51 results about "Antimicrobial drug" patented technology

This invention discloses a silk fibroin-based biomimetic artificial tympanic membrane with a gradient structure and its preparation method, comprising the following steps: encapsulating and dissolving an antibacterial drug in an organic solvent and then adding it dropwise to a silk fibroin solution; casting the film and inducing the formation of a β-sheet structure with methanol to obtain an outer dense layer; electrospinning the silk fibroin solution to obtain oriented silk fibroin fiber felt, and cross-linking it in an ethanol solution to obtain an intermediate fiber layer; mixing the silk fibroin solution with a pore-forming agent and casting it onto the intermediate fiber layer; covering the intermediate fiber layer with the outer dense layer; after pre-freezing and lyophilizing, immersing the membrane in deionized water to dissolve the pore-forming agent to form an inner porous layer; then placing it in a PBS buffer containing growth factors and shaking treatment; and finally drying to obtain the silk fibroin-based biomimetic artificial tympanic membrane with a gradient structure. This invention's three-layer biomimetic artificial tympanic membrane possesses antibacterial and regenerative functions, while also exhibiting excellent mechanical properties, meeting the requirements of a biomimetic tympanic membrane.

This invention provides the application of Vibrio receptor protein type VI collagen α2 from the tongue sole as a target protein for blocking Vibrio pathogen adhesion and infection of tongue sole cells, providing an important foundation for the research and development of strategies and disease control technologies for the prevention and treatment of vibrio infections in tongue sole. This invention discovers that tongue sole type VI collagen α2 can mediate the binding of various Vibrio pathogens to tongue sole, and can serve as a candidate protein for blocking Vibrio adhesion and infection of tongue sole cells, thus providing a new strategy for the prevention and treatment of vibrio diseases in tongue sole. This invention also provides a new approach for the development of novel antibacterial drugs, which has application value in the prevention and treatment of tongue sole diseases.

The invention discloses a perfluoroalkyl-substituted pyrimido [1, 2-b] indazole ketone compound and a preparation method thereof, and belongs to the technical field of compounds containing two or more heterocyclic rings. Comprising the following steps: with enaminone, a perfluoroalkane compound and aminoindazole as raw materials, carrying out a reaction under blue light irradiation in the presence of an organic solvent and alkali to prepare the perfluoroalkyl-substituted pyrimido [1, 2-b] indazole ketone compound; according to the invention, through visible light mediated dehalogenation and cyclization free radical addition, high-yield synthesis of the perfluoroalkyl substituted pyrimido [1, 2-b] indazole ketone compound is realized; the prepared perfluoroalkyl-substituted pyrimido [1, 2-b] indazolone compound has excellent antibacterial activity, can be used for preparing antibacterial drugs, and has outstanding industrial application value.

This invention belongs to the field of antimicrobial peptide technology, and particularly relates to a broad-spectrum antimicrobial peptide with low hemolytic activity and its applications, as well as a broad-spectrum antibacterial drug. The antimicrobial peptide is named AY6, and its amino acid sequence is shown in SEQ ID NO.1. Antimicrobial peptide AY6 exhibits significant antibacterial effects against both Gram-positive and Gram-negative bacteria, with a bactericidal rate far exceeding that of traditional antibiotics, enabling highly effective responses to bacterial infections. AY6 has low hemolytic activity and good biocompatibility, making it suitable for medical anti-infective applications. The antimicrobial peptide provided in this application has a short sequence, is easy to synthesize chemically, can save on large-scale production costs, and has broad application prospects.

The application discloses application of antibacterial peptide BMAP-28 and antibiotics in combined preparation of antibacterial drugs and belongs to the technical field of biological medicine. The antibiotics are selected from one or more of the following: ciprofloxacin, gentamicin and cefixime. The application combines the antibacterial peptide BMAP-28 with antibiotics such as ciprofloxacin and gentamicin, finds that the combination has a significant synergistic antibacterial effect on Enterobacter sakazii, can greatly save the dosage of the drug, reduce the toxic side effect and block the evolution process of drug resistance. Through the destruction of the bacterial cell membrane and the assistance of the antibiotic effect, the combination can effectively overcome the multiple drug resistance, widen the antibacterial spectrum and has a wide clinical application prospect.

