title: Ionic derivatives of betulinic acid exhibit antiviral activity against herpes simplex virus type-2 (HSV-2), but not HIV-1 reverse transcriptase.
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.
authors.affiliation: Department of Biomedical Sciences, Mercer University School of Medicine, 4700 Waters Ave., Savannah, GA 31404, USA.
authors.forename: Robert J
authors.initials: RJ
authors.lastname: Visalli
authors.affiliation: Department of Biomedical Sciences, Mercer University School of Medicine, 4700 Waters Ave., Savannah, GA 31404, USA.
authors.forename: Hannah
authors.initials: H
authors.lastname: Ziobrowski
authors.affiliation: Department of Biology, Savannah State University, Savannah, GA 31404, USA.
authors.forename: Kameswara R
authors.initials: KR
authors.lastname: Badri
authors.affiliation: Department of Cell Biology and Immunology, University of North Texas Health Science Center, Fort Worth, TX 76107, USA.
authors.forename: Johnny J
authors.initials: JJ
authors.lastname: He
authors.affiliation: Department of Cell Biology and Immunology, University of North Texas Health Science Center, Fort Worth, TX 76107, USA.
authors.forename: Xiugen
authors.initials: X
authors.lastname: Zhang
authors.affiliation: Department of Biology, Savannah State University, Savannah, GA 31404, USA.
authors.forename: Sri Ranjini
authors.initials: SR
authors.lastname: Arumugam
authors.affiliation: Department of Chemistry and Forensic Science, Savannah State University, 3219 College Street, Savannah, GA 31404, USA. Electronic address: huazhao98@gmail.com.
authors.forename: Hua
authors.initials: H
authors.lastname: Zhao
mesh_terms: D000212:Acyclovir / Q000494:pharmacology; D000818:Animals; D000998:Antiviral Agents / Q000737:chemistry / Q000494:pharmacology; D002522:Chlorocebus aethiops; D054303:HIV Reverse Transcriptase / Q000037:antagonists & inhibitors / Q000378:metabolism; D015497:HIV-1 / Q000201:enzymology; D018258:Herpesvirus 2, Human / Q000502:physiology*; D006801:Humans; D053978:Pentacyclic Triterpenes; D014315:Triterpenes / Q000737:chemistry* / Q000494:pharmacology; D014709:Vero Cells; D014779:Virus Replication / Q000187:drug effects; D000094062:Betulinic Acid
chemical_list: D000998:Antiviral Agents; D053978:Pentacyclic Triterpenes; D014315:Triterpenes; C514824:reverse transcriptase, Human immunodeficiency virus 1; D054303:HIV Reverse Transcriptase; D000212:Acyclovir; D000094062:Betulinic Acid
keywords: Betulinic acid; HIV-1 reverse transcriptase; Herpes simplex type 2 (HSV-2); Inhibitor