Browsing by Subject "Dose-Response Relationship, Drug"

Article

Design, synthesis and biological evaluation of benzo[e][1,2,4]triazin-7(1H) -one and [1,2,4]-triazino[5,6,1-jk]carbazol-6-one derivatives as dual inhibitors of beta-amyloid aggregation and acetyl/butyryl cholinesterase

Catto, M.; Berezin, Andrey A.; Lo Re, D.; Loizou, G.; Demetriades, Marina; De Stradis, A.; Campagna, F.; Koutentis, Panayiotis Andreas; Carotti, A. (2012)

Alzheimer's disease (AD) onset and progression are associated with the dysregulation of multiple and complex physiological processes and a successful therapeutic approach should therefore address more than one target. Two ...

Article

The effect of topoisomerase inhibitors on the expression of differentiation markers and cell cycle progression in human K-562 leukemia cells

Constantinou, Andreas I.; Grdina, D.; Kiguchi, K.; Huberman, E. (1992)

Treatment of human K-562-J leukemia cells for 1 h with the topoisomerase II-reactive drugs VP-16, VM-26, or mAMSA resulted in a dose-dependent inhibition of proliferation and in an increase in the percentage of cells ...

Article

Genistein induces apoptosis and topoisomerase II-mediated DNA breakage in colon cancer cells

Salti, G. I.; Grewal, S.; Mehta, R. R.; Das Gupta, T. K.; Boddie, A. W., Jr.; Constantinou, Andreas I. (2000)

The present study was undertaken to determine if (a) genistein induces topo II-mediated DNA damage in HT-29 colon cancer cells

Article

Genistein-induced cell differentiation and protein-linked DNA strand breakage in human melanoma cells

Kiguchi, K.; Constantinou, Andreas I.; Huberman, E. (1990)

Article

Inactivation of the glutamine/amino acid transporter ASCT2 by 1,2,3-dithiazoles: Proteoliposomes as a tool to gain insights in the molecular mechanism of action and of antitumor activity

Oppedisano, F.; Catto, M.; Koutentis, Panayiotis Andreas; Nicolotti, O.; Pochini, L.; Koyioni, Maria G.; Introcaso, A.; Michaelidou, Sophia S.; Carotti, A.; Indiveri, C. (2012)

The ASCT2 transport system catalyses a sodium-dependent antiport of glutamine and other neutral amino acids which is involved in amino acid metabolism. A library of 1,2,3-dithiazoles was designed, synthesized and evaluated ...

Article

Intraperitoneal melatonin is not neuroprotective in the G93ASOD1 transgenic mouse model of familial ALS and may exacerbate neurodegeneration

Dardiotis, Efthymios; Panayiotou, Elena; Feldman, M. L.; Hadjisavvas, Andreas; Malas, Stavros; Vonta, Filia; Hadjigeorgiou, Georgios M.; Kyriakou, Kyriakos; Kyriakides, Theodoros (2013)

In amyotrophic lateral sclerosis (ALS) reactive oxygen species and apoptosis are implicated in disease pathogenesis. Melatonin with its anti-oxidant and anti-apoptotic properties is expected to ameliorate disease phenotype. ...

Article

A metabolite of equine estrogens, 4-hydroxyequilenin, induces DNA damage and apoptosis in breast cancer cell lines

Chen, Y.; Liu, X.; Pisha, E.; Constantinou, Andreas I.; Hua, Y.; Shen, L.; Van Breemen, R. B.; Elguindi, E. C.; Blond, S. Y.; Zhang, Fengwangdong; Bolton, J. L. (2000)

Estrogen replacement therapy has been correlated with an increased risk of developing breast or endometrial cancer. 4-Hydroxyequilenin (4-OHEN) is a catechol metabolite of equilenin which is a minor component of the estrogen ...

