Abstract:

To investigate the chemical constituents in eggs of Bufo gargarizans, the dichloromethane extract was subjected to isolation and purification using various chromatographic techniques. Compound structures were elucidated through comprehensive methods such as NMR, MS, and UV spectroscopy, with in vitro anti-breast cancer cell MCF-7and MDA-MB-231activity evaluated via the MTT assay. Five compounds were isolated and identified as 3-(14-hydroxy-7Z-tetradecenoyl)-hellebrigenol (1), 3-(16-hydroxy-9Z-hexadecanoyl)-hellebrigenol (2), 3-(14-hydroxy-7Z-tetradecenoyl)-1β-hydroxytelecinobufagin (3), 3-(14-hydroxy-tetradecanoyl)-hellebrigenol (4), and 3-oxo-arenobufagin (5). Compounds 1 and 2 are novel, while 5 is a newly reported natural product. The activity test results showed that all compounds exhibited significant anti-breast cancer activities. The IC₅₀ values of compounds 1 and 2 against the triple-negative breast cancer cell line MDA-MB-231 were 0.230 ± 0.028 and 0.215 ± 0.064 μmol/L, respectively.

Key words:

 toad Bufo gargarizans, bufadienolides, fatty acid esters, anti-breast cancer activity