IN VITRO AND IN VIVO ANTI-HELICOBACTER PYLORI ACTIVITIES OF ZINC AMOXICILLIN COMPLEX: A COMPARATIVE EVALUATION WITH SOME STANDARD ANTIBIOTICS USED IN MULTIPLE THERAPY
Muhammad Amin,*Amin Shah, Muhammad Ramzan Saeed Ashraf Janjua
ABSTRACT
Antibiotic resistance in Helicobacter pylori (H. pylori) is a global threat
for human society. Therefore, development of new antimicrobial agents
and modification of the existing therapeutic regimens currently being in
curing H. pylori related infections is one of the most priority areas of
pharmaceutical research. In the present investigation we have modified an
active antibiotic, amoxicillin, widely used in curing H. pylori related
infections by chelating it with a bio-element, zinc. The synergistic
antibacterial activity of zinc complex of amoxicillin (Zn-amox) was tested
against 34 clinical isolates and two reference strains of Helicobacter
pylori and was compared with parent drug amoxicillin (AMX) and some other antibiotics
used in triple therapy against H. pylori like, clarithromycin (CLA), tetracycline (TET) and
metronidazole (MNZ). Derivatization of amoxicillin with zinc enhanced the antibacterial
activity of the drug by inhibiting the growth of H. pylori as indicated by in vitro and in vivo
tests. Zn-amox, exhibiting MICs in the range of .008-0.5 ïg mL-1, was found stronger anti-
H. pylori agent than AMX, CLA, TET and MNZ showing MICs range of 0.125-32, 0.25-8,1-
64 and 1-512 ïg mL-1, respectively. The complex under study was found equally potent
against the antibiotic-resistant and antibiotic-susceptible strains of H. pylori. Furthermore,
Zn-amox was found efficacious in the treatment of gastric infection caused by H. pylori in
Wistar rates. The complex was found to be far less toxic than the parent drug as demonstrated
by its higher LD50 values. The present investigation indicates that the complex is potentially
more useful in eradicating both the antibiotic-susceptible and antibiotic-resistant strains of H. pylori and can be developed as a safe and potent single antibiotic for the treatment of
H. pylori infection.
Keywords: Zinc-amoxicillin complex, In vivo Helicobacter pylori, In vitro time-dose killing kinetics, gastric ulcer, LD50 values.
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