The lectin Griffonia simplicifolia I-A4 (GS I-A4) specifically recognizes terminal alpha-linked N-acetylgalactosaminyl groups and is cytotoxic to the human colon cancer cell lines LS174t and SW1116

Int J Cancer. 1994 May 15;57(4):561-7. doi: 10.1002/ijc.2910570420.


The lectin GS I-A4 binds to terminal alpha-N-acetylgalactosaminyl (GalNAc) groups (which include the Tn antigen), but not to the closely related tumor-associated epitope, sialylated Tn antigen. The lectin also precipitates asialo OSM, but not its native sialylated form. Lectin histochemistry with human colonic tissues showed that GS I-A4 specifically stained specimens of colon cancer and colonic tissues from individuals with FAP; however, normal colonic tissues from patients without colonic disease were rarely stained with this lectin. Glycoconjugates bound by GS I-A4 were observed on the surface membranes of 2 human colon cancer cell lines, LS174t and SW1116, when fluorescein isothiocyanate (FITC)-conjugated GS I-A4 was used. GS I-A4 was toxic to these 2 human colon cancer cell lines in monolayer culture. A dose-response study conducted using 10-160 micrograms/ml, of GS I-A4 demonstrated significant dose-related toxicity against LS174t and SW1116 cells. At concentrations > 80 micrograms/ml, > 99% of LS174t and > 90% of SW1116 cells were killed. Four mM GalNAc specifically inhibited the cytotoxic effect of GS I-A4 (p < 0.001), whereas 4mM N-acetylglucosamine (GlcNAc) had no effect. Two other lectins that recognize terminal alpha-GalNAc residues, DBA and LBL, were significantly less cytotoxic to the colon cancer cells than GS I-A4. In the light of these findings, we speculate that GS I-A4 may have potential use as a diagnostic agent against colorectal cancer.

Publication types

  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, Non-P.H.S.
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Acetylgalactosamine / metabolism*
  • Antigens, Tumor-Associated, Carbohydrate / metabolism
  • Cell Division / drug effects
  • Colon / drug effects
  • Colon / metabolism
  • Colonic Neoplasms / drug therapy*
  • Colonic Neoplasms / metabolism*
  • Epithelium / drug effects
  • Epithelium / metabolism
  • Epitopes / metabolism
  • Glycoconjugates / metabolism
  • Humans
  • Lectins / metabolism*
  • Lectins / toxicity*
  • Plant Lectins*
  • Sensitivity and Specificity
  • Tumor Cells, Cultured / drug effects


  • Antigens, Tumor-Associated, Carbohydrate
  • Epitopes
  • Glycoconjugates
  • Griffonia simplicifolia lectins
  • Lectins
  • Plant Lectins
  • Tn antigen
  • dolichos biflorus agglutinin
  • lima bean lectin
  • sialosyl-Tn antigen
  • Acetylgalactosamine