Drug intelligence / Profile preview

asperulosidic acid

Development stage
Preclinical
Modality
Small Molecules
Administration
Oral, Intravitreal (preclinical/animal Studies)
01

Overview

Asperulosidic acid is a naturally occurring iridoid glycoside mainly isolated from plants such as *Hedyotis diffusa* and *Galium rivale*. It is a small molecule classified as a cyclic enol ether-derived terpene. Asperulosidic acid has demonstrated potent *anti-inflammatory*, *antioxidant*, and *anti-tumor* activities in preclinical studies. Mechanistically, it acts by inhibiting inflammatory cytokine production (such as TNF-α, IL-6, MCP-1, ICAM-1), suppressing the activation of key pathways including *NF-κB* (nuclear factor kappa-light-chain-enhancer of activated B cells), *MAPK* (mitogen-activated protein kinase), and *PI3K/Akt*. Studies in cellular and animal models show that it limits the release and dispersal of cytokines and mediators, notably in models of inflammatory diseases like endotoxin-induced uveitis and inflammation-driven tumor progression[1][5][7]. There is also evidence for reduction of oxidative stress, resistance of certain tumors to chemotherapy, and possible activity in metabolic disease models[1].

Other names
asperuloside acid(1S,4aS,5S,7aS)-7-(acetyloxymethyl)-5-hydroxy-1-[(2S,3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl]oxy-1,4a,5,7a-tetrahydrocyclopenta[c]pyran-4-carboxylic acid25368-11-0asperulosidic acid-RMAsperulosidic acid, 10 mM in DMSOAsperulosidic acid >=90% (LC/MS-ELSD)Cyclopenta[c]pyran-4-carboxylic acid, 7-[(acetyloxy)methyl]-1-(β-D-glucopyranosyloxy)-1,4a,5,7a-tetrahydro-5-hydroxy-(1S,4aS,5S,7aS)-
02

Targets

MEKAKT (RAC-alpha serine/threonine-protein kinase)NF-κBPTGS2 (Prostaglandin-Endoperoxide Synthase 2)NOS2 (Nitric Oxide Synthase 2)PI3K (Phosphoinositide-3-kinase regulatory subunit 6)

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