Antibacterial activity of isolated phenolic compounds from cranberry (Vaccinium macrocarpon) against Escherichia coli

2016 ◽  
Vol 7 (3) ◽  
pp. 1564-1573 ◽  
Author(s):  
Celia Rodríguez-Pérez ◽  
Rosa Quirantes-Piné ◽  
José Uberos ◽  
Cecilia Jiménez-Sánchez ◽  
Alejandro Peña ◽  
...  
Keyword(s):  
Escherichia Coli ◽  
Antibacterial Activity ◽  
Phenolic Compounds ◽  
Surface Hydrophobicity ◽  
Vaccinium Macrocarpon ◽  
E Coli

Apart from proanthocyanidins, isolated polyphenols from cranberry can act againstE. coliadherence and/or modify its surface hydrophobicityin vitro.

scholarly journals Synthesis of antibiotic loaded polylactic acid nanoparticles and their antibacterial activity against Escherichia coli O157:H7 and methicillin-resistant Staphylococcus aureus

Biomédica ◽  
2017 ◽  
Vol 37 (1) ◽  
pp. 11 ◽  
Author(s):  
Mónica Tatiana Herrera ◽  
Jhon Jhamilton Artunduaga ◽  
Claudia Cristina Ortiz ◽  
Rodrigo Gonzalo Torres
Keyword(s):  
Escherichia Coli ◽  
Staphylococcus Aureus ◽  
Antibacterial Activity ◽  
Polylactic Acid ◽  
Methicillin Resistant Staphylococcus Aureus ◽  
Escherichia Coli O157 ◽  
Methicillin Resistant ◽  
E Coli

Introducción. Las nanopartículas poliméricas constituyen una herramienta nanotecnológica que podría ayudar a combatir los microorganismos patógenos que han desarrollado resistencia a los antibióticos convencionales.Objetivo. Sintetizar nanopartículas de ácido poliláctico cargadas con ofloxacina y vancomicina, y determinar su actividad antibacteriana frente a Escherichia coli O157:H7 y Staphylococcus aureus resistente a la meticilina (SARM).Materiales y métodos. Las nanopartículas de ácido poliláctico cargadas con ofloxacina y vancomicina se sintetizaron utilizando el método de emulsión y evaporación de solvente. Se caracterizaron mediante dispersión de luz en modo dinámico, electroforesis Doppler con láser y microscopía electrónica de barrido (S-TEM). Se evaluó la actividad antibacteriana in vitro de las nanopartículas de ácido poliláctico con ofloxacina contra E. coli O157:H7 y nanopartículas de ácido poliláctico con vancomicina contra SARM, mediante el método de microdilución en caldo.Resultados. Se obtuvieron nanopartículas poliméricas con tamaños inferiores a 379 nm y carga superficial positiva de hasta 21 mV. Las nanopartículas cargadas con ofloxacina presentaron una concentración inhibitoria mínima (CIM50) de 0,001 μg/ml frente a E. coli O157:H7, valor 40 veces menor que la concentración de antibiótico libre necesaria para lograr el mismo efecto (CIM50=0,04 μg/ml). Para SARM, las nanopartículas mejoraron la potencia farmacológica in vitro de la vancomicina alexhibir una MIC50 de 0,005 μg/ml, comparada con la de 0,5 μg/ml del antibiótico libre.Conclusiones. Se mejoró el efecto antibacteriano de la ofloxacina y la vancomicina incorporadas en la matriz polimérica de ácido poliláctico. Las nanopartículas poliméricas constituirían una alternativa para el control de cepas bacterianas de interés en salud pública.

