Comparative cell biological study of in vitro antitumor and antimetastatic activity on melanoma cells of GnRH-III-containing conjugates modified with short-chain fatty acids

• Eszter Lajkó,
• Sarah Spring,
• Rózsa Hegedüs,
• Beáta Biri-Kovács,
• Sven Ingebrandt,
• Gábor Mező and
• László Kőhidai

Beilstein J. Org. Chem. 2018, 14, 2495–2509, doi:10.3762/bjoc.14.226

• . [4Lys(Bu)]-GnRH-III(Dau=Aoa) possessing the butyryl side chain acting as a “second drug” proved to be the best candidate for targeted tumor therapy due to its cytotoxicity and immobilizing effect on tumor cell spreading. The applicability of impedimetry and holographic phase imaging for characterizing

• cancer cell behavior and effects of targeted chemotherapeutics with small structural differences (e.g., length of the side chain in 4Lys) was also clearly suggested. Keywords: drug-targeting conjugates; gonadotropin-releasing hormone-III; holographic microscopy; impedimetry; short-chain fatty acids

• concentration. This apparent lack of consistence between the results of impedimetry and the basic morphometric parameters provided by holographic microscopy can be attributed to some method- and cell-related factors. The change in impedance (Cell index) during cell adhesion depends on (i) the cell–cell

Drug targeting to decrease cardiotoxicity – determination of the cytotoxic effect of GnRH-based conjugates containing doxorubicin, daunorubicin and methotrexate on human cardiomyocytes and endothelial cells

• Livia Polgár,
• Eszter Lajkó,
• Pál Soós,
• Orsolya Láng,
• Marilena Manea,
• Béla Merkely,
• Gábor Mező and
• László Kőhidai

Beilstein J. Org. Chem. 2018, 14, 1583–1594, doi:10.3762/bjoc.14.136

• : cardiotoxicity; drug targeting; GnRH-conjugates; HCM; HUVEC; impedimetry; Introduction Gonadotropin-releasing hormone (GnRH) is a peptide hormone secreted by the hypothalamus, which stimulates the release of follicle-stimulating hormone (FSH) and luteinizing hormone (LH) from the pituitary. Thus, it represents

• cardiomyocytes. The rate of cytotoxicity (antitumor effect) vs cardiotoxicity (toxic effects on cardiomyocytes and vascular endothelium) is an important factor for efficient drug development for targeted tumor therapy with minimized side effects. The technique used in this work – impedimetry – is a dedicated one

• for real-time monitoring of cells to distinguish short-term (0–2 hours) and long-term (0–72 hours) effects elicited by the drug or carrier–drug conjugates. The basic theory of impedimetry is that proliferation/viability of cells is well detectable by monitoring of the electric impedance (Z) in an AC