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Hymeglusin

Hymeglusin用途

Hymeglusin是一种真菌β-内酯抗生素,是一种HMG-CoA合酶抑制剂(IC50=0.12μM)。处女膜葡萄球菌素共价修饰酶的活性Cys129残基[2][3]。

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Hymeglusin名称

[ CAS 号 ]:
29066-42-0

[ 中文名 ]:
(R,R)-半乳糖苷

[ 英文名 ]:
hymeglusin

[英文别名 ]:

hymeglusin

Hymeglusin生物活性

[ 描述 ]:

Hymeglusin是一种真菌β-内酯抗生素,是一种HMG-CoA合酶抑制剂(IC50=0.12μM)。处女膜葡萄球菌素共价修饰酶的活性Cys129残基[2][3]。

[ 相关类别 ]:

研究领域 >> 癌症

研究领域 >> 感染

研究领域 >> 代谢疾病

[ 靶点 ]

IC50: 1.2 μM (HMG-CoA)[2][3]

[体外研究]

膜壳聚糖抑制登革热2型(DEN-2)新几内亚C(NGC)活病毒在K562细胞中的复制。Hymeglusin的治疗指数(CC50/IC50)为11。Hymeglusin在K562细胞中的EC50为4.5μM[1]。

[体内研究]

当剂量为25 mg/kg时,hymeglusin可抑制大鼠胆固醇生物合成45%[2]。

[参考文献]

[1]. Rothwell C, et al. Cholesterol biosynthesis modulation regulates dengue viral replication. Virology. 2009 Jun 20;389(1-2):18-19.

[2]. Greenspan MD, et al. Inhibition of hydroxymethylglutaryl-coenzyme A synthase by L-659,699. Proc Natl Acad Sci U S A. 1987 Nov;84(21):7488-92.

[3]. Tomoda H, et al. Binding site for fungal beta-lactone hymeglusin on cytosolic 3-hydroxy-3-methylglutaryl coenzyme A synthase. Biochim Biophys Acta. 2004 Feb 27;1636(1):22-8.

Hymeglusin物理化学性质

[ 密度 ]:
1.1±0.1 g/cm3

[ 沸点 ]:
516.6±15.0 °C at 760 mmHg

[ 分子式 ]:
C₁₈H₂₈O₅

[ 分子量 ]:
324.412

[ 闪点 ]:
181.3±13.9 °C

[ 精确质量 ]:
324.193665

[ PSA ]:
83.83000

[ LogP ]:
2.59

[ 蒸汽压 ]:
0.0±3.0 mmHg at 25°C

[ 折射率 ]:
1.510

[ 储存条件 ]:
-20°C，密闭，干燥

Hymeglusin毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: YQ1170000

CHEMICAL NAME :: 2,4-Undecadienoic acid, 11-(3-(hydroxymethyl)-4-oxo-2-oxetanyl)-3,5,7-trimeth yl-, (2R-(2-alpha(2E,4E,7R*),3-beta))-

CAS REGISTRY NUMBER :: 29066-42-0

LAST UPDATED :: 199406

DATA ITEMS CITED :: 2

MOLECULAR FORMULA :: C18-H28-O5

MOLECULAR WEIGHT :: 324.46

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LD - Lethal dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: >500 mg/kg

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

REFERENCE :: JANTAJ Journal of Antibiotics. (Japan Antibiotics Research Assoc., 2-20-8 Kamiosaki, Shinagawa-ku, Tokyo, 141, Japan) V.2-5, 1948-52; V.21- 1968- Volume(issue)/page/year: 41,247,1988

TYPE OF TEST :: LD - Lethal dose

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: >100 mg/kg

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

REFERENCE :: JANTAJ Journal of Antibiotics. (Japan Antibiotics Research Assoc., 2-20-8 Kamiosaki, Shinagawa-ku, Tokyo, 141, Japan) V.2-5, 1948-52; V.21- 1968- Volume(issue)/page/year: 41,247,1988

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Hymeglusin安全信息

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

[ RTECS号 ]:
YQ1170000

Hymeglusin合成路线

详细合成路线

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Hymeglusin文献

Characterization of peroxisomal 3-hydroxy-3-methylglutaryl coenzyme A reductase in UT2 cells: sterol biosynthesis, phosphorylation, degradation, and statin inhibition.

Biochemistry 39(1) , 237-47, (2000)

We have previously identified a CHO cell line (UT2 cells) that expresses only one 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase protein which is localized exclusively in peroxisomes [Engfe...

Binding site for fungal beta-lactone hymeglusin on cytosolic 3-hydroxy-3-methylglutaryl coenzyme A synthase.

Biochim. Biophys. Acta 1636(1) , 22-8, (2004)

We studied the molecular mechanism through which the fungal beta-lactone, hymeglusin, potently and specifically inhibits 3-hydroxy-3-methylglutaryl-CoA (HMG-CoA) synthase. [(14)C]Hymeglusin covalently...

Biosynthesis of antibiotic 1233A (F-244) and preparation of [14C]1233A.

J. Antibiot. 45(4) , 563-7, (1992)

The biosynthesis of antibiotic 1233A (F-244) was studied by feeding 13C-labeled precursors to the producing organism, Scopulariopsis sp. F-244. 13C NMR spectroscopy established that 1233A is derived f...

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