Novel antiseptic compound OPB-2045G shows potent bactericidal activity against methicillin-resistant Staphylococcus aureus and vancomycin-resistant Enterococcus both in vitro and in vivo: a pilot study in animals.

Abstract

There is a need for new compounds to effectively treat methicillin-resistant Staphylococcus aureus (MRSA) and vancomycin-resistant Enterococcus (VRE). The novel monobiguanide compound 1-(3,4-dichlorobenzyl)-5-octylbiguanide gluconate (OPB-2045G) has potential bactericidal activity. We sought to elucidate the potency of OPB-2045G bactericidal activity against MRSA and VRE compared to those of chlorhexidine digluconate (CHG) and povidone iodine (PVP-I). In vitro bactericidal activity was analysed using minimum bactericidal concentration (MBC) as the index. The in vivo bactericidal efficacy of OPB-2045G was examined by determining MRSA and VRE contamination of the normal dorsal skin of mice following removal of hair. After a 3 min treatment period, the MBC of OPB-2045G was lower than that of CHG and PVP-I against standard strains and clinical isolates. Additionally, in our in vivo mouse model, the in vivo bactericidal activity of 1.5 % OPB-2045G (a clinically relevant dose) was higher than that of 0.5 % CHG and equivalent to that of 10 % PVP-I against MRSA. Similarly, the in vivo bactericidal activity of OPB-2045G was higher than that of 0.5 % CHG and 10 % PVP-I against VRE. OPB-2045G showed more potent bactericidal activity against MRSA and VRE both in vitro and in vivo compared to CHG and PVP-I, indicating that OPB-2045G may provide better protection against health care-associated infections caused by these pathogens.

• Authors: Yasuhide Inoue, Akifumi Hagi, Takuya Nii, Yoshie Tsubotani, Hikaru Nakata, Koushi Iwata
• Journal: Journal of medical microbiology (J Med Microbiol) Vol. 64 Issue Pt 1 Pg. 32-36 (Jan 2015) ISSN: 1473-5644 [Electronic] England
• PMID: 25351713 (Publication Type: Comparative Study, Journal Article, Research Support, Non-U.S. Gov't)
• Copyright: © 2015 The Authors.

Chemical References

• Anti-Infective Agents, Local
• Povidone-Iodine
• Chlorhexidine

Topics

• Administration, Topical
• Animals
• Anti-Infective Agents, Local (pharmacology, therapeutic use)
• Bacterial Infections (prevention & control)
• Chlorhexidine (therapeutic use)
• Male
• Methicillin-Resistant Staphylococcus aureus (drug effects)
• Mice, Inbred ICR
• Microbial Viability (drug effects)
• Pilot Projects
• Povidone-Iodine (therapeutic use)
• Skin (microbiology)
• Treatment Outcome
• Vancomycin-Resistant Enterococci (drug effects)