Card-20(22)-enolide,3,5,14-trihydroxy-19-oxo-, (3b,5b)-

Strophanthidin is a naturally available cardiac glycoside[1]. Strophanthidin 0.1 and 1 nmol/L increases and 1~100 µmol/L inhibits the Na+/K+-ATPase activities, but Strophanthidin 10 and 100 nmol/L does not affect Na+/K+-ATPase activities in cardiac sarcolemmal[2]. Strophanthidin increases both diastolic and systolic intracellular Ca2+ concentration[3].

Research Areas >> Cardiovascular Disease

Na+/K+-ATPase[2]

Strophanthidin (0~10 μM; 24 hours; MCF-7, A549, and HepG2 cells) is effective at suppressing the growth of cancer cells and has no toxicity in normal cells[1]. Strophanthidin (0.5 to 500 µM; PBMCs) does not show significant cytotoxicity in PBMCs. Strophanthidin (2 µM; MCF-7 cells) can arrest cell cycle at the G2/M phase[1]. Strophanthidin (MCF-7, A549, and HepG2 cells) is effective at suppressing the growth of cancer cells and has no toxicity in normal cells. Strophanthidin (MCF-7, A549, and HepG2 cells) inhibits the expression of checkpoint and cyclin-dependent kinases in three cancer cells compared to untreated controls. Strophanthidin can modulate the protein localization from the nucleus to the membrane as well as to the cytoplasm. Strophanthidin is a monosaccharide cardiac glycoside with one aglycone portion and without any sugar unit. Strophanthidin induces apoptosis by the attenuation of multiple biochemical signaling pathways and by arresting cell cycle at the G2/M phase through p53-dependent and p53-independent mechanisms[1]. Cell Viability Assay[1] Cell Line: MCF-7, A549, and HepG2 cells Concentration: 0~10 μM Incubation Time: 24 hours Result: Inhibited the proliferation in three different cancer cells.

[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.

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