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氧化偶联反应制备生物活性木脂素的研究。I. 与裂环鹅掌楸素相关的苯并呋喃木脂素的制备及其对脂质过氧化的抑制作用。

Studies on the preparation of bioactive lignans of oxidative coupling reaction. I. Preparation and lipid peroxidation inhibitory effect of benzofuran lignans related to schizotenuins.

作者信息

Maeda S, Masuda H, Tokoroyama T

机构信息

New Drug Research Laboratories, Kanebo Co., Ltd., Osaka, Japan.

出版信息

Chem Pharm Bull (Tokyo). 1994 Dec;42(12):2500-5. doi: 10.1248/cpb.42.2500.

DOI:10.1248/cpb.42.2500
PMID:7697764
Abstract

The parent benzofuran lignan 4 of schizotenuins 1-3 and related compounds were efficiently prepared by a judicious use of the oxidative coupling reaction, and were tested for their inhibitory effects on lipid peroxidation in rat brain homogenate and rat liver microsomes. Among twelve compounds tested in rat brain homogenate, compounds 13, 14 and 16 showed prominent inhibitory activity. Compounds 13 and 16 were then tested in rat liver microsomes, and their activity was found to be more potent than schizotenuin A (1) and much more potent than that of (+/-)-alpha-tocopherol.

摘要

通过合理运用氧化偶联反应高效制备了裂环鹅掌楸素1 - 3及其相关化合物的母体苯并呋喃木脂素4,并测试了它们对大鼠脑匀浆和大鼠肝微粒体脂质过氧化的抑制作用。在大鼠脑匀浆中测试的十二种化合物中,化合物13、14和16表现出显著的抑制活性。随后在大鼠肝微粒体中对化合物13和16进行了测试,发现它们的活性比裂环鹅掌楸素A(1)更强,且比(±)-α-生育酚的活性强得多。

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