毒毛旋花子苷元

毒毛旋花子苷元用途

毛托菌素是一种天然的强心苷[1]。0.1和1 nmol/L的毒毛菊素增加,1~100µmol/L抑制Na+/K+-ATP酶活性,但10和100 nmol/L毒毛菊素不影响心肌膜Na+/K+-ATP酶活性[2]。毒毛茛菪碱增加舒张和收缩期细胞内Ca2+浓度[3]。

毒毛旋花子苷元名称

[ CAS 号 ]:
66-28-4

[ 中文名 ]:
毒毛旋花子苷元

[ 英文名 ]:
Card-20(22)-enolide,3,5,14-trihydroxy-19-oxo-, (3b,5b)-

[中文别名 ]:

毒毛旋花苷配基

[英文别名 ]:

Convallatoxigenin
Corchorgenin
Corchsularin
Strophanthidin K
MFCD00046266
EINECS 200-626-6
k-Strophanthidin
Strophanthidine
Erysimupicrone
Corchorin

毒毛旋花子苷元生物活性

[ 描述 ]:

[ 相关类别 ]:

研究领域 >> 心血管疾病

[ 靶点 ]

Na+/K+-ATPase[2]

[体外研究]

毒毛茛菪碱(0~10μM；24小时；MCF-7、A549和HepG2细胞)能有效抑制癌细胞的生长,对正常细胞没有毒性[1]。毒毛菊素(0.5至500µM；PBMCs)在PBMCs中未显示出显著的细胞毒性。毒毛菊素(2µM；MCF-7细胞)可将细胞周期阻滞在G2/M期[1]。毒毛菊素(MCF-7、A549和HepG2细胞)能有效抑制癌细胞的生长,对正常细胞没有毒性。与未经治疗的对照组相比,毒毛菊素(MCF-7、A549和HepG2细胞)抑制三种癌细胞中检查点和细胞周期素依赖性激酶的表达。白屈菜素可以调节蛋白质从细胞核到细胞膜以及细胞质的定位。毒毛茛菪素是一种单糖强心苷,含有一个苷元部分,不含任何糖单位。通过多种生物化学信号通路的减弱以及通过p53依赖和p53非依赖机制将细胞周期阻滞在G2/M期来诱导细胞凋亡[1]。细胞活力测定[1]细胞系：MCF-7、A549和HepG2细胞浓度：0~10μM培养时间：24小时结果：抑制三种不同癌细胞的增殖。

[参考文献]

[1]. Reddy D, et al. Strophanthidin Attenuates MAPK, PI3K/AKT/mTOR, and Wnt/β-Catenin Signaling Pathways in Human Cancers. Front Oncol. 2020;9:1469. Published 2020 Jan 17.

[2]. Su SW, et al. Relationship between cardiotonic effects and inhibition on cardiac sarcolemmal Na+,K+-ATPase of strophan-thidin at low concentrations. Acta Pharmacol Sin. 2003;24(11):1103-1107.

[3]. Bennett DL, et al. Strophanthidin-induced gain of Ca2+ occurs during diastole and not systole in guinea-pig ventricular myocytes. Pflugers Arch. 1999;437(5):731-736.

毒毛旋花子苷元物理化学性质

[ 密度 ]:
1.432 g/cm3

[ 沸点 ]:
620.7ºC at 760 mmHg

[ 熔点 ]:
169ºC

[ 分子式 ]:
C₂₃H₃₂O₆

[ 分子量 ]:
404.49700

[ 闪点 ]:
214.9ºC

[ 精确质量 ]:
404.22000

[ PSA ]:
104.06000

[ LogP ]:
1.89820

[ 外观性状 ]:
固体

[ 折射率 ]:
1.674

[ 储存条件 ]:
室温

毒毛旋花子苷元MSDS

详细MSDS(安全技术说明书)

毒毛旋花子苷元毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: FH5425000

CHEMICAL NAME :: 5-beta-Card-20(22)-enolide, 3-beta,5,14-trihydroxy-19-oxo-

CAS REGISTRY NUMBER :: 66-28-4

BEILSTEIN REFERENCE NO. :: 0097859

LAST UPDATED :: 199612

DATA ITEMS CITED :: 8

MOLECULAR FORMULA :: C23-H32-O6

MOLECULAR WEIGHT :: 404.55

WISWESSER LINE NOTATION :: L E5 B666TJ AVH E1 IQ MQ OQ F- DT5OV EHJ

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 :: 330 ug/kg

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

REFERENCE :: 85GDA2 "CRC Handbook of Antibiotic Compounds," Vols.1- , Berdy, J., Boca Raton, FL, CRC Press, 1980- Volume(issue)/page/year: 8(2),224,1982

