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Your search keyword '"Borstnik, Kristina"' showing total 17 results
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17 results on '"Borstnik, Kristina"'

6. Enantiomeric 1,2,4-Trioxanes Display Equivalent in vitro Antimalarial Activity Versus Plasmodium falciparum Malaria Parasites: Implications for the Molecular Mechanism of Action of the Artemisinins

Author

O’Neill, Paul M., primary, Rawe, Sarah L., additional, Borstnik, Kristina, additional, Miller, Alison, additional, Ward, Stephen A., additional, Bray, Patrick G., additional, Davies, Jill, additional, Oh, Chang Ho, additional, and Posner, Gary H., additional

Published
2005
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14. Biological Mechanisms of Action of Novel C-10 Non-Acetal Trioxane Dimers in Prostate Cancer Cell Lines

Author

A. Alagbala, Adebusola, J. McRiner, Andrew, Borstnik, Kristina, Labonte, Tanzina, Chang, Wonsuk, G. D'Angelo, John, H. Posner, Gary, and A. Foster, Barbara

Abstract

The mechanisms of action of three C-10 non-acetal trioxane dimers (TDs) were examined in human (LNCaP) and mouse (TRAMP-C1A and -C2H) prostate cancer cell lines. 1(AJM3/23), 2(GHP-TM-III-07w), and 3(GHP-KB-06) inhibited cell growth with 3being the most potent in C1A (GI50 18.0 nM), C2H (GI50 17.0 nM), and LNCaP (GI50 17.9 nM) cells. In comparison to a standard cytotoxic agent such as doxorubicin (GI50 45.3 nM), 3(GI50 17.9 nM) inhibited LNCaP cell growth more potently. TDs induced G0/G1cell cycle arrest in LNCaP cells and decreased cells in the S phase. These changes correlated with modulation of G1phase cell cycle proteins including decreased cyclin D1, cyclin E, and cdk2 and increased p21waf1and p27Kip1. TDs also promoted apoptosis in LNCaP cells with increased expression of proapoptotic bax. These results demonstrate that TDs are potentially useful agents that warrant further preclinical development for treatment of prostate cancer.

Published
2006
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16. Enantiomeric 1,2,4-trioxanes display equivalent in vitro antimalarial activity versus Plasmodium falciparum malaria parasites: implications for the molecular mechanism of action of the artemisinins.

Author

O'Neill PM, Rawe SL, Borstnik K, Miller A, Ward SA, Bray PG, Davies J, Oh CH, and Posner GH

Subjects
Animals, Antimalarials chemical synthesis, Antimalarials chemistry, Artemisinins metabolism, Drug Design, Heterocyclic Compounds chemical synthesis, Heterocyclic Compounds chemistry, Inhibitory Concentration 50, Molecular Structure, Parasitic Sensitivity Tests, Stereoisomerism, Antimalarials pharmacology, Artemisinins pharmacology, Heterocyclic Compounds pharmacology, Plasmodium falciparum drug effects
Abstract

The aim of this study was to synthesise pure enantiomers of potent antimalarial 1,2,4-trioxanes, which are related to the natural antimalarial artemisinin, and then to assay each against a panel of Plasmodium falciparum strains. The working hypothesis was that if the artemisinin derivatives interact with a specific protein-target site, then there should be stereoselective differences in their activity. In five different P. falciparum isolates, however, the trioxane enantiomers (+)-7 a, (-)-7 a and (+)-7 b, (-)-7 b, showed the same level of in vitro antiparasitic activity.

Published
2005
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17. Malaria: new chemotherapeutic peroxide drugs.

Author

Borstnik K, Paik IH, and Posner GH

Subjects
Animals, Antimanic Agents chemistry, Humans, Molecular Structure, Peroxides chemistry, Plasmodium isolation & purification, Structure-Activity Relationship, Antimanic Agents therapeutic use, Malaria drug therapy, Peroxides therapeutic use, Plasmodium drug effects
Abstract

Chemical insights into artemisinin's biological mechanism of action have allowed rational design of some new trioxane and endoperoxide antimalarial drug candidates that are efficacious and safe. This review summarizes recent achievements in this area of peroxide drug development for malaria chemotherapy.

Published
2002
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