期刊
CHEMICAL & PHARMACEUTICAL BULLETIN
卷 56, 期 12, 页码 1738-1743出版社
PHARMACEUTICAL SOC JAPAN
DOI: 10.1248/cpb.56.1738
关键词
neoechinulin A; structure-activity relationship; reactive oxygen species; reactive nitrogen species; antioxidant
We synthesized a series of neoechinulin A derivatives and examined the structure-activity relationships in terms of their anti-nitration and anti-oxidant activities as well as their cytoprotective activity against peroxynitrite from SIN-1 (3-(4-morpholinyl)sydnonimine hydrochloride) using PC12 cells. Our results showed that the C-8/C-9 double bond, which constitutes a conjugate system with indole and diketopiperazine moieties of neoechinulin A is essential for anti-nitration and anti-oxidant activities as well as protection against SIN-1 cytotoxicity. The presence of an intact diketopiperazine moiety is an additional requirement for anti-nitration activity but not for the cytoprotective action. Our results suggest that the antioxidant activity or electrophilic nature of the C-8 carbon, both of which are afforded by the C-8/C-9 double bond, may play, a role in the cytoprotective properties of this alkaloid.
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