Abstract In this work the susceptibility of mobile and
cystic forms of Borrelia burgdorferi to hydroxychloroquine
(HCQ) was studied. The minimalba ctericidal
concentration (MBC) of HCQ against the mobile spirochetes
was >32 lg/mlat 37 C, and >128 lg/mlat
30 C. Incubation with HCQ significantly reduced the
conversion of mobile spirochetes to cystic forms. When
incubated at 37 C, the MBC for young biologically
active cysts (1-day old) was >8 lg/ml, but it was
> 32 lg/ml for old cysts (1-week old). Acridine orange
staining, dark-field microscopy and transmission electron
microscopy revealed that the contents of the cysts
were partly degraded when the concentration of HCQ
was ‡MBC. At high concentrations of HCQ (256 lg/ml)
about 95% of the cysts were ruptured. When the concentration
of HCQ was ‡MBC, core structures did not
develop inside the cysts, and the amount of RNA in
these cysts decreased significantly. Spirochetal structures
inside the cysts dissolved in the presence of high concentrations
of HCQ. When the concentration of HCQ
was ‡MBC, the core structures inside the cysts were
eliminated. These observations may be valuable in the
treatment of resistant infections caused by B. burgdorferi,
and suggest that a combination of HCQ and a
macrolide antibiotic could eradicate both cystic and
mobile forms of B. burgdorferi.
www.im.microbios.org/articles0203/2002/march/06%20Brorson.pdf