The application belongs to the technical field of pharmaceutical chemistry, and particularly relates to a pyrimidine and thienopyrimidine derivative, a preparation method and application thereof. The pyrimidine derivative in the application is a compound with the structure of formula I, and the thienopyrimidine derivative is a compound with the structure of formula II. The pyrimidine and thienopyrimidine derivative can be used as an AcrB efflux pump inhibitor, and can significantly enhance the antibacterial activity when combined with an antibacterial drug. The Nile red experiment shows that the compound 64c can completely inhibit the AcrB-mediated efflux at a concentration of 50 μM, and the effect is better than that of the positive control PA beta N. The compound in the application has novel structure and excellent activity, and can be used for preparing an AcrB efflux pump inhibitor for reversing bacterial drug resistance and an antibacterial sensitizing drug.

This invention discloses an antimicrobial peptide SI-20 and its application in the preparation of antimicrobial drugs, belonging to the field of biomedical technology. The amino acid sequence of the antimicrobial peptide SI-20 is shown in SEQ ID NO.2. The antimicrobial peptide SI-20 provided by this invention has a highly efficient killing ability against a variety of Gram-negative / positive bacteria, effectively retaining antimicrobial activity while significantly reducing cytotoxicity and improving therapeutic efficacy. Simultaneously, this antimicrobial peptide SI-20 exhibits good stability in serum environments and under heat treatment, strongly inhibits biofilm formation, and possesses rapid and efficient antimicrobial properties, providing a highly promising candidate resource for the development of highly effective and low-toxicity antimicrobial drugs, with broad application potential.

The invention discloses a parameterized constraint system and method for efflux pump avoidance and off-target risk inhibition, which are applied to the field of biological medicines, and aims to solve the dual problem that toxic risks are caused by efflux pump mediated drug resistance enhancement and off-target combination of existing antibacterial drugs. The method comprises the following steps: constructing an efflux pump identification avoidance five-dimensional feature space and a target spot specificity geometric-electrical constraint boundary, performing structure mapping and deviation degree evaluation on candidate molecules, and triggering directional modification; the target matching is verified through molecular docking, and if the target does not reach the standard, the pharmacophore is locally adjusted; virtual screening is carried out based on an off-target protein database, a secondary structure disturbance mechanism is started for high-risk molecules, and a stereoisomerism or electrical reversal group is introduced to destroy non-target binding; according to the method, collaborative optimization of antibacterial efficacy, drug resistance avoidance and safety risk is achieved, and the research and development efficiency and druggability of candidate molecules are remarkably improved.

The application discloses application of tegaserod maleate in preparation of an antibacterial drug synergist, and proves that the tegaserod maleate can produce a synergistic antibacterial effect with a plurality of commonly used antibacterial drugs (including tylosin, tetracycline, enrofloxacin, ampicillin and the like), can significantly enhance the antibacterial activity of the antibacterial drugs on gram-negative bacteria, and reduce the drug resistance of bacteria to the antibacterial drugs; the antibacterial composition composed of the tegaserod maleate and the antibacterial drugs can be used for preparing a drug for treating escherichia coli infection, and the synergistic antibacterial mechanism is mainly to destroy the inner and outer membrane permeability of bacteria, regulate the proton motive force of bacteria, inhibit the activity of bacterial efflux pumps, interfere with the energy metabolism homeostasis of bacteria and induce the bacteria to produce oxidative stress. The application provides a new technical strategy for the treatment of clinical escherichia coli infection, and has important clinical application value and industrialization potential.

The application discloses a D-amino acid modified pillararene compound and a preparation method and application thereof. The D-amino acid modified pillararene delivers D-amino acids to a biological membrane or cells by using pillararene as a carrier, exhibits synergistic activity of anti-biofilm and antibacterial, and is expected to be used for developing a novel anti-biofilm agent and an antibacterial drug. The compound can not only efficiently inhibit the growth of a bacterial biofilm, but also can be used in combination with an antibiotic to enhance antibacterial activity, and provides a new strategy for coping with biofilm-related infections and drug resistance.

