scholarly journals Structure-Based Discovery of Inhibitors Against MurE in Methicillin-Resistant Staphylococcus Aureus

2019 ◽  
Vol 35 (2) ◽  
pp. 618-625
Author(s):  
Junie B. Billones ◽  
Marielle Alyanna T. Bangalan
Keyword(s):  
Staphylococcus Aureus ◽  
Methicillin Resistant Staphylococcus Aureus ◽  
Drug Repurposing ◽  
Health Concern ◽  
Drug Candidate ◽  
Drug Resistant ◽  
Public Health Concern ◽  
Methicillin Resistant ◽  
Peptidoglycan Biosynthesis ◽  
Experimental Drugs

The rise of superbugs is a serious public health concern. It is estimated to kill around 10 million people a year by 2050 and will overtake cancer as the number one cause of death worldwide. One of the most prevalent drug-resistant pathogen is Methicillin-resistant Staphylococcus aureus (MRSA). Intense efforts have been devoted to the discovery and development of anti-MRSA drug. Muramyl ligase E (MurE), an enzyme involved in the peptidoglycan biosynthesis of the bacterial cell wall, is a highly druggable target in MRSA. In this study, virtual screening of approved and experimental drugs in the Drug Bank database was performed based on a pharmacophore derived from the structure of MurE. Molecular docking was subsequently done with the top hits. The top hits and their derivatives were further evaluated for their predicted pharmacokinetics properties. This drug repurposing effort has identified four experimental drugs that are predicted to bind more strongly to MurE than the drug Fosfomycin. One of the top hits, DB01758, exhibited all the characteristics of a good drug candidate, albeit it is likely to be non-biodegradable.

scholarly journals Virulent gene detection and antibiogramic profile of methicillin resistant Staphylococcus aureus isolated from birds of a poultry farm

2020 ◽  
Vol 22 (2) ◽  
pp. 045-055
Author(s):  
I.M. Omoruyi ◽  
I.C. Obodo ◽  
E.O. Obukohwo ◽  
F.E. Otoide
Keyword(s):  
Public Health ◽  
Staphylococcus Aureus ◽  
Methicillin Resistant Staphylococcus Aureus ◽  
Meca Gene ◽  
Health Concern ◽  
Drug Resistant ◽  
Methicillin Resistant ◽  
Poultry Birds ◽  
Poultry Droppings ◽  
Potential Public Health

Methicillin-resistant strains of Staphylococcus aureus (MRSA) are gaining global attention, largely due to their potential public health significance. In  the current study, we investigated the prevalence of MRSA in poultry birds from Benson Idahosa University farm. Twenty-five samples each from poultry droppings, cloacae and nostrils were collected aseptically and screened for total heterotrophic and Staphylococcus aureus counts usingstandard culture-based methods. Phenotypic identification of MRSA was carried out using mannitol-oxacillin agar, while the presence of virulence genes (mecA, entA, entB, entC, SCCmec (I, II, III) and tsstI) was investigated by polymerase chain reaction using specific primers. Also, the  antibiogramic activities and multi drug-resistant index were investigated against 6 clinically relevant antibiotics (oxacillin (1 μg), vancomycin (30 μg), ceftazidime (30 μg), ceftriaxone (30 μg), amikacin (30 μg) and ofloxacin (5 μg)). The results showed that total heterotrophic  bacterial and S. aureus are prevalent in poultry birds, with mean heterotrophic counts of 243.08 ± 21.01 × 105 cfu, 169.37 ± 25.30 × 105 cfu and 216 ± 15.89× 105 cfu for poultry droppings, cloacae and nostrils respectively and mean S. aureus counts of 176.30 ± 28.85 × 105 cfu for poultry droppings, 16.52 ± 11.92 × 105 cfu for cloacae and 5 2.72 ± 0.41 × 105 cfu for nostrils. Interestingly, 93.33%, 25% and 10.5% of S. aureus isolated from the droppings, cloacae and nostrils respectively were methicillin resistant. The antibiogramic activities showed the majority of isolates to be multi drug-resistant, while only one MRSA (from poultry droppings) had the mecA gene. The presence of these isolates in poultry birds is of a potential public health concern as they may travel through the food chain and efforts should be made by poultry owners to avoid the indiscriminate use of antibiotics. Keywords: Methicillin-Resistant Staphylococcus aureus; Poultry; Public Health; Virulence Gene

scholarly journals Anti-methicillin resistant Staphylococcus aureus (MRSA) activity of an acetone extract from the leaves of Canarium odontophyllum (Miq.)

