Exploration of the correlation between the structure, hemolytic activity, and cytotoxicity of steroid saponins.
The hemolytic activity of a collection of 63 steroid saponins was determined. The correlations between these structures and their hemolytic and cytotoxic activities are discussed. It has been demonstrated that the hemolytic activity of steroid saponins is highly dependent on their structures, that is, the sugar length, the sugar linkage, the substitutes on the sugar, as well as the aglycone. It has also been disclosed that the hemolytic activity and cytotoxicity of steroid saponins are not correlated. These results suggest that steroid saponins execute hemolysis and cytotoxic activity in different mechanisms, and encourage to develop steroid saponins into potent antitumor agents devoid of the detrimental effect of hemolysis.
Wang
Yibing
Y
State Key Laboratory of Bio-organic and Natural Products Chemistry, Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences, Shanghai 200032, China.
Zhang
Yichun
Y
Zhu
Ziyan
Z
Zhu
Shilei
S
Li
Yingxia
Y
Li
Ming
M
Yu
Biao
B
D000972:Antineoplastic Agents, Phytogenic / Q000737:chemistry* / Q000494:pharmacology*; D002240:Carbohydrate Sequence; D018922:HL-60 Cells; D006461:Hemolysis / Q000187:drug effects*; D006801:Humans; D066298:In Vitro Techniques; D008969:Molecular Sequence Data; D012503:Saponins / Q000737:chemistry* / Q000494:pharmacology*; D013256:Steroids / Q000737:chemistry* / Q000494:pharmacology*; D013329:Structure-Activity Relationship
D000972:Antineoplastic Agents, Phytogenic; D012503:Saponins; D013256:Steroids