42 results about "Mic values" patented technology

The invention relates to Mulin acetate containing substituted squaric acid and an application thereof which belong to the technical field of medicines, specifically to substituted squaric acid containing Mulin acetate as shown in a general formula (I), pharmaceutically acceptable salt, a hydrate and an isomer thereof, wherein R1, R2, R3, R4, R5 and B are defined in the specification. The invention also relates to a preparation method of these compounds, a pharmaceutical composition containing these compounds and an application of these compounds in the preparation of drugs for treating or preventing bacteria and virus. As for staphylococcus aureus and Streptococcus equin MIC value, the compounds have an antibacterial effect 15-20 times higher than a control commercially-available antibiotic tiamulin in the test. And the compounds provided by the invention are effective antimicrobial agents. And the compounds provided by the invention are effective antimicrobial agents.

The invention relates to a Chinese medicinal extractum and an extraction process thereof. The Chinese medicinal extractum comprises the following components: lightyellow sophora root, glabrous greenbrier rhizome and cortex dictamni, wherein the mass ratio of the three components is 1-6:1-6:1-3. The preparation process is characterized by comprising the following steps: grinding the raw materials of lightyellow sophora root, glabrous greenbrier rhizome and cortex dictamni into fine powders; putting the fine powders into 50 to 95 percent ethanol to carry out reflux extraction for 1 to 3 hours at a temperature of between 75 and 95 DEG C, wherein the ratio of the raw materials to ethanol is 1:10-20 (weight / volume); carrying out filtration on the obtained product after extraction; putting the powders obtained by filtration into the ethanol repeatedly to extract 1 to 2 times again; after mixing the medical solution extracted repeatedly, carrying out pressure reduction and concentration on the mixture, and carrying out low-temperature vacuum drying on the obtained product to obtain the Chinese medicinal extractum. The process is simple, has short time consumption and high yield, and is convenient for the industrial production. The yield of the Chinese medicinal extractum is over 26 percent. Bacteriostasis test shows that the MIC value of the Chinese medicinal extractum to Candida albicans is 0.195mg / ml, the MBC value of the Chinese medicinal extractum to Candida albicans is 0.78mg / ml, and the Chinese medicinal extractum has obvious effect of inhibiting and killing Candida albicans.

A new class of imidazolines as 4-position acids or esters with very potent anti-inflammatory as well as antimicrobial activity is described. The synthesis of these imidazolines includes a multicomponent reaction applicable to a combinatorial synthetic approach. The combination of these two key characteristics provides an effective therapeutic drug in the treatment of septic shock as well as many other inflammatory (arthritis and asthma) and infectious disorders. The use of this novel class of non-steroidal agents as anti-inflammatory agents (for the treatment of asthma etc.), antibacterial agents and antiseptic agents is described. The compounds are also useful in the treatment of tumors (such as cancers). The imidazolines are potent inhibitors of the transcription factor NF-κB as well as potent activity against the Gram (+) bacterium B. subtillus and B. cereus with MIC values in the range of 50 μm / mL.

Three new alkaloids, Hirsutellones A, B, and C, are produced in cultures of fungus such as Hirsutella nivea strain BCC 2594 and Trichoderma sp. strain BCC 7579. The Hirsutellones exhibited potent growth inhibitory activity against Mycobacterium tuberculosis (H37Ra strain) with an MIC value of 0.78 μg / ml, while showing weak or no cytotoxicity to mammalian cells. Therefore, Hirsutellones and pharmaceutical compositions containing Hirsutellones may be useful for the treatment of tuberculosis. Also described herein are methods of isolating the Hirsutellones.

A kit capable of rapidly and quantitatively detecting sensitivity of an antibacterial agent is provided with a reagent capable of directly detecting bacteria ATP. After the reagent is added at a time, bacteria lysis and releasing and detection of ATP are realized at one step. By the kit, a drug sensitivity experimental result can be obtained within 2 hours. Requirements on hardware are low, any micropore plate type luminous detecting instrument can be used, and an automatic sample injection system is not required. The method is simple and convenient to operate, one-step sample adding is implemented, and lysate and an ATP detecting reagent are not required to be injected separately. An MIC value can be determined, and whether drug resistance exists or not can be reported simultaneously.

