Antitumor agents.: 228.: Five new agarofurans, reissantins A-E, and cytotoxic principles from Reissantia buchananiii

Antitumor agents.: 228.: Five new agarofurans, reissantins A-E, and cytotoxic principles from Reissantia buchananiii
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DOI:
10.1021/np030241v
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发表时间:
2003-11-01
影响因子:
5.1
通讯作者:
Lee, KH
Lee, KH
中科院分区:
生物学2区
文献类型:
--
作者:
Chang, FR;Hayashi, K;Lee, KH

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采用生物活性导向的分级分离方法,从布氏瑞仙(Reissantia buchananii)中分离得到21个化合物,其中包括5个新的沉香呋喃倍半萜,reissantins A-E(1-5),并通过波谱数据鉴定了其结构。瑞桑素A-C是首次报道的含有5-羧基-N-甲基-2-吡啶酮(CNMP)取代基的简单沉香呋喃倍半萜,其先前仅在大环沉香呋喃吡啶生物碱中发现。主要的萜类成分雷公藤红素(6)及其甲酯衍生物普里司他林(7)对9种癌细胞系(包括A549、MCF-7、HCT-8、KB、KB-VIN、U-87-MG、PC-3、1A 9和PTX 10细胞系)具有显著活性,ED 50值范围为0.076至0.34 mug/mL。
Twenty-one compounds, including five new agarofuran sesquiterpenes, reissantins A-E (1-5), were isolated from Reissantia buchananii by means of bioassay-directed fractionation and their structures identified from spectral data. Reissantins A-C are the first reported simple agarofuran sesquiterpenes to contain a 5-carboxy-N-methyl-2-pyridone (CNMP) substituent, which has previously been found only in macroring agarofuran pyridine alkaloids. The major terpenoid components, celastrol (6) and its methyl ester derivative, pristimerin (7), were significantly active against nine cancer cell lines, including A549, MCF-7, HCT-8, KB, KB-VIN, U-87-MG, PC-3, 1A9, and PTX10 cell lines, with ED50 values ranging from 0.076 to 0.34 mug/mL.