Rapid structural identification of cytotoxic bufadienolide sulfates in toad venom from Bufo melanosticus by LC-DAD-MS(n) and LC-SPE-NMR.
Toad venom, namely, "Chansu" in China, has been widely used for the treatment of heart failure, sores, pains, and various cancers. Upon LC-MS analysis of the venom from Bufo melanosticus collected in Indonesia, new bufadienolide sulfates were identified. For a complete characterization, the MeOH extract of the toad venom from B. melanosticus was fractionated by preparative HPLC, and the structures of five new buadienolide sulfates (1-5) along with one new bufogenin (6) were rapidly elucidated on the basis of LC-DAD-MS(n) and LC-SPE-NMR data. The in vitro growth inhibitory activity of these six compounds along with hellebrin (positive control) has been assayed by means of the MTT colorimetric assay in four human and two mouse cancer cell lines. Compound 3 and hellebrin displayed similar and marked in vitro cytotoxicity.
Gao
Huimin
H
Institute of Chinese Materia Medica, China Academy of Chinese Medical Sciences, Beijing 100700, People's Republic of China.
Zehl
Martin
M
Kaehlig
Hanspeter
H
Schneider
Peter
P
Stuppner
Hermann
H
Moreno Y Banuls
Laetitia
L
Kiss
Robert
R
Kopp
Brigitte
B
D000664:Amphibian Venoms / Q000737:chemistry*; D000818:Animals; D000970:Antineoplastic Agents / Q000032:analysis / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology; D002018:Bufanolides / Q000032:analysis / Q000737:chemistry / Q000494:pharmacology; D002025:Bufonidae; D004354:Drug Screening Assays, Antitumor; D005260:Female; D006801:Humans; D007214:Indonesia; D051379:Mice; D015394:Molecular Structure; D019906:Nuclear Magnetic Resonance, Biomolecular; D013463:Sulfuric Acid Esters / Q000032:analysis / Q000737:chemistry / Q000494:pharmacology
D000664:Amphibian Venoms; D000970:Antineoplastic Agents; D002018:Bufanolides; D013463:Sulfuric Acid Esters; C087925:bufadienolide