title: [Solid-phase synthesis and in vitro activity research of tumor-targeting cell-penetrating peptide].
abstract: OBJECTIVE
  To synthesize a tumor-targeting cell-penetrating peptide (CPP) and evaluate its biological activity and cytotoxicity in vitro.
  
  
  METHODS
  With fluorenylmethyloxycarbonyl (Fmoc) as the protective group of α-amino acid, the tumor-targeting CPP were synthesized with stepwise amino acid extension using solid-phase synthesis method. 5-carboxytetramethylrhodamine was added for fluorescence labeling in the presence of the coupling agents HATU and DMF. The purity of the CPP was measured by high-performance liquid chromatography and its molecular weight measured by mass spectrometry. Fluorescence microscope was used to assess the cell-penetrating activity?of the CPP in hepatocellular carcinoma cell lines SMMC-7721 and normal hepatocellular cell lines LO2. The growth activity of CPP-treated SMMC-7721 cells was measured by MTT assay.
  
  
  RESULTS
  With a purity of 96.05% and a relative molecular mass of 3504.9, the synthesized CPP showed no translocation activity in normal hepatocellular cell lines LO2, but showed strong ability to translocate into SMMC-7721 cells without affecting the biological activity of the cells.
  
  
  CONCLUSIONS
  Using Fmoc solid-phase synthesis method, we have successfully synthesized the CPP with tumor-targeting activity.
authors.affiliation: Liver Transplantation Center, Sun Yat-sen University, Guangzhou 510630, China. hejiwenst@163.com
authors.forename: Ji-wen
authors.initials: JW
authors.lastname: He
authors.forename: Hua
authors.initials: H
authors.lastname: Li
authors.forename: Nan
authors.initials: N
authors.lastname: Jiang
authors.forename: Yan
authors.initials: Y
authors.lastname: Tai
authors.forename: Qi
authors.initials: Q
authors.lastname: Zhang
authors.forename: Yang
authors.initials: Y
authors.lastname: Yang
authors.forename: Gui-hua
authors.initials: GH
authors.lastname: Chen
mesh_terms: D045744:Cell Line, Tumor; D057846:Cell-Penetrating Peptides / Q000138:chemical synthesis* / Q000494:pharmacology*; D016503:Drug Delivery Systems; D015195:Drug Design; D006801:Humans; D008113:Liver Neoplasms / Q000188:drug therapy / Q000378:metabolism* / Q000473:pathology; D020778:Matrix Metalloproteinase 2 / Q000378:metabolism*; D012235:Rhodamines / Q000737:chemistry; D060327:Solid-Phase Synthesis Techniques
chemical_list: C437523:5-carboxytetramethylrhodamine; D057846:Cell-Penetrating Peptides; D012235:Rhodamines; D020778:Matrix Metalloproteinase 2