scholarly journals Stability of Novel Siderophore Cephalosporin S-649266 against Clinically Relevant Carbapenemases

2016 ◽  
Vol 60 (7) ◽  
pp. 4384-4386 ◽  
Author(s):  
Tsukasa Ito-Horiyama ◽  
Yoshikazu Ishii ◽  
Akinobu Ito ◽  
Takafumi Sato ◽  
Rio Nakamura ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Hydrolysis Of

ABSTRACTTo better understand the antibacterial activity of S-649266 against carbapenemase producers, its stability against clinically relevant carbapenemases was investigated. The catalytic efficiencies (kcat/Km) of IMP-1, VIM-2, and L1 for S-649266 were 0.0048, 0.0050, and 0.024 μM−1s−1, respectively, which were more than 260-fold lower than that for meropenem. Only slight hydrolysis of S-649266 against KPC-3 was observed. NDM-1 hydrolyzed meropenem 3-fold faster than S-649266 at 200 μM.

scholarly journals Purification and characterization of ascamycin-hydrolysing aminopeptidase from Xanthomonas citri

1986 ◽  
Vol 233 (2) ◽  
pp. 459-463 ◽  
Author(s):  
H Osada ◽  
K Isono
Keyword(s):  
Antibacterial Activity ◽  
Enzyme Inhibitors ◽  
Polyacrylamide Gel Electrophoresis ◽  
Gel Filtration ◽  
Deae Cellulose ◽  
Homogeneous State ◽  
Xanthomonas Citri ◽  
Gram Positive Bacteria ◽  
Xanthomonas Species ◽  
Hydrolysis Of

A nucleoside antibiotic, ascamycin (9-beta-[5′-0-(N-L-alanyl) sulphamoyl-D-ribofuranosyl]-2-chloroadenine), has a selective antibacterial activity against Xanthomonas species. When ascamycin was dealanylated, dealanylascamycin showed a broad antibacterial activity against various Gram-negative and Gram-positive bacteria. Xanthomonas citri is susceptible to ascamycin by virtue of the ascamycin-dealanylating enzyme on the cell surface [Osada & Isono (1985) Antimicrob. Agents Chemother. 27, 230-233]. The enzyme (Xc aminopeptidase) was purified from X. citri cells by successive DEAE-cellulose, chromatofocusing and Sephadex G-100 column chromatography to a homogeneous state. The purified enzyme exhibited a single band with an Mr of 38 000 in SDS/polyacrylamide-gel electrophoresis. Gel filtration on a calibrated column indicated a similar Mr value. The isoelectric point of the enzyme was 5.7. The enzyme catalysed the hydrolysis of the alanyl group of ascamycin and liberated alanine from the sulphamoyl nucleoside. The enzyme also catalysed the hydrolysis of L-proline beta-naphthylamide and L-alanine beta-naphthylamide. The optimal pH and temperature for enzyme activity were pH 7.5-8.0 and 35-40 degrees C respectively. The enzyme was inhibited by thiol-enzyme inhibitors (i.e. rho-chloromercuribenzoate and N-ethylmaleimide), but was not affected by various naturally occurring aminopeptidase inhibitors (i.e. amastatin, bestatin, pepstatin and leupeptin). Mn2+ and Mg2+ activated the enzyme, whereas Cu2+, Zn2+ and Cd2+ were inhibitory.

Morpholine- and Thiomorpholine-Based Amidodithiophosphonato Nickel Complexes: Synthesis, Characterization, P–N Cleavage, Antibacterial Activity and Silica Nano-Dispersion

2021 ◽  
Vol 21 (5) ◽  
pp. 2879-2891
Author(s):  
Enrico Podda ◽  
M. Carla Aragoni ◽  
Massimiliano Arca ◽  
Giulia Atzeni ◽  
Simon J. Coles ◽  
...  
Keyword(s):  
Staphylococcus Aureus ◽  
Antimicrobial Activity ◽  
Antibacterial Activity ◽  
Nickel Complex ◽  
Nickel Complexes ◽  
Silica Matrix ◽  
Gram Negative Bacteria ◽  
Gram Negative ◽  
Ft Ir ◽  
Hydrolysis Of

