title: In vitro anti-leukemic activity of the ethno-pharmacological plant Scutellaria orientalis ssp. carica endemic to western Turkey.
abstract: OBJECTIVE
  Within the genus Scutellaria various species are used in different folk medicines throughout Asia. Traditional Chinese Medicine (TCM) uses S. baicalensis (Labiatae) to treat various inflammatory conditions. The root shows strong anticancer properties in vitro and was suggested for clinical trials against multiple myeloma. Further, S. barbata was successfully tested against metastatic breast cancer in a phase I/II trial. Therefore, we investigated the anti-cancer properties of S. orientalis L. ssp. carica Edmondson, an endemic subspecies from the traditional medicinal plant S. orientalis L. in Turkey, which is used to promote wound healing and to stop haemorrhage.
  
  
  METHODS
  Freeze-dried plant material was extracted with petroleum ether, dichloromethane, ethyl acetate, and methanol and the bioactivity of these extracts was analysed by proliferation assay, cell death determination, and by investigating protein expression profiles specific for cell cycle arrest and apoptosis.
  
  
  RESULTS
  The strongest anti-leukemic activity was shown by the methanol extract, which contained apigenin, baicalein, chrysin, luteolin and wogonin, with an IpC50 of 43 microg/ml (corresponding to 1.3mg/ml of dried plant material) which correlated with cyclin D1- and Cdc25A suppression and p21 induction. At 132 microg/ml (=4 mg/ml of the drug) this extract caused genotoxic stress indicated by substantial phosphorylation of the core histone H2AX (gamma-H2AX) followed by activation of caspase 3 and signature-type cleavage of PARP resulting in a 55% apoptosis rate after 48 hours of treatment.
  
  
  CONCLUSIONS
  Here, we report for the first time that S. orientalis L. ssp. carica Edmondson exhibited potent anti-leukaemic properties likely through the anti-proliferative effect of baicalein and the genotoxic property of wogonin.
authors: Institute of Biology, Fen-Edebiyat Fakültesi, Adnan Menderes Universitesi, Aydin, Turkey.
authors: Ali
authors: A
authors: Ozmen
authors: Sibylle
authors: S
authors: Madlener
authors: Sabine
authors: S
authors: Bauer
authors: Stanimira
authors: S
authors: Krasteva
authors: Caroline
authors: C
authors: Vonach
authors: Benedikt
authors: B
authors: Giessrigl
authors: Manuela
authors: M
authors: Gridling
authors: Katharina
authors: K
authors: Viola
authors: Nicole
authors: N
authors: Stark
authors: Philipp
authors: P
authors: Saiko
authors: Barbara
authors: B
authors: Michel
authors: Monika
authors: M
authors: Fritzer-Szekeres
authors: Thomas
authors: T
authors: Szekeres
authors: Tülay
authors: T
authors: Askin-Celik
authors: Liselotte
authors: L
authors: Krenn
authors: Georg
authors: G
authors: Krupitza
mesh_terms: D000972:Antineoplastic Agents, Phytogenic / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use*; D017209:Apoptosis / Q000187:drug effects; D053148:Caspase 3 / Q000378:metabolism; D002851:Chromatography, High Pressure Liquid; D019938:Cyclin D1 / Q000037:antagonists & inhibitors; D050759:Cyclin-Dependent Kinase Inhibitor p21 / Q000378:metabolism; D018922:HL-60 Cells; D006657:Histones / Q000378:metabolism; D006801:Humans; D020128:Inhibitory Concentration 50; D015473:Leukemia, Promyelocytic, Acute / Q000188:drug therapy*; D010766:Phosphorylation; D008517:Phytotherapy; D010936:Plant Extracts / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use*; D011065:Poly(ADP-ribose) Polymerases / Q000378:metabolism; D031363:Scutellaria / Q000737:chemistry*; D014421:Turkey; D020687:cdc25 Phosphatases / Q000037:antagonists & inhibitors
chemical_list: D000972:Antineoplastic Agents, Phytogenic; C493956:CDKN1A protein, human; D050759:Cyclin-Dependent Kinase Inhibitor p21; D006657:Histones; D010936:Plant Extracts; D019938:Cyclin D1; D011065:Poly(ADP-ribose) Polymerases; C517004:CDC25A protein, human; D020687:cdc25 Phosphatases; D053148:Caspase 3