Biopolym. Cell. 2019; 35(1):54-63.
Bioorganic Chemistry
Use of lectins as vector molecules for delivery of drugs to cells and tissues. Report 2.
1, 2Antonyuk V. O., 1Skorohyd N. R., 2Lozynskyi A. V., 3Antonyuk R. V., 2, 4Lesyk R. B., 1Stoika R. S.
  1. Institute of Cell Biology, NAS of Ukraine
    14/16, Drahomanov Str., Lviv, Ukraine, 79005
  2. Danylo Halytsky Lviv National Medical University
    69, Pekarska Str., Lviv, Ukraine, 79010
  3. Bureau of Forensic Medical Expertise of the Lviv Regional Council
    61, Pekarska Str., Lviv, Ukraine, 79010
  4. University of Information Technology and Management in Rzeszow
    2, Sucharskiego Str., Rzeszow, Poland, 35-225


Aim.To determine cytotoxic effects towards a tumor cells culture of the heterocyclic derivative conjugated with lectins of different carbohydrate specificity. Methods. Conjugation of lectins (Pea seeds (PSA), peanuts (PNA) and erythroagglyutinin from bean seeds (PHA-E) with thiopyrano[2,3-d]thiazole Les-1895, biotesting these conjugates in the cell culture. Results. The conjugates of Les-1895 with specific lectins posses increased cytotoxic effects towards Jurkat cells — by 23 % for PSA-Les-1895, 34 % for PNA-Les-1895, and by 12 % for PHA-E-Les-1895. IC50 of Les-1895 conjugates was ≈ 10 μg/ml, whereas at using free Les-1895 – it was ≈ 30 μg/ml. The PNA and PHA-E conjugates with Les-1895 suppressed the viability of HCT 116 cells more considerably than the PSA conjugate. A cytotoxic action of PNA (IC50 = 4 μg/ml) and PHA-E (IC50 = 3 μg/ml) conjugates was more pronounced than the effect of free Les-1895 (IC50 = 10 μg/ml) or intact lectins. The conjugation of Les-1895 with human serum albumin (HSA) increased the water solubility, however, such conjugation decreased the cytotoxic effect towards Jurkat cells by 40 %. The pseudonormal cells line HEK 293 was less sensitive to the action of native lectins — PSA, PNA and PHA-E as well as to the action of conjugates of these lectins. Conclusions. Conjugation of Les-1895 with specific lectins enhanced a cytotoxic effect. The obtained results suggest a possibility of the addresed delivery of biologically active compounds to specific cells of tissues and organs of the human body.
Keywords: pea lectin, peanut lectin, FGA-R, conjugates, thiopyrano[2,3-d]thiazoles, antitumor activity