粉蝶霉素A_MSDS_用途_密度_粉蝶霉素ACAS号【2738-64-9】

Piericidin A (AR-054) 是一种天然线粒体 NADH-泛醌氧化还原酶 (复合物 I; complex I) 抑制剂。Piericidin A 是一种有效的神经毒素,通过其对 NADH-泛醌还原酶 (NADH-ubiquinone reductase) 的作用破坏电子传输系统,从而抑制线粒体呼吸。Piericidin A 还是一种潜在的群体感应抑制剂,可抑制胡萝卜欧文氏菌亚种 atroseptica (Eca) 的毒力基因的表达。Piericidin A 是一种 ADC 细胞毒素,具有抗菌,抗癌,杀虫活性。

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[ 描述 ]:

Piericidin A (AR-054) 是一种天然线粒体 NADH-泛醌氧化还原酶 (复合物 I; complex I) 抑制剂。Piericidin A 是一种有效的神经毒素,通过其对 NADH-泛醌还原酶 (NADH-ubiquinone reductase) 的作用破坏电子传输系统,从而抑制线粒体呼吸。Piericidin A 还是一种潜在的群体感应抑制剂,可抑制胡萝卜欧文氏菌亚种 atroseptica (Eca) 的毒力基因的表达。Piericidin A 是一种 ADC 细胞毒素,具有抗菌,抗癌,杀虫活性。

[ 相关类别 ]:

研究领域 >> 癌症

研究领域 >> 感染

信号通路 >> 抗体- 药物偶联物 >> ADC细胞毒素

研究领域 >> 神经疾病

信号通路 >> 抗感染 >> 细菌

[体外研究]

在无细胞试验中,粉蝶毒素a抑制线粒体复合物I的效力比番荔枝苷小2倍。在培养的神经元中,青霉素A能诱导磷酸化tau从树突重新分布到细胞体中,并诱导细胞死亡[1]。piericina对Tn5B1-4细胞活性有时间和浓度依赖性的抑制作用,IC50值为0.061μM,而piericina对HepG2和Hek293细胞的活性有轻微的抑制作用,IC50值分别为233.97μM和228.96μM。粉蝶呤A诱导Tn5B1-4细胞凋亡与线粒体膜电位降低一致[3]。

[体内研究]

piericina(0.5mg/kg/d；通过渗透微型泵持续28天)显著增加P301S+/+小鼠大脑皮层中磷酸化tau免疫反应细胞的数量。仅在P301S+/+小鼠中,piericina导致病理性磷酸化tau水平升高。piericina治疗P301S+/+小鼠的突触密度降低。暴露于piericina会加重基因决定的tau病理过程[1]。

[参考文献]

[1]. Matthias Höllerhage, et al. Piericidin A Aggravates Tau Pathology in P301S Transgenic Mice. PLoS One. 2014 Dec 1;9(12):e113557.

[2]. Ji Eun Kang, et al. Efficacies of Quorum Sensing Inhibitors, Piericidin A and Glucopiericidin A, Produced by Streptomyces Xanthocidicus KPP01532 for the Control of Potato Soft Rot Caused by Erwinia Carotovora Subsp. Atroseptica. Microbiol Res. 2016 Mar;184:32-41.

[3]. Solange Muhayimana, et al. Cytotoxic Selectivity and Apoptosis Induction of Piericidin A Contributes Potentially to Its Insecticidal Effect Against Mythimna Separata (Lepidoptera: Noctuidae) Larvae. Pestic Biochem Physiol. 2019 Jun;157:19-25.

[ 密度 ]:
1.1±0.1 g/cm3

[ 沸点 ]:
591.7±50.0 °C at 760 mmHg

[ 分子式 ]:
C₂₅H₃₇NO₄

[ 分子量 ]:
415.566

[ 闪点 ]:
311.6±30.1 °C

[ 精确质量 ]:
415.272247

[ PSA ]:
71.81000

[ LogP ]:
4.26

[ 蒸汽压 ]:
0.0±3.8 mmHg at 25°C

[ 折射率 ]:
1.534

[ 储存条件 ]:
2-8°C

详细MSDS(安全技术说明书)

CHEMICAL IDENTIFICATION

RTECS NUMBER :: YD4588000

CHEMICAL NAME :: 2,6,9,11-Tridecatetraen-4-ol, 13-(4-hydroxy-5,6-dimethoxy-3-methyl-2-pyridyl)-3,5,7 ,11- tetramethyl-, (all-E)-(4S,5S)-

CAS REGISTRY NUMBER :: 2738-64-9

LAST UPDATED :: 199612

DATA ITEMS CITED :: 5

MOLECULAR FORMULA :: C25-H37-N-O4

MOLECULAR WEIGHT :: 415.63

WISWESSER LINE NOTATION :: T6NJ B2UY1&1U2Y1&U1Y1&YQY1&U2 C1 DQ EO1 FO1

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 360 ug/kg

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

REFERENCE :: ABCHA6 Agricultural and Biological Chemistry. (Maruzen Co. Ltd., POB 5050, Tokyo International, Tokyo 100-31, Japan) V.25- 1961- Volume(issue)/page/year: 34,1101,1970

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 3170 ug/kg

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

REFERENCE :: ABCHA6 Agricultural and Biological Chemistry. (Maruzen Co. Ltd., POB 5050, Tokyo International, Tokyo 100-31, Japan) V.25- 1961- Volume(issue)/page/year: 32,1115,1968

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

ROUTE OF EXPOSURE :: Administration onto the skin

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 2520 ug/kg

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

REFERENCE :: ABCHA6 Agricultural and Biological Chemistry. (Maruzen Co. Ltd., POB 5050, Tokyo International, Tokyo 100-31, Japan) V.25- 1961- Volume(issue)/page/year: 32,1115,1968

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 870 ug/kg

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

REFERENCE :: ABCHA6 Agricultural and Biological Chemistry. (Maruzen Co. Ltd., POB 5050, Tokyo International, Tokyo 100-31, Japan) V.25- 1961- Volume(issue)/page/year: 27,576,1963

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 1 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: 40,149,1987

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[ 个人防护装备 ]:
Eyeshields;Faceshields;full-face respirator (US);Gloves;multi-purpose combination respirator cartridge (US);type ABEK (EN14387) respirator filter

[ 危害码 (欧洲) ]:
T+

[ 风险声明 (欧洲) ]:
26/27/28-20/21/22

[ 安全声明 (欧洲) ]:
28-36/37-45

[ 危险品运输编码 ]:
UN 3382 6.1/PG 1

Isolation and characterizations of quinone analogue-resistant mutants of bo-type ubiquinol oxidase from Escherichia coli.

Biochemistry 37(37) , 12744-52, (1998)

Cytochrome bo is a member of the heme-copper terminal oxidase superfamily and serves as a four-subunit ubiquinol oxidase in the aerobic respiratory chain of Escherichia coli. To probe the location and...

Etoposide-resistant HT-29 human colon carcinoma cells during glucose deprivation are sensitive to piericidin A, a GRP78 down-regulator.

J. Cell Physiol. 215(1) , 243-50, (2008)

Glucose deprivation, a pathophysiological cell condition, causes up-regulation of GRP78 and induction of etoposide resistance in human cancer cells. The induction of drug resistance can be partly expl...

Genetic evidence for the existence of two quinone related inhibitor binding sites in NADH-CoQ reductase.

Biochim. Biophys. Acta 1319(1) , 1-4, (1997)

Using the NADH-CoQ reductase of Rhodobacter capsulatus as a model for the mitochondrial Complex I, we have for the first time isolated bacterial mutants resistant to piericidin-A, a classical inhibito...

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