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
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
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DOI：
10.1021/np50104a008
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发表时间：
1994-02-01
影响因子：
5.1
通讯作者：
LEE, KH
中科院分区：
文献类型：
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作者：
FUJIOKA, T;KASHIWADA, Y;LEE, KH
白桦酸[1]和白桦酸[2]是从棒花雪草叶中分离得到的两种化合物，它们对H9淋巴细胞中的HIV复制有抑制作用。对1的8个衍生物的抗HIV活性的评价表明，二氢白桦酸[3]也是一种有效的HIV复制抑制剂。C-3羟基和C-17羧酸基以及C-19取代基有助于增强抗HIV活性。我们还研究了这些化合物对蛋白激酶C(PKC)的抑制活性，因为抗HIV和抗PKC活性之间存在相关性。然而，这些化合物的抗HIV活性与抑制PKC活性之间没有明显的相关性。
Betulinic acid [1] and platanic acid [2], isolated from the leaves of Syzigium claviflorum, 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.