IN-VITRO ACTIVITY OF ACYCLIC NUCLEOSIDE PHOSPHONATE DERIVATIVES AGAINST FELINE IMMUNODEFICIENCY VIRUS IN CRANDELL FELINE KIDNEY-CELLS AND FELINE PERIPHERAL-BLOOD LYMPHOCYTES

被引:21
作者
HARTMANN, K
BALZARINI, J
HIGGINS, J
DECLERCQ, E
PEDERSEN, NC
机构
[1] CATHOLIC UNIV LEUVEN,REGA INST MED RES,B-3000 LOUVAIN,BELGIUM
[2] UNIV CALIF DAVIS,SCH VET MED,DEPT MED,DAVIS,CA 95616
关键词
D O I
10.1177/095632029400500103
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
Several novel fluorinated acyclic nucleoside phosphonates [i.e. 9-(3-fluoro-2-phosphonylmethoxy propyl)adenine (FPMPA) and 9-(3-fluoro-2-phosphonylmethoxypropyl)-2,6-diaminopurine (FPMP-DAP)] were evaluated for their inhibitory effect against feline immunodeficiency virus (FIV) replication in Crandell feline kidney (CrFK) cells and feline peripheral blood lymphocytes (PBL) in vitro. Whereas 3'-azido-3'-deoxythymidine (AZT) was not able to achieve complete suppression of viral antigen expression and reverse transcriptase activity in the FIV-infected cell culture supernatants at 25 mum, FPMPA, FPMPDAP, and the 9-(2-phosphonylmethoxyethyl)purine derivatives PMEA and PMEDAP fully protected FIV-infected cells at 5 mum. Both FPMPA and FPMPDAP were endowed with a higher antiviral potency and/or therapeutic selectivity than PMEA and PMEDAP in inhibiting FIV infection, mainly due to a markedly lower toxicity for the cell cultures.
引用
收藏
页码:13 / 19
页数:7
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