Ionic derivatives of betulinic acid exhibit antiviral activity against herpes simplex virus type-2 (HSV-2), but not HIV-1 reverse transcriptase

Robert J. Visalli, Hannah Ziobrowski, Kameswara R. Badri, Johnny J. He, Xiugen Zhang, Sri Ranjini Arumugam, Hua Zhao

Research output: Contribution to journalArticlepeer-review

12 Scopus citations

Abstract

Abstract Betulinic acid (1) has been modified to ionic derivatives (2-5) to improve its water solubility and biological activities. The binding properties of these derivatives with respect to human serum albumin (HSA) was examined and found to be similar to current anti-HIV drugs. These compounds did not inhibit HIV reverse transcriptase, however, 1, 2 and 5 inhibited herpes simplex type 2 (HSV-2) replication at concentrations similar to those reported for acyclovir (IC50 ∼0.1-10 μM) and with minimal cellular cytotoxicity. IC50 values for antiviral activity against HSV-2 186 were 1.6, 0.6, 0.9, 7.2, and 0.9 μM for compounds 1-5, respectively.

Original languageEnglish
Article number22789
Pages (from-to)3168-3171
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Volume25
Issue number16
DOIs
StatePublished - 3 Jul 2015

Keywords

  • Betulinic acid
  • HIV-1 reverse transcriptase
  • Herpes simplex type 2 (HSV-2)
  • Inhibitor

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