Casearin X, Its Degradation Product and Other Clerodane Diterpenes from Leaves of Casearia sylvestris: Evaluation of Cytotoxicity against Normal and Tumor Human Cells
Casearin X, Its Degradation Product and Other Clerodane Diterpenes from Leaves of Casearia sylvestris: Evaluation of Cytotoxicity against Normal and Tumor Human Cells
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DOI：
10.1002/cbdv.200800342
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发表时间：
2010-01-01
影响因子：
2.9
通讯作者：
Cavalheiro, Alberto Jose
中科院分区：
文献类型：
--
作者：
dos Santos, Andre Gonzaga;Pinheiro Ferreira, Paulo Michel;Cavalheiro, Alberto Jose
Casearia sylvestris叶片的EtOH提取物产生新的cleodane二萜，casearin X，以及已知的化合物casearins B， D， L， O和casearin F， casearin X在CDCl3中储存时降解为相应的双醛。所分离的二萜对人癌细胞具有细胞毒性，其中casearin F活性最强，而新克罗丹casearin X是第二种活性化合物，IC50值与阳性对照阿霉素相当。所有分离的二萜对正常人类细胞的活性均低于对癌细胞的活性，这可能表明二萜对癌细胞有选择性作用。Casearin X双醛对癌细胞没有细胞毒性，表明这些CO基团在C（18）和C（19）的出现与细胞毒性活性不相容。
An EtOH extract of the leaves of Casearia sylvestris afforded new clerodane diterpene, casearin X, together with the known compounds casearins B, D, L, and O, and caseargrewiin F Casearin X degraded to the corresponding dialdehyde when stored in CDCl3. The diterpenes isolated were cytotoxic to human cancer cell lines, with caseargrewiin F being the most active and the new clerodane, casearin X, the second active compound with IC50 values comparable to the positive control doxorubicin. All isolated diterpenes showed lower activities against normal human cells than against cancer cell lines, which might indicate a possible selective action on cancer cells. Casearin X dialdehyde was not cytotoxic to cancer cells indicating that the occurrence of these CO groups at C(18) and C(19) is incompatible with the cytotoxic activity.