Antibioticos

Páginas: 11 (2579 palabras) Publicado: 8 de diciembre de 2012
Antibiotics:
Antibiotics are specific chemical substances derived from or produced by living organisms that are capable of inhibiting the life processes of other organisms. The first antibiotics were isolated from microorganisms but some are now obtained from higher plants and animals. Over 3,000 antibiotics have been identified but only a few dozen are used in medicine.
Penicillins
Thepenicillins were the first antibiotics discovered as natural products from the mold Penicillium
Penicillins as well as cephalosporins are called beta-lactam antibiotics and are characterized by three fundamental structural requirements: the fused beta-lactam structure (shown in the blue and red rings, a free carboxyl acid group (shown in red bottom right), and one or more substituted amino acid sidechains (shown in black). The lactam structure can also be viewed as the covalent bonding of pieces of two amino acids - cysteine (blue) and valine (red).

Penicillin Mode of Action - Enzyme Inhibition:
All penicillin derivatives produce their bacteriocidal effects by inhibition of bacterial cell wall synthesis. Specifically, the cross linking of peptides on the mucosaccharide chains isprevented. If cell walls are improperly made cell walls allow water to flow into the cell causing it to burst.
Resemblances between a segment of penicillin structure and the backbone of a peptide chain have been used to explain the mechanism of action of beta-lactam antibiotics. The structures of a beta-lactam antibiotic and a peptide are shown on the left for comparison. Follow the trace of the redoxygens and blue nitrogen atoms.

Beta-lactam antibiotic
β-lactam antibiotics are indicated for the prophylaxis and treatment of bacterial infections caused by susceptible organisms. At first, β-lactam antibiotics were mainly active only against Gram-positive bacteria, yet the recent development of broad-spectrum β-lactam antibiotics active against various Gram-negative organisms has increased theirusefulness.
Beta-lactam antibiotics inhibit the growth of sensitive bacteria by inactivating enzymes located in the bacterial cell membrane, which are involved in the third stage of cell wall synthesis. It is during this stage that linear strands of peptidoglycan are cross-linked into a fishnet-like polymer that surrounds the bacterial cell and confers osmotic stability in the hypertonic milieuof the infected patient. Beta-lactams inhibit not just a single enzyme involved in cell wall synthesis, but a family of related enzymes (four to eight in different bacteria), each involved in different aspects of cell wall synthesis. These enzymes can be detected by their covalent binding of radioactively-labeled penicillin (or other beta-lactams) and hence have been called penicillin bindingproteins (PBPs).
Different PBPs appear to serve different functions for the bacterial cell. As an example, PBP2 in Escherichia coli is important in maintaining the rod-like shape of the bacillus, while PBP3 is involved in septation during cell division. Different beta-lactam antibiotics may preferentially bind to and inhibit certain PBPs more than others. Thus, different agents may producecharacteristic effects on bacterial morphology and have different efficacies in inhibiting bacterial growth or killing the organism.
β-lactam antibiotics have a β-lactam ring in their structure. The effectiveness of these antibiotics relies on their ability to reach the PBP intact and their ability to bind to the PBP. Hence, there are 2 main modes of bacterial resistance to β-lactams, as discussed below.The first mode of β-lactam resistance is due to enzymatic hydrolysis of the β-lactam ring. If the bacteria produces the enzymes β-lactamase or penicillinase, these enzymes will break open the β-lactam ring of the antibiotic, rendering the antibiotic ineffective. The genes encoding these enzymes may be inherently present on the bacterial chromosome or may be acquired via plasmid transfer, and...
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