Blockage of HIV-1 production through inhibition of proviral DNA synthesis by N,O-didecanoyl serinal dimethylacetal.
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.
Takamune
N
N
Department of Biochemistry, Faculty of Pharmaceutical Sciences, Kumamoto University, Japan.
Misumi
S
S
Furuishi
K
K
Shoji
S
S
D000080:Acetals / Q000737:chemistry / Q000494:pharmacology*; D019380:Anti-HIV Agents / Q000737:chemistry / Q000494:pharmacology*; D002460:Cell Line; D004279:DNA, Viral / Q000187:drug effects; D015658:HIV Infections / Q000188:drug therapy*; D015497:HIV-1 / Q000187:drug effects* / Q000502:physiology; D006801:Humans; D011533:Proviruses / Q000187:drug effects* / Q000235:genetics; D012694:Serine / Q000031:analogs & derivatives* / Q000737:chemistry / Q000494:pharmacology; D013601:T-Lymphocytes / Q000821:virology*; D014779:Virus Replication / Q000187:drug effects
D000080:Acetals; D019380:Anti-HIV Agents; D004279:DNA, Viral; C405666:N,O-didecanoyl serinal dimethylacetal; D012694:Serine