PMID: 8585765Oct 1, 1995Paper

Phosphatidyl-2',3'-dideoxy-3'-thiacytidine: synthesis and antiviral activity in hepatitis B-and HIV-1-infected cells

Antiviral Research
H XieK Y Hostetler

Abstract

We recently found that phosphatidyl-2',3'-dideoxycytidine (phosphatidyl-ddC) had substantial anti-hepatitis B virus (HBV) activity in vitro compared to 2',3'-dideoxycytidine (ddC) (Hostetler et al. (1994) Antiviral Res. 24, 59-67). Upon administration of liposomal phosphatidyl-ddC to mice, a 40-fold higher drug area under curve was observed in the liver. To evaluate the possibility of using liver-targeted anti-HBV nucleosides to treat woodchuck hepatitis virus, we wanted to find the most potent and selective lipid conjugates. It has been shown that 2',3'-dideoxy-3'-thiacytidine as a racemic mixture of the cis-isomer (cis-(+/-)-BCH-189) has much greater activity against HBV viruses than ddC in vitro. Recently, it was shown that the (-)-beta-L-enantiomer (3TC) is more active and less toxic than the (+)-beta-D-form ((+)-BCH-189). To determine whether phospholipid conjugates of 3TC retain antiviral activity in 2.2.15 cells as demonstrated previously with ddC, we synthesized the 1,2-dipalmitoyl-sn-glycerol-3-phosphate conjugates of (+/-)-BCH-189 and 3TC and assessed their anti-HBV and anti-HIV activities, in vitro. Phosphatidyl-3TC and phosphatidyl-BCH-189 had antiviral activity comparable to the respective free drugs in 2.2.15 cell...Continue Reading

References

Oct 1, 1991·Proceedings of the National Academy of Sciences of the United States of America·S L DoongY C Cheng
Jan 1, 1987·AIDS Research and Human Retroviruses·J E GroopmanL A Weymouth

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Citations

Jun 10, 1998·Hepatology : Official Journal of the American Association for the Study of Liver Diseases·K ChayamaH Kumada
May 15, 2002·Archives of Pharmacal Research·Henry J LeeDong-Hoon Ko
May 29, 2000·Hepatology : Official Journal of the American Association for the Study of Liver Diseases·C T YehY F Liaw
Oct 8, 2008·Annals of the New York Academy of Sciences·Wei ZhangYing-Ming Feng
Apr 20, 2011·Hepatology : Official Journal of the American Association for the Study of Liver Diseases·Chao-Wei Hsu, Chau-Ting Yeh

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