13 results about "Biological evaluation" patented technology

The present invention describes the synthesis and biological evaluation of new substituted pyridine derivatives as foxj1 activity enhancers. In embodiments, novel pyridine derivatives were synthesized and the ability thereof to enhance foxj1 activity was evaluated. The novel pyridine derivatives synthesized in the present invention not only exhibited excellent activity but also exhibited excellent metabolic safety and pharmacokinetic profile in a Tg (foxj1: egfp) transgenic zebrafish animal model. In addition, the novel pyridine derivatives synthesized in the present invention enhanced cilia-promoting capability in a motile ciliated cell differentiation experiment in which mouse tracheal epithelial cells (mTECs) were isolated from the airways of mice and cultured by ALI. As a result, a series of foxj1 activity enhancers with substituted pyridine skeleton has the potential to be developed as preventive and therapeutic agents for respiratory diseases.

The application discloses a rat fixing device based on biological evaluation of medical instruments. The device comprises an operation panel, a fixing cover, a sliding sheet and a sliding groove. A rectangular opening is designed in the center of the base of the operation panel, which is specially used for abdominal cavity injection operation of rats. The rat fixing cover is divided into four sections and is arranged on the operation panel. The two sides of the fixing cover are provided with the sliding sheets. The shape of the two sliding sheets after being spliced together is the same as that of the fixing cover. The lower end of the sliding sheet is in contact with the operation panel, and the sliding groove is arranged at the contact part. The rat fixing device can effectively adjust the size, so that rats with different body types can be effectively fixed, and the smooth operation of the test is ensured. The device is convenient to operate and stable in rat fixing.

This invention belongs to the field of biomedical materials technology, specifically disclosing a core-shell microneedle, a core-shell microneedle patch, its preparation method, and its application. Through structural design and carrier material optimization, this invention provides a core-shell microneedle with a programmed sequential release of tannic acid in the outer shell and verteporfen in the core layer, successfully matching the dynamic physiological rhythm of wound healing and ensuring effective wound repair. In vitro and in vivo biological evaluations have confirmed that the core-shell microneedle patch prepared using the core-shell microneedles of this invention possesses excellent antibacterial, antioxidant, and immune microenvironment-regulating abilities. It can effectively induce macrophage polarization towards the M2 type, specifically inhibit YAP protein expression, and significantly accelerate the closure process of infected wounds. From both upstream immune regulation and downstream fibrosis inhibition levels, it dually blocks the pathological scar formation pathway, ultimately achieving high-quality, scar-free regenerative repair of infected wounds.

The application discloses a furan amide compound and application thereof, and belongs to the technical field of medicines.The structural general formula of the furan amide compound is shown as formula (I).The application provides a novel furan amide AR antagonist, the compound and the derivative thereof have obvious antagonistic activity on an androgen receptor, and exhibit good biological activity in in-vivo and in-vitro biological evaluation, the androgen receptor antagonistic activity is better than that of enzalutamide, the compound is effective in an AR F877L / T878A double-point mutant cell model resistant to enzalutamide, the activity is better than that of darolutamide, and the compound has good safety.Therefore, the compound can be applied to the treatment of diseases related to the androgen receptor as an androgen receptor antagonist, including but not limited to the treatment of prostate cancer, breast cancer, ovarian cancer and the like.

The application discloses a kind of PROTAC molecules with crizotinib as target head, preparation method and application, belong to the field of biological medicine;Preparation method includes: chloro carboxylic acid, thionyl chloride and anhydrous DMF are mixed, after heating reflux reaction, remove thionyl chloride, obtain acyl chloride;Pomalidomide, acyl chloride, organic solvent are mixed and reacted, then filtered to obtain intermediate M;Intermediate M, crizotinib, Na2CO3 are mixed and reacted, then filtered to obtain the PROTAC molecule with crizotinib as target head.The in vitro biological evaluation shows that the new PROTAC molecule can efficiently and selectively induce ubiquitination and degradation of target protein, and exhibits significant antiproliferative activity in drug-resistant tumor cell models and animal models;The application proves that the PROTAC molecule has great potential in overcoming drug resistance of traditional inhibitors, and provides a promising lead compound for developing new therapies for treating refractory diseases such as cancer.

The invention belongs to the technical field of medicinal chemistry, and discloses a 7-oxabicyclo [2.2. 1] heptane-2, 3-dicarboxylic acid derivative and an application of the 7-oxabicyclo [2.2. 1] heptane-2, 3-dicarboxylic acid derivative in preparation of a protein phosphatase 5 degradation agent. The compound can directly target PP5 and induce the PP5 to degrade, has the advantages of novel structure and excellent physical and chemical properties, and shows high selectivity to PP5. In various biological evaluations, the molecules all show remarkable anti-proliferative activity and degradation effect.

