Abstract
AbstractThere is an urgent need to discover new anti-microbial agents that can overcome the increasing antibiotic resistance posed by multidrug resistant, β-lactamase producing bacteria. β-Lactam antibiotics are structurally related through the presence of a core β-lactam ring. Resistant pathogens are able to produce β-lactamase enzymes that hydrolyze the β-lactam ring and inactivate the antibiotic. One approach to counteract this resistance is to develop β-lactamase inhibitors, which, on administration with β-lactams, restores the antibiotic activity for its continued clinical use. In the present study, a fungal Penicillium strain was isolated, identified and characterized for its antimicrobial and β-lactamase inhibition activities. The strain was identified as Penicillium piceum and was grown in suitable media under submerged cultivation. The antibacterial activity was observed against Bacillus subtilis, Staphylococcus aureus, Escherichia coli and Pseudomonas aeruginosa. Higher antimicrobial activity was observed against gram-positive bacteria as compared to gram-negative bacteria. A certain amount of antifungal activity was also observed against the fungal strains of Penicilium chrysogenum, Rhizopus stolonifer, Fusarium moniliforme, Aspergillus niger, Giberella fujikuroi and Saccharomyces cerevisiae. Iodometric and bioassay analyses confirmed that P. piceum produced β-lactamase inhibitors having activity against penicillinase (Bacillus cereus). Solvent-solvent extraction with butanol yielded a three-fold increase in β-lactamase inhibition activity. High-performance liquid chromatography analysis of the concentrated product proved it to be a single compound. The infrared (IR) spectrum of the compound was compared with the reference IR spectra of sulbactam sodium, tazobactam and potassium clavulanate. It was found to be different thereby inferring the need for extensive structural elucidation for future applications.
Published Version
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