Bone Research

Table 1 Overview of protein biosynthesis inhibitors tested against intracellular S. aureus

From: Can intracellular Staphylococcus aureus in osteomyelitis be treated using current antibiotics? A systematic review and narrative synthesis

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
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	Bone cell	Other cells	In vivo
Lincosamides	Clindamycin	0.40–0.67¹⁰⁷ 0.21–0.44^40,191 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-log^43,56,57,58 1-log SCV¹⁷	MG63^43,53 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	512^74,75	0.5^74,75	<1-log^74,75		THP-1⁷⁴ J774⁷⁵
	Telithromycin	1.5–2.6⁴⁰		27.9⁷⁴ 8.6–8.7⁷⁵	4^74,75	0.06^74,75	<1-log^74,75		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⁻¹⁵³ 6.3–9.1 μg·mL⁻¹⁹⁴	0.5⁷⁴	2–4⁴³ 4⁷⁴	2–4⁴³ 2 SCV & 4 WT¹⁷ 1^31,53 1–16⁹⁵ 2⁷⁴	3-log⁵³ <1-log^31,95,97,98 1-log immediately and after 7 d⁵⁵ 1-log⁷⁴ SCV 1-log, no difference in phenotype¹⁷ 2-log^97,99	MG63^53,98 pHOBs⁵⁵ MC3T3⁹⁹ NHOst⁹⁵	THP-1^17,74,95 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⁻¹⁵³		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 16^74,75	0.125 SCV & 0.5 WT¹⁷ 1 SCV & 0.25 WT¹²⁵ 0.5^74,75	1-log SCV much better against WT/revertant¹⁷ <1-log^108,129,141 2-log¹²⁵ 1-3-log¹²⁶ 1-log^74,75 immediately and after 7 d⁵⁵	pHOBs^55,108 Saos-2¹²⁶ MC3T3^129,141 BMOC¹⁴¹	THP-1^17,74,125 J774⁷⁵ RAW164.7¹²⁹	C57BL/6 mice⁵⁵ BALB/c mice¹²⁹

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