The biological activity of natural and semisynthetic lupane triterpenoids is discussed in a two-part review. The first part is devoted to the pharmacological properties of natural lupane triterpenoids. Betulinic acid has proven to be the most effective antitumor agent among more than fifty natural lupanes.

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A series of new triterpene hemisuccinates, hemiphthalates and nicotinates have been obtained with 52 -95% yields via reactions of monoacetates of betulin, betulinic acid, and allobetulin with succinic and phthalic anhydrides and with nicotinic acid chloroanhydride. 3-O-Acetylbetulin-28-O-hemiphthalate showed the most pronounced antiinflammatory activity comparable with the effect of ortophen (diclofenac). 3-O-Acetylbetulin-28-O-hemisuccinate exhibited the most pronounced antiulcer activity comparable with that of carbenoxolone.