title: Inflammation-responsive antioxidant nanoparticles based on a polymeric prodrug of vanillin.
abstract: Oxidative stress is induced by accumulation of hydrogen peroxide (H2O2), and therefore, H2O2 could serve as a potential biomarker of various oxidative stress-associated inflammatory diseases. Vanillin is one of the major components of natural vanilla and has potent antioxidant and anti-inflammatory activities. In this work, we developed a novel inflammation-responsive antioxidant polymeric prodrug of vanillin, termed poly(vanillin oxalate) (PVO). In design, PVO incorporates H2O2-reacting peroxalate ester bonds and bioactive vanillin via acid-responsive acetal linkages in its backbone. Therefore, in cells undergoing damages by oxidative stress, PVO readily degrades into three nontoxic components, one of which is antioxidant and anti-inflammatory vanillin. PVO nanoparticles exhibit potent antioxidant activities by scavenging H2O2 and inhibiting the generation of ROS (reactive oxygen species) and also reduce the expression of pro-inflammatory cytokines in activated macrophages in vitro and in vivo. We, therefore, anticipate that PVO nanoparticles have great potential as novel antioxidant therapeutics and drug delivery systems for ROS-associated inflammatory diseases.
authors.affiliation: Department of BIN Fusion Technology, Chonbuk National University, Jeonju, 561-756, Korea.
authors.forename: Jeongil
authors.initials: J
authors.lastname: Kwon
authors.forename: Jihye
authors.initials: J
authors.lastname: Kim
authors.forename: Seunggyu
authors.initials: S
authors.lastname: Park
authors.forename: Gilson
authors.initials: G
authors.lastname: Khang
authors.forename: Peter M
authors.initials: PM
authors.lastname: Kang
authors.forename: Dongwon
authors.initials: D
authors.lastname: Lee
mesh_terms: D000818:Animals; D000893:Anti-Inflammatory Agents / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000494:pharmacology; D000975:Antioxidants / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000494:pharmacology; D001547:Benzaldehydes / Q000737:chemistry*; D015415:Biomarkers / Q000737:chemistry; D004146:Dioxanes / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000494:pharmacology; D006861:Hydrogen Peroxide / Q000737:chemistry*; D007249:Inflammation / Q000517:prevention & control; D008264:Macrophages / Q000187:drug effects / Q000378:metabolism; D051379:Mice; D053758:Nanoparticles / Q000737:chemistry* / Q000627:therapeutic use; D018384:Oxidative Stress; D011091:Polyesters / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000494:pharmacology; D011355:Prodrugs / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000494:pharmacology; D017382:Reactive Oxygen Species / Q000037:antagonists & inhibitors; D014409:Tumor Necrosis Factor-alpha / Q000037:antagonists & inhibitors / Q000096:biosynthesis
chemical_list: D000893:Anti-Inflammatory Agents; D000975:Antioxidants; D001547:Benzaldehydes; D015415:Biomarkers; D004146:Dioxanes; D011091:Polyesters; D011355:Prodrugs; D017382:Reactive Oxygen Species; D014409:Tumor Necrosis Factor-alpha; C584945:poly(vanillin oxalate); D006861:Hydrogen Peroxide; C100058:vanillin