兰考韦泰

兰考韦泰用途

Duramycin (Moli1901;Lancovutide) 是一种衍生自肉桂链霉菌的环肽羊毛硫抗生素。Duramycin 可刺激气道上皮中的氯化物分泌,并可用于囊性纤维化的研究。Duramycin 与磷脂酰乙醇胺 (PE) 相互作用并具有抗菌,抗病毒作用。

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兰考韦泰名称

[ CAS 号 ]:
1391-36-2

[ 中文名 ]:
兰考韦泰

[ 英文名 ]:
Duramycin

[中文别名 ]:

杜拉霉素

[英文别名 ]:

UNII-BPR0F3X56H
Lancovutide [INN]
Leucopeptin
LANCOVUTIDE

兰考韦泰生物活性

[ 描述 ]:

[ 相关类别 ]:

信号通路 >> 抗感染 >> 流感病毒

研究领域 >> 感染

研究领域 >> 炎症/免疫

信号通路 >> 抗感染 >> 细菌

[体外研究]

杜拉霉素确实在较窄的浓度范围(约1μM)内刺激囊性纤维化支气管上皮细胞(CFBE)的Cl-流出。然而,100μM和250μM的杜拉霉素抑制循环流化床细胞的Cl-外排。16HBE细胞中[Ca2+]i增加3μM杜拉霉素,但1μM杜拉霉素后下降,CFBE细胞中[1]杜拉霉素增加3μM杜拉霉素。杜拉霉素影响蛋白-脂质相互作用,损害蛋白移位,诱导脂质囊泡聚集,抑制肌浆网对ATP依赖的Ca2+摄取[1]。

[体内研究]

【68Ga】诺达加杜拉霉素作为正电子发射断层显像(PET)细胞死亡示踪剂用于全身化疗所致器官毒性检测的评价。在静脉注射[68Ga]NODAGA杜拉霉素2小时后,分析未经治疗和阿霉素、丁磺胺和顺铂治疗的小鼠的器官摄取。【68Ga】NODAGA-Duramycin-PET/CT成功地应用于小鼠化疗所致器官毒性的无创检测,具有较高的敏感性[3]。

[参考文献]

[1]. Oliynyk I, et al. Effect of duramycin on chloride transport and intracellular calcium concentration in cystic fibrosis and non-cystic fibrosis epithelia. APMIS. 2010 Dec;118(12):982-90.

[2]. Huo L, et al. Insights into the Biosynthesis of Duramycin. Appl Environ Microbiol. 2017 Jan 17;83(3). pii: e02698-16.

[3]. Rix A, et al. Assessment of Chemotherapy-Induced Organ Damage with Ga-68 Labeled Duramycin. Mol Imaging Biol. 2019 Aug 8.

兰考韦泰物理化学性质

[ 密度 ]:
1.0238 (rough estimate)

[ 熔点 ]:
271-273ºC

[ 分子式 ]:
C₈₉H₁₂₅N₂₃O₂₅S₃

[ 分子量 ]:
1999.25000

[ 精确质量 ]:
1997.82000

[ PSA ]:
835.99000

[ 折射率 ]:
1.6680 (estimate)

[ 储存条件 ]:
2-8°C

[ 水溶解性 ]:
0.1 M HCl: soluble10mg/mL

兰考韦泰毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: BV7100000

CHEMICAL NAME :: Ancovenin, 2-L-lysine-6-(3-aminoalanine)-10-L-phenylalanine-12-L -phenylalanine-13-L-v aline- 15-(erythro-3-hydroxy-L-aspartic acid)-, cyclic 6-19)-imine

CAS REGISTRY NUMBER :: 1391-36-2

LAST UPDATED :: 199801

DATA ITEMS CITED :: 1

MOLECULAR FORMULA :: C89-H125-N23-O25-S3

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 20 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: JAJAAA Journal of Antibiotics, Series A. (Tokyo, Japan) V.6-20, 1953-67. For publisher information, see JANTAJ. Volume(issue)/page/year: 17,262,1964

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兰考韦泰安全信息

[ 个人防护装备 ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

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

[ RTECS号 ]:
BV7100000

兰考韦泰文献

Stimulation of sodium transport by duramycin in cultured human colonic epithelia.

J. Pharmacol. Exp. Ther. 259 , 1050, (1991)

Effects of two peptide antibiotics, duramycin and Ro 09-0198, on ion transport in cultured human colonic epithelia were investigated. Both peptides acted on the apical face of epithelial monolayers, c...

Upregulated function of mitochondria-associated ER membranes in Alzheimer disease.

EMBO J. 31 , 4106-23, (2012)

Alzheimer disease (AD) is associated with aberrant processing of the amyloid precursor protein (APP) by γ-secretase, via an unknown mechanism. We recently showed that presenilin-1 and -2, the catalyti...

Phosphatidylethanolamine is externalized at the surface of microparticles.

Biochim. Biophys. Acta 1821(12) , 1501-7, (2012)

Microparticles (MPs) are membrane-bound vesicles shed normally or as a result of various (pathological) stimuli. MPs contain a wealth of bio-active macromolecules. Aminophospholipid phosphatidylserine...

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