A simple, rapid, and sensitive system for the evaluation of anti-viral drugs in rats

Xiaoguang Li, Hua Qian, Fusako Miyamoto, Takeshi Naito, Kumi Kawaji, Kazumi Kajiwara, Toshio Hattori, Masao Matsuoka, Kentaro Watanabe, Shinya Oishi, Nobutaka Fujii, Eiichi N. Kodama

Research output: Contribution to journalArticlepeer-review

9 Citations (Scopus)


The lack of small animal models for the evaluation of anti-human immunodeficiency virus type 1 (HIV-1) agents hampers drug development. Here, we describe the establishment of a simple and rapid evaluation system in a rat model without animal infection facilities. After intraperitoneal administration of test drugs to rats, antiviral activity in the sera was examined by the MAGI assay. Recently developed inhibitors for HIV-1 entry, two CXCR4 antagonists, TF14016 and FC131, and four fusion inhibitors, T-20, T-20EK, SC29EK, and TRI-1144, were evaluated using HIV-1 IIIB and HIV-1 BaL as representative CXCR4- and CCR5-tropic HIV-1 strains, respectively. CXCR4 antagonists were shown to only possess anti-HIV-1 IIIB activity, whereas fusion inhibitors showed both anti-HIV-1 IIIB and anti-HIV-1 BaL activities in rat sera. These results indicate that test drugs were successfully processed into the rat sera and could be detected by the MAGI assay. In this system, TRI-1144 showed the most potent and sustained antiviral activity. Sera from animals not administered drugs showed substantial anti-HIV-1 activity, indicating that relatively high dose or activity of the test drugs might be needed. In conclusion, the novel rat system established here, " phenotypic drug evaluation" , may be applicable for the evaluation of various antiviral drugs in vivo.

Original languageEnglish
Pages (from-to)257-261
Number of pages5
JournalBiochemical and Biophysical Research Communications
Issue number2
Publication statusPublished - 2012 Jul 27


  • CXCR4 antagonist
  • Fusion inhibitor
  • HIV-1
  • MAGI assay
  • Rat


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