The invention discloses a pH-responsive drug delivery agent based on a copper-based metal organic framework as well as a preparation method and application thereof, and belongs to the technical field of biomedical materials. The delivery agent is prepared by taking MOF-199 as a carrier and loading an anti-cancer drug 5-fluorouracil (5-Flu) through an in-situ stirring method. The preparation method is simple, and the drug loading efficiency is high. The delivery system realizes intelligent drug release by using the acidic characteristic of a tumor microenvironment: under the simulated tumor acidic condition of pH 5.0, the cumulative drug release rate within 50 hours reaches 74.64%, which is significantly improved compared with a neutral environment (pH 7.4); the release mechanism of the compound is derived from acid-triggered Cu-O bond hydrolysis and phosphate radical competitive coordination. Biological evaluation shows that the drug carrier has higher than 80% of high biocompatibility for normal cells (Raw264.7), and has a remarkable inhibition effect on proliferation of meibomian adenocarcinoma cells (SCG) at the same time. The invention provides a new strategy for developing an anti-cancer drug delivery system with strong targeting property and high safety.

This invention belongs to the field of pharmaceutical technology, specifically relating to a tetravalent platinum complex based on cinnamic acid, its preparation method, and its application. This invention is the first to introduce a cinnamic acid group into the structure of a tetravalent platinum complex, designing and synthesizing a series of novel platinum-based anticancer prodrugs, namely cinnamic acid-platinum (IV) complexes. Biological evaluation shows that these complexes exhibit stronger anticancer activity than classic divalent platinum drugs and good selectivity for cancer cells, demonstrating the potential of highly effective, low-toxicity, and drug-resistant novel anticancer drugs.

The present disclosure provides technologies for predicting a phenotype of a microbial cell using machine learning models trained using high-content imaging data (HCI). Also provided are methods of engineering a microbial cell to possess a phenotype of interest. Example phenotypes include the production of a target compound or biomolecule of interest. The provided technologies are useful for the efficient biomanufacturing of target compounds.

The utility model belongs to the field of sample analysis, and provides a multi-source mass spectrum sample testing system which comprises an online pretreatment unit, a dynamic biological evaluation unit and a multi-source chromatography-mass spectrum analysis unit, the online pretreatment unit comprises at least two parallel extraction branches, and all the extraction branches are connected with the high-speed counter-current chromatograph through a first switching valve; the high-speed counter-current chromatograph is respectively connected with the dynamic biological evaluation unit and the multi-source chromatography-mass spectrometry analysis unit through a second switching valve; the dynamic biological evaluation unit comprises a multi-channel injection pump module, a micro-fluidic chip / organ chip cell culture module and a micro solid-phase extraction module; the input end of the multi-channel injection pump module is respectively connected with the high-speed counter-current chromatograph and the cell culture fluid vessel, and the output end of the multi-channel injection pump module is connected with the micro-fluidic chip / organ chip cell culture module; the input end of the micro solid-phase extraction module is connected with the micro-fluidic chip / organ chip cell culture module, and the output end of the micro solid-phase extraction module is connected with the multi-source chromatography-mass spectrometry unit.

The invention discloses a thermoplastic polyurethane (TPU) film for a creep-resistant hemostasis pressurizing belt and a preparation method thereof and the hemostasis pressurizing belt, the TPU film for the creep-resistant hemostasis pressurizing belt provided by the invention is prepared from the following raw materials in parts by mass: 80-95 parts of polyester type TPU resin; 5 to 20 parts of a creep-resistant reinforcing auxiliary agent; wherein the creep-resistant reinforcing auxiliary agent is prepared from the following components in parts by mass: 50 to 80 parts of polyester type TPU (Thermoplastic Polyurethane) resin, 20 to 40 parts of nano reinforcing agent, 0.5 to 1.5 parts of antioxidant and 0.5 to 2 parts of lubricating agent. The prepared TPU film for the creep-resistant hemostasis pressurizing belt has good creep resistance, and the creep deformation rate within 24 hours is 10% or below; good mechanical properties are achieved, the tensile strength is larger than or equal to 40 MPa, and the elongation at break is larger than or equal to 400%; good biological safety: the biological evaluation requirements of medical instruments are met; industrialization feasibility: the process is simple and suitable for large-scale production.

The invention discloses a system for evaluating spleen deficiency and phlegm stasis syndromes of diabetic nephropathy based on combined detection of basophilic granulocytes and total bilirubin and application, and belongs to the technical field of biology. A ZDF (fa / fa) rat model is used, BASO% and TBIL levels are quantitatively detected, a modernization biology evaluation system capable of simultaneously reflecting DKD'spleen deficiency 'and'phlegm stasis' core pathogenesis is provided for the first time, and the technical problem that objective and quantitative traditional Chinese medicine syndrome evaluation indexes are lacked in the existing DKD model research field is solved. The method specifically comprises the following steps: associating two indexes belonging to an immune system and a metabolic system for the first time to form a brand-new collaborative evaluation combination, and overcoming the limitation of single index evaluation; a quantifiable and repeatable operation method is provided, and a key tool is provided for traditional Chinese medicine mechanism research and new drug research and development of DKD; traditional Chinese medicine syndromes and modern medical indexes are organically combined, and modernization and internationalization development of traditional Chinese medicine is promoted.