Antibacterial Activities of Semipurified Fractions of Quercus infectoria against Enterohemorrhagic Escherichia coli O157:H7 and Its Verocytotoxin Production

2008 ◽  
Vol 71 (6) ◽  
pp. 1223-1227 ◽  
Author(s):  
SUPAYANG PIYAWAN VORAVUTHIKUNCHAI ◽  
SAKOL SUWALAK
Keyword(s):  
Escherichia Coli ◽  
Antibacterial Activity ◽  
Latex Agglutination ◽  
Enterohemorrhagic Escherichia Coli ◽  
Natural Food ◽  
Escherichia Coli O157 ◽  
E Coli ◽  
Broth Microdilution Method ◽  
Quercus Infectoria

Escherichia coli O157:H7 is one of the most important foodborne pathogens, causing nonbloody and bloody diarrhea, hemorrhagic colitis, and hemolytic uremic syndrome. Use of antibiotics has been demonstrated to result in increased levels of verocytotoxin (VT) production as well as antibiotic resistance. Quercus infectoria was investigated for its antibacterial activity against E. coli O157:H7 and other VT-producing enterohemorrhagic E. coli (VTEC). The MIC was determined by a broth microdilution method, and the MBC was assessed by subculturing the bacteria from the wells that showed no apparent growth onto Mueller-Hinton agar. The fractions Qi2, Qi3, and Qi4 of Q. infectoria were demonstrated to possess good antibacterial activity, with MICs and MBCs ranging from 250 to 500 μg/ml. The effect of the effective fraction, Qi4, on the production of VT was determined using a reversed passive latex agglutination. The results indicate that at 20 h, fraction Qi4 markedly inhibits the release of VT1 and VT2 from VTEC cells at both inhibitory and subinhibitory concentrations. Furthermore, verotoxicity assay demonstrated that bacterial cultures treated with fraction Qi4 exerted less toxic effect on Vero cells. These in vitro results clearly indicate that the fraction Qi4 might constitute a promising natural food additive for the control of food poisoning by E. coli O157:H7 as well as other VTEC strains.

scholarly journals In vitro synergistic potentials of novel antibacterial combination therapies against Salmonella Typhimurium, Escherichia coli and Staphylococcus aureus

2019 ◽  
Author(s):  
Md Akil Hossain ◽  
Hae-Chul Park ◽  
Kwang-jick Lee ◽  
Sung-Won Park ◽  
Seung-Chun Park ◽  
...  
Keyword(s):  
Escherichia Coli ◽  
Staphylococcus Aureus ◽  
Phenolic Compounds ◽  
Phenolic Compound ◽  
Virulence Factors ◽  
In Vitro Cytotoxicity ◽  
E Coli ◽  
And Staphylococcus Aureus

Abstract Background: Bacteria have remarkable abilities to acquire resistance against antibiotics by several mechanisms. New strategies are needed to block the development of resistance and to prolong the life of traditional antibiotics. This study aimed to increase the efficacy of existing antibiotics by combining them with the opportunistic phenolic compound gallic acid (GA) and its derivatives. Fractional inhibitory concentration (FIC) indexes of phenolic compound-antibiotic combinations against Salmonella enterica serovar Typhimurium, Escherichia coli and Staphylococcus aureus were determined. Based on the FIC indexes and clinical importance, 3 combinations were selected to evaluate their effects on the virulence factors of these bacteria. The in vitro cytotoxicity of GA and hamamelitannin in the Rattus norvegicus (IEC-6) cell line were evaluated. Results: Phenolic compounds demonstrated considerable antibacterial effects as the minimum inhibitory concentrations (MICs) of epigallocatechin, GA and hamamelitannin found against different strains were (32–1024), (128–1024) and (512–≥2048) μg/mL, respectively. The FIC indexes of the combined antibacterials against these strains were 0.281–1.016. The ultrastructural morphology and time-kill assays showed that the GA-ceftiofur combination, and hamamelitannin-erythromycin and GA-ampicillin combinations more efficiently inhibited the growth of S. Typhimurium and E. coli, respectively, compared to the individual antibiotics. Biofilm viability and the swimming and swarming motilities of S. Typhimurium in the presence of GA-ceftiofur and E. coli in the presence of the hamamelitannin-erythromycin and GA-ampicillin combinations were more competently inhibited than individual antimicrobials. The 50% inhibitory concentrations (IC50) of GA and hamamelitannin in IEC-6 cells were 564.55 μM and 988.54 μM, respectively. Conclusions: The phenolic compounds increase the efficacy of existing antibiotics might be by disrupting virulence factors. We can conclude that these antibacterial combinations are safe and can be potential medications to treat S. Typhimurium, E. coli and S. aureus infections in animals and humans. Further study to confirm this effect in in vivo system and to determine the precise mechanism of action should be undertaken to establish these combinations as medications.

