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| Targets |
The primary target of deslanoside is Na⁺/K⁺-ATPase, a membrane-bound enzyme that maintains the electrochemical gradient of sodium and potassium ions across the cell membrane. Na⁺/K⁺-ATPase is a critical enzyme for cellular homeostasis, and its inhibition by cardiac glycosides such as deslanoside leads to increased intracellular sodium concentrations. The elevated intracellular sodium reduces the activity of the sodium-calcium exchanger, leading to increased intracellular calcium concentrations. The increased intracellular calcium enhances the interaction between actin and myosin filaments in cardiac myocytes, resulting in increased cardiac contractility (positive inotropy). Deslanoside's mechanism of action is similar to that of digoxin and other digitalis glycosides.
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| ln Vitro |
Deslanoside (Desacetyllanatoside C) is tricanoside C's metabolite[4]. Deslanoside lowers heart rate, raises forearm blood flow and cardiac index, and considerably lowers tibial muscle sympathetic nerve activity, which is a measure of the activity of the centrally controlled sympathetic nervous system [1].
In vitro, deslanoside demonstrates potent inhibition of Na⁺/K⁺-ATPase activity, leading to increased intracellular calcium concentrations in cardiac myocytes. This results in enhanced cardiac contractility (positive inotropy). The compound's in vitro activity is typically assessed using Na⁺/K⁺-ATPase enzyme assays, where the inhibition of ATP hydrolysis or the release of inorganic phosphate is measured. Additionally, the compound's effects on cardiac myocyte contractility can be assessed using isolated cardiac tissue preparations or cultured cardiac myocytes, where the force of contraction is measured. Deslanoside's in vitro potency is similar to that of other cardiac glycosides. Its effects on cardiac function have been well-characterized in vitro. |
| ln Vivo |
In vivo, deslanoside is used for the treatment and management of congestive cardiac insufficiency, arrhythmias, and heart failure. It lowers heart rate, raises forearm blood flow and cardiac index, and considerably lowers tibial muscle sympathetic nerve activity. These effects contribute to its therapeutic benefits in heart failure and arrhythmias. Deslanoside's positive inotropic effect increases cardiac output, while its negative chronotropic effect (slowing heart rate) reduces myocardial oxygen demand. The compound is administered parenterally (intravenously) for rapid onset of action. Its in vivo efficacy has been demonstrated in clinical studies, where it has been used for decades as a cardiotonic agent.
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| Enzyme Assay |
In vitro enzyme assays for deslanoside measure its ability to inhibit Na⁺/K⁺-ATPase activity. In these assays, purified Na⁺/K⁺-ATPase enzyme is incubated with ATP and the compound, and the release of inorganic phosphate is measured using a colorimetric method. The compound's inhibition of Na⁺/K⁺-ATPase activity is quantified and compared to that of known inhibitors such as ouabain or digoxin. Additionally, the compound's binding to Na⁺/K⁺-ATPase can be assessed using radioligand binding assays with [³H]-ouabain as a tracer. These assays are essential for characterizing the compound's mechanism of action and potency at the enzyme level.
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| Cell Assay |
In vitro cell-based assays for deslanoside evaluate its effects on cardiac myocyte function. Cultured cardiac myocytes or cardiomyocyte cell lines are treated with varying concentrations of deslanoside, and intracellular calcium concentrations are measured using fluorescent calcium indicators such as Fura-2 or Fluo-4. The compound's effects on cell contractility can be assessed using video-based edge detection or electrical field stimulation systems. Cell viability and cytotoxicity are assessed using standard assays such as MTT or LDH release. These assays confirm the compound's mechanism of action and provide functional data on its cellular activity.
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| Animal Protocol |
In vivo animal studies for deslanoside are conducted to evaluate its cardiovascular effects and pharmacokinetic properties. In typical studies, animals (such as dogs, cats, or guinea pigs) are administered deslanoside intravenously, and cardiovascular parameters including heart rate, blood pressure, cardiac output, and contractility are measured. The compound's effects on sympathetic nerve activity can also be assessed. Efficacy studies in animal models of heart failure demonstrate the compound's positive inotropic and negative chronotropic effects. These studies are essential for understanding the compound's hemodynamic effects and for guiding clinical use.
