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雷莫拉宁

雷莫拉宁用途

Ramoplanin 是一种源于 Actinoplanes spp 的糖肽类抗生素,具有抗革兰氏阳性菌活性。

雷莫拉宁名称

[ CAS 号 ]:
76168-82-6

[ 中文名 ]:
雷莫拉宁

[ 英文名 ]:
ramoplanin A2

[英文别名 ]:

A 16686A
ramoplanin A2
A 16686
Antibiotic A 16686

雷莫拉宁生物活性

[ 描述 ]:

Ramoplanin 是一种源于 Actinoplanes spp 的糖肽类抗生素,具有抗革兰氏阳性菌活性。

[ 相关类别 ]:

研究领域 >> 感染

信号通路 >> 抗感染 >> 细菌

[ 靶点 ]

Bacteria[1]

[体外研究]

雷莫普兰通过脂质II阻断肽聚糖合成,对革兰氏阳性需氧菌和厌氧菌发挥杀菌作用[1]。

[体内研究]

雷莫普兰(100,500μg/ml；p.o.；8天)在治疗期间将万古霉素耐药肠球菌(VRE)抑制到无法检测的水平[1]。动物模型：雌性CF1小鼠(25-30g)[1]剂量：100μg/ml,500μg/ml,口服；连续8天结果：治疗过程中出现大便VRE不可检测水平。

[参考文献]

[1]. Stiefel U, et al. Efficacy of oral ramoplanin for inhibition of intestinal colonization by vancomycin-resistant enterococci in mice. Antimicrob Agents Chemother. 2004 Jun;48(6):2144-8.

[2]. Cheng M, et al. Ramoplanin at bactericidal concentrations induces bacterial membrane depolarization in Staphylococcus aureus. Antimicrob Agents Chemother. 2014 Nov;58(11):6819-27.

雷莫拉宁物理化学性质

[ 密度 ]:
1.5±0.1 g/cm3

[ 熔点 ]:
>218 °C(dec.)

[ 分子式 ]:
C₁₀₆H₁₇₀ClN₂₁O₃₀

[ 分子量 ]:
2554.066

[ 精确质量 ]:
2552.035156

[ LogP ]:
-6.39

[ 外观性状 ]:
固体

[ 折射率 ]:
1.689

[ 储存条件 ]:
-20°C

雷莫拉宁安全信息

[ 符号 ]:

GHS05

[ 信号词 ]:
Danger

[ 危害声明 ]:
H318

[ 警示性声明 ]:
P280-P305 + P351 + P338

[ 个人防护装备 ]:
dust mask type N95 (US);Eyeshields;Gloves

[ 危害码 (欧洲) ]:
C

[ 危险品运输编码 ]:
NONH for all modes of transport

[ RTECS号 ]:
VE5050000

雷莫拉宁文献

Functional identification of the gene encoding the enzyme involved in mannosylation in ramoplanin biosynthesis in Actinoplanes sp.

Biotechnol. Lett. 35(9) , 1501-8, (2013)

Ramoplanin is a lipopeptide antibiotic active against multi-drug-resistant, Gram-positive pathogens. Structurally, it contains a di-mannose moiety attached to the peptide core at Hpg(11). The biosynth...

Dissecting ramoplanin: mechanistic analysis of synthetic ramoplanin analogues as a guide to the design of improved antibiotics.

J. Am. Chem. Soc. 126(24) , 7462-3, (2004)

Ramoplanin is a potent cyclic lipoglycodepsipeptide antibiotic that disrupts bacterial cell wall synthesis by binding to the peptidoglycan intermediate Lipid II and blocking its polymerization to form...

Total synthesis and examination of three key analogues of ramoplanin: a lipoglycodepsipeptide with potent antibiotic activity.

J. Am. Chem. Soc. 126(4) , 1041-3, (2004)

The total synthesis and evaluation of three key ramoplanin aglycon analogues are detailed. The first (5a) represents replacement of the labile depsipeptide ester with a stable amide (HAsn2 --> Dap2) w...

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