Synthesis and Antiproliferative Activity of Conjugates of Anthracycline Antibiotics with Sesquiterpene Lactones of the Elecampane
- Authors: Semakov A.V.1, Anikina L.V.1, Afanasyeva S.V.1, Pukhov S.A.1, Klochkov S.G.1
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Affiliations:
- Institute of Physiologically Active Compounds
- Issue: Vol 44, No 5 (2018)
- Pages: 538-546
- Section: Article
- URL: https://journals.rcsi.science/1068-1620/article/view/229021
- DOI: https://doi.org/10.1134/S1068162018040167
- ID: 229021
Cite item
Abstract
The daunorubicin and doxorubicin anthracycline antibiotics were modified with the Inula helenium L. sesquiterpene lactones (alantolactone, isoalantolactone, and alloalantolactone) and with their epoxy derivatives. Antiproliferative properties of these conjugates were studied on tumor and normal cell lines. The daunorubicin conjugates with the sesquiterpene lactones (isoalantolactone, allantolactone, and alloalantolactone) and with their epoxy derivatives were found to exhibit the higher activity against human tumor cell lines than the corresponding doxorubicin conjugates. The daunorubicin conjugate with epoxyisoalantolactone proved to be the most effective compound, because it was more cytotoxic than daunorubicin towards a number of cell lines, including those daunorubicin-resistant, and did not affect normal human cells.
About the authors
A. V. Semakov
Institute of Physiologically Active Compounds
Author for correspondence.
Email: l_vok@list.ru
Russian Federation, Chernogolovka, 142432
L. V. Anikina
Institute of Physiologically Active Compounds
Email: l_vok@list.ru
Russian Federation, Chernogolovka, 142432
S. V. Afanasyeva
Institute of Physiologically Active Compounds
Email: l_vok@list.ru
Russian Federation, Chernogolovka, 142432
S. A. Pukhov
Institute of Physiologically Active Compounds
Email: l_vok@list.ru
Russian Federation, Chernogolovka, 142432
S. G. Klochkov
Institute of Physiologically Active Compounds
Email: l_vok@list.ru
Russian Federation, Chernogolovka, 142432