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| ADME/Pharmacokinetics |
Absorption, Distribution and Excretion
Low gastrointestinal absorption (40%). Biological Half-Life 36 hours Deslanoside has a molecular weight of 943.08 and a chemical formula of C₄₇H₇₄O₁₉. It is a cardenolide glycoside that is typically administered intravenously for rapid onset of action. The compound is well-distributed to tissues and is bound to plasma proteins. Deslanoside is metabolized in the liver and excreted primarily in urine, with a half-life of approximately 1-2 days in patients with normal renal function. Its pharmacokinetics can be affected by renal function, and dose adjustment is necessary in patients with renal impairment. The compound's solubility in DMSO is 95 mg/mL (100.73 mM). |
| Toxicity/Toxicokinetics |
Protein Binding
20% Deslanoside has a narrow therapeutic index, similar to other cardiac glycosides. Common side effects include nausea, vomiting, anorexia, and diarrhea due to its effects on the gastrointestinal tract. Cardiac side effects include arrhythmias, bradycardia, and heart block, which can be life-threatening. The compound can also cause visual disturbances, confusion, and other neurological effects. Deslanoside is contraindicated in patients with ventricular tachycardia, ventricular fibrillation, or hypersensitivity to digitalis glycosides. Serum levels should be monitored during therapy to avoid toxicity. The compound is classified as a pregnancy category C drug. |
| References | |
| Additional Infomation |
Deslanoside is a cardiac glycoside formed by replacing the acetoxy group with a hydroxyl group in lanatoside C. It has antiarrhythmic, cardiotonic, metabolite, and EC 3.6.3.9 (Na(+)/K(+)-transporter ATPase) inhibitory effects. It is a 14β-hydroxysteroid, a 12β-hydroxysteroid, a cardiac glycoside, and a tetrasaccharide derivative. Deslanoside C is a cardiac glycoside extracted from the leaves of foxglove (Digitalis lanata). It has been reported that lanatosides are present in green foxglove (Digitalis viridiflora), purple foxglove (Digitalis purpurea), and other organisms with relevant data. Deslanoside C is a cardiac glycoside extracted from the leaves of foxglove (Digitalis lanata). Indications: Used for the treatment and control of congestive heart failure, arrhythmias, and heart failure. Mechanism of Action Digoxin inhibits the Na-K-ATPase membrane pump, leading to increased intracellular sodium and calcium ion concentrations. Increased intracellular calcium ion concentration may promote the activation of contractile proteins (such as actin and myosin). Digoxin also affects cardiac electrical activity, increasing the slope of phase 4 depolarization, shortening the action potential duration, and reducing the maximum diastolic potential. Pharmacodynamics Digoxin is a cardiac glycoside used to treat congestive heart failure and supraventricular arrhythmias caused by reentry mechanisms, as well as to control ventricular rate in the treatment of chronic atrial fibrillation.
Deslanoside (CAS# 17598-65-1) is a cardiac glycoside that inhibits Na⁺/K⁺-ATPase and increases cardiac contractility. It is used for the treatment of congestive cardiac insufficiency, arrhythmias, and heart failure. Deslanoside lowers heart rate and sympathetic nerve activity while increasing cardiac output. It is a cardenolide glycoside and a tetrasaccharide derivative. The compound has a molecular weight of 943.08. It has a narrow therapeutic index and requires careful monitoring during therapy. |
| Molecular Formula |
C47H74O19
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|---|---|
| Molecular Weight |
943.09
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| Exact Mass |
942.482
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| CAS # |
17598-65-1
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| PubChem CID |
28620
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| Appearance |
White to off-white solid powder
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| Density |
1.4±0.1 g/cm3
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| Melting Point |
220-235ºC
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| Index of Refraction |
1.620
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| LogP |
-1.4
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| Hydrogen Bond Donor Count |
9
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| Hydrogen Bond Acceptor Count |
19
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| Rotatable Bond Count |
10
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| Heavy Atom Count |
66
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| Complexity |
1760
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| Defined Atom Stereocenter Count |
26
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| SMILES |
C[C@@H]1[C@H]([C@H](C[C@@H](O1)O[C@H]2CC[C@]3([C@@H](C2)CC[C@@H]4[C@@H]3C[C@H]([C@]5([C@@]4(CC[C@@H]5C6=CC(=O)OC6)O)C)O)C)O)O[C@H]7C[C@@H]([C@@H]([C@H](O7)C)O[C@H]8C[C@@H]([C@@H]([C@H](O8)C)O[C@H]9[C@@H]([C@H]([C@@H]([C@H](O9)CO)O)O)O)O)O
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| InChi Key |
OBATZBGFDSVCJD-LALPQLPRSA-N
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| InChi Code |
InChI=1S/C47H74O19/c1-20-41(64-36-16-30(50)42(21(2)60-36)65-37-17-31(51)43(22(3)61-37)66-44-40(56)39(55)38(54)32(18-48)63-44)29(49)15-35(59-20)62-25-8-10-45(4)24(13-25)6-7-27-28(45)14-33(52)46(5)26(9-11-47(27,46)57)23-12-34(53)58-19-23/h12,20-22,24-33,35-44,48-52,54-57H,6-11,13-19H2,1-5H3/t20-,21-,22-,24-,25+,26-,27-,28+,29+,30+,31+,32-,33-,35+,36+,37+,38-,39+,40-,41-,42-,43-,44+,45+,46+,47+/m1/s1
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| Chemical Name |
3-[(3S,5R,8R,9S,10S,12R,13S,14S,17R)-12,14-dihydroxy-3-[(2R,4S,5S,6R)-4-hydroxy-5-[(2S,4S,5S,6R)-4-hydroxy-5-[(2S,4S,5S,6R)-4-hydroxy-6-methyl-5-[(2S,3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl]oxyoxan-2-yl]oxy-6-methyloxan-2-yl]oxy-6-methyloxan-2-yl]oxy-10,13-dimethyl-1,2,3,4,5,6,7,8,9,11,12,15,16,17-tetradecahydrocyclopenta[a]phenanthren-17-yl]-2H-furan-5-one
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| Synonyms |
Lekozid; Ceglunat; Deslanosid
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~106.04 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (2.21 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (2.21 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (2.21 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.0603 mL | 5.3017 mL | 10.6034 mL | |
| 5 mM | 0.2121 mL | 1.0603 mL | 2.1207 mL | |
| 10 mM | 0.1060 mL | 0.5302 mL | 1.0603 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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