2018 ◽  
Vol 7 (3) ◽  
pp. 225-229
Author(s):  
Nur Amira Mohd Shamsuddin ◽  
◽  
Dayang Fredalina Basri ◽  
Keyword(s):  
Staphylococcus Aureus ◽  
Methicillin Resistant Staphylococcus Aureus ◽  
Acetone Extract ◽  
Health Concern ◽  
Antimicrobial Drugs ◽  
Methicillin Resistant ◽  
Bacteriostatic Action ◽  
Broth Microdilution Method ◽  
Canarium Odontophyllum ◽  
Time Kill

Methicillin-resistant Staphylococcus aureus (MRSA) is a global health concern that has caused nosocomial and community infections over the past decade. The emergence of multi-drug resistant strains and limitations of present antimicrobial drugs have led to continuous search for natural products as curative agents for MRSA infections. Canarium odontophyllum Miq., locally known as dabai, has been considered an alternative phytotherapeutic treatment for MRSA. The aim of this study was to evaluate the bacteriostatic activity of an acetone extract from C. odontophyllum leaves against MRSA. The minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) of the extract against the ATCC 33591 and Mu50 strains were determined using the broth microdilution method, and a time-kill assay was employed to assess the type of bacteriostatic action of the extract against the Mu50 strain only. The MIC and MBC values of the extract against Mu50 were 312.5 µg/ml and 625 µg/ml, respectively, whereas the MIC and MBC values for ATCC 33591 were 625 µg/ml and 1,250 µg/ml, respectively, confirming the bacteriostatic effect against both MRSA strains. A time-kill assay showed that the acetone extract of C. odontophyllum leaves exhibited concentrationdependent bacteriostatic action against the Mu50 strain at 1/2× MIC, 1× MIC and 2× MIC. However, the extract was bactericidal only at the highest concentration (4× MIC) with a reduction in cell viability of more than 3 log10 within 24 hours. These findings confirm that an acetone extract from C. odontophyllum leaves inhibited growth of MRSA at low concentration and could be utilised as an alternative anti-MRSA agent in immune uncompromised hosts

scholarly journals Antibacterial activity of Taxodium ascendens Diterpenes against Methicillin-resistant Staphylococcus aureus

2014 ◽  
Vol 9 (8) ◽  
pp. 1934578X1400900 ◽  
Author(s):  
Courtney M. Starks ◽  
Vanessa L. Norman ◽  
Russell B. Williams ◽  
Matt G. Goering ◽  
Stephanie M. Rice ◽  
...  
Keyword(s):  
Staphylococcus Aureus ◽  
Antibacterial Activity ◽  
Bacterial Infections ◽  
Methicillin Resistant Staphylococcus Aureus ◽  
Clinical Isolates ◽  
Drug Resistant ◽  
Methicillin Resistant

One new and seven known diterpenes were identified from an antibacterial chromatographic fraction of Taxodium ascendens. Of these, demethylcryptojaponol (2), 6-hydroxysalvinolone (3), hydroxyferruginol (4), and hinokiol (5) demonstrated potent activity against clinical isolates of methicillin-resistant Staphylococcus aureus (MRSA). These compounds represent a class of synthetically accessible compounds that could be further developed for treatment of drug-resistant bacterial infections.

scholarly journals Novel organophosphorus aminopyrimidines as unique structural DNA-targeting membrane active inhibitors towards drug-resistant methicillin-resistant Staphylococcus aureus

MedChemComm ◽  
2018 ◽  
Vol 9 (9) ◽  
pp. 1529-1537 ◽  
Author(s):  
Di Li ◽  
Rammohan R. Yadav Bheemanaboina ◽  
Narsaiah Battini ◽  
Vijai Kumar Reddy Tangadanchu ◽  
Xian-Fu Fang ◽  
...  
Keyword(s):  
Staphylococcus Aureus ◽  
Molecular Modeling ◽  
Methicillin Resistant Staphylococcus Aureus ◽  
Antibacterial Mechanism ◽  
Drug Resistant ◽  
Methicillin Resistant ◽  
Dna Targeting

Molecular modeling of organophosphorus aminopyrimidine and the possible antibacterial mechanism.

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