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Semisynthetic Esters of 17-Hydroxycativic Acid with in Vitro Cytotoxic Activity against Leukemia Cell Lines
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SYSNO ASEP 0481497 Document Type J - Journal Article R&D Document Type Journal Article Subsidiary J Článek ve WOS Title Semisynthetic Esters of 17-Hydroxycativic Acid with in Vitro Cytotoxic Activity against Leukemia Cell Lines Author(s) Cavallaro, V. (AR)
Řezníčková, Eva (UEB-Q) RID, ORCID
Jorda, Radek (UEB-Q) ORCID, RID
Alza, N.P. (AR)
Murray, A.P. (AR)
Kryštof, Vladimír (UEB-Q) RID, ORCIDNumber of authors 6 Source Title Biological & Pharmaceutical Bulletin. - : Pharmacetical Society of Japan - ISSN 0918-6158
Roč. 40, č. 11 (2017), s. 1923-1928Number of pages 6 s. Language eng - English Country JP - Japan Keywords biological evaluation ; derivatives ; andrographolide ; apoptosis ; cancer ; agents ; diterpenes ; inhibition ; activation ; chemistry ; diterpenoid ; 17-hydroxycativic acid ; cytotoxic activity ; human cancer cell ; apoptosis Subject RIV EB - Genetics ; Molecular Biology OECD category Hematology R&D Projects LO1204 GA MŠMT - Ministry of Education, Youth and Sports (MEYS) Institutional support UEB-Q - RVO:61389030 UT WOS 000414236100014 DOI https://doi.org/10.1248/bpb.b17-00477 Annotation A collection of sixteen semisynthetic 17-hydroxycativic acid esters with alcohols containing a tertiary amine group was evaluated for their in vitro cytotoxicity against two human cancer cell lines, THP-1 and U937, and for their effects on the cell cycle and cell death. While 17-hydroxycativic acid itself is not cytotoxic, all the esters displayed cytotoxic activity, with 50% growth inhibition (GI(50)) values ranging between 3.2 and 23.1 mu m. In general, the most potent compounds in both cell lines were esters with four carbon long alcohol residues. There was no clear relationship between the identity of the terminal secondary amine and the activity of the compound. Experiments using the 6-(pyrrolidin-1-yl)pentyl ester, 2c, revealed that this compound activates caspases-3/7 and causes poly(ADP-ribose)polymerase 1 (PARP-1) fragmentation in THP-1 and U937 cells, indicating the induction of apoptotic cell death. These results suggest that further investigation into the anticancer activity of diterpene derivatives and other labdane diterpenes may be fruitful. Workplace Institute of Experimental Botany Contact David Klier, knihovna@ueb.cas.cz, Tel.: 220 390 469 Year of Publishing 2018
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