The reactivity of thiomorpholinium P-(4-methoxyphenyl)-N-thiomorpholin-amidodithiophosphonate (S-MorH+2)(S-Mor-adtp−) and morpholinium P-(4-methoxyphenyl)-N-morpholin-amidodithiophosphonate (O-MorH+2)(O-Mor-adtp−) towards nickel (II) dichloride hexahydrated is presented and the hydrolysis of the relevant metal complexes investigated. The hydrolytic products (S-MorH+2)2 [Ni(dtp)2]2− and (O-MorH+2)2[Ni(dtp)2]2− were characterized by means of FT-IR, 1H, and 31P NMR and XRD and the experimented P–N cleavage investigated and elucidated by means of DFT calculations. The antimicrobial activity of the neutral nickel complex [Ni(S-Mor-adtp)2] was tested against a set of Gram-positive and Gram-negative bacteria alongside with its nanodispersion in a silica matrix. The complex [Ni(S-Mor-adtp)2] did not show antibacterial activity, whilst the nano-dispersed sample [Ni(S-Mor-adtp)2]_SiO2 demonstrated inhibition to growth of Staphylococcus aureus. The nanocomposites were fully characterized by means of XRPD, TGA, SEM and dinitrogen sorption techniques.

scholarly journals TRANSFORMATION OF ETHYL-P-METHOXYCINNAMATE TO P –METHOXYCINNAMIC ACID FROM KENCUR (Kaempheria galanga L.) AND THEIR ANTIBACTERIAL ACTIVITY

2017 ◽  
Vol 13 (2) ◽  
pp. 176
Author(s):  
Muhamad Salman Fareza ◽  
Rehana Rehana ◽  
Nuryanti Nuryanti ◽  
Didin Mujahidin
Keyword(s):  
Antibacterial Activity ◽  
Antibacterial Properties ◽  
Separation And Purification ◽  
E Coli ◽  
H Nmr ◽  
Alkaline Conditions ◽  
Methoxycinnamic Acid ◽  
Vacuum Liquid Chromatography ◽  
Hydrolysis Of ◽  
C Nmr

This study aimed to evaluate the antibacterial properties of ethyl-<em>p</em>-methoxycinnamate and <em>p</em>-methoxycinnamate acid from Kaempheria galanga L. Ethyl-<em>p</em>-methoxycinnamate was isolated from the <em>n</em>-hexane rhizome extract of <em>Kaempheria galanga L</em>. Separation and purification of this compound was carried out with vacuum liquid chromatography and column chromatography. Hydrolysis of ethyl-<em>p</em>-methoxycinnamic under alkaline conditions obtained <em>p</em>-methoxycinnamic acid with a good yield of 85 %. The structure of the compounds were charactrized with IR, NMR spectrophotometer (<sup>1</sup>H-NMR and <sup>13</sup>C-NMR) and mass spectrophotometer. The antibacterial properties of the compounds were evaluated using microdilution methods against <em>B. cereus</em> ATCC 11778, <em>L. monocytogenes</em> ATCC 7644, <em>E. coli</em> ATCC 25922, <em>S. enterica sv Typhimurium</em> ATCC 14028, and <em>E. aerogenes</em> ATCC 13048. The compounds showed weak antibacterial properties. Only ethyl <em>p</em>-methoxycinnamate showed the strongest antibacterial activity, especially against <em>B. cereus</em> ATCC 11778 bacteria with MIC values of 62.5 mg /mL. The change of the functional groups provided no significant impact on the antibacterial activity.

scholarly journals Uji Aktivitas Sitotoksik dan Antibakteri Ekstrak Daun Tumbuhan Rengas (Gluta renghas L)

