Screening, functional analysis and application of polyunsaturated fatty acid-desaturase inhibitors

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(A)Four groups of polyunsaturated fatty acid-desaturase inhibitors were found.(1)Lignan compounds ; both (+) and (-) isomers are DELTA5-desaturase noncompetitive inhibitors. (+)-Sesamin and (-)-asarinin in sesame seeds specifically inhibit DELTA5-desaturase.(2)Alkyl gallate : noncompetitive inhibitors of DELTA5 and DELTA6-desaturases. Propyl gallate inhibits DELTA5 and DELTA6-desaturases. Esterification of carboxylate and 3-hydroxy group in its molecule are essential for the inhibitory activity.(3)Curcumin : noncompetitive inhibitors of DELTA5 and DELTA6-desaturases. The half part of its symmetrical structure is important for the inhibitory activity. Aromatic structure conjugated with double bond, 4-hydroxy and 3-methoxy group in its molecule is essential.(4)Dihydropyridine Ca channel blocker : uncompetitive inhibitors of DELTA5 or DELTA6-desaturases. Nicardipine and nifedipine specifically inhibit DELTA5 and DELTA6-desaturases, respectively.(B)The effects of antioxidants and related compounds, which affects on polyunsaturated fatty acid biosynthesis, on the furan fatty acid (F-acid) biosynthesis were investigated. p-Nitrobenzoic acid was found to inhibit F-acid biosynthesis.(C)The effects of antioxidants and related compounds, which affects on polyunsaturated fatty acid biosynthesis, on docosahexanoic acid (DHA) biosynthesis were investigated. p-Toluic acid affected on DHA biosynthesis. It increased 22 : 5 and decreased 20 : 5.