Fujioka T, Kashiwada Y, Kilkuskie R E, Cosentino L M, Ballas L M, Jiang J B, Janzen W P, Chen I S, Lee K H
Natural Products Laboratory, Division of Medicinal Chemistry, University of North Carolina, Chapel Hill 27599.
J Nat Prod. 1994 Feb;57(2):243-7. doi: 10.1021/np50104a008.
Betulinic acid [1] and platanic acid [2], isolated from the leaves of Syzigium claviforum, were found to be inhibitors of HIV replication in H9 lymphocyte cells. Evaluation of anti-HIV activity with eight derivatives of 1 revealed that dihydrobetulinic acid [3] was also a potent inhibitor of HIV replication. The C-3 hydroxy group and C-17 carboxylic acid group, as well as the C-19 substituents, contribute to enhanced anti-HIV activity. The inhibitory activity of these compounds against protein kinase C (PKC) was also examined, since a correlation between anti-HIV and anti-PKC activities has been suggested. However, there was no apparent correlation between anti-HIV activity and the inhibition of PKC among these compounds.
从菲律宾蒲桃叶中分离得到的桦木酸[1]和悬铃木酸[2]被发现是H9淋巴细胞中HIV复制的抑制剂。对1的八种衍生物的抗HIV活性评估表明，二氢桦木酸[3]也是一种有效的HIV复制抑制剂。C-3羟基和C-17羧酸基团以及C-19取代基有助于增强抗HIV活性。由于有人提出抗HIV和抗蛋白激酶C（PKC）活性之间存在相关性，因此还检测了这些化合物对PKC的抑制活性。然而，在这些化合物中，抗HIV活性与PKC抑制之间没有明显的相关性。
