Roxithromycin

Roxithromycin (RU-28965) is an orally active semi-synthethic macrolide antibiotic. Roxithromycin inhibits protein biosynthesis in the elongation step by binding to 50S bacterial ribosome. Roxithromycin has antimicrobial, antiproliferative, anti-inflammatory, tumour vasculature inhibiting and lung injury ameliorating effects^{[1][2][3][4][5][6][7][8][9][10][11]}. IC50 & Target:Roxithromycin (RU-28965) is a semi-synthetic macrolide antibiotic. It is used to treat respiratory tract, urinary and soft tissue infections. Roxithromycin (RU-28965) is derived from erythromycin, containing the same 14-membered lactone ring. Roxithromycin (RU-28965) prevents bacteria from growing, by interfering with their protein synthesis. Roxithromycin binds to the subunit 50S of the bacterial ribosome, and thus inhibits the translocation of peptides. Roxithromycin (RU-28965) has similar antimicrobial spectrum as erythromycin, but is more effective against certain gram-negative bacteria, particularly Legionella pneumophila. In Vitro:Roxithromycin is active against various Gram-positive and Gram-negative bacteria, including five strains each of Staphylococcus and Streptococcus (geometric mean MICs = 0.08 and 0.79 µg/mL, respectively), as well as several strains each of Corynebacterium, Haemophilus, and S. pneumoniae (MIC₅₀s = 0.02, 0.01, and 2.5 µg/mL, respectively)^[5].
Roxithromycin (48 h) shows antiproliferative effect and inhibition of metabolic activity in HeLa (IC₅₀ of 160 and 90 μg/mL, respectively), MG-63 (IC₅₀ of 180 and 110 μg/mL, respectively) and Osteoblast cells (IC₅₀ of 70 and 210 μg/mL, respectively)^[1].
Roxithromycin (12.5-200 μM, 72 h) shows antiproliferative effect in HUVEC cells^[2].
Roxithromycin (20-50 μM) inhibits endothelial cell migration and tube formation^[6].
Roxithromycin (10 μM) inhibits chemokine-induced chemotaxis of Th1 and Th2 cells but regulatory T cells^[7].
Roxithromycin (1-10 μM, 24 h) decreases ultraviolet B irradiation-induced reactive oxygen intermediates production and apoptosis of keratinocytes (SVHK cells)^[8].
Roxithromycin (40-120 μM, 3 days) induces apoptosis to eliminate senescent cells (WI-38)^[9].
Roxithromycin (10-80 μM, 24 h-72 h) inhibits senescent cell-induced fibroblast activation by inhibiting profibrotic SASP factors in MRC-5 cells^[9].
In Vivo:Roxithromycin (20 mg/kg, s.c. or p.o., single) is protective against infection by strains of S. aureus, S. pyogenes, S. pneumoniae, or L. monocytogenes in mice, with 50% protective dose (PD₅₀) values ranging from 23 to 98 mg/kg^[5].
Roxithromycin (40-100 mg/kg, i.p., twice daily) dose-dependently inhibits tumor angiogenesis in a mouse dorsal air sac model of angiogenesis, with reducing the dense capillary network area^[6].
Roxithromycin (40-160 mg/kg, p.o., 16 days) attenuates Bleomycin (HY-108345)-induced lung injury, inflammation, and pulmonary fibrosis in mice^[9].
Roxithromycin (40-100 mg/kg, i.p., thrice per week from week 10 to 17) inhibits constitutive activation of NF-κB by diminishing oxidative stress in a rat model of hepatocellular carcinoma^[10].
Roxithromycin (5-40 mg/kg, i.p., 1 h) attenuates airway inflammation via MAPK/NF-κB activation in a mouse model of allergic asthma^[11].