Počet záznamů: 1
Semisynthetic Esters of 17-Hydroxycativic Acid with in Vitro Cytotoxic Activity against Leukemia Cell Lines
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SYSNO ASEP 0481497 Druh ASEP J - Článek v odborném periodiku Zařazení RIV J - Článek v odborném periodiku Poddruh J Článek ve WOS Název Semisynthetic Esters of 17-Hydroxycativic Acid with in Vitro Cytotoxic Activity against Leukemia Cell Lines Tvůrce(i) 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, ORCIDCelkový počet autorů 6 Zdroj.dok. Biological & Pharmaceutical Bulletin. - : Pharmacetical Society of Japan - ISSN 0918-6158
Roč. 40, č. 11 (2017), s. 1923-1928Poč.str. 6 s. Jazyk dok. eng - angličtina Země vyd. JP - Japonsko Klíč. slova biological evaluation ; derivatives ; andrographolide ; apoptosis ; cancer ; agents ; diterpenes ; inhibition ; activation ; chemistry ; diterpenoid ; 17-hydroxycativic acid ; cytotoxic activity ; human cancer cell ; apoptosis Vědní obor RIV EB - Genetika a molekulární biologie Obor OECD Hematology CEP LO1204 GA MŠMT - Ministerstvo školství, mládeže a tělovýchovy Institucionální podpora UEB-Q - RVO:61389030 UT WOS 000414236100014 DOI 10.1248/bpb.b17-00477 Anotace 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. Pracoviště Ústav experimentální botaniky Kontakt David Klier, knihovna@ueb.cas.cz, Tel.: 220 390 469 Rok sběru 2018
Počet záznamů: 1