Table 1.

Overview of protein biosynthesis inhibitors tested against intracellular S. aureus

Antibiotic Class	Antibiotic	Bone: plasma ratio	Bone concentration	Intra: extracellular ratio	MIC at ca pH5 (μg·mL−1 or mg·L−1)	MIC at ca pH7 (μg·mL−1 or mg·L−1)	Intracellular effectivity against S. aureus		Model tested
								Bone cell	Other cells	In vivo
Lincosamides	Clindamycin	0.40–0.67107 0.21–0.4440,191 0.451 0.3553	2.6–5 μg·g−1 107 2.6 g·g−1 51 1.4 μg·mL−1 50 9.6 μg·mL−1 41 4 μg·mL−1 53		≥3243	0.12517 0.03253 0.00454 4–843	5-log53 Only effective immediately, not after 12 h54 1-log immediately, not after 7 days55 <1-log43,56–58 1-log SCV17	MG6343,53 NHOst54 Normal Mouse OBs54 pHOBs55 MC3T357 UMR10658	THP-117 Primary polymorphonuclear leukocytes56
StreptoGramins	Quinupristin/ Dalfopristin					0.517	2-log SCV, other phenotype better17		THP-117
Macrolides	Azithromycin	2.5–6.340		37.874 45–5075	51274,75	0.574,75	<1-log74,75		THP-174 J77475
	Telithromycin	1.5–2.640		27.974 8.6–8.775	474,75	0.0674,75	<1-log74,75		THP-174 J77475
	Erythromycin	0.18–0.2840					Only effective immediately, not after 12 h54	Normal Mouse Osteoblasts54
	Spiramycin	0.04740	1.7–5.3 μg·g−176
Oxazolidinones	Linezolid	0.37–0.51107 0.23–0.5140 0.553 0.47–0.6094	4–9 μg·g−1 107 6.4 μg·mL−1 17 8 μg·mL−1 53 6.3–9.1 μg·mL−1 94	0.574	2–443 474	2–443 2 SCV & 4 WT17 131,53 1–1695 274	3-log53 <1-log31,95,97,98 1-log immediately and after 7 d55 1-log74 SCV 1-log, no difference in phenotype17 2-log97,99	MG6353,98 pHOBs55 MC3T399 NHOst95	THP-117,74,95 Primary rat fibroblasts95 HUVEC95 Calu-395 Primary human keratinocytes95 RAW264.797	Sprague-Dawley rats31 Kunming mice97
	Tedizolid						<1-log98	MG6398
	Radezolid					0.25–295	1-log95	NHOst95	THP-195 Primary rat fibroblasts95 HUVEC95 Calu-395 Primary human keratinocytes95
Tetracyclines	Doxycycline	0.02–0.85107	0.13–2.6 μg·g−1 107 3 μg·mL−1 41		0.062 5–0.12543	0.12543
Glycolcycline	Tigecycline	0.35–1.840 0.3553	0.3 μg·mL−1 53		143	0.125 all phenotypes17 0.062 5–0.25 0.12553	4-log53 <1-log108 SCV 1-log, no difference in phenotype17	MG6353 pHOBs108	THP-117
Fusidic Acid		0.44–0.93107 0.12–0.9440	15–45 μg·g−1 107			0.03–0.125 SCV < WT17	<1-log SCV much better against WT/revertant17		THP-117
Aminoglycosides	Gentamicin		Detectable41	4.474 6.3–6.875	32-64 SCV & 1 WT125 1674,75	0.125 SCV & 0.5 WT17 1 SCV & 0.25 WT125 0.574,75	1-log SCV much better against WT/revertant17 <1-log108,129,141 2-log125 1-3-log126 1-log74,75 immediately and after 7 d55	pHOBs55,108 Saos-2126 MC3T3129,141 BMOC141	THP-117,74,125 J77475 RAW164.7129	C57BL/6 mice55 BALB/c mice129