Biotransformation of the flavonoid tiliroside to 7-methylether tiliroside: bioactivity of this metabolite and of its acetylated derivative |
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Authors: | C Demetzos P Magiatis M A Typas K Dimas R Sotiriadou S Perez D Kokkinopoulos |
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Institution: | (1) Laboratory of Pharmacognosy, Department of Pharmacy, University of Athens, GR-157 71 Athens (Greece), GR;(2) Division of Genetics and Biotechnology, GR-157 01 Athens (Greece), e-mail: cdemetzo@atlas.uoa.gr, GR;(3) Hellenic Anticancer Institute, Department of Immunology, 171 Alexandras Ave., GR-115 22 Athens (Greece), GR |
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Abstract: | Incubation of kaempferol-3-O-β-D-(6"-E-p-coumaroyl)-glucopyranoside (tiliroside) (1) with Aspergillus nidulans gives the 7-methyl ether of tiliroside (2) which is a new compound. Its structure is determined by spectroscopic methods. Cytotoxic studies of 2 and of its acetylated derivative 2a were carried out in vitro against fourteen human leukemic cell lines. Results clearly show that compound 2 is ineffective against all leukemic cell lines tested. On the contrary, compound 2a exhibited cytotoxic activity against four of the cell lines (HL60, DAUDI, HUT78 and MOLT3) and additionally, a dose- and
time-dependent effect on DNA synthesis.
Received 18 February 1997; received after revision 8 April 1997; accepted 6 May 1997 |
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Keywords: | ,Aspergillus nidulans, tiliroside, kaempferol glycosides, biotransformation, cytotoxicity, DNA synthesis, |
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