Takamune N, Misumi S, Furuishi K, Shoji S
Department of Biochemistry, Faculty of Pharmaceutical Sciences, Kumamoto University, Japan.
IUBMB Life. 1999 Sep;48(3):311-5. doi: 10.1080/713803526.
Six serinal derivatives were synthesized and tested for their anti-human immunodeficiency virus type-1 (HIV-1) activity against HIV-1-infected cells. Of the 6 serinal derivatives tested, only N,O-didecanoyl serinal dimethylacetal (DDSD) was found to strongly suppress progeny virus production from acute HIV-1-infected CEM cells, while not suppressing the HIV-1 p24 production from latent HIV-1-infected ACH-2 cells after stimulation with phorbol 12-myristate 13-acetate. DDSD also inhibited the synthesis of HIV-1 proviral DNA at 20-50 microM, not only 1 h but also 24 h after HIV-1 infection. Taken together, DDSD is a potent inhibitor of HIV-1 production, and may become a unique leading compound for chemotherapy of acquired immunodeficiency syndrome.
合成了六种丝氨酸衍生物，并测试了它们对感染HIV-1的细胞的抗人免疫缺陷病毒1型（HIV-1）活性。在测试的6种丝氨酸衍生物中，仅发现N，O-二十二烷酰丝氨酸二甲缩醛（DDSD）能强烈抑制急性HIV-1感染的CEM细胞产生子代病毒，而在用佛波醇12-肉豆蔻酸酯13-乙酸酯刺激后，不抑制潜伏HIV-1感染的ACH-2细胞产生HIV-1 p24。DDSD在20-50 microM时还抑制HIV-1感染后1小时和24小时的HIV-1前病毒DNA合成。综上所述，DDSD是一种有效的HIV-1产生抑制剂，可能成为获得性免疫缺陷综合征化疗的独特先导化合物。
