- Semisynthesis of triptolide analogues: Effect of B-ring substituents on cytotoxic activities
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A series of B-ring modified analogues of triptolide were synthesized and tested for their cytotoxicity against two human tumor cell lines (U251 and PC-3). From the current investigation, the structure-cytotoxic activity relationships of these analogues su
- Xu, Hongtao,Chen, Yi,Tang, Huanyu,Feng, Huijin,Li, Yuanchao
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supporting information
p. 5671 - 5674
(2015/01/08)
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- Cytotoxic Biotransformed Products from Triptonide by Aspergillus niger
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The diterpenoid triepoxides are the major active constituents of Tripterygium wilfordii with potent antitumor and immune activities. But the strong toxicity of these compounds has restricted their application to a great extent. In order to find more effective compounds with less toxicity, structural modifications of triptonide (1) by Aspergillus niger (AS 3.739) were investigated and four biotransformed products were obtained. Based on their chemical and spectral data, their structures were elucidated as 5α-hydroxytriptonide (2), triptolide (3), 17-hydroxytriptonide (4), and 16-hydroxytriptonide (5), among which 2, 4 and 5 are new compounds. All the three new transformed products showed cytotoxic activities against the majority of the human tumor cell lines tested, however, they are found to possess less cytotoxic activity when compared with 1. Both compounds 4 and 5 showed similar cytotoxic activity and their IC50 values were 5-15 fold less than 1, while 2 is about 100 times less active than 1.
- Ning, Lili,Qu, Guiqin,Ye, Min,Guo, Hongzhu,Bi, Kaishun,Guo, Dean
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p. 804 - 808
(2007/10/03)
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