Rimando A M, Pezzuto J M, Farnsworth N R, Santisuk T, Reutrakul V, Kawanishi K
Department of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, University of Illinois at Chicago 60612.
J Nat Prod. 1994 Jul;57(7):896-904. doi: 10.1021/np50109a004.
Anolignan A [1] and anolignan B [3] are new dibenzylbutadiene lignans isolated from Anogeissus acuminata. Compounds 1 and 3 were identified as the active HIV-1 reverse transcriptase (RT) inhibitory constituents of this plant obtained by bioassay-guided fractionation. Compound 3, which was very weakly active when tested alone, showed high activity when combined with 1. The activity of 1 was likewise enhanced in the presence of 3. A concave isobole obtained from a plot of data derived from assays with 1 and 3 in combination indicated their synergistic effects. Another new lignan, anolignan C [5], and a known lignan, (-)-secoisolariciresinol [10], were also isolated from this plant. Compounds 5 and 10 did not have activity against HIV-1 RT. Compounds 1, 3 and 5 were either weakly cytotoxic or noncytotoxic when tested in various cancer cell lines. The structures of 1-5 and 10 were established by spectroscopic methods, especially by 1D and 2D nmr experiments.
阿诺木脂素A [1]和阿诺木脂素B [3]是从尖叶非洲栋中分离得到的新型二苄基丁二烯木脂素。化合物1和3经生物活性追踪分离法鉴定为该植物中具有抗HIV-1逆转录酶（RT）活性的成分。化合物3单独测试时活性较弱，但与1联合使用时显示出高活性。在有3存在的情况下，1的活性同样增强。根据1和3联合检测的数据绘制的凹形等效应线表明了它们的协同作用。另一种新木脂素，阿诺木脂素C [5]，以及一种已知木脂素，(-)-开环异落叶松脂素[10]，也从该植物中分离得到。化合物5和10对HIV-1 RT没有活性。在各种癌细胞系中测试时化合物1、3和5要么具有弱细胞毒性，要么无细胞毒性。通过光谱方法，特别是一维和二维核磁共振实验确定了1-5和10的结构。
