Geranylated flavanone tomentodiplacone B inhibits proliferation of human monocytic leukaemia (THP-1) cells

0367955 - ÚEM 2012 RIV GB eng J - Journal Article
Kollár, P. - Bárta, Tomáš - Závalová, V. - Šmejkal, K. - Hampl, Aleš
Geranylated flavanone tomentodiplacone B inhibits proliferation of human monocytic leukaemia (THP-1) cells.
British Journal of Pharmacology. Roč. 162, č. 7 (2011), s. 1534-1541. ISSN 0007-1188. E-ISSN 1476-5381
Grant - others:GA MŠk.(CZ) LC06077
Program: LC
Institutional research plan: CEZ:AV0Z50390703; CEZ:AV0Z50390512
Keywords : flavonoids * CDK2 * antiproliferative effect
Subject RIV: FR - Pharmacology ; Medidal Chemistry
Impact factor: 4.409, year: 2011

Paulownia tomentosa is a rich source of geranylated flavanones, some of which we have previously shown to have cytotoxic activity. Cell viability was measured by dye exclusion and proliferation by WST-1 assays; cell cycle was monitored by flow cytometry. Regulatory proteins were assessed by immunoprecipitation and kinase assays, and Western blotting. Tomentodiplacone B had no effect during the first 24 h of cell growth at concentrations between 1 and 2.5 mu M, but inhibited cell growth in a dose-dependent manner at concentrations of 5 mu M or higher. Phase G1 accumulation was associated with down-regulation of cyclin-dependent kinase 2 activity and also protein levels of cyclins E1 and A2. Our study provides the first evidence that TOM B directly inhibits proliferation of human monocytic leukaemia cells, and thus is a potential anticancer agent, preventing leukaemia cells from progressing from G1 phase into DNA synthesis.
Permanent Link: http://hdl.handle.net/11104/0202450