Botulinum neurotoxins (BoNTs), a group of bacterial proteins that comprise a light chain disulfide linked aheavy chain, are the most lethal biotoxins known to mankind. By inhibiting neurotransmitter release, BoNTs causesevere neuroparalytic disease, botulism. A series of important findings in the past 10 years which displayed themolecular targets of BoNTs and hence proposed a four-step action mechanism to explain BoNT intoxication greatlyadvanced the study of antibotulismic drug. In this article, we reviewed these progresses and anti-botulismiccompounds found in recent years. These compounds function due to their facilitation on neurotransmitter releaseor to their interference on the binding, intealization, translocation, and endopeptidase activity of the toxins.Toosendanin is a triterpenoid derivative extracted from a digestive tract-parasiticide in Chinese traditional medicine.Chinese scientists have found that the compound is a selective prejunctional blocker. In spite of sharing somesimilar action with BoNT, toosendanin can protect botulism animals that have been administrated with lethal dosesof BoNT/A or BoNT/B for several hours from death and make them restore normal activity. The neuromuscularjunction preparations isolated from the rats that have been injected with toosendanin tolerate BoNT/A challenge.Toosendanin seems to have no effect on endopeptidase activity of BoNT, but blocks the toxin approach to itsenzymatic substrate.