, in particular to a polysaccharide composition, nano-polysaccharide and its preparation method and application.The polysaccharide composition comprises polysaccharide and lipid material;the weight ratio of polysaccharide to lipid material is 2-50:1.The composition disclosed in the present application can change the mode of polysaccharide and cell interaction, pharmacokinetics and tissue distribution behavior, improve the cell uptake of polysaccharide, improve the oral bioavailability, delay the clearance of polysaccharide from blood circulation, prolong the residence time in vivo, thereby significantly improving the in vitro and in vivo activity and efficacy of active polysaccharide.

The application provides an ALK5 PROTAC compound and application thereof, and belongs to the field of pharmaceutical chemistry and biological medicine. A series of PROTAC small-molecule compounds for targeted degradation of ALK5 protein are prepared, and the structure is shown as formula I. The compounds can be degraded through an ALK5 ubiquitination-proteasome pathway, the bioavailability of intraperitoneal injection is greater than 70%, and the tissue distribution is good. The ALK5 PROTAC compound provided by the application provides a new precise intervention means for treating ALK5-mediated fibrosis diseases and tumors.

This invention belongs to the field of biomedical technology and relates to a smart drug delivery system for cantharidin. This invention utilizes a polymer hybrid carrier with precise pH response to deliver cantharidin, achieving efficient delivery and significantly improving the tissue distribution and drug release properties of cantharidin. In particular, this system exhibits excellent lysosomal escape capabilities, significantly enhancing the efficacy and safety of cantharidin in treating breast cancer.

The invention discloses a coronavirus 2 '-O-methyltransferase inhibitor and an application of the coronavirus 2'-O-methyltransferase inhibitor. The inhibitor provided by the invention takes the coronavirus 2 '-O-methyltransferase as a target spot, can effectively inhibit the enzymatic activity of the coronavirus 2'-O-methyltransferase, shows a good antiviral effect on human and animal coronaviruses (including new coronaviruses and mutant strains thereof) on a cellular level, and shows good pharmacokinetic level, tissue distribution and safety in a mouse body. The inhibitor can effectively inhibit the enzymatic activity of coronavirus 2 '-O-methyltransferase, so that an efficient antiviral effect is achieved; the safety is high, and the clinical application potential is high; the method is wide in applicability and can be used for various types of coronaviruses; moreover, the oral administration utilization rate is high, the antiviral effect is good, and the application scene is greatly enriched. The application scheme also provides another thought for developing more safe, effective and broad-spectrum anti-coronavirus small molecule drugs, and has extremely high scientific research significance and practical value.

The invention belongs to the field of biological nano medicines, and particularly relates to a preparation method of water-soluble lipid nanoparticles based on combination of film dispersion and active drug loading. According to the invention, a polyethylene glycol derivative is used as a carrier skeleton, a specific targeting group is introduced to construct an intelligent delivery system, and a film dispersion method and a pH response type active drug loading technology are innovatively combined, so that the key problems of non-selective tissue distribution, narrow therapeutic window and the like of a traditional chemotherapeutic drug are effectively improved. The prepared nanoparticles have the following remarkable advantages that a tumor part is positioned through a targeting ligand-receptor recognition mechanism, the bioavailability of the medicine is effectively improved, the dosage is reduced, the toxic and side effects are reduced, and a scheme with high efficiency and safety is provided for tumor treatment through the diagnosis and treatment integrated design.

The invention belongs to the technical field of tumor diagnosis and treatment, and particularly relates to a drug delivery system loaded with a radionuclide-labeled natural polyphenol compound as well as a preparation method and application of the drug delivery system. The drug delivery system provided by the invention comprises a responsive liposome, a radionuclide-labeled natural polyphenol compound encapsulated in the responsive liposome, an unlabeled natural polyphenol compound and artificial metalloenzyme. The drug delivery system of the natural polyphenol compound loaded with the radionuclide label provided by the invention realizes specific delivery of radionuclide (131I), reduces non-specific distribution of the radionuclide, and prolongs the residence time of tumors, so that the growth of the tumors can be effectively inhibited; the drug delivery system of the natural polyphenol compound loaded with the radionuclide label can also be used for PET imaging, and tumor targeting, tumor treatment effect and drug in-vivo tissue distribution can be effectively monitored.

The invention provides a target protein of an aconitine analgesic active ingredient and application thereof, aims to overcome the defects that the toxicity of an existing aconitine medicine is difficult to reduce and an action target is limited, and provides benzoyl aconitine as an effective ingredient of an analgesic medicine, and the combination target of the benzoyl aconitine is ankle protein Talin2. Aconitine is a main analgesic active ingredient of an aconite herbal medicine, but has circulation and nervous system toxicity, through pharmacokinetic research, tissue distribution detection, target screening and verification and the like, it is determined that BAC is a main metabolite of the aconitine, the content of BAC in dorsal root ganglions is the highest, the analgesic effect is achieved, and the BAC can be used as an analgesic drug. Through Lip-sMap screening, serum proteomics analysis, molecular docking and dynamic simulation, surface plasmon resonance detection and other methods, it is determined that Talin2 is a potential binding target of BAC, it is found that the binding affinity of BAC and Talin2 is superior to that of Talin1, a new target and a theoretical basis are provided for development of safer and more effective analgesic drugs, and the application of Talin2 and Talin2 is developed. The medicine is expected to be applied to treating various pain diseases.