16-acetylgitoxin is a **modified form of the cardiac glycoside gitoxin**. It is a **potent inhibitor of the Na+/K+ ATPase pump**, a crucial enzyme found in the cell membranes of various tissues, especially the heart.
Here's why it's important for research:
**1. Understanding Cardiac Function and Pharmacology:**
* 16-acetylgitoxin's strong inhibitory effect on the Na+/K+ ATPase pump makes it a valuable tool to study the **mechanisms of cardiac contractility and arrhythmias.**
* Researchers can use it to **investigate the role of the Na+/K+ ATPase pump in heart disease** and the development of new therapeutic strategies.
**2. Development of New Cardiac Drugs:**
* 16-acetylgitoxin can serve as a **lead compound for the development of new cardiac drugs** that target the Na+/K+ ATPase pump.
* By understanding its structure and activity, scientists can create **modified versions with improved therapeutic properties and reduced toxicity.**
**3. Drug Discovery and Development:**
* 16-acetylgitoxin can be used in **high-throughput screening assays** to identify new drug candidates that interact with the Na+/K+ ATPase pump.
* This can lead to the discovery of **novel drugs for various medical conditions**, including heart failure, hypertension, and cancer.
**4. Understanding the Toxicity of Cardiac Glycosides:**
* 16-acetylgitoxin is a **highly toxic compound** due to its potent effects on the heart.
* Research on this compound helps **understand the mechanisms of cardiac glycoside toxicity** and develop strategies to mitigate their side effects.
**5. Studying Membrane Transport Processes:**
* 16-acetylgitoxin's interaction with the Na+/K+ ATPase pump provides insights into the **general principles of membrane transport processes.**
* This can be crucial for understanding the function of other membrane transporters and developing new therapies for various diseases.
In summary, 16-acetylgitoxin is a valuable tool in research due to its potent effect on the Na+/K+ ATPase pump, its potential for drug discovery and development, and its role in understanding the toxicity of cardiac glycosides and membrane transport processes.
16-acetylgitoxin: main cardioactive metabolite of penta-acetylgitoxin [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
16-O-acetylgitoxin : A cardenolide glycoside that is the 16-acetate of gitoxin. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]
| ID Source | ID |
|---|---|
| PubMed CID | 10373263 |
| CHEBI ID | 71020 |
| MeSH ID | M0085779 |
| Synonym |
|---|
| 7242-07-1 |
| gitoxin 16-beta-acetate |
| 16-o-acetylgitoxin |
| 16-acetylgitoxin |
| b0p0och2k3 , |
| 16beta-(acetyloxy)-3beta-[2,6-dideoxy-beta-d-ribo-hexopyranosyl-(1->4)-2,6-dideoxy-beta-d-ribo-hexopyranosyl-(1->4)-2,6-dideoxy-beta-d-ribo-hexopyranosyloxy]-14-hydroxy-5beta-card-20(22)-enolide |
| CHEBI:71020 |
| gitoxin 16-acetate |
| Q27139258 |
| 16-acetyl gitoxin |
| gitoxin 16.beta.-acetate |
| card-20(22)-enolide, 16-(acetyloxy)-3-((o-2,6-dideoxy-.beta.-d-ribo-hexopyranosyl-(1->4)-o-2,6-dideoxy-.beta.-d-ribo-hexopyranosyl-(1->4)-2,6-dideoxy-.beta.-d-ribo-hexopyranosyl)oxy)-14-hydroxy-, (3.beta.,5.beta.,16.beta.)- |
| gitoxigenin tridigitoxoside-16-acetate |
| [(3s,5r,8r,9s,10s,13r,14s,16s,17r)-3-[(2r,4s,5s,6r)-5-[(2s,4s,5s,6r)-5-[(2s,4s,5s,6r)-4,5-dihydroxy-6-methyloxan-2-yl]oxy-4-hydroxy-6-methyloxan-2-yl]oxy-4-hydroxy-6-methyloxan-2-yl]oxy-14-hydroxy-10,13-dimethyl-17-(5-oxo-2h-furan-3-yl)-1,2,3,4,5,6,7,8,9, |
| Excerpt | Reference | Relevance |
|---|---|---|
| " Following an open two-compartment model a mean elimination half-life of 60." | ( On the pharmacokinetics of pengitoxin and its cardioactive derivative 16-acetyl-gitoxin. Alken, RG; Becker, U; Haustein, KO; Lach, HJ; Rietbrock, N, 1983) | 0.27 |
| Excerpt | Reference | Relevance |
|---|---|---|
| " In six volunteers the bioavailability of 16AG from two PAG tablet formulations (1." | ( On the pharmacokinetics of 16-acetyl-gitoxin and its bioavailability from pengitoxin-containing tablet formulations. Haustein, KO, 1986) | 0.27 |
| Class | Description |
|---|---|
| cardenolide glycoside | Any member of the class of cardenolides with glycosyl residues attached to position 3. |
| acetate ester | Any carboxylic ester where the carboxylic acid component is acetic acid. |
| [compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res] | |
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 9 (90.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 1 (10.00) | 29.6817 |
| 2010's | 0 (0.00) | 24.3611 |
| 2020's | 0 (0.00) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 0 (0.00%) | 5.53% |
| Reviews | 0 (0.00%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 11 (100.00%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||