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Bioorg Med Chem Lett. 2015 Aug 15;25(16):3168-71. doi: 10.1016/j.bmcl.2015.05.099. Epub 2015 Jun 6.

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

Author information

1
Department of Biomedical Sciences, Mercer University School of Medicine, 4700 Waters Ave., Savannah, GA 31404, USA.
2
Department of Biology, Savannah State University, Savannah, GA 31404, USA.
3
Department of Cell Biology and Immunology, University of North Texas Health Science Center, Fort Worth, TX 76107, USA.
4
Department of Chemistry and Forensic Science, Savannah State University, 3219 College Street, Savannah, GA 31404, USA. Electronic address: huazhao98@gmail.com.

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.

KEYWORDS:

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

PMID:
26112446
PMCID:
PMC4494873
DOI:
10.1016/j.bmcl.2015.05.099
[Indexed for MEDLINE]
Free PMC Article

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