Triphenyltin salicylate-antimicrobial effect and resistance--the pyrophosphatase connection.
The effect of Triphenyltin salicylate (TPS) was tested against six bacteria, Escherichia coli, Staphylococcus aureus, Shigella flexneri, Pseudomonas aeruginosa, Klebsiella pneumoniae and Salmonella typhi and five fungi, Aspergillus flavus, Aspergillus fumigatus, Aspergillus niger, Rhodotorula spp. and Saccharomyces spp. Sensitivity tests were determined with 5-500 microg/ml of TPS. All organisms were sensitive to the compound except Klebsiella pneumoniae, Pseudomonas aeruginosa, Rhodotorula spp. and Saccharomyces spp. The minimum dose of TPS that can kill 50% of the susceptible microorganisms is in the range 5-50 microg/ml. Membrane bound pyrophosphatase(s) from the organisms was non-competitively inhibited by 5 microM TPS with Ki values of 7.6, 18, 8.8 and 6.9 microM for Escherichia coli, Shigella flexneri, Aspergillus niger, and Aspergillus fumigatus, respectively. The physiological index of efficiency of the enzyme (Vmax/KM) for TPS susceptible organisms was reduced by 17-68% in the presence of 5-10 microM of the compound. In contrast the index for the non-susceptible organisms was unaffected. The mode of action of TPS is discussed.
Nok
A J
AJ
Institute of Tropical Medicine, Nagasaki University, Japan. f1197@cc.nagasaki-u.ac.jp
Shuaibu
M N
MN
Bonire
J J
JJ
Dabo
A
A
Wushishi
Z
Z
Ado
S
S
D000900:Anti-Bacterial Agents; D000890:Anti-Infective Agents / Q000494:pharmacology*; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000494:pharmacology*; D001419:Bacteria / Q000187:drug effects / Q000201:enzymology*; D004352:Drug Resistance, Microbial; D004791:Enzyme Inhibitors / Q000494:pharmacology*; D005658:Fungi / Q000187:drug effects* / Q000201:enzymology; D007700:Kinetics; D008826:Microbial Sensitivity Tests; D009947:Organotin Compounds / Q000494:pharmacology*; D011755:Pyrophosphatases / Q000037:antagonists & inhibitors* / Q000378:metabolism; D012459:Salicylates / Q000494:pharmacology*
D000900:Anti-Bacterial Agents; D000890:Anti-Infective Agents; D000894:Anti-Inflammatory Agents, Non-Steroidal; D004791:Enzyme Inhibitors; D009947:Organotin Compounds; D012459:Salicylates; C417088:triphenyltin salicylate; D011755:Pyrophosphatases