Physicochemical and biopharmaceutical characterization of new sulfonamide derivatives of gallic acid

Gallic acid (GA) is known for its antioxidant activity which is restricted due to its low oral permeability. In this project the carboxylic group of (GA) was substituted with sulfonamide group and hydroxyl groups were methylated which resulted in significantly (p<0.01) increased permeability of 3...

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Published inBritish Journal of Pharmacy Vol. 7; no. 2; pp. S1 - S2
Main Authors Alhyari, Dania Hussein, Sheldrake, Helen Sheldrake, Kantamneni, Sriharsha, Isreb, Mohammad, Soumehsaraei, Shohreh Jafarinejad, Martin, William, Qinna, Nidal, Paluch, Krzysztof
Format Journal Article
LanguageEnglish
Published Huddersfield, United Kingdom University of Huddersfield Press 01.11.2022
Subjects
Analysis
Antioxidants
cyp2d6
Gallic acid
Measurement
Mescaline
Permeability
thbs
tmbs
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Summary:Gallic acid (GA) is known for its antioxidant activity which is restricted due to its low oral permeability. In this project the carboxylic group of (GA) was substituted with sulfonamide group and hydroxyl groups were methylated which resulted in significantly (p<0.01) increased permeability of 3,4,5-trimethoxybenzene sulfonamide (TMBS) and 3,4,5-trihydroxybenzenesulfonamide (THBS) over GA, in Parallel Artificial Membrane Permeability Assay studies with simulated gastrointestinal fluids and Human intestinal epithelial cells HIEC-6 cells. Biochemical studies confirmed TMBS was O-demethylated by CYP2D6. THBS and GA had increased antioxidant activity with increased concentration in DPPH assay while TMBS indicated lower activity at all tested concentration. The antioxidant activity of TMBS was greater than GA in HIEC-6 cells which mainly related to its O-demethylation by CYP2D6.
Bibliography:British Journal of Pharmacy, Vol. 7, No. 2, Nov 2022, S1-S2
Informit, Melbourne (Vic)
ISSN:2058-8356
2058-8356
DOI:10.5920/bjpharm.1138