title: [Anticancer effect of triptolide-polyethylenimine-cyclodextrin in vitro].
abstract: To develop a drug delivery system triptolide-polyethylenimine-cyclodextrin and to evaluate its anticancer activity in vitro.
  
  
  
  Triptolide was conjugated to polyethylenimine-cyclodextrin by N, N'-carbonyldiimidazole to form triptolide-polyethylenimine-cyclodextrin. (1)H-NMR, FT-IR and XRD were used to confirm its structure. The anticancer effect of the polymer was assessed by MTT assay, erasion trace test and hematoxylin-eosin staining. The potential to condense siRNA and to delivery siRNA into cytoplasm was demonstrated by gel retardation assay, zeta-potential determination and fluorescence staining.
  
  
  
  Triptolide was successfully conjugated to polyethylenimine-cyclodextrin and the conjugation rate of triptolide was 10% (w/w). siRNA was effectively condensed by the polymer at the N/P ratio of 5, and its particle size was 300 ±15 nm and zeta potential was 8 ±2.5 mV. MTT assay, erasion trace test and hematoxylin-eosin staining revealed that triptolide-polyethylenimine-cyclodextrin had anticancer effect and low cytotoxicity to normal cells. The polymer was able to deliver siRNA to the cytoplasm effectively as demonstrated by fluorescence staining.
  
  
  
  Triptolide-polyethylenimine-cyclodextrin is able to inhibit the growth and migration of cancer cells in vitro and to carry siRNA into cells effectively. It is potential to be used as a novel prodrug for co-delivery of gene and drug in cancer treatment.
authors.affiliation: Institute of Chemical Biology and Pharmaceutical Chemistry, Zhejiang University, Hangzhou, China.
authors.forename: Tian-nan
authors.initials: TN
authors.lastname: Hu
authors.forename: Qi-wen
authors.initials: QW
authors.lastname: Wang
authors.forename: Xue
authors.initials: X
authors.lastname: Jin
authors.forename: Qi-da
authors.initials: QD
authors.lastname: Hu
authors.forename: Xun-shi
authors.initials: XS
authors.lastname: Wang
authors.forename: Sang
authors.initials: S
authors.lastname: Xu
authors.forename: Jun
authors.initials: J
authors.lastname: Zhou
authors.forename: Gu-ping
authors.initials: GP
authors.lastname: Tang
mesh_terms: D000970:Antineoplastic Agents / Q000008:administration & dosage* / Q000494:pharmacology; D045744:Cell Line, Tumor; D003505:Cyclodextrins; D004224:Diterpenes / Q000008:administration & dosage* / Q000494:pharmacology; D004337:Drug Carriers; D004852:Epoxy Compounds / Q000008:administration & dosage / Q000494:pharmacology; D006801:Humans; D053758:Nanoparticles; D010616:Phenanthrenes / Q000008:administration & dosage* / Q000494:pharmacology; D011094:Polyethyleneimine; D011108:Polymers
chemical_list: D000970:Antineoplastic Agents; D003505:Cyclodextrins; D004224:Diterpenes; D004337:Drug Carriers; D004852:Epoxy Compounds; D010616:Phenanthrenes; D011108:Polymers; C001899:triptolide; D011094:Polyethyleneimine