title: Anti-proliferative properties of commercial Pelargonium sidoides tincture, with cell-cycle G0/G1 arrest and apoptosis in Jurkat leukaemia cells.
abstract: Context Pelargonium sidoides DC (Geraniaceae) is an important medicinal plant indigenous to South Africa and Lesotho. Previous studies have shown that root extracts are rich in polyphenolic compounds with antibacterial, antiviral and immunomodulatory activities. Little is known regarding the anticancer properties of Pelargonium sidoides extracts. Objective This study evaluates the anti-proliferative effects of a Pelargonium sidoides radix mother tincture (PST). Materials and methods The PST was characterized by LC-MS/MS. Anti-proliferative activity was evaluated in the pre-screen panel of the National Cancer Institute (NCI-H460, MCF-7 and SF-268) and the Jurkat leukaemia cell line at concentrations of 0-150 μg/mL. The effect on cell growth was determined with sulphorhodamine B and 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assays after 72 h. The effect on cell cycle and apoptosis induction in Jurkat cells was determined by flow cytometry with propidium iodide and Annexin V: fluorescein isothiocyanate staining. Results Dihydroxycoumarin sulphates, gallic acid as well as gallocatechin dimers and trimers were characterized in PST by mass spectrometry. Moderate anti-proliferative effects with GI50 values between 40 and 80 μg/mL were observed in the NCI-pre-screen panel. Strong activity observed with Jurkat cells with a GI50 value of 6.2 μg/mL, significantly better than positive control 5-fluorouracil (GI50 value of 9.7 μg/mL). The PST arrested Jurkat cells at the G0/G1 phase of the cell cycle and increased the apoptotic cells from 9% to 21%, while the dead cells increased from 4% to 17%. Conclusion We present evidence that P. sidoides has cancer cell type-specific anti-proliferative effects and may be a source of novel anticancer molecules.
authors.affiliation: a Department of Biochemistry, Faculty of Natural and Agricultural Sciences , University of Pretoria , Pretoria , South Africa ;
authors.forename: Andreia
authors.initials: A
authors.lastname: Pereira
authors.affiliation: b Department of Anatomy, Faculty of Health Sciences , University of Pretoria , Pretoria , South Africa ;
authors.forename: Megan
authors.initials: M
authors.lastname: Bester
authors.affiliation: c Department of Crop Sciences, Faculty of Science , Tshwane University of Technology , Pretoria , South Africa.
authors.forename: Puffy
authors.initials: P
authors.lastname: Soundy
authors.affiliation: a Department of Biochemistry, Faculty of Natural and Agricultural Sciences , University of Pretoria , Pretoria , South Africa ;
authors.forename: Zeno
authors.initials: Z
authors.lastname: Apostolides
mesh_terms: D000972:Antineoplastic Agents, Phytogenic / Q000302:isolation & purification / Q000494:pharmacology*; D017209:Apoptosis / Q000187:drug effects*; D049109:Cell Proliferation / Q000187:drug effects*; D002853:Chromatography, Liquid; D004305:Dose-Response Relationship, Drug; D059585:G1 Phase Cell Cycle Checkpoints / Q000187:drug effects*; D006801:Humans; D019169:Jurkat Cells; D015458:Leukemia, T-Cell / Q000188:drug therapy* / Q000473:pathology; D061986:MCF-7 Cells; D031316:Pelargonium / Q000737:chemistry; D008517:Phytotherapy; D010936:Plant Extracts / Q000302:isolation & purification / Q000494:pharmacology*; D018517:Plant Roots; D010946:Plants, Medicinal; D016192:Resting Phase, Cell Cycle / Q000187:drug effects*; D053719:Tandem Mass Spectrometry; D013997:Time Factors
chemical_list: D000972:Antineoplastic Agents, Phytogenic; D010936:Plant Extracts
keywords: Anticancer; apoptosis; cell-cycle arrest; polyphenolics