A new bufadienolide with cytotoxic activity from the Chinese traditional drug Ch'an Su.
10.1016/S1875-5364(14)60095-9
- Author:
Ran XU
1
;
Hai-Qin XIE
1
;
Lu-Lu DENG
1
;
Jian-Xin ZHANG
1
;
Fu-Mei YANG
1
;
Jian-Hua LIU
1
;
Xiao-Jiang HAO
1
;
Yuan-Hu ZHANG
2
Author Information
1. The Key Laboratory of Chemistry for Natural Products of Guizhou Province and Chinese Academy of Sciences, Guiyang 550002, China.
2. The Key Laboratory of Chemistry for Natural Products of Guizhou Province and Chinese Academy of Sciences, Guiyang 550002, China. Electronic address: zhangyuanhu@263.net.
- Publication Type:Journal Article
- Keywords:
Bufalin 3β-acrylic ester;
Cytotoxicity;
New bufadienolide;
“Ch'an Su”
- MeSH:
Amphibian Venoms;
chemistry;
pharmacology;
therapeutic use;
Antineoplastic Agents;
chemistry;
isolation & purification;
pharmacology;
therapeutic use;
Biological Products;
chemistry;
pharmacology;
therapeutic use;
Bufanolides;
chemistry;
isolation & purification;
pharmacology;
therapeutic use;
Humans;
Inhibitory Concentration 50;
K562 Cells;
Medicine, Chinese Traditional;
Molecular Structure;
Neoplasms;
drug therapy;
Structure-Activity Relationship
- From:
Chinese Journal of Natural Medicines (English Ed.)
2014;12(8):623-627
- CountryChina
- Language:English
-
Abstract:
AIM:To study the bufadienolides in the Chinese traditional drug "Ch'an Su" and their cytotoxic activity.
METHOD:Various chromatographic techniques were used to isolate the constituents, and their structures were elucidated through physical and spectroscopic data.
RESULTS:Twenty compounds were isolated, and eighteen were evaluated in vitro for their cytotoxic activity against A-549 and K-562 cells.
CONCLUSION:Compound 1 (bufalin 3β-acrylic ester) was a new bufadienolide and exhibited the most potent activity against the two tumor cell lines with IC50 values of 7.16 and 6.83 nmol · L(-1). The relationships between structure and activity are discussed.
