关键词: (+)-Narciclasine 3-O-Demethyl-6a-dehydroxynortazettine 6a-Dehydroxynortazettine 8-Butoxypretazettine Amaryllidaceae Immunosuppressive activity Narcissus tazetta subsp. chinensis

Mesh : Narcissus / chemistry Humans Animals Alkaloids / pharmacology chemistry isolation & purification Immunosuppressive Agents / pharmacology chemistry isolation & purification Mice Cell Proliferation / drug effects T-Lymphocytes / drug effects Molecular Structure NF-kappa B / metabolism antagonists & inhibitors Benzophenanthridines / pharmacology chemistry isolation & purification Structure-Activity Relationship Dose-Response Relationship, Drug Stereoisomerism Signal Transduction / drug effects Phenanthridines Amaryllidaceae Alkaloids

来  源:   DOI:10.1016/j.phytochem.2024.114198

Abstract:
Three previously undescribed and sixteen known alkaloids were bioguidedly isolated from the bulbs of Narcissus tazetta subsp. chinensis (M.Roem.) Masamura & Yanagih. The structures were elucidated by spectroscopic data, including HRESIMS, NMR, and ECD. Eleven of the isolated alkaloids exhibited immunosuppressive activity on the proliferation of human T cells. (+)-Narciclasine (18) showed the most significantly suppressive activity with an IC50 value of 14 ± 5 nM. In vitro, (+)-narciclasine (18) blocked NF-κB signal transduction, but did not affect PI3K/AKT signal transduction. What was more, (+)-narciclasine significantly reduced ALT and AST levels and alleviated liver damage induced by ConA in AIH mouse model.
摘要:
从Narcissustazetta亚种的鳞茎中生物分离出三种以前未描述的生物碱和16种已知的生物碱。中国(M.Roem.)Masamura&Yanagih。通过光谱数据阐明了结构,包括HRESIMS,NMR,和ECD。11种分离的生物碱对人T细胞增殖具有免疫抑制活性。(+)-Narciclasine(18)显示最显著的抑制活性,IC50值为14±5nM。体外,(+)-沙西拉辛(18)阻断NF-κB信号转导,但不影响PI3K/AKT信号转导。更重要的是,在AIH小鼠模型中,()-沙西拉辛显着降低了ConA诱导的ALT和AST水平,减轻了肝损伤。
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