| Description | Nosiheptide (Multhiomycin), a thiopeptide antibiotic synthesized by Streptomyces actuosus, serves as a potent feed additive to promote animal growth. It functions by hindering bacterial protein synthesis and is distinguished by an indole side ring system and regiospecific hydroxyl groups on its macrocyclic core. |
| In vitro | 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]. |
| In vivo | Nosiheptide（20 mg/kg；腹腔注射；感染后1小时及8小时注射；雌性CD1小鼠）明显提高了存活率。在诺 Nosiheptide 处理的小鼠中，10/10在第三天仍然存活，而对照组中有6/10在第一天死亡[1]。 |
| Synonyms | RP 9671, Multhiomycin, 那西肽 |
| molecular weight | 1222.36 |
| Molecular formula | C51H43N13O12S6 |
| CAS | 56377-79-8 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 125 mg/mL (102.26 mM), Sonication is recommended. |
| References | 1. Haste NM, et al. Activity of the thiopeptide antibiotic nosiheptide against contemporary strains of methicillin-resistant Staphylococcus aureus. J Antibiot (Tokyo). 2012 Dec;65(12):593-8. 2. Yu Y, et al. Nosiheptide biosynthesis featuring a unique indole side ring formation on the characteristic thiopeptide framework. ACS Chem Biol. 2009 Oct 16;4(10):855-64. |