Journal
FITOTERAPIA
Volume 105, Issue -, Pages 7-15Publisher
ELSEVIER SCIENCE BV
DOI: 10.1016/j.fitote.2015.05.013
Keywords
Skins of Bufo bufo gargarizans; Bufadienolides; Cytotoxicity
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Funding
- Program for National Natural Science Foundation of China [81273391]
- Ministry of Science and Technology of China [2013DFM30080, 2013BAI11B05, 2012ZX09103201-056]
- Program of Pearl River Young Talents of Science and Technology in Guangzhou, China [2013J2200058]
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Twelve new bufadienolides (1-12), along with fourteen known analogues (13-26) were isolated from the skins of Bufo bufo gargarizans Cantor. Their chemical structures were elucidated on the basis of NMR, HRESIMS and X-ray diffraction analysis. Compound 1 was an unusual bufadienolide with 3,19-epoxy moiety and A/B trans ring junction. Compounds 2-4 were rare bufadienolides possessing 10-H or 10-carboxyl units. All the isolated compounds were tested for their cytotoxic effects on HepG2, A549 and HeLa cells. Six new compounds (2, 3, 5, 6, 10 and 12) displayed significant anti-proliferative activities with IC50 values ranging from 0.049 to 1.856 mu M. Arenobufagin (24) exhibited the most potent cytotoxic activity with IC50 value 0.011 mu M. In addition, the present data provided more insight into the structure-activity relationships of bufadienolides. (C) 2015 Elsevier B.V. All rights reserved.
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