Inhibitory effects of alkyl gallate and its derivatives on fatty acid desaturation |
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| Affiliation: | 1. Department of Pharmacy, The Second Affiliated Hospital Of Bengbu Medical College, Hongye Road, Bengbu 233000, China;2. Institute for Liver Diseases, Anhui Medical University, Meishan Road No.81, Hefei 230032, China;1. Institute (College) of Integrative Medicine, Dalian Medical University, No.9 West Section Lvshun South Road, Dalian 116044, China,;2. Institute of Virology and AIDS Research, The First Hospital of Jilin University, Jilin University, Changchun, Jilin Province 130000, China |
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| Abstract: | Alkyl gallate, which is known as an antioxidant, intensively inhibited Δ5 and Δ6 desaturation in both rat liver microsomes and an arachidonic acid-producing fungus Mortierella alpina 1S-4. The rat liver microsomal Δ5 and Δ6 desaturases were inhibited by gallic acid esterified with alcohols with various numbers of carbons, suggesting that the necessary structure in an esterified alcohol for the inhibition is not so strict. Among the three hydroxy groups in gallic acid, the m-hydroxy group was shown to be the necessary structure. Kinetic analyses revealed that propyl gallate is a noncompetitive inhibitor of Δ5 desaturase (Ki = 2.6 · 10−5 M) and Δ6 desaturase (Ki = 1.7 · 10−4 M). These data indicate that alkyl gallate is a new type of desaturase inhibitor and different from known natural inhibitors, i.e., sesamin and curcumin. |
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