Article

Modeling the effects of toxins in metabolic networks

Tamaddoni-Nezhad, A.; Chaleil, R.; Kakas, Antonis C.; Sternberg, M.; Nicholson, J.; Muggleton, S. (2007)

Article

Nanoscopic cationic methacrylate star homopolymers: Synthesis by group transfer polymerization, characterization and evaluation as transfection reagents

Georgiou, Theoni K.; Vamvakaki, Maria; Patrickios, Costas S.; Yamasaki, E. N.; Phylactou, Leonidas A. (2004)

Seven star polymers with degrees of polymerization (DPs) of the arms from 10 to 100 and dimensions in the nanometer range were prepared using sequential group transfer polymerization of 2-(dimethylamino)-ethyl methacrylate ...

Article

Phenoxodiol (2H-1-benzopyran-7-0,1,3-(4-hydroxyphenyl)), a novel isoflavone derivative, inhibits DNA topoisomerase II by stabilizing the cleavable complex

Constantinou, Andreas I.; Husband, A. (2002)

Cancer therapeutic drugs that inhibit DNA topoisomerase (topo) II by stabilizing the cleavable complex are collectively known as topo II poisons. Phenoxodiol is a synthetic derivative of the plant isoflavone daidzein and ...

Article

Phenoxodiol, a novel isoflavone derivative, inhibits dimethylbenz[a]anthracene (DMBA)-induced mammary carcinogenesis in female Sprague-Dawley rats

Constantinou, Andreas I.; Mehta, R.; Husband, A. (2003)

The present study was undertaken to evaluate the potential cancer chemopreventive effects of novel synthetic derivatives of isoflavones. Initially these agents were tested in a mouse mammary organ culture (MMOC) model. ...

Article

Prevention of preneoplastic mammary lesion development by a novel vitamin D analogue, 1α-hydroxyvitamin D5

Mehta, R. G.; Moriarty, R. M.; Mehta, R. R.; Penmasta, R.; Lazzaro, G.; Constantinou, Andreas I.; Guo, L. (1997)

Background: The form of vitamin D (vitamin D3) in fortified milk and the provitamin D produced by the body undergo metabolic activation to a biologically active form, 1α,25-dihydroxyvitamin D3 [1α,25(OH)2D3]. This compound ...

Article

Reversal of ER-β silencing by chromatin modifying agents overrides acquired tamoxifen resistance

Pitta, Chara A.; Papageorgis, P.; Charalambous, Christina; Constantinou, Andreas I. (2013)

The purpose of this work is to determine the molecular mechanisms underlying tamoxifen resistance. We show here that ER-β is epigenetically silenced in a cell line with acquired tamoxifen resistance (MCF-7/TAM-R) and this ...

Article

Structure based inhibitor design targeting glycogen phosphorylase b. Virtual screening, synthesis, biochemical and biological assessment of novel N-acyl-β-d-glucopyranosylamines

Parmenopoulou, Vanessa; Kantsadi, Anastassia L.; Tsirkone, Vicky G.; Chatzileontiadou, Demetra S. M.; Manta, Stella; Zographos, Spyros E.; Molfeta, Christina; Archontis, Georgios Z.; Agius, Loranne; Hayes, Joseph M.; Leonidas, Demetres D.; Komiotis, Dimitris (2014)

Glycogen phosphorylase (GP) is a validated target for the development of new type 2 diabetes treatments. Exploiting the Zinc docking database, we report the in silico screening of 1888 N-acyl-β-d-glucopyranosylamines ...

Article

Trifolium pratense (red clover) exhibits estrogenic effects in vivo in ovariectomized sprague-dawley rats

Burdette, J. E.; Liu, J.; Lantvit, D.; Lim, E.; Booth, N.; Bhat, K. P. L.; Hedayat, S.; Van Breemen, R. B.; Constantinou, Andreas I.; Pezzuto, J. M.; Farnsworth, N. R.; Bolton, J. L. (2002)

Studies were conducted using an ovariectomized rat model to determine the estrogenic and antiestrogenic activity of Trifolium pratense L. (red clover) extracts. A red clover extract, standardized to contain 15% isoflavones ...