Mefloquine and Its Enantiomers Are Active against Mycobacterium tuberculosis In Vitro and in Macrophages

Table 4

Mefloquine and enantiomer activity against H37Rv in macrophages. Serum level of mefloquine (4 g/mL).

Compound	CFU/mL of lysate	value
No treatment time 0	3.0 ± 0.5 × 10^5	—
No treatment day 4	1.7 ± 0.3 × 10^6	—
Mefloquine (4 µg/mL)	5.9 ± 0.4 × 10^4	<0.05
(+)Erythro (4 µg/mL)	3.4 ± 0.3 × 10^4	<0.05
(−)Erythro (4 µg/mL)	6.1 ± 0.5 × 10^4	<0.05
(+)Threo (4 µg/mL)	5.1 ± 0.3 × 10^5	>0.05
(−)Threo (4 µg/mL)	7.4 ± 0.5 × 10^5	>0.05

THP-1 macrophages: 1 × 10⁵.
Monolayers treated daily for 4 days. No toxicity observed.
Results of 3 distinct experiment (mean ± SD).