ANTI-AIDS AGENTS .11. BETULINIC ACID AND PLATANIC ACID AS ANTI-HIV PRINCIPLES FROM SYZIGIUM-CLAVIFLORUM, AND THE ANTI-HIV ACTIVITY OF STRUCTURALLY RELATED TRITERPENOIDS

Betulinic acid [1] and platanic acid [2], isolated from the leaves of Syzigium claviflorum, were found to be inhibitors of HIV replication i n H9 lymphocyte cells. Evaluation of anti-HIV activity with eight deri vatives of 1 revealed that dihydrobetulinic acid [3] was also a potent inhibitor of HIV replication. The C-3 hydroxy group and C-17 carboxyl ic acid group, as well as the C-19 substituents, contribute to enhance d anti-HIV activity. The inhibitory activity of these compounds agains t protein kinase C (PKC) was also examined, since a correlation betwee n anti-HIV and anti-PKC activities has been suggested. However, there was no apparent correlation between anti-HIV activity and the inhibiti on of PKC among these compounds.