The application discloses application of bio-organic acid in preparation of plasmid conjugation transfer inhibitor and / or antibacterial drugs. The bio-organic acid in the application includes one or more of citric acid, fumaric acid or alpha-ketoglutaric acid. The application finds the possibility of the bio-organic acid as the conjugation transfer inhibitor in preventing and controlling the spread of antibiotic resistance level through in-vivo and in-vitro conjugation tests. The application provides the use of the bio-organic acid as the conjugation transfer inhibitor, limits the conjugation transfer of various clinical drug-resistant plasmids, and is one of strategies for solving the problem of bacterial drug resistance.

The application belongs to the field of microbiology and veterinary microbiological technology, and relates to a strain of enterotoxigenic Escherichia coli carrying F5 and F41 fimbriae and application thereof. The strain is isolated from a fecal sample of a diarrheal calf, and is confirmed to be enterotoxigenic Escherichia coli carrying F5 fimbriae-related genes, F41 fimbriae-related genes and ST enterotoxin estA gene through isolation and culture, morphological identification, biochemical identification, fimbriae gene and virulence gene PCR detection and whole genome sequencing analysis. The strain has been preserved in the China General Microbiological Culture Collection Center on June 13, 2022, and the preservation number is CGMCC No. 25077. Pathogenicity tests show that the strain has strong virulence and can stably establish an animal infection model. Drug sensitivity tests show that the strain has a specific sensitivity spectrum to a variety of antibacterial drugs. The strain can be used for animal infection model establishment, antibacterial drug evaluation, calf diarrhea pathogenesis research, prevention and control technology research, and can also be used for preparing biological agents for preventing or diagnosing calf diarrhea.

The application discloses a truncated pleuromutilin oxazolopyridinium salt derivative having allosteric regulation on a bacterial peptide transferase center, a preparation method and application thereof, and belongs to the field of medicinal chemistry. 14 The truncated pleuromutilin oxazolopyridinium salt derivative is successfully prepared by modifying the structure of pleuromutilin C and then modifying the structure of pleuromutilin C by using a bromomethyl aromatic compound. In-vitro antibacterial activity determination proves that the compound has good in-vitro antibacterial activity and strong mycoplasma inhibiting activity, and has good antibacterial activity on pathogenic microorganisms. Meanwhile, the compound can combine with a novel allosteric pocket on a pathogenic microorganism related target, induce conformation remodeling and expansion of a neighboring active pocket, promote further occupation of the compound on the active pocket, and improve the antibacterial activity. Therefore, the compound can improve the poor solubility problem of the truncated pleuromutilin derivative, and can be developed and applied as a potential antibacterial drug.

This invention relates to the field of biomedical data processing technology, specifically to a stratification system for sepsis-related secondary invasive fungal infections based on laboratory data. The invention obtains the degree of static intestinal baseline damage by considering serum lactate concentrations at different historical testing times, temporal characteristics, and a preset maximum backtracking period; it obtains the cumulative dosage of antimicrobial drugs and the hourly cumulative distribution value of drug use based on the drug dosage distribution at different medication times within a neighborhood of the real-time trigger time; it obtains the overall degree of inflammation reduction and the hourly cumulative distribution value of inflammation regression based on the procalcitonin concentration distribution at testing times within a neighborhood; and it further obtains the net drug-induced intervention level. Based on the degree of static intestinal baseline damage and the net drug-induced intervention level, the fungal infection characteristics are stratified. This invention, by considering non-drug-induced interference, accurately obtains the comprehensive risk level of fungal infection, improving the effectiveness of fungal infection stratification.

