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Ismail S.,Center for Drug Research | Man C.N.,Universiti Sains Malaysia
Journal of Essential Oil Research | Year: 2012

The essential oil of Cymbopogan citratus (lemon grass) was isolated by steam distillation method and subjected to cytotoxicity activity using two different cell lines, human colon carcinoma (HCT-116), breast carcinoma cell lines (MCF-7) and anti-angiogenic activity. The cytotoxicity activity study was determined using the MTT [3-(4,5-dimethylthiazol- 2-y1)-2,5-diphenyl-2,4- tetrazolium bromide] assay and anti-angiogenic activity using rat aortic ring model. The chemical composition of the essential oil was determined by gas chromatography-mass spectrometry (GC-MS) and GC-flame ionization detection (FID). Forty-one compounds, representing 88.5% of the lemon grass oil was identified and the main components were neral (29.8%) and geranial (44.6%). The free radical scavenging activity of the essential oil showed an IC50 value of 156.1 μg/mL. The results showed that essential oil of lemon grass possessed potential cytotoxic effect on HCT-116 and with the IC50 value of 27.41 ± 4.3 μg/mL comparing to MCF-7 with IC50 value of 41.90 ± 1.2 μg/mL. Significant anti-angiogenic activity of the sample was observed with 99 ± 0.8% of inhibition at 100 μg/mL. © 2012 Taylor & Francis.

Alhoranta A.M.,Laboratory of Polymer Chemistry | Lehtinen J.K.,Center for Drug Research | Urtti A.O.,Center for Drug Research | Butcher S.J.,University of Helsinki | And 2 more authors.
Biomacromolecules | Year: 2011

A series of amphiphilic star and linear block copolymers were synthesized using ATRP. The core consisted of either polystyrene (PS) or poly(n-butyl acrylate) (PBuA), having different glass-transition (T g) values. These polymers were used as macroinitiators in the polymerization of the cationic 2-(dimethylamino)ethyl methacrylate (DMAEMA). The polymers were used to study the effects of polymer architecture and flexibility on the self-assembling properties, DNA complexation, and transfection. All polymers formed core-shell micelles in aqueous solutions and condensed plasmid DNA. Linear PDMAEMA-PBuA-PDMAEMA has transfection efficiency comparable to PEI25K in ARPE19 cell line. Glassy state of the micellar core and star-shaped architecture decreased the DNA transfection compared with the rubbery and linear polymer structures. The polymers showed low cellular toxicity at low nitrogen/phosphate (n/p) ratios. © 2011 American Chemical Society.

Valtola L.,University of Helsinki | Karesoja M.,University of Helsinki | Tenhu H.,University of Helsinki | Ihalainen P.,Åbo Akademi University | And 5 more authors.
Journal of Applied Polymer Science | Year: 2014

Patterning of functionalized polymeric surfaces enables the adjustment of their characteristics and use in novel applications. We prepared breath figure (BF) films from three semifluorinated diblock copolymers, which all are composed of a polystyrene block and a semifluorinated one to compare their surface properties. "Click" chemistry was employed to one of the polymers, containing a poly(pentafluorostyrene) block to incorporate hydrophilic sugar or carboxylic acid moieties. The structure of the polymer alters the obtained porous morphology of the films. Contact angle (CA) analyses of the BF films reveals that the surface porosity increases water CAs compared with solvent cast films, and, in the case of hydrophobic polymers, leads to significant increase in the CAs of dodecane. The hydrophobicity of the BF films is further amplified by the removal of the topmost layer which leads in some cases to superhydrophobic surfaces. BF films containing glucose units are hydrophilic exhibiting water CAs below 90°. These glycosylated porous surfaces are shown to bind lectin Con A-FITC or can be labelled with isothiocyanate marker. © 2014 Wiley Periodicals, Inc.

Thoenes L.,Center for Drug Research | Hoehn M.,Center for Drug Research | Kashirin R.,Gene Center | Ogris M.,Center for Drug Research | And 3 more authors.
Journal of Proteomics | Year: 2010

A human prostate cancer (PC3) xenograft model was established which reflects acquired in vivo resistance towards metronomic cyclophosphamide (CPA) treatment. Cell cultures of two in vivo resistant PC3 tumors were established which maintain chemoresistant phenotypes upon xenografting into mice. A comparative proteome analysis of the two resistant cell lines PC3-D3 and -D4 versus the non-resistant parental PC3 cell line by 2D-DIGE approach followed by MALDI-TOF-TOF analysis revealed a total of 25 differently expressed proteins. Validation of protein candidates by Western blot analysis of the corresponding in vivo tumor xenografts identified three differentially expressed proteins (thioredoxin containing protein 5, cathepsin B, and annexin A3). Thioredoxin containing protein 5 was up-regulated in resistant xenografts only upon in vivo CPA therapy. A truncated version of cathepsin B translocated into mitochondria in the resistant clones whereas it stays cytoplasmic in corresponding parental PC3 cells. Annexin A3 (ANXA3) presents a very interesting candidate which was found to be up-regulated both in vitro and in xenografts, with protein levels further increased by metronomic CPA treatment in vivo. It is noteworthy that independent studies in other epithelial cancers recently identified ANXA3 as cancer progression and resistance marker. © 2010 Elsevier B.V. All rights reserved.

PubMed | Center for Drug Research
Type: | Journal: Methods in molecular medicine | Year: 2011

The ability of antisense oligonucleotides to interdict, sequence-specifically, the expression of pathogenic genes affords an exciting new strategy for therapeutic intervention (1-3). Oligonucleotides with physiological phosphodiester internucleotide bonds are rapidly degraded, predominantly by exonucleases. Numerous oligonucleotide analogs have therefore been synthesized to confer resistance toward nuclease activity (3). The phosphorothioate analog is the most extensively studied, and phosphorothioate oligodeoxynucleotides have been shown to be potent inhibitors of the expression of their target genes in vitro and in vivo (1,3). However, phosphorothioate oligodeoxynucleotides also bind avidly and nonspecifically to proteins, thus provoking a variety of non-antisense effects (4). Oligonucleotide analogs that do not bind to proteins are therefore expected to display less nonantisense side effects. However, protein binding also affects the in vivo disposition of oligonucleotides. Nonphosphorothioate oligonucelotide analogs generally do not bind to serum proteins, and are therefore rapidly cleared from the circulation, protein-bound phosphorothioate oligodeoxynucelotides circulate much longer (5,6).

PubMed | Center for Drug Research
Type: Journal Article | Journal: Cancer letters | Year: 2013

Natural compounds derived from marine organisms have shown a wide variety of anti-tumor effects and a lot of attention has been drawn to further development of the isolated compounds. A vast quantity of individual chemical structures from different organisms has shown a variety of apoptosis inducing mechanisms in a variety of tumor cells. The bis-steroidal cephalostatin 1 for example, induces apoptosis via activation of caspases whereas the polyketide discodermolide inhibits cell growth by binding to and stabilizing microtubule and salisporamide A, the product of an actinobacterial strain, is an inhibitor of the proteasome. This great variety of mechanisms of action can help to overcome the multitude of resistances exhibited by different tumor specimens. Products from marine organisms and their synthetic derivates are therefore an important source for new therapeutics for single agent or combined therapy with other chemotherapeutics to support the struggle against cancer.

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