Solutions are stable at pH 4-9 (most stable at pH 7);
Below pH 4 tylosin B (desmycosin) is formed as a result of acid hydrolysis;
In neutral and alkaline pH – tylosin aldol (TAD) is formed together with polar degradation products of unknown identity;
When tylosin solution is exposed to daylight, a photodegradation product - isotylosin A (isoTA) is formed.
Tylosin (10-500 mg/kg; s.c.) generally suppresses the elevated TNF-α and IL-1β levels and increases the IL-10 levels in the Lipopolysaccharide (LPS) -treated animals.
Animal Model:
Balb/C mice (2-3 months old, 20-25 g)
Dosage:
10 mg/kg, 100 mg/kg, 500 mg/kg
Administration:
Subcutaneous injection
Result:
Reduced the elevated TNF-α and IL-1β in LPS (250 µg)-treated mice but increased their IL-10 levels.
体外研究
Tylosin exerts antibacterial effects by binding to 23S rRNA of the bacterial ribosomal 50S subunit .
Tylosin also prevents growth of Gram-negative strains, with MICs of 64 μg/mL, 32 μg/mL, 512 μg/mL and 1 μg/mL for
M. haemolytica
11935,
P. multocida
4407,
E. coli
ATCC 25922 and
E. coli
AS19rlmA
I
, respectively.
Tylosin base and its salts were shown to be of low acute oral toxicity with LD50 values in excess 5000 mg/kg bw in the rat and mouse and greater than 800 mg/kg bw in the dog.
编辑结构