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

ROUTE OF EXPOSURE :: Intracerebral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 63 ug/kg

TOXIC EFFECTS :: Behavioral - convulsions or effect on seizure threshold

REFERENCE :: ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 11,908,1961

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Mammal - cat

DOSE/DURATION :: 224 ug/kg

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

REFERENCE :: JPETAB Journal of Pharmacology and Experimental Therapeutics. (Williams & Wilkins Co., 428 E. Preston St., Baltimore, MD 21202) V.1- 1909/10- Volume(issue)/page/year: 103,420,1951

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Unreported

SPECIES OBSERVED :: Mammal - cat

DOSE/DURATION :: 260 ug/kg

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

REFERENCE :: AIPTAK Archives Internationales de Pharmacodynamie et de Therapie. (Heymans Institute of Pharmacology, De Pintelaan 185, B-9000 Ghent, Belgium) V.4- 1898- Volume(issue)/page/year: 148,471,1964

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rabbit

DOSE/DURATION :: 110 ug/kg

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

REFERENCE :: AEPPAE Naunyn-Schmiedeberg's Archiv fuer Experimentelle Pathologie und Pharmakologie. (Berlin, Ger.) V.110-253, 1925-66. For publisher information, see NSAPCC. Volume(issue)/page/year: 185,329,1937

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - guinea pig

DOSE/DURATION :: 240 ug/kg

TOXIC EFFECTS :: Cardiac - cardiomyopathy including infarction Lungs, Thorax, or Respiration - dyspnea

REFERENCE :: AIPTAK Archives Internationales de Pharmacodynamie et de Therapie. (Heymans Institute of Pharmacology, De Pintelaan 185, B-9000 Ghent, Belgium) V.4- 1898- Volume(issue)/page/year: 155,251,1965

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Mammal - species unspecified

DOSE/DURATION :: 526 ug/kg

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

REFERENCE :: APJUA8 Acta Pharmaceutica Jugoslavica. (FDH, Masarykova 2, 41000 Zagreb, Yugoslavia) V.1-41, 1951-1991. Volume(issue)/page/year: 24,179,1974 *** REVIEWS *** TOXICOLOGY REVIEW CHIMAD Chimia. (Postfach 2027, CH-4001 Basel, Switzerland) V.1- 1947- Volume(issue)/page/year: 5,93,1951

毒毛旋花子苷元安全信息

[ 符号 ]:

GHS06

[ 信号词 ]:
Danger

[ 危害声明 ]:
H300-H310-H330

[ 警示性声明 ]:
P260-P264-P280-P284-P302 + P350-P310

[ 个人防护装备 ]:
Eyeshields;Faceshields;full-face particle respirator type N100 (US);Gloves;respirator cartridge type N100 (US);type P1 (EN143) respirator filter;type P3 (EN 143) respirator cartridges

[ 危害码 (欧洲) ]:
T+: Very toxic;

[ 风险声明 (欧洲) ]:
R26/27/28

[ 安全声明 (欧洲) ]:
S22;S36/S37/S39;S45

[ 危险品运输编码 ]:
UN 2811 6

[ RTECS号 ]:
FH5425000

毒毛旋花子苷元合成路线

详细合成路线

毒毛旋花子苷元上下游产品

毒毛旋花子苷元上游产品

毒毛旋花子苷元下游产品

毒毛旋花子苷元文献

Determination of strophanthidin in ingesta and plant material by LC-MS/MS.

J. Agric. Food Chem. 52 , 2174-8, (2004)

An LC-MS/MS method was developed for the semiquantitative determination of strophanthidin glycosides in ingesta from animals. Strophanthidin glycosides were simultaneously extracted and hydrolyzed to ...

Mechanistic insight into the functional and toxic effects of Strophanthidin in the failing human myocardium.

Eur. J. Heart Fail. 9(11) , 1086-94, (2007)

Cardiac glycosides are characterized by a narrow therapeutic range with Ca2+-overload and arrhythmias occurring at higher concentrations. Data on cardiac glycosides in isolated failing human myocardiu...

Summer pheasant's eye (Adonis aestivalis) poisoning in three horses.

Vet. Pathol. 41(3) , 215-20, (2004)

Three horses died as a result of eating grass hay containing summer pheasant's eye (Adonis aestivalis L.), a plant containing cardenolides similar to oleander and foxglove. A 9-year-old thoroughbred g...

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