ArticlePharmaceutical research1998
Lectin-mediated drug targeting: preparation, binding characteristics, and antiproliferative activity of wheat germ agglutinin conjugated doxorubicin on Caco-2 cells.
Article in Pharmaceutical research, 1998. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 9 papers.
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Who cites it
9 citing papers in PubMed, 82 citations in OpenAlex.
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- Lipid-Based Drug Delivery Systems in Cancer Therapy: What Is Available and What Is Yet to Come.Pharmacological reviews · 2016Review
- Biomimickry of UPEC Cytoinvasion: A Novel Concept for Improved Drug Delivery in UTI.Pathogens (Basel, Switzerland) · 2016Article
- Intracellular delivery of nanoparticles of an antiasthmatic drug.AAPS PharmSciTech · 2008Article
- Analysis of unconventional approaches for the rapid detection of surface lectin binding ligands on human cell lines.Acta histochemica · 2006Article
- Direct targeting of cancer cells: a multiparameter approach.Acta histochemica · 2005Article
- Lectins as endocytic ligands: an assessment of lectin binding and uptake to rabbit conjunctival epithelial cells.Pharmaceutical research · 2004Article
- Wheat germ agglutinin binds to the epidermal growth factor receptor of artificial Caco-2 membranes as detected by silver nanoparticle enhanced fluorescence.Pharmaceutical research · 2003Article
- Inhibition of vesicular secretion in both neuronal and nonneuronal cells by a retargeted endopeptidase derivative of Clostridium botulinum neurotoxin type A.Infection and immunity · 2000Article
Corrections and comments
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Authors and funding
5 authors at 2 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
purposeTo investigate the usefulness of wheat germ agglutinin as a targeting carrier protein for an acid-labile chemotherapeutic prodrug directed against colon carcinoma cells in vitro.
methodsCis-aconityl-linked doxorubicin-wheat germ agglutinin was prepared by a two step procedure and the conjugate-binding capacity of target- and non-target cells was assayed by flow cytometry. The antiproliferative activity of the prodrug on Caco-2 and MOLT-4 cells was determined by the XTT- and BrdU-test and compared with that of the parent drug and the lectin alone.
resultsAt pH 4.0, about 50% of the conjugated doxorubicin were released within 24 h from the water soluble prodrug exhibiting a conjugation number of 24 (mol doxorubicin/mol WGA). The prodrug-binding capacity of colon carcinoma cells exceeded that of human colonocytes and lymphoblastic MOLT-4 cells 4.5-fold. Additionally, the antiproliferative effect of the conjugate on Caco-2 cells was 39% as opposed to 5% in case of MOLT-4 cells. As the unmodified carrier protein inhibited or stimulated Caco-2 cell growth in a concentration-dependent manner, the cytostatic activity of the conjugate was determined at WGA concentrations without an effect on cell-proliferation. Considering 50% release of conjugated drug at the most, the prodrug yielded 160% of the cytostatic activity of free doxorubicin.
conclusionsWGA-prodrug targeting offers new perspectives for site-specific, cytoinvading drug delivery in colon cancer chemotherapy.
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