Efflux pump mechanisms perform important physiological functions such as prevention of toxin absorption from the gastrointestinal tract, elimination of bile from the hepatocytes, effective functioning of the blood–brain barrier and placental barrier, and renal excretion of drugs. They exist in all living cells, but those in the bacterial and mammalian cells are more important to the clinician and pharmacologist, as they constitute an important cause of antimicrobial drug resistance, which contributes to treatment failure, high medical bills, and increased mortality / morbidity. This review was aimed at highlighting the role of efflux pump mechanisms in microbial resistance to chemotherapeutic agents. It was also aimed to elucidate their structure and mechanisms of action so as to integrate the efflux pump mechanisms in the design and development of novel antimicrobial agents. Findings from previous studies and research on this subject assessed through Google search, Pubmed, Hinari websites, as well as standard textbooks on chemotherapy, provided the needed information in the process of this review. Efflux pump inhibitors are promising strategies for preventing and reverting efflux-mediated resistance to chemotherapeutic agents. They are usually employed as adjuncts in antimicrobial and cancer chemotherapy. Toxicity, more common with the older-generation inhibitors such as verapamil and reserpine, constitutes the greatest impediment to their clinical applications. No efflux pump inhibitor has been approved for routine clinical use, as a result of doubtful clinical efficacy and unacceptably high incidence of adverse effects, particularly inhibition of the P-450 drug metabolizing enzyme. At present, their applications are mainly restricted to epidemiological studies. Nonetheless, the search for efficacious and tolerable efflux pump inhibitors continues because of the potential benefits. There is a need to consider efflux pump substrate selectivity in the design and development of novel chemotherapeutic agents.
This study evaluated the antibacterial effect of ethanolic extract of Ficus exasperate leaf. Clinical isolates of Escherichia coli, Pseudomonas aeruginosa, Staphyllococcus aureus and Klebsiella pneumoniae were incubated in agar plates after serial dilutions of the extract were added in wells made in the agar and incubated for 24 h at 37°C. Thereafter, zones of inhibition (in mm) around the wells were measured. The same organisms were tested for sensitivity against standard antibiotics using disk diffusion. The extract demonstrated significant antibacterial activity. It was concluded that the extract had significant antibacterial activity against test organisms with minimum inhibitory concentration (MIC) of 250 µg/ml. Its use for treatment of infections by traditional healers is justified.
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