Ocotillol-type saponins are one kind of tetracyclic triterpenoids, sharing a tetrahydrofuran ring. Natural ocotillol-type saponins have been discovered in Panax. quinquefolius L., Panax japonicus, Hana Mina, and Vietnamese ginseng. In recent years, the semi-synthesis of 20(S/R)-ocotillol-type saponins has been reported. The biological activities of ocotillol-type saponins include neuroprotective effect, anti-myocardial ischemia, anti-inflammatory, anti-bacterial, anti-tumor etc. Owing to characteristics of their chemical structure, pharmacological actions and the stereoselective activity on anti-myocardial ischemia, ocotillol-type saponins are subjected to extensive consideration.