2020 ◽  
Vol 11 (1) ◽  
pp. 52-60
Author(s):  
Sanusi Ibrahim ◽  
Suryati Suryati ◽  
Enda Desriansyah Aziz
Keyword(s):  
Antibacterial Activity ◽  
Ethyl Acetate ◽  
Methanol Extract ◽  
Ethyl Acetate Extract ◽  
Inhibition Zone ◽  
Cytotoxicity Activity ◽  
E Coli ◽  
Rate Of Hydrolysis ◽  
Hydrolysis Of ◽  
Ethyl Acetate Extracts

Generally, Gluta renghas L. is known because of its very toxic latex which can cause hard irritations to skin. Although, rengas latex has efficacy as an antibacterial agent. Related to previous research, it has been reported that there are urisol, rengol, glutarengol, laccol, and thitsiol in rengas latex. The woody trunk was reported to contain flavonoid, benzenoid, lipid, and steroid compounds. The leaves, were reported shows that the leaves of G. renghas contain an anticholinesterase substance and can be reduced the rate of hydrolysis of acetylcholine. Extraction of rengas leaves has been carried out. It has been shown phenols, steroids, and coumarins compounds in methanol extract, flavonoids, phenols, saponins and alkaloids compounds in ethyl acetate extract, steroids and alkaloids compounds in hexane extract. In the present, cytotoxicity and antibacterial activity have been tested. The results show that the great cytotoxicity activity by ethyl acetate extracts which have an LC50 value is 123,718 µg/mL (R2 0.9822), while the great antibacterial activity shown by methanol extract 1,000 µg/mL with a diameter of inhibition zone 19.02 mm (S. aureus) and 16.06 mm (E. coli). 

Antibacterial Activity of Chitooligosaccharides Derived from the Hydrolysis of Complex Consisting of Chitosan and Hyaluronic Acid

2021 ◽  
Vol 26 (3) ◽  
pp. 118-126
Author(s):  
Suwan Kim ◽  
Min Sik Jeong ◽  
Sang Hun Jung ◽  
Yong Hyun Lee ◽  
Jae Kweon Park
Keyword(s):  
Antibacterial Activity ◽  
Hyaluronic Acid ◽  
Hydrolysis Of

Antibacterial Activity of an Oligosaccharide of Native Paecilomyces sp. and its Aminoglycosylated Derivative

2011 ◽  
Vol 66 (3-4) ◽  
pp. 123-128
Author(s):  
Luis Lillo ◽  
Julio Alarcón ◽  
Carlos L. Céspedes ◽  
Gerardo Cabello ◽  
Patricia Canto ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Acid Hydrolysis ◽  
Reductive Alkylation ◽  
Partial Acid Hydrolysis ◽  
E Coli ◽  
Hydrolysis Of

This study reports the antibacterial activity of an oligosaccharide, prepared by partial acid hydrolysis of a native Paecilomyces sp. exopolysaccharide, and of its aminoglycosylated derivative, prepared by reductive alkylation of the oligosaccharide, against E. coli and S. aureus

Nuclear analogs of β-lactam antibiotics. II. Synthesis of O-2-isocephems

1977 ◽  
Vol 55 (3) ◽  
pp. 484-507 ◽  
Author(s):  
Terrence W. Doyle ◽  
Bernard Belleau ◽  
Bing-Yu Luh ◽  
Terry Thomas Conway ◽  
Marcel Menard ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Total Synthesis ◽  
Spectral Characteristics ◽  
Ring Closure ◽  
Phenoxyacetic Acid ◽  
New Class ◽  
High Antibacterial Activity ◽  
Hydrolysis Of

The preparation by total synthesis of a new class of β-lactam antibiotics is reported. Conversion of alcohol 1b to its mesylate 9b followed by hydrolysis of the acetal to the enol 1b and base-catalyzed ring closure gave benzyl 7- β-azido-Δ3-O-2-isocephem-4-carboxylate 8b. Similarly prepared were the 3 -methyl, 3 -benzyl, and 3 -phenethyl analogs (32b–d). Reduction of the azides followed by coupling of the resultant amines with phenoxyacetic acid and removal of the benzyl groups by hydrogenolysis gave the acids 35a–e which exhibited high antibacterial activity. The structural assignments to the O-2-isocephems which were made on the basis of their spectral characteristics (ir, uv, and nmr) are discussed.