The invention relates to mulin acetate comprising substituted squaric acid, and an application thereof. The invention belongs to the field of chemical medicine. A mulin acetate compound comprising substituted squaric acid, a pharmaceutically acceptable salt thereof, a solvate thereof, an isomer thereof, a prodrug thereof, or a prodrug of salt thereof have a structural general formula represented by the formula (I). The MIC values of the compound against staphylococcus aureus and strepococcus equi are higher by 20-30 times than the antibacterial effect of a reference product of tiamulin in market. The mulin acetate comprising substituted squaric acid is a high-efficiency antibacterial medicine.

The invention belongs to the field of pharmacy, and relates to compound 3, 4',5-trihydroxy-diphenyl (resveratrol) and applications of the compound 3, 4',5-trihydroxy-diphenyl (resveratrol) in preparing sensitivity enhancing medicines of methicillin-resistant staphylococcus aureus capable of resisting fluoroquinolones. The compound 3, 4',5- trihydroxy-diphenyl (resveratrol) is wide in distribution,at present, resveratrol has been found in plants of at least 21 families, 31 categories and 72 kinds, wherein the contents in grape, polygonum cuspidatum and peanut are relatively high, and no obvious toxic and side effects exist. The antibacterial test shows that the compound has the pharmacological activity of improving the sensitivity of the multidrug-resisting staphylococcus aureus for norfloxacin, especially aiming at the methicillin-resistant staphylococcus aureus SA1199B containing fluoroquinolones-resisting gene NorA, the MIC value of norfloxacin can be reduced by 16 times after the compound and norfloxacin are mixed for use, and further, the composition can be used for preparing antibiotic synergistic medicines.

Belonging to the field of medicinal chemistry, the invention discloses a metal beta-lactamase inhibitor open chain pyridine carboxylic acid derivative and a preparation method thereof. The compound has the following structure shown as the specification. The derivative can restore the sensitivity of metal beta-lactamase enterobacteriaceae bacteria to carbapenem antibiotics. In vitro antibacterial experiment results prove that the derivative can reduce the MIC value of carbapenem resistant Escherichia coli (producing NDM-1 type metal beta-lactamase) to meropenem by about 40960 times maximumly. In vitro red blood cell toxicity experiments also prove that the compound has very small red blood cell toxicity. Therefore, the compound is expected to be used as a candidate drug of novel metal beta-lactamase inhibitor.

The invention discloses indole[3,2-c]quinoline compounds represented by formula I or pharmaceutically acceptable salts thereof, and a preparation method and an application thereof, and belongs to the technical field of the pharmaceutical chemistry. The indole[3,2-c]quinoline compounds or pharmaceutically acceptable salts thereof have a very good tubercle bacillus resisting activity, and the MIC value of the most compounds is 2.5mug / mL.

The invention provides a group of NZ2114 histidine mutants, and a preparation method thereof. Two histidine sites existing in an NZ2114 sequence are selectively mutated by using a protein directional transformation. The histidine mutants with the amino acid sequences represented by SEQ ID NO:1 to SEQ ID NO:5 are designed, and recombinant expression of the histidine mutants in Pichia pastoris is realized. Design of an NZ2114 histidine mutantderivative is realized for the first time, and a determination result shows that the mutants (especially the 16th histidine mutant) has substantial bacteriostatic activity on Staphylococcus aureus ATCC 25923, ATCC 43300 and ATCC 6538 and Streptococcus suis CVCC 3928 and CVCC 3309, and the MIC value is 0.0625-2 [mu]g / ml. The NZ2114 histidine mutants obtained through the method can be applied to the fields of antibacterial drugs, food additives, cosmetics and feed additives, and has wide application values and market prospect.

The invention discloses a polypeptide compound with antimicrobial and anti-inflammatory activities and belongs to the technical field of biology. The polypeptide compound has an amino acid sequence ofIGKLFKRIVQLIK or IGKLFKRIVQLIL, named as IG-13-1 and IG-13-2 respectively. The polypeptide compound is a novel polypeptide compound which efficiently acts on bacterial membrane of Streptococcus mutans, inhibits activity of Streptococcus mutans and the formation of its biological membrane by interfering the integrity of the bacterial membrane, and therefore, prevents and treats dental caries. Antibacterial activity test shows that the two polypeptides have MIC value of 5.0 mu M, having antimicrobial rate prior to anti-caries drug CHX used often at present. It is worth notification: the biological membrane formation inhibition test shows that both IG-13-1 and IG-13-2 can inhibit the growth of the biological membrane of Streptococcus mutans when MBIC50 have the concentrations of 5.91+ / -0.91and 7.58+ / -0.23 mu M.

