Drug intelligence / Profile preview

ligstroside aglycone

Development stage
Preclinical
Modality
Small Molecules
Administration
Oral
01

Overview

Ligstroside aglycone is a **secoiridoid polyphenol** naturally present in extra virgin olive oil and olives, chemically classified as an iridoid and a monoterpenoid derivative[2][1][8]. It is practically insoluble in water and weakly acidic. It demonstrates **antioxidant and anti-inflammatory properties**, capable of reducing oxidative stress and neutralizing free radicals[3][6][5]. Ligstroside aglycone has been shown to modulate key inflammatory and oxidative stress pathways, including downregulation of **NF-κB, MAPKs, JAK/STAT**, and **NLRP3 inflammasome** activity as well as upregulation of **Nrf2/HO-1**[3][5]. This leads to reduction in pro-inflammatory cytokines, nitric oxide production, and extracellular matrix degradation. It has potential as a **nutraceutical** for conditions characterized by inflammation and cartilage degradation such as osteoarthritis, and it is not currently approved as a pharmaceutical drug[7][9][5]. It is under investigation primarily as a natural extract or dietary supplement compound, not as a synthesized pharmaceutical entity.

Other names
Ligstroside-aglyconeLigustroside Aglyconemethyl (4S,5E,6R)-5-ethylidene-6-hydroxy-4-(2-(2-(4-hydroxyphenyl)ethoxy)-2-oxoethyl)-4H-pyran-3-carboxylatemethyl (2R,3E,4S)-3-ethylidene-2-hydroxy-4-{2-[2-(4-hydroxyphenyl)ethoxy]-2-oxoethyl}-3,4-dihydro-2H-pyran-5-carboxylatep-HPEA-Elenolic acid
02

Targets

PTGS2 (Prostaglandin-Endoperoxide Synthase 2)HMOX1 (Heme oxygenase 1)JAK2 (Janus kinase 2)MEKNF-κBNOX1 (NADPH oxidase 1)NFE2L2 (Nuclear factor (erythroid-derived 2)-like 2)STAT3 (Signal Transducer and Activator of Transcription 3)PTGES (Microsomal prostaglandin E synthase-1)NOS2 (Nitric Oxide Synthase 2)NLRP3 (Nod-like receptor family pyrin domain-containing protein 3)

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