scholarly journals Effect of Phaseolus vulgaris on E. coli induced peritonitis and bacteraemia in mice

2019 ◽  
Vol 9 (4-s) ◽  
pp. 310-314
Author(s):  
Dipika Khadagwanshi ◽  
Sonkia Trivedi ◽  
Preeti Patel ◽  
Megha Jha
Keyword(s):  
Antioxidant Activity ◽  
Antibacterial Activity ◽  
Phenolic Compounds ◽  
Phaseolus Vulgaris ◽  
Methanolic Extract ◽  
Health Benefits ◽  
E Coli ◽  
Peritoneal Infection ◽  
Dose Dependent

Infectious or non-infectious peritonitis leads to systemic inflammation due to violation of the peritoneum which is often fatal. Evidences suggest that common bean (Phaseolus vulgaris L.) is a source of nutrients and contains phenolic compounds having antioxidant activity and its consumption has been linked with improved health benefits. The aim of the present investigation was evaluate the in vitro antibacterial, antioxidant activity and protective potential of the methanolic extract of P. vulgaris in E. coli induced model of peritonitis in albino wistar rats. Rats were pre-treated with 200 mg/kg and 400 mg/kg/bwt dose for 3 days and fourth day with E. coli (1×108 CFU/ml) strain and consecutively 3 days treatment. Mortality was monitored for 14 days. After the death of rats or completion of the experiment rats were sacrifice and kidney were used for our protocol. Colonies were count and statically analysis was done. Results showed dose dependent antibacterial activity. Thus the methanolic extract of P. vulgaris exhibited significant protection against E. coli induced peritonitis in normal rats. It significantly reduced the viable cells of E. coli when inoculated in rats. Activity is attributed to flavonoids and phenolic compounds. The present study thus suggests that methanolic extract of P. vulgaris significantly reverses peritoneal infection by E. coli in rats. It can be suggest that this medicinal formulation will be used as herbal medicine with no side effects. The high content of phenolic compounds, antioxidant activity and antibacterial activity of P. vulgaris indicate that they may impart health benefits when consumed and should be regarded as a valuable source of antioxidants. Thus, consumption of P. vulgaris seed along with coats might be recommended to gaining better nutritive benefits. Keywords:  P. vulgaris, Peritonitis, Antioxidant, Antibacterial, E. coli

scholarly journals Preliminary phytochemical screening and in vitro antibacterial activity of Plumbago indica (Laal chitrak) root extracts against drug-resistant Escherichia coli and Klebsiella pneumoniae

2021 ◽  
Vol 6 (1) ◽  
pp. 435-444
Author(s):  
Salim Faruk Bashir ◽  
Gaurav Kumar
Keyword(s):  
Escherichia Coli ◽  
Antibacterial Activity ◽  
Klebsiella Pneumoniae ◽  
Aqueous Extract ◽  
Drug Resistant ◽  
Phytochemical Screening ◽  
E Coli ◽  
Root Extracts ◽  
Plumbago Indica

