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抗霉素A1

抗霉素A1用途

Antimycin A1 是泛醇-细胞色素 c 氧化还原酶的特定电子转移 (electron transfer) 抑制剂。Antimycin A1 通过抑制 HIF-1α 激活导致的 VEGF 产生减少来抑制血管生成。

抗霉素A1名称

[ CAS 号 ]:
642-15-9

[ 中文名 ]:
抗霉素A1

[ 英文名 ]:
Antimycin A

[中文别名 ]:

[英文别名 ]:

dihydrosamidin
Antimycin A1
Antimycin A

抗霉素A1生物活性

[ 描述 ]:

Antimycin A1 是泛醇-细胞色素 c 氧化还原酶的特定电子转移 (electron transfer) 抑制剂。Antimycin A1 通过抑制 HIF-1α 激活导致的 VEGF 产生减少来抑制血管生成。

[ 相关类别 ]:

研究领域 >> 癌症

[体外研究]

抗霉素A是抗霉素A1、A2、A3和A4的混合物,是由链霉菌属产生的抗生素,具有抗真菌、杀虫、杀线虫和杀鱼等特性[3]。抗霉素A抑制Bcl-2和Bcl-xL蛋白,诱导细胞凋亡[4]。

[参考文献]

[1]. Hoeon Kim, et al. Structure of Antimycin A1, a Specific Electron Transfer Inhibitor of Ubiquinol-Cytochrome c Oxidoreductase. J. Am. Chem. Soc. 1999, 121, 20, 4902-4903.

[2]. Maeda M, et al. Inhibition of angiogenesis and HIF-1alpha activity by antimycin A1. Biol Pharm Bull. 2006;29(7):1344-1348.

[3]. Liu J, et al, Biosynthesis of antimycins with a reconstituted 3-formamidosalicylate pharmacophore in Escherichia coli. ACS Synth Biol. 2015;4(5):559-565.

[4]. Tzung SP, et al. Antimycin A mimics a cell-death-inducing Bcl-2 homology domain 3. Nat Cell Biol. 2001;3(2):183-191.

抗霉素A1物理化学性质

[ 密度 ]:
1.2±0.1 g/cm3

[ 沸点 ]:
757.9±60.0 °C at 760 mmHg

[ 熔点 ]:
139-140ºC

[ 分子式 ]:
C₂₈H₄₀N₂O₉

[ 分子量 ]:
548.625

[ 闪点 ]:
412.1±32.9 °C

[ 精确质量 ]:
548.273376

[ PSA ]:
157.33000

[ LogP ]:
4.68

[ 蒸汽压 ]:
0.0±2.6 mmHg at 25°C

[ 折射率 ]:
1.545

[ 储存条件 ]:
-20°C，干燥，密封

抗霉素A1毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: NY1503500

CHEMICAL NAME :: Isovaleric acid, 8-ester with 3-formamido-N-(7-hexyl-8-hydroxy-4,9-dimethyl-2,6-dio xo-1,5- dioxonan-3-yl)salicylamide

CAS REGISTRY NUMBER :: 642-15-9

LAST UPDATED :: 199309

DATA ITEMS CITED :: 5

MOLECULAR FORMULA :: C28-H40-N2-O9

MOLECULAR WEIGHT :: 548.70

WISWESSER LINE NOTATION :: T B666 COV KO&&TJ L1 L1 MOV1Y1&1 NOV1

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 1469 mg/kg

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

REFERENCE :: JDGRAX Journal of Drug Research. (National Organization for Drug Research and Control, POB 29, Cairo, Egypt) V.2- 1969- Volume(issue)/page/year: 7(2),1,1975

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 7600 ug/kg

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

REFERENCE :: 85FZAT "Index of Antibiotics from Actinomycetes," Umezawa, H. et al., eds., Tokyo, Univ. of Tokyo Press, 1967 Volume(issue)/page/year: -,144,1967

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 25 mg/kg

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

REFERENCE :: 85FZAT "Index of Antibiotics from Actinomycetes," Umezawa, H. et al., eds., Tokyo, Univ. of Tokyo Press, 1967 Volume(issue)/page/year: -,144,1967

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 900 ug/kg

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

REFERENCE :: 85FZAT "Index of Antibiotics from Actinomycetes," Umezawa, H. et al., eds., Tokyo, Univ. of Tokyo Press, 1967 Volume(issue)/page/year: -,144,1967

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

ROUTE OF EXPOSURE :: Intramuscular

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 1 gm/kg

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

REFERENCE :: JDGRAX Journal of Drug Research. (National Organization for Drug Research and Control, POB 29, Cairo, Egypt) V.2- 1969- Volume(issue)/page/year: 7(2),1,1975

抗霉素A1安全信息

[ 危害码 (欧洲) ]:
Xi

[ 风险声明 (欧洲) ]:
23/24/25

[ 危险品运输编码 ]:
UN 3172

[ 包装等级 ]:
II

[ 危险类别 ]:
6.1(a)

抗霉素A1制备

链霉菌培养液经醇提、浓缩制得复合物粗晶，再在甲醇：水：四氯化碳：己烷中逆流分配分离而得纯品。