The invention relates to an application of ellagic acid to preparation of drugs for treating and preventing fungal infection of a human body. According to the application, the in-vitro fungi inhibition activity of ellagic acid to 23 fungi is studied and the MIC (minimal inhibitory concentration) value is measured; an in-vitro activity result of ellagic acid to the fungi shows that the MIC value of ellagic acid to 6 dermatophytes is 6.25-50 microgram / ml, and ellagic acid has a better inhibition effect on clinical common superficial pathogenic fungi and is especially sensitive to trichophyton rubrum; the MIC value of ellagic acid to 6 clinical common candida is 25-200 microgram / ml; ellagic acid is orally taken and externally used to treat a cavy skin trichophyton rubrum infection model, and the effect of treating a mouse fungal infection model by injecting ellagic acid or ellagic acid and fluconazole is studied; a study result shows that ellagic acid has a certain treatment effect on the cavy skin trichophyton rubrum infection model after being orally taken and externally used.

The invention relates to a small peptide resisting MDR (multiple resistant bacteria). The small peptide is characterized in that the small peptide has the function of resisting clinically isolated MDR. In-vitro activity assay results prove that 11 small peptides have different antibacterial activities for multiple MDR and have the MIC value ranging from 4 mu g / L to 128 mu g / L according to different bacteria. Compared with a mother pattern, the small peptide has enhanced pseudomonas aeruginosa and candida albicans resistant activity. 6 peptides with better antibacterial activity are selected for an in vivo experiment, results prove that the 6 peptides can notably reduce the death rate of a model mouse because of a pseudomonas aeruginosa standard strain and clinical pan-drug-resistant pseudomonas aeruginosa septicemia and have a synergistic effect with polymyxin; no hemolytic reaction is caused when the concentration of 6 small peptides is 10 mg / ml, and the product safety is higher; local stimulation experiment results of rabbit eye conjunctiva show that the small peptide has no acute toxic stimulus reaction.

The invention relates to the technical field of bacterium prevention of microorganisms, in particular to application of polyphyllin in products for resisting malassezia fufur and candida albicans. Itis discovered that in-vitro drug sensitivity tests by an inventor that polyphyllin has an inhibition effect on malassezia fufur and candida albicans. The weight fraction of polyphyllin I, VI and VII and MIC, with an inhibition effect on malassezia fufur, of rhizoma paridis total saponin is 2 mug / mL, 19 mug / mL, 39 mug / mL and 0.5 mug / mL; The weight fraction of polyphyllin I, II, VI and VII and MIC,with an inhibition effect on candida albicans, of rhizoma paridis total saponin is 0.125 mug / mL, 0.03125 mug / mL, 78 mug / mL, 0.625 g / L and 0.5 g / L. Compared with an existing bacteriostat, polyphyllin has small MIC value on malassezia fufur and candida albicans and has good antimicrobial activity. Polyphyllin can be used as an antimicrobial active component and added to external medicine, oral medicine, a disinfectant, a washing agent and an antimicrobial coating and has the functions of inhibiting growth of malassezia fufur and candida albicans.

The invention provides a drying process of an antimicrobial susceptibility test plate. The drying process has simple equipment and easy operation. The inventive drying process has equal drying effect to the vacuum freeze drying process, but is predominant in the analysis of a MIC value as test result. Therefore, the inventive drying process can reduce the cost, increase the accuracy of susceptibility test, and has high value in the clinical application.

The invention relates to the technical field of medical biological detection, and provides an application of rattlerin in preparing an anti-fungal drug sensitizer, an anti-fungal drug sensitizer taking rattlerin as an active ingredient and an anti-fungal combination preparation. According to experimental measurement, when fluconazole and rattlerin are combined, FICI of all experimental strains isless than or equal to 0.50, so that a strong synergistic effect is shown, meanwhile, the MIC value of fluconazole is decreased by 2-16 times, the sensitivity of fluconazole to cryptococcus is improved, so that the rattlerin not only is beneficial to reducing clinical dosage, but also is beneficial to slowing down the phenomenon of high drug resistance rate of cryptococcus, and conducts beneficialexploration for clinical anti-fungal infection.

