Sigapedil

Names

[ Name ]:
Sigapedil

[Synonym ]:
erythroped
Refkas
erythromycin gluceptate
Monomycin
erythromycin ethyl succinate
D-Glucoheptonat
erythromycin A 2'-ethyl succinate
Erythromycin glucoheptonate
Evesin
Erythromycin-A,D-glycero-D-gulo-Heptonat
Eryliquid
Anamycin
E-Mycin e
Esinol
O''-(3-ethoxycarbonyl-propionyl)-erythromycin
erythromycin-A,D-glycero-D-gulo-heptonate
Erythromycinethylsuccinat
Arpimycin

Biological Activity

[Description]:

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].

[Related Catalog]:

Research Areas >> Cancer

Research Areas >> Infection

Signaling Pathways >> Anti-infection >> Bacterial

[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]. Cell Viability Assay[4] Cell Line: Embryos primary cortical neuron (from the cerebral cortices of 17-day-old Sprague-Dawley rat) Concentration: 10, 100 μM Incubation Time: 24, 72 hours Result: Improved the viability of cultured neuronal cells in vitro after 3 hours oxygen-glucose deprivation (OGD).

[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]. Animal Model: Female ddY mice (6-week-old) with EAC cells or CDF mice (6-week-old) with P388 cells[3] Dosage: 0.1 mg/kg; 0.5 mg/kg; 10 mg/kg; 30 mg/kg; 50 mg/kg Administration: Gastric intubation; 30-120 days Result: Decreased tumor growth and prolonged the mean survival time of mice from the dose of 5 mg/kg, however, the 50 mg/kg dosage shortened the MST in tumorbearing mice. Animal Model: Male Sprague-Dawley rats (8-week-old, 250-300 g)[4] Dosage: 50 mg/kg Administration: Subcutaneous single injection Result: Reduced infarct volume and edema volume, improved neurological deficit.

[References]

[1]. Gribble MJ, et al. Erythromycin. Med Clin North Am. 1982 Jan;66(1):79-89.

[2]. Nakornchai S, et al. Activity of azithromycin or erythromycin in combination with antimalarial drugs against multidrug-resistant Plasmodium falciparum in vitro. Acta Trop. 2006 Dec. 100(3):185-91.

[3]. K Hamada, et al. Antitumor effect of erythromycin in mice. Chemotherapy. 1995 Jan-Feb. 41(1):59-69.

[4]. Katayama Y, et al. Neuroprotective effects of erythromycin on cerebral ischemia reperfusion-injury and cell viability after oxygen-glucose deprivation in cultured neuronal cells. Brain Res. 2014 Nov 7. 1588:159-67.