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Echinacoside | CAS No: 82854-37-3 | GMP-certified suppliers

A medication that exhibits neuroprotective and anti-apoptotic properties, supporting potential applications in neurodegenerative diseases, atherosclerosis, osteoporosis, and inflammatory conditions.

Therapeutic categories

CarbohydratesCOMT SubstratesHerbs and Natural Products
Generic name
Echinacoside
Molecule type
small molecule
CAS number
82854-37-3
DrugBank ID
DB15488
Approval status
Experimental drug

Product Snapshot

  • Echinacoside is an oral small molecule compound
  • It is primarily used for its potential neuroprotective and antioxidant properties
  • The compound is currently in the experimental phase and has not received regulatory approval

Clinical Overview

Echinacoside is a phenylethanoid glycoside originally isolated from Echinacea angustifolia in 1950. Investigational interest centers on its potential therapeutic applications in neurodegenerative diseases such as Parkinson’s and Alzheimer’s, as well as conditions including atherosclerosis, osteoporosis, acute colitis, wound healing, and hepatitis.

The compound exhibits neuroprotective properties primarily through modulation of intracellular signaling pathways. Its mechanism of action involves influencing mitogen-activated protein kinase (MAPK) cascades, nuclear factor kappa-B (NF-κB), caspases 3 and 8, and C/EBP homologous protein (CHOP) pathways, which collectively may contribute to the inhibition of apoptosis in neural cells. This anti-apoptotic effect underpins its proposed utility in neurological disorders, although clinical indications have not been formally established.

Pharmacokinetic profiles, including absorption, distribution, metabolism, and excretion (ADME) parameters, are not comprehensively characterized in the current literature. As a natural product and carbohydrate derivative, metabolism is likely to involve hydrolytic and conjugative processes typical of glycosides, with considerations for bioavailability and blood-brain barrier penetration relevant to neuroprotective effects.

Safety and toxicity data remain limited due to the experimental status of echinacoside. Preclinical studies suggest favorable tolerability; however, extensive toxicological evaluations are necessary before definitive conclusions can be drawn. It is not currently approved for therapeutic use by major regulatory agencies and does not have established branded pharmaceutical products.

For API sourcing, attention to botanical origin, extraction method consistency, and purity specifications is critical to ensure reproducible pharmacological activity. Suppliers should provide detailed certificates of analysis confirming identity, purity, and absence of contaminants. Given its experimental status, rigorous quality control aligned with good manufacturing practices is advisable to support investigational and developmental use.

Identification & chemistry

Generic name Echinacoside
Molecule type Small molecule
CAS 82854-37-3
UNII I04O1DT48T
DrugBank ID DB15488

Pharmacology

SummaryThis compound exerts neuroprotective effects by modulating signaling pathways including mitogen-activated protein kinase, nuclear factor kappa-B, caspases 3 and 8, and CHOP. It targets the growth hormone secretagogue receptor type 1 and androgen receptor, influencing cellular survival and apoptosis mechanisms. The pharmacodynamic profile centers on mitigating neurodegeneration through regulation of inflammatory and apoptotic pathways.
Mechanism of actionThe neuroprotective effects are thought to be mediated via effects on mitogen-activated protein kinase, nuclear factor kappa-B, caspases 3 and 8, as well as CHOP pathways.
Targets
TargetOrganismActions
Growth hormone secretagogue receptor type 1Humansagonist
Androgen receptorHumansagonist

ADME / PK

AbsorptionAnimal studies suggest an oral bioavailability of 0.83%.
MetabolismThe metabolism of echinacoside has been investigated in rats and is thought to involve catechol O-methyltransferase as well as unspecified UDP-gluc- uronosyltransferases and sulfotransferases. A study of echinacoside's metabolism by human intestinal flora identified 13 metabolites which are produced independantly of human metabolism.

Formulation & handling

  • Echinacoside is a small molecule suitable for oral formulation given its moderate water solubility.
  • Its low logP value indicates hydrophilic character, influencing excipient selection for oral delivery.
  • Solid state requires consideration of stability under controlled humidity and temperature during storage and handling.

Regulatory status

Echinacoside is a type of Antimetabolites


Antimetabolites are a prominent category of pharmaceutical active pharmaceutical ingredients (APIs) utilized in the treatment of various diseases, particularly cancer. These compounds are structurally similar to naturally occurring metabolites essential for cellular processes such as DNA and RNA synthesis. By mimicking these metabolites, antimetabolites interfere with the normal functioning of cellular pathways, leading to inhibition of cancer cell growth and proliferation.

One of the widely used antimetabolites is methotrexate, a folic acid antagonist that inhibits the enzyme dihydrofolate reductase, disrupting the production of DNA and RNA. This disruption impedes the growth of rapidly dividing cancer cells. Another common antimetabolite is 5-fluorouracil (5-FU), which inhibits the enzyme thymidylate synthase, thereby interfering with DNA synthesis and inhibiting cancer cell proliferation.

Antimetabolites can be classified into several subcategories based on their mechanism of action and chemical structure. These include purine and pyrimidine analogs, folic acid antagonists, and pyrimidine synthesis inhibitors. Examples of antimetabolites in these subcategories include azathioprine, cytarabine, and gemcitabine.

Despite their effectiveness, antimetabolites can exhibit certain side effects due to their interference with normal cellular processes. These side effects may include gastrointestinal disturbances, myelosuppression (reduced production of blood cells), and hepatotoxicity.

In conclusion, antimetabolites are a vital category of pharmaceutical APIs used in the treatment of various diseases, especially cancer. By mimicking natural metabolites and disrupting crucial cellular processes, these compounds effectively inhibit cancer cell growth and proliferation. However, their usage should be carefully monitored due to potential side effects.