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
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
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DOI：
10.1099/jmm.0.080861-0
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发表时间：
2015-01-01
影响因子：
3
通讯作者：
Iwata, Koushi
中科院分区：
文献类型：
--
作者：
Inoue, Yasuhide;Hagi, Akifumi;Iwata, Koushi
需要有效治疗耐甲氧西林金黄色葡萄球菌（MRSA）和耐万古霉素肠球菌（VRE）的新化合物。新型单双胍化合物1-（3，4-二氯苄基）-5-辛基双胍葡萄糖酸盐（OPB-2045 G）具有潜在的杀菌活性。我们试图阐明OPB-2045 G与二葡萄糖酸氯己定（CHG）和聚维酮碘（PVP-I）相比对MRSA和VRE的杀菌活性效力。以最低杀菌浓度（MBC）为指标，分析其体外杀菌活性。通过测定脱毛后小鼠正常背部皮肤的MRSA和VRE污染来检查OPB-2045 G的体内杀菌功效。在3分钟处理期后，OPB-2045 G对标准菌株和临床分离株的MBC低于CHG和PVP-I。此外，在我们的体内小鼠模型中，1.5% OPB-2045 G（临床相关剂量）的体内杀菌活性高于0.5% CHG，相当于10% PVP-I对MRSA的杀菌活性。同样，OPB-2045 G对VRE的体内杀菌活性高于0.5% CHG和10% PVP-I。与CHG和PVP-I相比，OPB-2045 G在体外和体内均显示出对MRSA和VRE更有效的杀菌活性，表明OPB-2045 G可提供更好的保护，防止由这些病原体引起的医疗保健相关感染。
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-dichlorobenzy)-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.