The invention relates to a flow cytometry detection method for tetracycline resistance bacteria in drinking water. The method comprises the following steps of (1) adding a water sample to be detected into a brown test tube, adding tetracycline mother liquor, enabling the concentration of tetracycline in the water sample to be detected to be equal to an MIC value thereof, putting the water sample to be detected into a culture box, and culturing for 24h at 27 DEG C; (2) transferring the cultured water sample into a flow cytometry sample injection pipe, adding an SYBR Green I coloring agent and a propidium iodide coloring agent for coloring, and after fully vibrating, culturing in dark at 37 DEG C for 10 to 15min; (3) transferring the cultured flow cytometry sample injection pipe into a flow cytometry, starting to inject a sample, determining the number of the tetracycline resistance bacteria, and dividing by a sample injection volume so as to obtain the concentration of the tetracycline resistance bacteria in the drinking water. Compared with the prior art, the number of the tetracycline resistance bacteria is detected by utilizing the flow cytometry, so that the flow cytometry detection method has the advantages of quickness, accuracy and quantitation, overcomes the defect that the nonculturable resistance bacteria cannot be detected through a traditional culture method, and is more reliable in result.

The invention relates to a novel compound sciryagarol II having antineoplastic and antibiosis activities and a preparation method thereof, and belongs to the field of medicine technology. The sciryagarol II is a novel cis-form stilbene derivative with a structure formula shown below. The sciryagarol II can be prepared from dry tubers of scirpus yagara by extraction. The preparation method comprises steps of extracting with ethanol having a concentration of 80%; condensing under reduced pressure; extracting with petroleum ether and ethyl acetate individually; purifying the ethyl acetate extract by repeatedly performing column chromatography using silica gel; and performing gradient elution by using petroleum ether and ethyl acetate to obtain pure sciryagarol II. The sciryagarol II has good antineoplastic and antibiosis effects, has an IC[50] value of 7.218 [mu]M for human cervical cancer Hela cells, and has a MIC value of 79.3 [mu]g / mL for staphylococcus aureus and candida albicans individually.

The invention provides a common cephalanoplos herb trichloromethane extract. The common cephalanoplos herb trichloromethane extract is obtained by adding petroleum ether into common cephalanoplos herb crude powder or ethanol extract for extracting, then sequentially extracting extracts at corresponding solvent parts with trichloromethane, ethyl acetate, n-butyl alcohol and water, and collecting the extract at a trichloromethane part, so that the common cephalanoplos herb trichloromethane extract is obtained. The invention also provides application of the common cephalanoplos herb trichloromethane extract. The common cephalanoplos herb trichloromethane extract prepared by extracting by virtue of two systematic solvent processes has the minimum bactericidal concentration of 0.63mg / ml; and the experimental determination shows that the common cephalanoplos herb trichloromethane extract has the MIC value of 100mu g / ml and the MBC value of 400mu g / ml, and has better inhibiting and killing effects on a mycobacterium tuberculosis standard strain H37RV.

The invention belongs to the technical field of botanical pesticide, and in particular provides an application of shepherd's purse in prevention and cure of tobacco ralstonia solanacearum. The invention explores the inhibiting effect of shepherd's purse extract to the tobacco ralstonia solanacearum and finds out that the shepherd's purse extract has the inhibiting effect to the tobacco ralstonia solanacearum, and the inhibition ratio is 27.2 percents, wherein the inhibition effect of root extract, stem extract and seed extract is the strongest, and the inhibition effect of leaf extract is zero. Further research result shows that the MIC value of the root extract, the stem extract and the seed extract to the tobacco ralstonia solanacearum are all 80 mg / mL, and scientific basis is provided for developing and utilizing natural active materials of the shepherd's purse and researching and developing new biological pesticide.

The invention discloses a flora drug resistance intensity evaluation method. The flora drug resistance intensity evaluation method comprises the following steps of collecting and separating drug-resistant strains, and detecting drug-resistant MIC values of the drug-resistant strains; correcting the monitored drug-resistant MIC values; taking a logarithm of 10 from the drug resistance correction values, and solving a logarithm average value of MIC values of all monitoring drugs of a single strain; and judging the drug resistance strength of the target flora by adopting a simultaneous analysis method of the average values and the median values. By introducing the drug resistance coefficient, the drug resistance evaluation accuracy of the drug-resistant strain is improved, the antibiotic useintensity of the drug-resistant strain is quantified, and the method has a data reference value.

