Taxifolin and gastro-adhesive microparticles containing taxifolin promotes gastric healing in vivo, inhibits Helicobacter pylori in vitro and proton pump reversibly in silico
| Autor: | Bruna Longo, Larissa Venzon, Francesco Antonio Greco, Tauani Caroline Santos França, Antonio Macchiarulo, Tania Mari Bellé Bresolin, Maurizio Ricci, Luisa Mota da Silva, Mariane Meurer, Valdir Cechinel-Filho, Alexandre Bella Cruz, Lincon Bordignon Somensi, Fernanda Cristina Stenger Moura, Aurelie Marie Madeleine Schoubben, Luísa Nathália Bolda Mariano |
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| Rok vydání: | 2021 |
| Předmět: |
0301 basic medicine
Antioxidant medicine.medical_treatment Pharmacology Toxicology Antioxidants H(+)-K(+)-Exchanging ATPase chemistry.chemical_compound 0302 clinical medicine Acetic Acid biology Stomach General Medicine Proton Pumps Catalase medicine.anatomical_structure 030220 oncology & carcinogenesis Female Quercetin Helicobacter Infections 03 medical and health sciences In vivo Adhesives medicine Animals Taxifolin Computer Simulation Stomach Ulcer Rats Wistar Wound Healing Helicobacter pylori Plant Extracts Gastric Mucins Mucin Glutathione Anti-Ulcer Agents biology.organism_classification Rats 030104 developmental biology chemistry Gastric Mucosa biology.protein Protom pump reversible inhibition Phytotherapy |
| Zdroj: | Chemico-Biological Interactions. 339:109445 |
| ISSN: | 0009-2797 |
| Popis: | Taxifolin (3,5,7,3,4-pentahydroxy flavanone or dihydroquercetin, Tax) was identified as a gastroprotective compound and a gastroadhesive formulation was recently developed to prolong its residence time and release in the stomach. So, the gastric healing effectiveness of Tax and gastro-mucoadhesive microparticles containing Tax (MPTax) against the acetic acid induced-gastric ulcer in rats was investigated in this study. Moreover, the interactions between Tax and H+/K+-ATPase were investigated in silico, and its anti- H. pylori activity was determined in vitro. The oral treatment with MPTax (81.37 mg/kg, containing 12.29% of Tax) twice a day for seven days reduced the ulcer area by 63%, compared to vehicle-treated group (Veh: 91.9 ± 10.3 mm2). Tax (10 mg/kg, p.o) reduced the ulcer by 40% but with a p = 0.07 versus Veh group. Histological analysis confirmed these effects. Tax and MPTax increased the gastric mucin amount, reduced the myeloperoxidase activity, and increased the glutathione reduced content at ulcer site. However, only MPTax decreased the lipoperoxide accumulation at ulcer site. Besides, Tax and MPTax normalize the catalase and glutathione S-transferase activity. Tax showed reversible interaction with H+/K+-ATPase in silico and its anti-H. pylori effects was confirmed (MIC = 625 μg/mL). These results suggest that the antiulcer property of Tax involves the strengthening of the gastric protective factors in parallel to its inhibitory interaction with H+/K+-ATPase and H. pylori. Considering that ulcer healing action displayed by Tax was favored by gastroadhesive microparticles, this approach seems to be promising for its oral delivery to treat acid-peptic diseases. |
| Databáze: | OpenAIRE |
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