Abstract Drug resistance is one of the problems affecting the world where drug-resistant Escherichia coli and Klebsiella pneumoniae have been shown to be ubiquitous, frequently isolated from foods and commonly associated with surgical site infection in hospitals worldwide. The aims of this work were to analyze the antibacterial activity of root extracts of the plant obtained by serial extraction (using petroleum ether, chloroform, methanol, and water) and by in vitro techniques and preliminary screen phytochemicals present in the extract by qualitative means. Fresh roots of Plumbago indica were collected, oven-dried, and extracted using Soxhlet apparatus; antibacterial activity, minimum inhibitory concentrations (MICs), and minimum bactericidal concentrations (MBCs) of the active extract were evaluated by standard methods against clinically isolated drug-resistant E. coli and K. pneumoniae; preliminary phytochemical screening was taken to detect the presence of alkaloids, saponins, flavonoids, steroids, tannins, reducing sugars, phenolics, protein, and oil and fat; and bioactive compounds were detected by GCMS analysis of the active extracts. Determination of antibacterial activity showed that the test organisms were susceptible to methanol and aqueous extracts only. MIC of methanolic extract was found to be 20 µg/mL on both E. coli and K. pneumoniae, while aqueous extract had MIC of 10 and 20 µg/mL on E. coli and K. pneumoniae, respectively. Preliminary phytochemical screening showed the presence of all the above-mentioned phytochemicals except oil and fat. The significance of this work is to find a lasting solution to the current problem of emerging drug-resistant bacteria (E. coli and K. pneumoniae) through the use of extracts obtained from P. indica which have long history of use as traditional medicine. The methanolic and aqueous extract can be recommended as an alternative and candidates for drug development against drug-resistant E. coli and K. pneumoniae.

scholarly journals Antibacterial Activity of Four Plant Extracts Extracted from Traditional Chinese Medicinal Plants against Listeria monocytogenes, Escherichia coli, and Salmonella enterica subsp. enterica serovar Enteritidis

2020 ◽  
Vol 8 (6) ◽  
pp. 962
Author(s):  
R.L. McMurray ◽  
M.E.E. Ball ◽  
M.M. Tunney ◽  
N. Corcionivoschi ◽  
C. Situ
Keyword(s):  
Escherichia Coli ◽  
Antibacterial Activity ◽  
Listeria Monocytogenes ◽  
Plant Extracts ◽  
Bactericidal Activity ◽  
Salmonella Enteritidis ◽  
Antibacterial Properties ◽  
E Coli ◽  
Chinese Medicinal Plants

The worldwide ethnobotanical use of four investigated plants indicates antibacterial properties. The aim of this study was to screen and determine significant antibacterial activity of four plant extracts in vitro and in a poultry digest model. Using broth microdilution, the concentrations at which four plant extracts inhibited Listeria monocytogenes, Salmonella enteritidis, and Escherichia coli over 24 h was determined. Agrimonia pilosa Ledeb, Iris domestica (L.) Goldblatt and Mabb, Anemone chinensis Bunge, and Smilax glabra Roxb all exhibited a minimum inhibitory concentration (MIC) of 62.5 mg/L and a minimum bactericidal concentration (MBC) of 500 mg/L against one pathogen. A. pilosa Ledeb was the most effective against L. monocytogenes and E. coli with the exception of S. enteritidis, for which A. chinensis Bunge was the most effective. Time–kills of A. pilosa Ledeb and A. chinensis Bunge against L. monocytogenes, E. coli and S. enteritidis incubated in poultry cecum were used to determine bactericidal activity of these plant extracts. A. chinensis Bunge, significantly reduced S. enteritidis by ≥ 99.99% within 6 h. A. pilosa Ledeb exhibited effective significant bactericidal activity within 4 h against L. monocytogenes and E. coli. This paper highlights the potential of these plant extracts to control pathogens commonly found in the poultry gastrointestinal tract.

scholarly journals AKTIVITAS ANTIBAKTERI EKSTRAK METANOL BATANG BIDARA LAUT (Strychnos ligustrina) TERHADAP BAKTERI PATOGEN

2019 ◽  
Vol 19 (1) ◽  
Author(s):  
Edy Kurniawan ◽  
Dwi Soelistya Dyah Jekti ◽  
Lalu Zulkifli
Keyword(s):  
Escherichia Coli ◽  
Staphylococcus Aureus ◽  
Antibacterial Activity ◽  
Pathogenic Bacteria ◽  
Inhibitory Concentration ◽  
Methanol Extract ◽  
Klebsiella Pneumonia ◽  
E Coli

