Erythromycin A dihydrate 是由放线菌产生的大环内酯类抗生素 (antibiotic),具有广泛的抗菌活性。Erythromycin A dihydrate 通过结合细菌的 50S 核糖体亚基而起作用,并通过阻断转肽和/或易位反应来抑制 RNA 依赖性蛋白 (RNA-dependent protein synthesis) 的合成,而不会影响核酸的合成。Erythromycin A dihydrate 在不同领域的研究中显示出抗肿瘤特性和保护神经的作用。
生物活性 | Erythromycin A dihydrate is amacrolideantibioticproduced byactinomycete Streptomyceserythreus with a broad spectrum of antimicrobial activity. Erythromycin A dihydrate binds tobacterial50S 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 A dihydrate also exhibits antitumor and neuroprotective effect in different fields of research[3][4]. |
IC50& Target | |
体外研究 (In Vitro) | Erythromycin A dihydrate inhibits growth ofP. falciparumwith IC50and IC90values of 58.2 μM and 104.0 μM, respectively[1]. Erythromycin A dihydrate (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). |
|
体内研究 (In Vivo) | Erythromycin A dihydrate (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 A dihydrate (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 A dihydrate (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 at the age of 6 weeks with EAC cells or CDF mice at the age of 6 weeks 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. |
|
Clinical Trial | |
分子量 | |
Formula | |
CAS 号 | |
运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |