title: Studies on the antiproliferative effects of tropolone derivatives in Jurkat T-lymphocyte cells.
abstract: Thujaplicins are tropolone-derived natural products with antiproliferative properties. We recently reported that certain tropolones potently and selectively target histone deacetylases (HDAC) and inhibit the growth of hematological cell lines. Here, we investigated the mechanisms by which these compounds exert their antiproliferative activity in comparison with the pan-selective HDAC inhibitor, vorinostat, using Jurkat T-cell leukemia cells. The tropolones appear to work through a mechanism distinct from vorinostat. These studies suggest that tropolone derivatives may serve as selective epigenetic modulators of hematological cells with potential applications as anti-leukemic or anti-inflammatory agents.
authors.affiliation: Department of Pharmaceutical Sciences, University of Connecticut, 69 N. Eagleville Rd., Storrs, CT 06269, United States.
authors.forename: Sophia N
authors.initials: SN
authors.lastname: Ononye
authors.affiliation: Department of Pharmaceutical Sciences, University of Connecticut, 69 N. Eagleville Rd., Storrs, CT 06269, United States.
authors.forename: Michael D
authors.initials: MD
authors.lastname: Vanheyst
authors.affiliation: Department of Pharmaceutical Sciences, University of Connecticut, 69 N. Eagleville Rd., Storrs, CT 06269, United States.
authors.forename: Charles
authors.initials: C
authors.lastname: Giardina
authors.affiliation: Department of Pharmaceutical Sciences, University of Connecticut, 69 N. Eagleville Rd., Storrs, CT 06269, United States.
authors.forename: Dennis L
authors.initials: DL
authors.lastname: Wright
authors.affiliation: Department of Pharmaceutical Sciences, University of Connecticut, 69 N. Eagleville Rd., Storrs, CT 06269, United States. Electronic address: amy.anderson@uconn.edu.
authors.forename: Amy C
authors.initials: AC
authors.lastname: Anderson
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D002453:Cell Cycle / Q000187:drug effects; D049109:Cell Proliferation / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D019169:Jurkat Cells; D015458:Leukemia, T-Cell / Q000188:drug therapy* / Q000473:pathology; D015394:Molecular Structure; D013329:Structure-Activity Relationship; D014334:Tropolone / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D014407:Tumor Cells, Cultured
chemical_list: D000970:Antineoplastic Agents; D014334:Tropolone
keywords: HDAC inhibitor; Leukemia; Natural product; Tropolone; Vorinostat