本文对两种具有抗HIV-1活性的药物与RNA 的相互作用进行了探讨。紫外Tm测定及CD光谱结果表明，两种药物均可与polyA·polyU 相互作用，影响其构象的改变。流式细胞仪分析提示药物可不同程度地影响cos-7亚二倍体细胞含量，其中ribavirin的作用更显著。

Replication of human immunodeficiency virus type 1 (HIV-1) requires specific interactions of the Tat protein with the transactivation responsive region (TAR) RNA. Tat-TAR RNA Interaction is mediated by a short arginine-rich domain of the protein. Disruption of this interaction could, in theory, create a state of complete viral latency. Here, four novel 6-amino-6-deoxytrehalose guanidinoglycoside derivatives (10 and 13

目的 研究小分子化合物大环多胺类MP-A、MP-B和MP-C抗人类免疫缺陷病毒（HIV）-1的生物活性机制。方法 通过核酸Tm测定及圆二色（CD）光谱法观察大环多胺类化合物对聚腺尿苷酸PolyA：PolyU构象的影响；核酸断裂实验用琼脂糖凝胶电泳法、流式细胞计数法研究其对细胞凋亡和周期的影响；计算机分子模型Docking计算从理论上判断其与TAR RNA结合的可能性。结果 ①MP-A、MP-B 和MP-C不仅可引起PolyA：PolyU构象的变化使其发生断裂，而且可抑制Tat-RNA相互结合。②MP-A、MP-B和MP-C可影响细胞亚二倍体的含量。③分子模型理论计算结果与实验结果基本一致。结论 大环多胺MP-A、MP-B 和MP-C可能通过与病毒基因组RNA的作用抑制HIV-1 RNA与Tat蛋白的结合而发挥抗HIV-1的活性。

A series of 3-substituted-β-carboline derivatives was synthesized from L-tryptophan. The intercalating binding mode of these compounds with DNA, the effects of the flexible alkylamine side chain on the intercalating a bility and their antitumor activity were studied, which agreed well with the molecular modeling results.

A new Mn(II) complex with the planar ligand 6,7-dicycanodipyrido[2, 2-d: 29, 39-ƒ]quinoxaline (L) [MnL(NO3)(H2O)3]NO 3-CH3OH 3 (1) has been synthesized and characterized by elemental analysis, IR, TG-DTA and molar conductance. Its crystal structure was determined by X-ray diffraction, crystal data: yellow, triclinic, space group P1, Z=2, a =7.3743 (8)Å, b=11.2487 (15)Å, c=14.1655 (15)Å,α=79.412 (2)°,β=83.208(2) °, γ=80.466(2) °. The Mn atom was hexa-coordinated to form a distorted octahedral geometry by two nitrogen atoms of L and four oxygen atoms of three H2O and NO-3 in the complex. The binding mode of the complex with calf thymus DNA has also been investigated with spectrophotometric methods, viscosity and thermal denaturation measurements. The experimental results indicate that the complex intercalated into DNA base pairs via the ligand L. The intrinsic binding constant Kb values for 1 (5.00×10M-1) and L (1.65×105 M-1) were determined by absorption titration and calculated with the model of McGhee and Von Hippel. Biological tests against four different cell lines (HL-60, KB, Hela and BGC-823) in vitro showed that the complex had significant antitumor properties since the 50% inhibition concentrations (IC50) of the complex were within a μM range similar to those of antitumor 50 drug 5-fluorouracil.