Bozja J, Yi K, Shafer W M, Stojiljkovic I
Department of Microbiology and Immunology, Emory University School of Medicine, Atlanta, GA 30322, USA.
Int J Antimicrob Agents. 2004 Dec;24(6):578-84. doi: 10.1016/j.ijantimicag.2004.06.008.
A series of porphyrin based compounds without (nMP) or with (MP) metals were found to have potent bactericidal action in vitro against the sexually transmitted pathogens Neisseria gonorrhoeae and Haemophilus ducreyi. nMP and MP did not show bactericidal activity against five species of lactobacilli. An MP containing gallium had the capacity to block a gonococcal infection in a murine vaginal model, indicating that its development as a topical microbicide to block sexually transmitted bacterial infections is warranted. In contrast to other bacterial species, loss of the gonococcal haemoglobin uptake system encoded by hpuB or energy supplied through the TonB-ExbB-ExbD system did not significantly affect levels of MP-susceptibility in gonococci. In contrast, mutations in gonococci that inactivate the mtrCDE-encoded efflux pump were found to enhance gonococcal susceptibility to nMPs and MPs while over-production of this efflux pump decreased levels of gonococcal susceptibility to these compounds.
一系列不含金属(nMP)或含有金属(MP)的卟啉基化合物在体外被发现对性传播病原体淋病奈瑟菌和杜克嗜血杆菌具有强大的杀菌作用。nMP和MP对五种乳酸杆菌未显示出杀菌活性。一种含镓的MP能够在小鼠阴道模型中阻断淋球菌感染,这表明将其开发为一种局部杀菌剂以阻断性传播细菌感染是有必要的。与其他细菌种类不同,由hpuB编码的淋球菌血红蛋白摄取系统的缺失或通过TonB-ExbB-ExbD系统提供的能量,对淋球菌中MP的敏感性水平没有显著影响。相比之下,淋球菌中使mtrCDE编码的外排泵失活的突变被发现会增强淋球菌对nMP和MP的敏感性,而这种外排泵的过度产生则会降低淋球菌对这些化合物的敏感性水平。