Mode of Action of a Bacteriocin (J46) Produced by Lactococcus lactis subsp. cremoris J46

1996 ◽  
Vol 59 (9) ◽  
pp. 955-962 ◽  
Author(s):  
C. BARRENA-GONZALEZ ◽  
E. HUOT ◽  
H. PETITDEMANGE
Keyword(s):  
Antibacterial Activity ◽  
Lactococcus Lactis ◽  
Bactericidal Activity ◽  
Continuous Fermentation ◽  
Physiological State ◽  
Efflux Rate ◽  
No Adsorption ◽  
Lactococcus Lactis Subsp ◽  
Resistant Strains ◽  
Hydrolysis Of

The mode of antibacterial action of bacteriocin J46, a bacteriocin from Lactococcus lactis subsp. cremoris, was studied. Bacteriocin J46 specifically adsorbed on susceptible bacteria. Adsorption on gram-negative or gram-positive resistant strains was significantly lower. Bacteriocin J46 has been shown to be bactericidal towards log-phase indicator cells but ineffective against stationary cells. In addition energy-depleted log-phase cells were unaffected. It was shown that both a ΔpH and a Δ Ψ were required for bacteriocin J46 activity. Using a continuous fermentation procedure, we were able to confirm the crucial importance of the physiological state of the indicator on its sensitivity. Negligible antibacterial activity was detected against cells of the sensitive strain, L. lactis subsp. cremoris SC11 (μmax: 0.93) growing at dilution rates below about 0.6 h−1 even with high bacteriocin concentrations. When assays were conducted in a growth medium, there was a continuous decrease in bacterial viability as a function of time, suggesting that actively growing cells were sensitive to the bactericidal activity of bacteriocin J46. This antibacterial peptide caused an immediate loss of cellular K+ and a hydrolysis of internal ATP in L. lactis subsp. cremoris SC11. The initial rate of K+ efflux increased with increasing bacteriocin concentration, being saturated at approximately 10,000 AU/ml. Decreasing the ionic strength of the assay buffer did not result in a significant modification of the K+ efflux rate induced by J46 addition. Bacteriocin activity was pH dependent: at pH 7.0, no adsorption and no antibacterial activity were detected. These results suggest that the bactericidal activity of bacteriocin J46 was due to the formation of pores in the cytoplasmic membrane of log-phase cells, stationary cells remaining unaffected.

scholarly journals Syntheses and Antibacterial Activities of Tizoxanide, an N-(Nitrothiazolyl)salicylamide, and its O-Aryl Glucuronide

1999 ◽  
Vol 23 (1) ◽  
pp. 44-45
Author(s):  
Jean-François Rossignol ◽  
Andrew V. Stachulski
Keyword(s):  
Antibacterial Activity ◽  
Broad Spectrum ◽  
Antibacterial Activities ◽  
Major Metabolite ◽  
Mild Hydrolysis ◽  
Hydrolysis Of

Mild hydrolysis of the broad-spectrum anaerobic antibacterial and antiparasitic agent nitazoxanide 1 affords tizoxanide 2, which is a major metabolite of 1 retaining most of its activity; further metabolism of 2 leads to the O-aryl glucuronide 3, efficiently synthesised in four steps from benzyl salicylate and showing slight antibacterial activity.

Potential scorpionate antibiotics: Targeted hydrolysis of lipid II containing model membranes by vancomycin–TACzyme conjugates and modulation of their antibacterial activity by Zn-ions

2009 ◽  
Vol 19 (14) ◽  
pp. 3721-3724 ◽  
Author(s):  
H. Bauke Albada ◽  
Christopher J. Arnusch ◽  
Hilbert M. Branderhorst ◽  
Anne-Marie Verel ◽  
Wouter T.M. Janssen ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Model Membranes ◽  
Lipid Ii ◽  
Hydrolysis Of ◽  
Zn Ions
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