title: In vitro and in vivo evaluation of novel anticancer agents in triple negative breast cancer models.
abstract: Triple negative breast cancer (TNBC) is subtype of breast disease devoid of the estrogen, progesterone, and Her2/neu receptors which are targets for pharmacological intervention. There is a need for novel anti-breast cancer agents that target TNBC. Therefore, novel isochalcone DJ52 was evaluated using the alamar blue dye exclusion assay, the luciferase colony assay, and xenograft models to determine its efficacy and potency. DJ52 significantly decreased proliferation of cells measured by using the alamar blue dye method and produced IC50 values of DJ52, DJ56, and DJ82 at 10-6M, 10-5M, and 10-5M, respectively. In vivo studies were conducted by injecting MDA-MB-231 cells into SCID mice to determine tumor regression was measured over 20 days. DJ52 at 50 mg/kg caused significant decrease in tumor volume (p value <.05) by nearly 50% compared with the control with vehicle alone. These data suggest that DJ52 has merit for further evaluation as a novel anticancer agent.
authors: Division of Basic Pharmaceutical Sciences, Xavier University of Louisiana, School of Pharmacy, 1 Drexel Drive, New Orleans, LA 70125, USA. kparker1@xula.edu
authors: KiTani Parker
authors: KP
authors: Johnson
authors: Letitia A
authors: LA
authors: Yearby
authors: Diana
authors: D
authors: Stoute
authors: Matthew E
authors: ME
authors: Burow
authors: Lyndsay V
authors: LV
authors: Rhodes
authors: Marian
authors: M
authors: Gray
authors: Patrick
authors: P
authors: Carriere
authors: Syreeta L
authors: SL
authors: Tilghman
authors: John A
authors: JA
authors: McLachlan
authors: Josiah
authors: J
authors: Ochieng
mesh_terms: D000818:Animals; D000972:Antineoplastic Agents, Phytogenic / Q000494:pharmacology / Q000627:therapeutic use*; D001943:Breast Neoplasms / Q000188:drug therapy* / Q000473:pathology; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D002599:Chalcone / Q000494:pharmacology / Q000627:therapeutic use*; D005260:Female; D006801:Humans; D051379:Mice; D016513:Mice, SCID; D047368:Tumor Burden / Q000187:drug effects; D023041:Xenograft Model Antitumor Assays
chemical_list: D000972:Antineoplastic Agents, Phytogenic; D002599:Chalcone
references: Mod Pathol. 2005 Aug;18(8):1027-33
references: 15920544
references: Int J Cancer. 2008 Jul 1;123(1):236-40
references: 18398844
references: J Young Pharm. 2012 Apr;4(2):82-7
references: 22754259
references: J Pathol. 2005 Nov;207(3):260-8
references: 16167361
references: Clin Cancer Res. 2007 Aug 1;13(15 Pt 1):4429-34
references: 17671126
references: Bioorg Med Chem Lett. 2010 Oct 1;20(19):5818-21
references: 20729081
references: Cell Mol Biol (Noisy-le-grand). 2001 Sep;47(6):1039-45
references: 11785654
references: Cancer Res. 2010 May 1;70(9):3594-605
references: 20388778
references: Cold Spring Harb Perspect Biol. 2011 Feb 01;3(2):
references: 21047916
references: Breast Cancer Res. 2006;8(4):R34
references: 16846532
references: Anticancer Agents Med Chem. 2012 Oct 1;12(8):902-18
references: 22292766
references: Cancer. 2007 Jan 1;109(1):25-32
references: 17146782
references: Curr Med Chem. 2012;19(25):4324-47
references: 22830339
references: Planta Med. 2010 May;76(8):780-5
references: 20033868
references: Mod Pathol. 2006 Feb;19(2):264-71
references: 16341146
references: Histopathology. 2008 Jan;52(1):108-18
references: 18171422
references: CA Cancer J Clin. 2009 Jul-Aug;59(4):225-49
references: 19474385
references: Curr Med Chem. 2012;19(2):209-25
references: 22320299
references: Molecules. 2012 May 25;17(6):6179-95
references: 22634834
references: Eur J Cancer. 2006 Dec;42(18):3149-56
references: 17055256
references: Breast Cancer (Auckl). 2011;5:175-99
references: 21863131
references: Methods Mol Biol. 2009;471:3-29
references: 19109772
references: Biomed Pharmacother. 2012 Apr;66(3):213-20
references: 22440895