Tabuchi M, Okamoto H, Furutani T, Azuma M, Ooshima H, Otake T, Kawahata T, Kato J
Department of Bioapplied Chemistry, Osaka City University, Japan.
J Enzyme Inhib. 1997 Apr;12(1):27-36. doi: 10.3109/14756369709027661.
Several acyl amino acids and acyl alkanolamines were prepared and screened for their inhibition of octapeptide N-myristoylation and HIV-1 replication in MT-4 cells. Of the 62 acyl derivatives tested, N-myristoyl-O-caproyl-L-serine, N-myristoyl-O-caproyl-D-serine and N-decanoyl-O-myristoyl-L-serine were found to be uncompetitive inhibitors of N-myristoylation, but did not prevent HIV-induced cytopathicity in MT-4 cells. However, other acyl derivatives such as N-3-hydroxymyristoyl ethanolamine, N-3-hydroxymyristoyl-D-serine and N-myristoyl-L-cysteine, which did not inhibit N-myristoylation, suppressed the cytopathicity in the infected cells. The acyl derivatives described here may serve as lead compounds for antiviral agents.
制备了几种酰基氨基酸和酰基链烷醇胺，并对它们在MT - 4细胞中抑制八肽N - 肉豆蔻酰化和HIV - 1复制的能力进行了筛选。在所测试的62种酰基衍生物中，N - 肉豆蔻酰 - O - 己酰 - L - 丝氨酸、N - 肉豆蔻酰 - O - 己酰 - D - 丝氨酸和N - 癸酰 - O - 肉豆蔻酰 - L - 丝氨酸被发现是N - 肉豆蔻酰化的非竞争性抑制剂，但不能阻止HIV在MT - 4细胞中诱导的细胞病变效应。然而，其他酰基衍生物，如N - 3 - 羟基肉豆蔻酰乙醇胺、N - 3 - 羟基肉豆蔻酰 - D - 丝氨酸和N - 肉豆蔻酰 - L - 半胱氨酸，虽然不抑制N - 肉豆蔻酰化，但却能抑制感染细胞中的细胞病变效应。本文所述的酰基衍生物可能作为抗病毒药物的先导化合物。
