Isolation of cytotoxic chondropsins, macrolide lactams from the new-caledonian marine sponge Psammoclemma sp and electrospray ion trap multiple stage MS study of these macrolides
Isolation of cytotoxic chondropsins, macrolide lactams from the new-caledonian marine sponge Psammoclemma sp and electrospray ion trap multiple stage MS study of these macrolides
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DOI：
10.1080/14786410310001626811
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发表时间：
2004-10-01
影响因子：
2.2
通讯作者：
Sévenet, T
中科院分区：
文献类型：
--
作者：
Chevallier, C;Laprévote, O;Sévenet, T
沙棘属Psammoclema sp.通过在新喀里多尼亚进行的生物筛选，选定了(磷虾科)作为研究对象。沙棘的粗提物。对KB细胞具有很高的活性，分离得到两个大环内酯类化合物软骨素A1和73-脱氧软骨素A2。通过核磁共振、电喷雾串联质谱仪等波谱手段对其结构进行了鉴定。这些已知的化合物对几种肿瘤细胞株具有细胞毒活性，其IC50约为10(-10)M。流式细胞仪分析表明，软骨素A1和73-脱氧软骨素A2可阻断HL-60和KB细胞进入G(2)/M期，导致细胞死亡。
Psammoclemma sp. (Phoriospongiidae) was selected for study through biological screening carried out in New Caledonia. The crude extract of Psammoclemma sp. was highly active on KB cells and its fractionation led to the isolation of two macrolides chondropsin A 1 and 73-deoxychondropsin A 2. The complex structures were elucidated by a combination of spectroscopic methods (NMR, ESI-MS/MS). These known compounds were evaluated for their cytotoxic activity towards several tumor cell lines and exhibited an IC50 of approximately 10(-10) M. Flow-cytometric analysis revealed that chondropsin A 1 and 73-deoxychondropsin A 2 blocked the entry of HL 60 and KB cells into G(2)/M phase, leading to cell death by apoptosis.