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若干重要生理活性天然产物的化学与生物学研究：The Cytotoxicity of Saponins Correlates with Their Cellular Internalization

  • 关键字: The Cytotoxicity of Saponins 发布者：Yibing Wang, Biao Yu* 发布时间：2009-03-02 18:03:58 点击数: 5201次

ChemMedChem 2007, 2, 288-291
 
The Cytotoxicity of Saponins Correlates with Their Cellular Internalization
 
Yibing Wang, Yichun Zhang, and Biao Yu*
 
State Key Laboratory of Bioorganic and Natural Product Chemistry, Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences, Shanghai 200032, China.
 
Abstract. The cover picture shows three structurally similar steroid glycosides bearing fluorescent tags. One crosses the cell membrane faster (top, straight arrow) than the other (left, curved path) to localize in lysosome (red sphere). The third (middle), with a cholesterol aglycone moiety, does not enter into the cell at all. Steroid glycosides are abundant natural surfactants known as saponins, which have membrane-disrupting properties. However, the three saponins represented here are not found in the cell membrane, where cholesterol and sugar chains are abundant.

 

    

Figure. The common saponin dioscin and its fluorescently labeled analogs 1-3.
 
Table. The inhibitory activity of dioscin and its fluorescence-labeled probes (1-3) against the growth of tumor cell lines.
 
 
IC50 (μM)
H4
HeLa
A549
1a
0.15 ± 0.10
1.08 ± 0.09
11.93 ± 0.31
1b
6.31 ± 0.20
0.64 ± 0.14
9.87 ± 0.41
2
49.17 ± 2.60
36.57 ± 3.33
50.00 ± 5.54
3
>> 100
>> 100
>> 100
Dioscin
9.00±0.45
2.90 ± 0.09
4.16 ± 0.73