Drug intelligence / Profile preview

arzanol

Development stage
Preclinical
Modality
Small Molecules
Administration
Intraperitoneal
01

Overview

Arzanol is a prenylated phloroglucinol-α-pyrone heterodimer natural product isolated from the Mediterranean plant *Helichrysum italicum*. It functions as a multi-target small molecule with potent anti-inflammatory, antioxidant, and antimicrobial properties. Its primary mechanism involves the dual inhibition of microsomal prostaglandin E2 synthase-1 (mPGES-1) and 5-lipoxygenase (5-LOX), effectively blocking the biosynthesis of pro-inflammatory eicosanoids. Arzanol also modulates the NF-κB signaling pathway, activates SIRT1, and inhibits human dihydroorotate dehydrogenase (hDHODH) and brain glycogen phosphorylase. Research has explored its potential in treating inflammatory conditions, various cancers (notably bladder cancer), metabolic disorders, and viral infections including SARS-CoV-2. Currently in the preclinical stage, its development faces challenges such as high serum protein binding which impacts its pharmacokinetic profile.

Other names
prenylated phloroglucinol-alpha-pyrone heterodimer
02

Targets

ALOX12 (Arachidonate 12-lipoxygenase, 12S type)PYGB (Glycogen phosphorylase, brain form)PTGES (Microsomal prostaglandin E synthase-1)bc1 complex (Cytochrome bc1 complex (plasmodium))NDUFS4 (NADH:ubiquinone oxidoreductase subunit S4)NF-κBSIRT1 (NAD-dependent protein deacetylase sirtuin-1)ALOX5 (Arachidonate 5-lipoxygenase)DHODH (Dihydroorotate dehydrogenase (quinone), mitochondrial)

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