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

多不饱和脂肪酸去饱和酶抑制剂的筛选、功能分析及应用

基本信息

批准号：
08456050
负责人：
SHIMIZU Sakayu
金额：
$ 4.54万
依托单位：
KYOTO UNIVERSITY
依托单位国家：
日本
项目类别：
Grant-in-Aid for Scientific Research (B)
财政年份：
1996
资助国家：
日本
起止时间：
1996 至 1997
项目状态：
已结题

来源：
https://kaken.nii.ac.jp/grant/KAKENHI-PROJECT-08456050/
关键词：
Desaturase Inhibitor Propyl gallate Curcumin Ca channel blocker polyunsaturated fatty acid Furan fatty acid Docosahexaenoic acid 不飽和化酸素不飽和脂肪酸

项目摘要

(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.

(A)发现四组多不饱和脂肪酸-去饱和酶抑制剂。(1)木脂素类化合物；（+）和（-）异构体都是delta5 -去饱和酶的非竞争性抑制剂。芝麻中的(+)-芝麻素和(-)-细辛素特异性抑制delta5 -去饱和酶。(2)烷基没食子酸酯：DELTA5和delta6去饱和酶的非竞争性抑制剂。没食子酸丙酯抑制DELTA5和delta6去饱和酶。其分子中羧酸酯和3-羟基的酯化反应是抑制活性的必要条件。(3)姜黄素：DELTA5和delta6去饱和酶的非竞争性抑制剂。其对称结构的半部分对抑制活性起重要作用。其分子中具有双键、4-羟基和3-甲氧基共轭的芳香结构是必不可少的。(4)二氢吡啶钙通道阻滞剂：DELTA5或delta6去饱和酶的非竞争性抑制剂。尼卡地平和硝苯地平分别特异性抑制DELTA5和delta6去饱和酶。(B)研究了影响多不饱和脂肪酸生物合成的抗氧化剂及其相关化合物对呋喃脂肪酸（f -酸）生物合成的影响。对硝基苯甲酸对f酸的生物合成有抑制作用。(C)研究了影响多不饱和脂肪酸生物合成的抗氧化剂及其相关化合物对二十二碳己酸（DHA）生物合成的影响。对甲苯对DHA生物合成的影响。增加22.5%，减少20.5%。