The application provides a preparation of gramicidin and an antibacterial hydrogel preparation of the gramicidin, and discloses medical uses of the gramicidin, and provides a recombinant gramicidin, heterologous expression of the gramicidin is realized by constructing a Pichia pastoris recombinant strain, and the antibacterial activity of the gramicidin is retained, and the method has the advantages of simplicity and rapidness. Meanwhile, the hydrogel preparation of the gramicidin provided by the application shows good potential for treating wound infection of a diabetic mouse, and has the performance of rapid adhesion and hemostasis, lays a foundation for development of a new antibacterial drug, and provides a new direction for treatment of chronic inflammatory wounds and open bleeding.

This invention provides an artificial intelligence-based method for screening antimicrobial drug molecules and its applications, specifically relating to the field of drug screening technology. The method constructs a hierarchical virtual screening system. First, it performs two-stage screening using an affinity prediction model and molecular docking tools, and then constructs the affinity prediction model through machine learning. Subsequently, it integrates drug-likeness assessments such as water solubility and toxicity, as well as molecular similarity calculations, to reduce the probability of obtaining low-drug-likeness drug molecules or potentially cross-resistant molecules, filtering candidate molecules hierarchically. Finally, it verifies antimicrobial activity. This invention solves the problems of low efficiency and system scarcity in screening hundreds of millions of molecules by integrating deep learning with traditional computational methods. While improving screening accuracy, it introduces drug resistance risk screening, effectively reducing research components and shortening the cycle, providing high-quality candidate molecules for the clinical translation of anti-drug-resistant drugs, and has significant clinical translational value and application prospects.

The invention relates to the field of biomedicine, and provides an application of a Gram-negative bacterium infection target Kdo in research and development of antibacterial drugs. An authorized antibacterial peptide Ly (PEG)-1 is used as a probe; through computer simulation, affinity determination and gene defect strain identification, the key action target is lipopolysaccharide (LPS) internal core Kdo (3-deoxy-D-mannan-octanone acid), Kdo is used as a key component of bacteria LPS and is a basis for maintaining Gram-negative bacteria cell wall integrity, LPS biosynthesis and biological activity exertion, and the Kdo is used as a key component of bacteria LPS. The deletion or modification can directly cause the loss of LPS function and the reduction of the viability of bacteria. At present, no antibacterial drug aiming at the target spot exists, the problem that in the prior art, no biomolecule capable of targeting Kdo to exert strong antibacterial activity exists is solved, and the biomolecule can be used for developing drugs for diagnosing or treating related diseases.

This invention discloses an antimicrobial peptide LR-24 and its application in the preparation of antimicrobial drugs, belonging to the field of biomedical technology. The amino acid sequence of the antimicrobial peptide LR-24 is shown in SEQ ID NO.2. The antimicrobial peptide LR-24 provided by this invention has a highly efficient killing ability against a variety of Gram-negative / positive bacteria and exhibits broad-spectrum stability. It maintains strong antimicrobial activity under conditions of salt ions, 50% serum, proteases, and high temperatures, improving the problem that the activity of antimicrobial peptides decreases in some complex environments. Furthermore, while maintaining antimicrobial activity, the antimicrobial peptide LR-24 shows significantly reduced hemolytic activity and cytotoxicity, making it a promising candidate for novel antimicrobial drugs with great clinical application potential.

This invention discloses an antimicrobial peptide RY-10 and its application in the preparation of antimicrobial drugs, belonging to the field of biomedical technology. The amino acid sequence of the antimicrobial peptide RY-10 is shown in SEQ ID NO.2. The antimicrobial peptide RY-10 provided by this invention has a highly efficient killing ability against a variety of Gram-negative / positive bacteria, effectively retaining antimicrobial activity while significantly reducing cytotoxicity. Simultaneously, this antimicrobial peptide RY-10 can also produce synergistic antimicrobial effects with various antibiotics, showing significant application value in improving efficacy, overcoming antibiotic resistance, reducing drug dosage, delaying the development of drug resistance, and addressing complex infections. This invention provides a highly promising candidate material resource for the development of highly effective and low-toxicity antimicrobial drugs, and also provides an efficient, safe, and sustainable solution for developing novel combination therapies and addressing the global drug resistance crisis, possessing significant clinical application value and industrialization potential.

