Staphylococcus, inhibition

Echinomycin (131) has been shown to be an antitumor agent and to have antiviral and antibacterial properties. Its structure elucidation represents a triumph for and mass spectral studies (75JA2497). It has been demonstrated that echinomycin functions by inhibiting RNA synthesis in organisms such as Staphylococcus aureus. Echinomycin, levomycin and actinoleutin are members of the quinoxaline-peptide antibiotic family and all contain one or more quinoxaline rings (67MI21402). 

It is now believed that many of our useful drugs exert their beneficial action by the inhibition of enzyme activity in bacteria. Some bacteria, such as staphylococcus, require for their growth the simple organic compound poraaminobenzoic... 

Small GTPases of the Rho family are ADP-ribosylated (e.g., at Asn4l of RhoA) and inactivated by C3-like toxins from Clostridium botulinum, Clostridium limosum, and Staphylococcus aureus. These proteins have a molecular mass of 23-30 kDa and consist only of the enzyme domain. Specific inhibition of Rho functions (Rho but not Rac or Cdc42 are targets) is the reason why C3 is widely used as a pharmacological tool [2]. 

Oxazolidinones are a new class of synthetic antimicrobial agents, which have activity against many important pathogens, including methicillin-resistant Staphylococcus aureus and others. Oxazolidinones (e.g. linezolid or eperezolid) inhibit bacterial protein synthesis by inhibiting the formation of the 70S initiation complex by binding to the 50S ribosomal subunit close to the interface with the 3OS subunit. 

In some cases, catechins can also act in synergistic mode when used in association with currently used antibiotic molecules (Table 2). EGCG exhibited synergy with /3-lactams. Sudano Roccaro et al. [73] found that this compound is able to reverse tetracycline resistance in Staphylococcus epidermidis and S. aureus isolates. This synergistic interaction has been explained by inhibition of tetracycline efflux pump activity in microbial cells resulting in an... 

Deformylation of nascent polypeptides has been shown to be a function essential for growth in E. coli, Staphylococcus aureus and Streptococcus pneumoniae [15-18]. Moreover, antibacterial mode of action studies, using S. pneumoniae or S. aureus strains in which the expression of PDF is controlled by regulatable promoters, have shown that the antibacterial activity of PDF inhibitors is due to their inhibition of the PDF enzyme, as the susceptibility of the strains to these compounds is dependent on the amount of protein present in the cell [19-21]. These results further validate PDF as a target for novel antibiotics. 

Mn2+ active transport system in Staphylococcus aureus. These metal-microbe interactions result in decrease microbial growth, abnormal morphological changes, and inhibition of biochemical processes in individual (Akmal et al. 2005a,b). The toxic effects of metals can be seen on a community level as well. In response to metal toxicity, overall community numbers and diversity decrease. Soil is a living system where all biochemical activities proceed through enzymatic processes. Heavy metals have also adverse effects on enzyme activities (Fig. 1). 

Since the tragic human exposure to diethyltin salts for the therapy of an infectious skin disease by Staphylococcus in France in the 1950s, the toxic and biochemical effects of many of these derivatives have been explored. Di- and tri-ethyltin salts have been demonstrated to have pronounced effects on intermediary metabolism in brain and liver. These effects have been suggested to be due to inhibition of the mitochondrial functions9,27. 

Finally, indolo[l,2-r ]benzo[l,2,3]triazines 46 proved to be fairly potent and selective inhibitors of Streptococcus and Staphylococcus, up to 80 times more potent than the reference drug streptomycin, and inhibited the growth of the above Gram-positive bacteria at concentrations far lower than those cytotoxic for animal cells <1999JME2561>. 

Staphylococcus aureus is known for its ability to produce a variety of toxins and many disease syndromes. One of the most frequently observed diseases is staphylococcal tonsillitis. These bacteria are frequently present on tonsils of healthy carriers. Patients that are affected by tonsillitis swallow staphylococci hidden in tonsil crypts. However, in this case staphylococci do not cause any gastrointestinal symptoms in the host organism, even if they enter the gastrointestinal tract. The barrier of gastric juice and conditions in a small intestine inhibit the outgrowth of staphylococci and toxin production -gastroenteritis is caused solely by a toxin produced outside the host organism. 

Poly(aorylonitrile-co-oxazolidinone), 2 = poly(vinyl aoetate-co-oxazolidinone), 3 = poly(acrylonitrile-g-oxazolidinone), 4 = poly(vinyl aoetate-g-oxazolidinone), 5 = poly(vinyl alcohol-g-oxazolidinone). Coatings were soaked in 3,000 mg/L free ohiorine. Time after ohiorination when biooidal effioaoy was measured. TABLE 2. Zones of inhibition of A/-Chioramine Poiymerio Biooidai Coatings on Fabric against Staphylococcus aureus. ... 

The bacterium Staphylococcus aureus, which is a major cause of infection in the developed countries, is now resistant to most antibiotics. It is usually present on the skin, where it causes no problems, but it can invade the body through cuts and wounds, including those caused by surgery. These bacteria are now prevalent in many hospitals, so that infection is a major problem for the medical staff in hospitals. The resistant bacterium is known as methicillin-resistant Staphylococcus aureus (MRSA). It is also known in the mass media as the super bug . Penicillin kiUs bacteria because the P-lactam group in the antibiotic inhibits a reaction that is essential for bacterial ceU wall production. Consequently, the bacteria cannot proliferate. Resistance to penicillin in many bacteria is due to production of an enzyme, p-lactamase, that degrades P-lactams. The antibiotic methicillin is one of a group of semisynthetic penicillins in which the P-lactam group is not... 

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