1. Academic Validation
  2. Premna microphylla Turcz pectin-modified diosmetin nanoparticles: A galectin-3 targeting strategy for precise colitis intervention

Premna microphylla Turcz pectin-modified diosmetin nanoparticles: A galectin-3 targeting strategy for precise colitis intervention

  • Carbohydr Polym. 2025 Nov 15;368(Pt 1):124067. doi: 10.1016/j.carbpol.2025.124067.
Yuanyuan Chen 1 Qian Zhou 2 Yue Zhou 3 Jinlan Huang 4 Renjie Niu 4 Jian Ming 5 Mingfu Wang 6
Affiliations

Affiliations

  • 1 College of Civil and Transportation Engineering, Shenzhen University, Shenzhen 518060, PR China; Shenzhen Key Laboratory of Food Nutrition and Health, College of Chemistry and Environmental Engineering, Shenzhen University, Shenzhen 518060, PR China.
  • 2 School of Food Science and Technology, Jiangnan University, Wuxi 214122, PR China.
  • 3 Shenzhen Key Laboratory of Food Nutrition and Health, College of Chemistry and Environmental Engineering, Shenzhen University, Shenzhen 518060, PR China.
  • 4 Institute for Advanced Study, Shenzhen University, Shenzhen 518060, PR China.
  • 5 College of Food Science, Southwest University, Chongqing 400715, PR China. Electronic address: mingjian1972@163.com.
  • 6 Shenzhen Key Laboratory of Food Nutrition and Health, College of Chemistry and Environmental Engineering, Shenzhen University, Shenzhen 518060, PR China. Electronic address: mfwang@szu.edu.cn.
Abstract

Oral delivery of natural Antioxidants represents a promising therapeutic strategy for ulcerative colitis (UC), yet their therapeutic efficacy is hindered by instability and poor accumulation at inflamed sites. To address this, we developed Galectin-3 (Gal-3)-targeted nanoparticles (ZDP-NPs) by encapsulating diosmetin within zein complexes modified with a galactose- and rhamnogalacturonan-I (RG-I)-rich pectin (PMTP, Mw: 228.8 kDa, DM: 34.21 %, RG-I content: 43 %) extracted from Premna microphylla Turcz leaves. Surface plasmon resonance (SPR) analysis confirmed a strong binding affinity between PMTP and Gal-3 (KD = 2.83 μM). ZDP-NPs exhibited uniform spherical morphology (~170 nm), high drug loading (87.9 %) and colloidal stability. Under simulated gastrointestinal conditions, ZDP-NPs showed reduced Dio release (45.6 %) compared to PMTP-free nanoparticles (ZD-NPs, 75.6 %). In vitro studies showed that PMTP surface modification significantly enhanced nanoparticle uptake by LPS-induced macrophages via Gal-3-mediated endocytosis. In vivo colitis experiment of mice revealed that ZDP-NPs selectively accumulated in inflamed colons via Gal-3 targeting, prolonged retention, and significantly alleviated colonic damage by reducing oxidative stress, suppressing pro-inflammatory cytokines, and restoring epithelial barrier integrity. Biocompatibility assays confirmed minimal toxicity of ZDP-NPs. This study presented a food-derived pectin-based nanoplatform for precise colitis intervention through Gal-3 targeting, offering a multifaceted strategy to break the inflammation-oxidative stress cycle.

Keywords

Colitis; Diosmetin; Galectin-3 targeting; Nanoparticle drug delivery; Premna microphylla Turcz pectin.

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