Erythromycin (gluceptate)

Erythromycin gluceptate is a macrolide antibiotic produced by actinomycete?Streptomyces erythreus?with a broad spectrum of antimicrobial activity. Erythromycin gluceptate binds to bacterial 50S ribosomal subunits and inhibits?RNA-dependent protein synthesis?by blockage of transpeptidation and/or translocation reactions, without affecting synthesis of nucleic acid^[1][2]. Erythromycin gluceptate also exhibits antitumor and neuroprotective effect in different fields of research^[3][4]. IC50 & Target: Bacterial; RNA-dependent protein synthesis^[1] In Vitro: Erythromycin gluceptate inhibits growth of P. falciparum with IC₅₀ and IC₉₀ values of 58.2 μM and 104.0 μM, respectively^[1].
Erythromycin gluceptate (10 μM, 100 μM; 24 h, 72 h) shows antioxidant and anti-inflammatory effects and suppresses the accumulation of 4-HNE (p<0.01) and 8-OHdG (p<0.01), reduces Iba-1 (p<0.01) and TNF-α (p<0.01) expression significantly^[4]. In Vivo: Erythromycin gluceptate (gastric intubation; 0.1-50 mg/kg; 30-120 days) decreases tumor growth and prolong the survival time of mice from dose of 5 mg/kg in mice^[3].
Erythromycin gluceptate (gastric intubation; 5 mg/kg) protects mice alive even at 120 days after inoculation, but shortens mean survival time in tumor-bearing mice by 4-5 days with dose of 50 mg/kg^[3].
Erythromycin gluceptate (i.h.; single injection; 50 mg/kg) has a protective effect on the rat model with cerebral ischemia reperfusion-injury^[4].