DNA binding, cleavage and cytotoxicity of a novel dimetallic Fe(III) triaza-cyclononane complex

A novel bimetallic Fe(III) complex with the bis(triaza-cyclononane) ligand 2,6-bis(1,4,7-triazacyclonon-1-ylmethyl)-4-methylphenol (bcmp) is reported. [Fe-2(bcmp(-H))(mu-OH)Cl-2]Cl-2 (2) contains two octahedral Fe(III) centers bound to the two triaza-cyclononane rings of bcmp. The coordination sphere is completed by one chlorine, one bridging phenolate oxygen and one bridging hydroxide group. The complex has been characterized by elemental analysis, Mossbauer spectroscopy, UV-Vis spectroscopy, pH potentiometric titration, ESI mass spectrometry and cyclic voltammetry. The complex hydrolyzes the DNA model bis (2,4-dinitrophenyl) phosphate (BDNPP) with a maximum activity a pH 7. Michaelis-Menten behavior is observed with k(cat) = 3.56 x 10(-4)s(-1) and K-m = 0.56 mM (pH 7.0, 40 degrees C). The interaction of 2 with CT DNA was studied by electronic absorption spectroscopy and gel electrophoresis. Notably, the complex relaxes supercoiled pUC19 DNA into the nicked form at low micromolar concentration (10 mu M) in the presence of an external reducing agent (ascorbic acid). Finally, the in vitro antiproliferative activity of 2 was assessed on a panel of human cancer cell lines and results revealed that the complex exhibited a significant cytotoxic effects in particular versus colon LoVo cancer cells, wih IC50 value 2.5 times lower than that shown by the reference metallodrug cisplatin (3.54 versus 8.53 mu M). (C) 2016 Elsevier B.V. All rights reserved.Financial support from the European Commission (Marie Curie FP7-IEF to D.M.); the University of Padova (Grants 60A04-0443, 60A04-3189 and 60A04-4015/15) and Science Foundation Ireland are gratefully acknowledged. T. P. A. thanks the Brazilian Government and CAPES for a Science Without Border Scholarship.peer-reviewed2018-03-0

Chemical Composition, Antioxidant and Cytotoxic Activities of Essential Oil of the Inflorescence of Anacamptis coriophora subsp. fragrans (Orchidaceae) from Tunisia

The chemical composition of the essential oil produced by steam distillation of the inflorescences of naturally growing Anacamptis coriophora (L.) R. M. Bateman, Pridgeon & M. W. Chase subsp.fragrans (Pollini) R. M. Bateman, Pridgeon & M. W. Chase (Orchidaceae) from Kroumiria, north-west Tunisia was studied by GC-MS, which led to the identification of 19 volatile components, representing 97% of the oil. The main constituents were methyl-(E)-p-methoxycinnamate (29.3%), 13-heptadecyn-1-ol (18.6%), 2,5-dimethoxybenzyl alcohol (14.1%) and 4-(1,1,3,3-tetramethylbutyl)-phenol (9.0%). DPPH radical scavenging revealed a weak antioxidant activity. In addition, the antiproliferative effects were evaluated on BxPC3 human pancreatic carcinoma cells and on 2008 human ovarian cancer cells showing significant effect. This is the first report of the chemical composition of essential oils obtained from A. coriophora subsp. fragrans inflorescences for North Africa. Further studies are needed to understand fully the possible mechanism of action behind the cytotoxic activity of the essential oil

Chemical Composition, Antioxidant and Cytotoxic Activities of Essential Oil of the Inflorescence of Anacamptis coriophora subsp. fragrans (Orchidaceae) from Tunisia

The chemical composition of the essential oil produced by steam distillation of the inflorescences of naturally growing Anacamptis coriophora (L.) R. M. Bateman, Pridgeon & M. W. Chase subsp.fragrans (Pollini) R. M. Bateman, Pridgeon & M. W. Chase (Orchidaceae) from Kroumiria, north-west Tunisia was studied by GC-MS, which led to the identification of 19 volatile components, representing 97% of the oil. The main constituents were methyl-(E)-p-methoxycinnamate (29.3%), 13-heptadecyn-1-ol (18.6%), 2,5-dimethoxybenzyl alcohol (14.1%) and 4-(1,1,3,3-tetramethylbutyl)-phenol (9.0%). DPPH radical scavenging revealed a weak antioxidant activity. In addition, the antiproliferative effects were evaluated on BxPC3 human pancreatic carcinoma cells and on 2008 human ovarian cancer cells showing significant effect. This is the first report of the chemical composition of essential oils obtained from A. coriophora subsp. fragrans inflorescences for North Africa. Further studies are needed to understand fully the possible mechanism of action behind the cytotoxic activity of the essential oil