This invention discloses a multifunctional Schiff base-photocrosslinked drug-loaded hydrogel. The hydrogel comprises Dendrobium officinale polysaccharide (ODop), gelatin-hydroxyphenylpropionic acid (Gtn-HPA), an amino-containing antibacterial drug, a photocrosslinking agent, and an oxidizing agent. Specifically, Dendrobium officinale polysaccharide (ODop) undergoes Schiff base crosslinking with the amino-containing antibacterial drug and gelatin-hydroxyphenylpropionic acid (Gtn-HPA). Gtn-HPA itself undergoes photocrosslinking to enhance mechanical strength. Under acidic pH conditions, the Schiff base crosslinking hydrolyzes, releasing the amino-containing antibacterial drug from the hydrogel. The hydrogel prepared by this invention exhibits excellent mechanical properties, controlled drug release capability, and superior bioactivity.

The application belongs to the field of natural product chemistry and medicinal chemistry, and discloses 10,11-dehydrovariecolin cinnamic acid derivatives, a preparation method and purposes thereof. The preparation method takes 10,11-dehydrovariecolin from a fungus as a starting material, and the target derivative is prepared by esterification reaction of the 5-position hydroxyl group of the starting material with cinnamic acid. The series of compounds show good bacteriostatic activity and antitumor activity, and can be used for preparing antitumor drugs or antibacterial drugs.

This invention discloses the application of the QseC inhibitor ferrugin in the preparation of anti-Klebsiella pneumoniae products. Compared with existing technologies, this invention demonstrates that QseC can serve as a drug target against Klebsiella pneumoniae, and ferrugin can bind to QseC, effectively inhibiting the QseC protein. Therefore, ferrugin can act as a QseC inhibitor, effectively inhibiting Klebsiella pneumoniae. This compound possesses the advantages of low toxicity, safety, and significant antibacterial effect, providing solid theoretical support and candidate compounds for the subsequent development of novel targeted antibacterial drugs against Klebsiella pneumoniae, and also offering new ideas for the development of antibiotic alternatives to combat bacterial resistance.

This invention discloses a cell membrane-modified inflammatory-responsive release nanoparticle, its preparation method, and its applications. The nanoparticles use a polylactic-co-glycolic acid (PLA) core, and their surface is modified with an immune cell membrane. The PLA is loaded with an antibacterial drug and modified with a positively charged material and a responsive switch. The immune cell membrane is obtained by isolating immune cells pre-stimulated by pathogens. The nanoparticles prepared by this invention possess the function of rapidly releasing drugs targeting homologous bacteria and sites of inflammation. During systemic circulation, they tend to target sites of inflammation caused by bacterial infection, rapidly releasing the drug under the action of the highly expressed MMP-3 enzyme at the site of inflammation, achieving efficient delivery of antibacterial drugs. This invention has shown good therapeutic effects in a mouse model of bacterial infection, providing not only an effective means for the in vivo delivery of cationic antimicrobial peptides but also a promising therapeutic strategy against Gram-negative bacterial infections.

The application provides a kind of base hornet MP-B peptide site-directed mutation derivative antibacterial peptide and its preparation method and application, belong to biotechnology field, the sequence of antibacterial peptide is as shown in SEQ ID No.1.The application uses base hornet MP-B peptide as template, respectively, the serine of 5, 8 is replaced by threonine, the amino acid sequence formed as shown in SEQ ID No.1, and the C-terminal is acylated with-NH2, is synthesized by solid phase chemistry, and after reversed-phase high performance liquid chromatography purification and mass spectrometry identification, the preparation of the antibacterial peptide is completed, the application of the antibacterial peptide in preparing antibacterial drug for treating gram-negative bacteria and / or gram-positive bacteria and / or fungal infectious diseases is disclosed.The antibacterial peptide of the application has the characteristics of high activity, low toxicity and high stability, and has the application potential of becoming a high-efficiency antibiotic substitute.

