Nosiheptide是一种由 Streptomyces actuosus 生产的硫肽类抗生素,已被广泛用作动物生长的饲料添加剂。它抑制细菌蛋白质合成,并在特征性大环核心上带有独特的吲哚侧环系统和区域特异性羟基。
产品描述
Nosiheptide is a thiopeptide antibiotic produced by Streptomyces actuosus. Nosiheptide has been widely used as a feed additive for animal growth. Nosiheptide inhibits bacterial protein synthesis and bears a unique indole side ring system and regiospecific hydroxyl groups on the characteristic macrocyclic core.
体外活性
Nosiheptide is found to be non-cytotoxic against mammalian cells at >>100X MIC, and its anti-Staphylococcus aureus activity is not inhibited by 20% human serum. Nosiheptide is also highly active against Enterococcus spp and the contemporary hypervirulent BI strain of Clostridium difficile but is inactive against most Gram-negative strains tested. Nosiheptide shows extremely effective activity against all contemporary Staphylococcus aureus strains tested including multiple drug-resistant clinical isolates (MIC values ≤ 0.25 mg/L). Nosiheptide shows an obviously prolonged post-antibiotic effect against both healthcare- and community-associated Staphylococcus aureus compared to vancomycin. Time-kill analysis reveals Nosiheptide to be rapidly bactericidal against Staphylococcus aureus in a concentration- and time-dependent manner, with a nearly 2-log kill, noted at 6 hours at 10X MIC [1].
体内活性
Nosiheptide (20 mg/kg; intraperitoneal injection; injected at 1 and 8 h post-infection; female CD1 mice) offers obviously protection against mortality. Ten out of 10 of the Nosiheptide-treated mice remain alive on day 3, while 6/10 of the controls died on day 1[1].
Cas No.
56377-79-8
分子式
C51H43N13O12S6
分子量
1222.36
别名
RP 9671;那西肽;Multhiomycin;Nosiheptide
储存和溶解度
DMSO:125 mg/mL (102.26 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years