Report on Isoquercetin (DB12665): A Comprehensive Pharmacological and Clinical Monograph

Executive Summary

Isoquercetin (DrugBank ID: DB12665), a naturally occurring flavonoid glycoside, represents a molecule of significant interest at the intersection of pharmaceuticals, nutraceuticals, and functional foods. Its primary identity is not that of a direct therapeutic agent but rather as a highly effective prodrug, or oral delivery system, for its more famous aglycone, quercetin. The core value proposition of Isoquercetin lies in its superior pharmacokinetic profile; the presence of a glucose moiety facilitates active transport in the small intestine, leading to significantly greater bioavailability and higher plasma and tissue concentrations of quercetin compared to the administration of quercetin itself. This enhanced delivery unlocks the in vivo potential of quercetin's well-documented pleiotropic biological activities.

The pharmacodynamic profile of Isoquercetin, mediated by its conversion to quercetin, is characterized by a multi-target mechanism of action. It exhibits potent antioxidant effects by directly scavenging reactive oxygen species and bolstering endogenous defense systems. Its anti-inflammatory properties are linked to the modulation of key signaling pathways such as NF-κB, while its antithrombotic activity involves the inhibition of targets like protein disulfide isomerase (PDI) and platelet aggregation. Direct inhibitory action on enzymes such as Aldo-keto reductase family 1 member B1 (AKR1B1) and Angiotensin-Converting Enzyme (ACE) provides a molecular basis for its potential in managing complications of diabetes and hypertension, respectively.