This invention relates to the pharmaceutical field, specifically to a catechol compound containing formula (I) or formula (II) and its application in the preparation of bacterial biofilm inhibitors. The catechol compounds involved in this invention have been validated in vitro, and most of the obtained compounds exhibit excellent bacterial biofilm inhibitory activity. They can be used to prepare anti-biofilm agents and have the potential to be developed into novel antibacterial drugs.

This invention belongs to the field of bioengineering technology and relates to marine-derived antimicrobial peptide FP2664 and its use in preparing skin antimicrobial drugs. The amino acid sequence of the antimicrobial peptide FP2664 is shown in SEQ ID NO.1. This antimicrobial peptide FP2664 is derived from marine bacteria of the genus *Cordia*. Cordia This invention also provides the DNA molecule encoding the antimicrobial peptide, the recombinant expression vector, and the engineered strain, achieving efficient heterologous expression of FP2664 in vitro. Experimental verification shows that the antimicrobial peptide exhibits good stability under the tested conditions, has a stable spatial structure and possesses environmental adaptability unique to marine microorganisms, while also demonstrating highly efficient nucleic acid (DNA / RNA) binding activity and broad-spectrum antimicrobial activity, showing significant industrial application prospects in the fields of medicine, food, and environmental remediation.

This invention discloses a sulfonylpyridinone compound, its preparation method, and its applications. The compound is prepared by introducing a sulfonyl group at the 4-position of pyridazin-3(2H)one, giving it multiple functional groups such as sulfone, phenyl, and pyridazinone. The sulfonylpyridinone compound of this invention exhibits a certain antibacterial effect against *Escherichia coli* / *Staphylococcus aureus* and can be used to prepare broad-spectrum antibacterial drugs. Due to its multifunctional nature involving flame retardant groups, this compound is expected to be applied in the flame retardant field. This invention also provides a method for preparing the above-mentioned sulfonylpyridinone compound, achieved through a dehalogenation sulfonation reaction of 4,5-dihalo-2-phenylpyridazin-3(2H)one with sulfonylhydrazine. This reaction process not only avoids transition metal catalysis and the addition of oxidizing or reducing agents, but also features a simple reaction system, a wide range of applicable substrates, and a high yield, which is beneficial for industrial production.

The present invention relates to the field of therapeutics and, more in particular, to pharmaceutical compositions for the prevention and / or treatment of bacterial infections and antibacterial-induced dysfunctions. The compositions of the present invention demonstrate high species-specificity in inhibiting the growth of a small number of bacterial species, and most importantly are effective also against multi drug resistant (MDR) clinical isolate species. Interestingly, one of those combinations pairs a non-antibiotic drug, vanillin, with an antibiotic drug, spectinomycin, to demonstrate a surprisingly strong inhibitory effect on the growth of clinically relevant Gram-negative pathogenic and multi-drug resistant E. coli isolates. A second set of compounds combines the polymyxin colistin with loperamide, a rifamycin, or a macrolide. Importantly, this invention relates to combinations that enable narrow-spectrum antibacterial therapies, constituting a major effort of current and future drug development efforts in order to prevent major side effects of antibacterial strategies. This invention also relates to pharmaceutical combinations useful to prevent an adverse effect on the gut microbiome, induced by the use of antibacterial compounds.

To provide a novel antimicrobial product that enables the management of animal diseases while reducing reliance on conventional antibiotics. [Solution] The present invention relates to an antimicrobial composition comprising an extract of a coffee composition and an antibiotic, and to the use of the antimicrobial composition in the manufacture of antimicrobial drugs. The extract of the coffee composition comprises a solid component and water, the solid component comprising coffee beans and auxiliary materials. The antibiotic is selected from the group consisting of penicillin antibiotics, cephalosporin antibiotics, fluoroquinolone antibiotics, tetracycline antibiotics, chloramphenicol antibiotics, aminoglycoside antibiotics and combinations thereof, and the weight ratio of the coffee composition to the antibiotic is from 1.5:1 to 25000:1. The antimicrobial composition of the present invention can exhibit a superior antibacterial effect compared to the use of antibiotics alone, and this antibacterial effect can also be exerted against drug-resistant bacteria.