Penicillin; beta-lactamase

Presented by group 4
 Table of contents 

Introduction Type of inhibition Target enzyme  Mechanism  Medicinal uses Additional info. 
 Introduction
  Penicillin were the first antibiotics to be grown and used
against pathogenic bacteria in may human beings . 
 In 1928 Scottish bacteriologist Alexander Fleming first
observed that colonies of the bacterium Staphylococcus
aureus failed to grow in those areas of a culture that had
been accidentally contaminated by the green mold 
Penicillium notatum. He isolated the mold, grew it in a
fluid medium, and found that it produced a substance
capable of killing many of the common bacteria that
infect humans.
ü Types: 
 Penicillin is a secondary metabolite produced by certain • aminopenicillins
bacteria, which is used an antibiotic. Antibiotic' literally • antipseudomonal peni
means 'against life' - but antibiotics only kill life that is cillins
harmful to living creatures, i.e. bacteria.  • beta-lactamase inhibit
 A bacterial infection is caused by millions of tiny ors
bacteria that are trying to survive and in multiply the • natural penicillins
body. An antibiotic attacks and kill these bacteria. 
 Before the development of penicillin, many people
• penicillinase resistant
suffered and died from bacterial infections that are no penicillins
longer considered dangerous today.
Type of
inhibition 
Ø Penicillin, is a competitive inhibitor that blocks the
active site of an enzyme that many bacteria use to
construct their cell walls. 
Ø Penicillin binds at the active site of the
Target enzyme
transpeptidase enzyme that cross-links the
 Penicillin kills susceptible bacteria by
peptidoglycan strands. It does this by mimicking the
specifically inhibiting the transpeptidase that
D-alanyl-D-alanine residues that would normally
catalyzes the final step in cell wall
bind to this site. Penicillin irreversibly inhibits the
biosynthesis, the cross-linking
enzyme transpeptidase by reacting with a serine
of peptidoglycan.
residue in the transpeptidase. This reaction is
 Penicillin is a competitive inhibitor that
irreversible and so the growth of the bacterial cell
blocks the active site of an enzyme
wall is inhibited.
that many bacteria use to construct their
cell. 
 Mechanisms
 Penicillin and other antibiotics in the beta-lactam family contain a
characteristic four-membered beta-lactam ring. Penicillin kills bacteria
through binding of the beta-lactam ring to DD-transpeptidase, inhibiting its
cross-linking activity and preventing new cell wall formation.
 a bacterial cell is vulnerable to outside water and molecular pressures,
which causes the cell to quickly die. Since human cells do not contain a cell
wall, penicillin treatment results in bacterial cell death without affecting
human cells.
 Gram-positive bacteria have thick cell walls containing high levels of
peptidoglycan, while gram-negative bacteria are characterized by thinner
cell walls with low levels of peptidoglycan. The cell walls of gram-negative
bacteria are surrounded by a lipopolysaccharide (LPS) layer that prevents
antibiotic entry into the cell. Therefore, penicillin is most effective against
gram-positive bacteria where DD-transpeptidase activity is highest.

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Medicinal uses/side effects
Additional information!
 Penicillin is the most effective antibiotic, (why?) because it is an effective
drug to combat bacterial infections because it targets bacteria-specific
proteins and has no effect on human proteins. When a bacterium divides,
penicillin prevents it from reforming a new cell wall, and the two daughter
cells pop.
 Penicillin prevents the bacteria from synthesizing peptidoglycan, a
molecule in the cell wall that provides the wall with the strength it needs to
survive in the human body. The drug greatly weakens the cell wall and
causes bacteria to die, allowing a person to recover from a bacterial
infection.
 One of the first antibiotics discovered was penicillin. Penicillin was first
used to treat bacterial infections in 1942 and is derived from the fungus
Penicillium sp. When used as an antibiotic treatment, penicillin operates by
a very specific mechanism—Penicillin interferes with the production of a
molecule called peptidoglycan. Peptidoglycan molecules form strong links
that give the bacterial cell strength as well as preventing leakage from the
cytoplasm. Nearly every bacterium has a peptidoglycan cell wall.
 THANK YOU!!
Members: Andrea Singua, Lyka Ledesma, Andy Roddick Tolentino & Lei Bennett Angeles