Abstract : Strychnos ligustrina stem has been empirically used by the people of West Nusa Tenggara and Bali in the treatment of malaria, tooth ache and diarrhea, but there is no scientific data that supports it. This study aims to determine and prove the antibacterial activity of Strychnos ligustrina methanol extract to pathogenic bacteria in vitro and in vivo. This research is an experimental study conducted by measuring the inhibition zone (mm) growth of pathogenic bacteria, determining minimum inhibitory concentration (MIC) and minimum killing concentration (MKC) in vitro, and determining the percentage of antibacterial activity of methanol extract of S. ligustrina stem in vivo. The experiment was conducted using 4 groups of concentrations of S. ligustrina stem methanol extract in an in vitro study of 25, 50, 75, and 100% with ciprofloxacin as a positive control and aquadest as a negative control. In vivo studies experiments were carried out using 6 treatment groups of test animals male mice Balb / c (Mus musculus). The in vitro test results showed that methanol extract of S. ligustrina stems was able to inhibit the growth of pathogenic bacteria with medium categories of clinical isolates of Staphylococcus aureus and categories of weaks to Klebsiella pneumonia and Escherichia coli isolates. The minimum inhibitory concentration (MIC) for S. aureus and K. pneumonia bacteria isolates was at a concentration of 25% while for E. coli isolates at a concentration of 30%. The methanol extract of the S. ligustrina stem has no killing power against the pathogenic bacteria tested. Antibacterial activity in vivo was able to inhibit the growth of S. aureus pathogenic bacteria by 6.60% (at 25% concentration), 8.62% (at 50% concentration), and 17.31% (at 100% concentration), against K. pneumonia was 11.85% (at 25% concentration), 51.21% (at 50% concentration), and 65.92% (at 100% concentration), against E. coliat 19.18% (at concentration 25%), 29.98% (at 50% concentration), and 40.88% (at 100% concentration). Methanol extract of S. ligustrina stem proved to have antibacterial activity in vitro and in vivo. Key words: Srychnos ligustrina, pathogenic bacteria, antibacterial, in vitro, in Vivo. Abstrak : Strychnos ligustrina secara empiris  telah digunakan oleh masyarakat Nusa Tenggara Barat dan Bali dalam pengobatan penyakit malaria, sakit gigi, dan diare, tetapi belum ada data ilmiah yang mendukung. Penelitian ini bertujuan untuk menentukan dan membuktikan aktivitas antibakteri ekstrak metanol batang bidara laut terhadap bakteri patogen secara in vitrodan in vivo. Penelitian ini merupakan penelitian eksperimental yang dilakukan dengan mengukur zona hambat (mm) pertumbuhan bakteri patogen, menentukan konsentrasi hambat minimum (KHM) dan konsentrasi bunuh minimum (KBM) secara in vitro, serta menentukan persentase aktivitas antibakteri ekstrak metanol batang bidara laut secara in vivo. Percobaan dilakukan menggunakan 4 kelompok konsentrasi ekstrak metanol batang bidara laut pada penelitian in vitro yaitu 25, 50, 75, dan 100% dengan ciprofloxacin sebagai kontrol positif serta aquadest sebagai kontrol negatif. Pada penelitian in vivo percobaan dilakukan menggunakan 6 kelompok perlakuan hewan uji mencit jantan galur Balb/c (Mus musculus). Hasil uji in vitro menunjukkan ekstrak metanol batang bidara laut mampu menghambat pertumbuhan bakteri patogen dengan kategori sedang terhadap Staphylococcus aureus isolat klinis dan kategori lemah terhadap Klebsiella pneumonia dan Escherichia coli isolat klinis. Nilai konsentrasi hambat minimum (KHM) untuk isolat bakteri S. aureus dan K. pneumoniae adalah pada konsentrasi 25% sedangkan untuk isolat E. coli pada konsentrasi 30%. Ekstrak metanol batang bidara laut tidak memiliki daya bunuh terhadap bakteri patogen yang diuji. Aktivitas antibakteri secara in vivo mampu menghambat pertumbuhan bakteri patogen S. aureus sebesar 6,60% (pada konsentrasi 25%), 8,62% (pada konsentrasi 50%), dan 17,31% (pada konsentrasi 100%), terhadap K. pneumonia sebesar 11,85% (pada konsentrasi 25%), 51,21% (pada konsentrasi 50%), dan 65,92% (pada konsentrasi 100%),   terhadap E. coli sebesar 19,18% (pada konsentrasi 25%), 29,98% (pada konsentrasi 50%), dan 40,88% (pada konsentrasi 100%). Ekstrak metanol batang bidara laut terbukti memiliki aktivitas antibakteri secara in vitro dan in vivo. Kata kunci: Srychnos ligustrina, bakteri patogen, antibakteri, in vitro, in vivo