The invention relates to the application of a substituted piperazine compound in the preparation of a medicament for resisting fungal infection and particularly discloses a compound which is (4-chlorophenyl)-(piperazin-1-yl)-methanone or pharmaceutically acceptable salt thereof as well as a preparation method and medicinal application of the (4-chlorophenyl)-(piperazin-1-yl)-methanone or medicinally acceptable salt thereof. The steps for synthesizing the compound are simple, the method for preparing the compound is simple and practical, the sources of raw materials are easy to obtain, the cost is low, and less pollution is caused. The compound has an obvious activity of inhibiting the growth of fungi and has the MIC value of 62.5mcg / ml. The pharmacodynamic results show that the substituted piperazine compound or medicinally acceptable salt is expected to be used to prepare the medicament for preventing and treating the diseases caused by fungal infection.

The invention discloses a sandalwood endophytic fungus derived diphenolic acid compound, a preparation method and application thereof in preparation of antimicrobial drugs. The diphenolic acid compound has a structural formula shown as formula I, II or III. The new compound shows good bacteriostatic activity on two or more of multiple indicator strains. The MIC value is in the range of 3.0-12.5microg / mL, and compound can be used for preparation of antibacterial drugs. Therefore, the diphenolic acid compound provided by the invention has the potential of antibacterial clinical application.

The invention relates to a fluorobenzyl substituted piperazine compound and preparation and medical application thereof, and specifically discloses 2-(4-(4-fluorobenzyl)-piperazine-1-yl)-ethylamine or a medicinal salt thereof and a preparation method and medical application thereof. The synthesis steps of the compound are simple, the preparation method is simple and easy to implement, the raw materials are convenient and easily available, the cost is low, and little pollution is caused. The fluorobenzyl substituted piperazine compound has obvious inhibitory activity on the growth of fungi, and the MIC value is 62.5-125mg / ml. The result of pharmacodynamics indicates that the fluorobenzyl substituted piperazine compound or the medicinal salt thereof can be expected to serve as a medicine for preventing and treating the diseases caused by fungal infection.

The invention relates to xenopus laevis daudin skin antibacterial peptide and a preparing method and application thereof. The antibacterial peptide is separated from skin secretions of xenopus laevis daudin, it is obtained after purifying and sequencing are carried out that the sequence of the antibacterial peptide is Asp-Glu-Asp-Asp-Asp (DEDDD), and it is obtained through mass spectrometric that the molecular weight of the antibacterial peptide is 607.7 Da. According to the xenopus laevis daudin skin antibacterial peptide and the preparing method and application thereof, a physical method is adopted to stimulate the skin of xenopus laevis daudin, and thus the structure integrity and the biological activity of the antibacterial peptide are protected to a great degree. The antibacterial peptide has obvious bacteriostatic activity, low hemolytic activity and good breast cancer resisting activity. The molecular weight of the antibacterial peptide is low, so that the difficulty of chemosynthesis of the antibacterial peptide is lowered, and cost is greatly reduced. The antibacterial peptide has the obvious bacteriostatic action on gram-positive bacteria and gram-negative bacteria, is extremely low in hemolytic activity in the MIC value range, has high breast cancer resisting activity, can be used in various medical directions of preventing wound and trauma infection, resisting tumors, bacteriostatic preparations and the like, and has good application prospects.

The invention relates to an application of a housefly MSP protein in the antibiosis field, and belongs to the biotechnical field. The housefly MSP protein has an amino acid sequence represented by SEQ ID NO:1. A bioinformatics analysis result shows that the ORF full length of MSP gene is 495bp, the gene encodes 164 amino acids, the theoretic molecular weight is 17.4kDa, and the isoelectric point is 6.09; and the whole polypeptide chain is hydrophilic. An in-vitro antibiosis test result shows that the MSP has an inhibition effect on Escherichia coli, Staphylococcus aureus and Candida albicans, the corresponding MIC values are 0.3mg / ml, 0.2mg / ml and 0.002mg / ml respectively, and the MSP protein has protruding antibiosis activity to the Candida albicans. The housefly MSP protein is hopeful to become a clinically novel antibiotic.

The invention discloses indole[3,2-c]quinoline compounds represented by formula I or pharmaceutically acceptable salts thereof, and a preparation method and an application thereof, and belongs to the technical field of the pharmaceutical chemistry. The indole[3,2-c]quinoline compounds or pharmaceutically acceptable salts thereof have a very good tubercle bacillus resisting activity, and the MIC value of the most compounds is 2.5mug / mL.