Highly active antiretroviral therapy (HAART) has been successful in reducing human immunodeficiency virus (HIV)-1-associated morbidity and mortality since its introduction in 1996. However, it fails to eradicate HIV-1 infection. The high cost of life-long highly active antiretroviral therapy and the emergence of drug resistance among HIV-1-infected individuals have brought renewed pressure for the discovery of novel antivirals and alternative medicines. Traditional Chinese medicine (TCM) is a complementary and alternativemedicine, and serves as a rich resource for newdrug development. Despite the almost 100 plant-derived compounds that are in clinical trials, fewtargetHIV-1 infection. In this study,we discovered that Sanguisorba officinalis extract (SOE) has anti-HIV-1 properties. Using a cell-based assay and single-cycle luciferase reporter viruses pseudotyped with envelopes from HIV-1 or control viruses, we foundthat SOEexhibited significant inhibitory ability against bothCCR5 andCXCR4 tropicHIV-1 (ADAandHXB2),with respective IC50 values of 1.91 0.16 mg/mLand 3.70 0.53 mg/mL. SOE also inhibitedsimianimmunodeficiency virus infection but failed to block vesicular stomatitis virus, severe acute respiratory syndrome coronavirus, and influenza H5N1 pseudoviruses. Furthermore, we showed that SOE had no effect on postentry events of HIV-1 replication. Because SOE pretreatment with the virus but not with cell lines expressing viral receptors showed the maximal inhibitory activity, we can state that SOE probably blocks entry by acting on the viral envelope directly. In addition, SOE was able to inhibit reverse transcriptase inhibitor resistant viruses (K103N, Y188L, and K103N/Y188L/G190A) and a protease inhibitor resistant strain (PI- 2840).Our findingsdemonstrate SOE as anovel andspecific entry inhibitor,whichsheds light on the discovery of anti-HIV-1 drugs from traditional herbalmedicines. Copyright © 2013, Food and Drug Administration, Taiwan.

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