In silico and in vitro studies of Imidazolium ionic liquids as effective antibacterial agents against multidrug resistant Escherichia coli strains

2020 ◽  
Vol 16 ◽  
Author(s):  
Diana Hodyna ◽  
Vasyl Kovalishyn ◽  
Ivan Semenyuta ◽  
Volodymyr Blagodatny ◽  
Sergiy Rogalsky ◽  
...  
Keyword(s):  
Escherichia Coli ◽  
Antibacterial Activity ◽  
Ionic Liquids ◽  
Chain Length ◽  
Active Site ◽  
Alkyl Chain ◽  
Multidrug Resistant ◽  
Alkyl Chain Length ◽  
E Coli

Background: Escherichia coli especially its multiresistant strains as the common foodborne pathogens cause blood stream infections, nosocomial pneumonia, infections of the skin and soft tissues. Therefore, the search for new effective biologically active compounds has been rapidly increasing in recent few decades. In this paper, we describe Quantitative Structure-Activity Relationships (QSAR) studies, molecular docking and in vitro antibacterial activity evaluation of series imidazolium-based ionic liquids (ILs) against E. coli spp. Methods: 2D fragment-based, classification and regression QSAR models were created using machine learning methods and types of descriptors via the OCHEM server. Biological testing of series of synthesized imidazolium ILs with predicted activity was performed by disc diffusion method. The most typical structures of symmetric and asymmetric ILs with high anti-E.coli activity (1e, 1h) were docked into the active site of enoylacyl carrier protein reductase (ENR) in E. coli. Results: Symmetric imidazolium ILs with C8 alkyl chain length demonstrated the highest antibacterial activity in comparison to the high antibacterial potential of asymmetric ILs with C12 alkyl chain length against drug-sensitive and drug-resistant E. coli strains including hemolytic E. coli. It should be noted that symmetric ILs with C6 or C9 alkyl chain length have the slightly lower activity against certain E. coli strains. The key role in the binding of compounds (1e, 1h) in the E. coli ENR active site associated with the NAD molecule and the amino acid residue Tyr146. Conclusion: The highly active symmetric and asymmetric imidazolium ILs can be considered as promising drug-candidates effective against E. coli spp. pathogens including multidrug resistant strains.

scholarly journals Antimicrobial assesment of aroylhydrazone derivatives in vitro

2019 ◽  
Vol 69 (2) ◽  
pp. 277-285 ◽  
Author(s):  
Saša Polović ◽  
Vanja Ljoljić Bilić ◽  
Ana Budimir ◽  
Darko Kontrec ◽  
Nives Galić ◽  
...  
Keyword(s):  
Escherichia Coli ◽  
Staphylococcus Aureus ◽  
Antibacterial Activity ◽  
Antifungal Activity ◽  
Biofilm Formation ◽  
Good Activity ◽  
E Coli ◽  
Fluconazole Resistant ◽  
Gentamicin Sulphate

Abstract Aroylhydrazones 1–13 were screened for antimicrobial and antibiofilm activities in vitro. N′-(2-hydroxy-phenylmethylidene)-3-pyridinecarbohydrazide (2), N′-(5-chloro-2-hydroxyphenyl-methylidene)-3-pyridinecarbohydrazide (10), N′-(3,5-chloro-2-hydroxyphenylmethylidene)-3-pyridinecarbohydrazide (11), and N′-(2-hydroxy-5-nitrophenylmethylidene)-3-pyridinecarbohydrazide (12) showed antibacterial activity against Escherichia coli, with MIC values (in µmol mL−1) of 0.18–0.23, 0.11–0.20, 0.16–0.17 and 0.35–0.37, resp. Compounds 11 and 12, as well as N′-(2-hydroxy-3-methoxyphenylmethylidene)-3-pyridinecarbohydrazide (6) and N′-(2-hydroxy-5- methoxyphenylmethylidene)-3-pyridinecarbohydrazide (8) showed antibacterial activity against Staphylococcus aureus, with the lowest MIC values of 0.005–0.2, 0.05–0.12, 0.06–0.48 and 0.17–0.99 µmol mL−1. N′-(2-hydroxy-5-methoxyphenylmethylidene)-3-pyridinecarbohydrazide (7) showed antifungal activity against both fluconazole resistant and susceptible C. albicans strains with IC90 range of 0.18–0.1 µmol mL−1. Only compound 11 showed activity against C. albicans ATCC 10231 comparable to the activity of nystatin (the lowest MIC 4.0 ×10−2 vs. 1.7 × 10−2 µmol mL−1). Good activity regarding multi-resistant clinical strains was observed for compound 12 against MRSA strain (MIC 0.02 µmol mL−1) and compounds 2, 6 and 12 against ESBL+ E. coli MFBF 12794, with the lowest MIC for compound 12 (IC50 0.16 µmol mL−1). Anti-biofilm activity was found for compounds 2 (MBFIC 0.015–0.02 µmol mL−1 against MRSA) and 12 (MBFIC 0.013 µmol mL−1 against EBSL+ E. coli). In the case of compound 2 against MRSA biofilm formation, MBFIC values were comparable to those of gentamicin sulphate, whereas in the case of compound 12 and EBSL+ E. coli even more favourable activity compared to gentamicin was observed.

Substituted 4-Formyl-2H-chromen-2-ones: Their Reaction with N-(2,3,4,6-Tetra-Oacetyl- β-D-galactopyranosyl)thiosemicarbazide, Antibacterial and Antifungal Activity of Their Thiosemicarbazone Products

2020 ◽  
Vol 24 (19) ◽  
pp. 2272-2282
Author(s):  
Vu Ngoc Toan ◽  
Nguyen Minh Tri ◽  
Nguyen Dinh Thanh
Keyword(s):  
Escherichia Coli ◽  
Staphylococcus Aureus ◽  
Candida Albicans ◽  
Selenium Dioxide ◽  
Antibacterial And Antifungal Activity ◽  
E Coli ◽  
Antibacterial And Antifungal Activities ◽  
Alkyl Ethers ◽  
Antibacterial And Antifungal

Several 6- and 7-alkoxy-2-oxo-2H-chromene-4-carbaldehydes were prepared from corresponding alkyl ethers of 6- and 7-hydroxy-4-methyl-2-oxo-2H-chromen-2-ones by oxidation using selenium dioxide. 6- and 7-Alkoxy-4-methyl-2H-chromenes were obtained with yields of 57-85%. Corresponding 4-carbaldehyde derivatives were prepared with yields of 41-67%. Thiosemicarbazones of these aldehydes with D-galactose moiety were synthesized by reaction of these aldehydes with N-(2,3,4,6-tetra-O-acetyl-β-Dgalactopyranosyl) thiosemicarbazide with yields of 62-74%. These thiosemicarbazones were screened for their antibacterial and antifungal activities in vitro against bacteria, such as Staphylococcus aureus, Escherichia coli, and fungi, such as Aspergillus niger, Candida albicans. Several compounds exhibited strong inhibitory activity with MIC values of 0.78- 1.56 μM, including 8a (against S. aureus, E. coli, and C. albicans), 8d (against E. coli and A. niger), 9a (against S. aureus), and 9c (against S. aureus and C. albicans).

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