Abstract
Development and progression of breast cancer can be caused by increased estradiol activity, which stimulates cell proliferation. Inhibitors of type 1 17β-hydroxysteroid dehydrogenase (17β-HSD) enzyme inhibit estradiol biosynthesis and therefore have potential anticancer activity. In this study two new trans-cinnamic acid esters were established as inhibitors of the human recombinant type 1 17β-HSD enzyme. Studied compounds are poorly water soluble and have low stability in aqueous medium. Free inhibitors were tested on T-47D cells, which express the target enzyme, but did not exert any biological effect up to 100 μM. Therefore, novel poly(η- caprolactone) nanoparticles loaded with the inhibitors were formulated and their effects on T-47D cells were investigated. Prepared nanoparticles had regular spherical shape and mean diameters in the range of 130-170 nm, low polydispersity, high zeta potential and entrapment efficiency. Effective uptake of nanoparticles into T-47D breast cancer cells was confirmed, indicating the possibility to deliver incorporated inhibitor into the cell cytoplasm, where it is released and inhibits the target enzyme. Furthermore, the effect of delivered inhibitors resulted in reduced cell viability and changes in cell morphology. It is anticipated that engineering of efficient delivery system for new poorly soluble inhibitors led to a significant improvement of their biological activity and stability.
Keywords: Nanoparticles, enzyme inhibitors, T-47D cells, cellular uptake, drug delivery, breast cancer
Current Nanoscience
Title: Effect of Free and in Poly(η-caprolactone) Nanoparticles Incorporated New Type 1 17β -Hydroxysteroid Dehydrogenase Inhibitors on Cancer Cells
Volume: 6 Issue: 1
Author(s): Petra Kocbek, Karmen Teskac, Petra Brozic, Tea Lanisnik Rizner, Stanislav Gobec and Julijana Kristl
Affiliation:
Keywords: Nanoparticles, enzyme inhibitors, T-47D cells, cellular uptake, drug delivery, breast cancer
Abstract: Development and progression of breast cancer can be caused by increased estradiol activity, which stimulates cell proliferation. Inhibitors of type 1 17β-hydroxysteroid dehydrogenase (17β-HSD) enzyme inhibit estradiol biosynthesis and therefore have potential anticancer activity. In this study two new trans-cinnamic acid esters were established as inhibitors of the human recombinant type 1 17β-HSD enzyme. Studied compounds are poorly water soluble and have low stability in aqueous medium. Free inhibitors were tested on T-47D cells, which express the target enzyme, but did not exert any biological effect up to 100 μM. Therefore, novel poly(η- caprolactone) nanoparticles loaded with the inhibitors were formulated and their effects on T-47D cells were investigated. Prepared nanoparticles had regular spherical shape and mean diameters in the range of 130-170 nm, low polydispersity, high zeta potential and entrapment efficiency. Effective uptake of nanoparticles into T-47D breast cancer cells was confirmed, indicating the possibility to deliver incorporated inhibitor into the cell cytoplasm, where it is released and inhibits the target enzyme. Furthermore, the effect of delivered inhibitors resulted in reduced cell viability and changes in cell morphology. It is anticipated that engineering of efficient delivery system for new poorly soluble inhibitors led to a significant improvement of their biological activity and stability.
Export Options
About this article
Cite this article as:
Kocbek Petra, Teskac Karmen, Brozic Petra, Rizner Lanisnik Tea, Gobec Stanislav and Kristl Julijana, Effect of Free and in Poly(η-caprolactone) Nanoparticles Incorporated New Type 1 17β -Hydroxysteroid Dehydrogenase Inhibitors on Cancer Cells, Current Nanoscience 2010; 6 (1) . https://dx.doi.org/10.2174/157341310790226397
DOI https://dx.doi.org/10.2174/157341310790226397 |
Print ISSN 1573-4137 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-6786 |
Call for Papers in Thematic Issues
Role of nanomaterials in fabrication of coatings, Machining and Joining
The application of nanoscience has brought about a revolution in the field of mechanical engineering by providing novel materials, boosting manufacturing processes, and generating cutting-edge products. The purpose of this special issue is to investigate the enormous impact that nanoscience has had on mechanical engineering, with a particular emphasis on ...read more
Advanced Inorganic Nanocomposites and Their Emerging Applications
This special issue collection will highlight developments on the recent trends about the synthesis of metal oxides, nanoclusters, biomaterials, 2D nanomaterials, nanocrystals, nanocomposites, etc. and their applications in electrochemical systems, tissue regeneration, energy storage and harvesting, sensors, etc. The novelty of the methods in the chemical synthesis and their characterizations, ...read more
Applicability of Nanotechnology for Performance Enhancement of Clean Energy Technologies
Population growth, industrialization, and improvement in living quality would lead to further increase in energy demand in near future. Regarding the disadvantages of fossil fuels such as fluctuations in their price, high emissions of greenhouse gases and restriction of their sources, it is crucial to use and exploit alternative energy ...read more
Graphene and 2D Materials for Energy Storage and Conversion
This thematic issue will discuss the recent advances in graphene-based nanomaterials for different energy technologies. Graphene possesses a high surface area, and stable structure and exhibits many interesting electronic, optical, and mechanical properties due to its 2D crystal structure. Graphene is of both fundamental interest and suitable for a wide ...read more
Related Journals
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
Related Articles
-
The Potential for Targeting Oncogenic WNT/β -Catenin Signaling in Therapy
Current Drug Targets Attenuated Oncolytic Measles Virus Strains as Cancer Therapeutics
Current Pharmaceutical Biotechnology Defective and Excessive Immunities in Pediatric Diseases
Current Pharmaceutical Design Dual Modulators of p53 and Cyclin D in ER Alpha Signaling by Albumin Nanovectors Bearing Zinc Chaperones for ER-positive Breast Cancer Therapy
Mini-Reviews in Medicinal Chemistry The Emerging Role of microRNA in Stroke
Current Topics in Medicinal Chemistry Highly Efficient, Chemoselective Syntheses of 2-Methoxy-4-substituted Pyrimidines
Letters in Organic Chemistry Synergistic Effect of the Combination of Novel Suberoylanilide Hydroxamic Acid Derivatives with Cisplatin on Anti-proliferation of Human Cancer Cells
Medicinal Chemistry Pharmacology of Appetite Suppression: Implication for the Treatment of Obesity
Current Drug Targets DNA Repair and Resistance to Topoisomerase I Inhibitors: Mechanisms, Biomarkers and Therapeutic Targets
Current Medicinal Chemistry HHT in Childhood: Screening for Special Patients
Current Pharmaceutical Design The Importance of Stereochemistry on the Actions of Vitamin D
Current Topics in Medicinal Chemistry Evaluation of In-Vivo Anti-Implantation and In-Vitro Anti-Proliferative Activities of Substituted 3-phenyl-4-phenylvinyl Benzopyranone Derivatives
Letters in Drug Design & Discovery BRCA2 Dysfunction Promotes Malignant Transformation of Pancreatic Intraepithelial Neoplasia
Anti-Cancer Agents in Medicinal Chemistry Revolutionary Impact of Nanodrug Delivery on Neuroscience
Current Neuropharmacology Rational Design and Development of RDP58
Current Pharmaceutical Design A Practical Approach to Diagnosis and Treatment of Symptomatic Thromboembolic Events in Children with Acute Lymphoblastic Leukemia: Recommendations of the “Coagulation Defects” AIEOP Working Group
Recent Patents on Cardiovascular Drug Discovery Targeting the Kinetochore in Cancer Therapy: The Ndc80/Hec1 Complex
Current Drug Therapy Meet Our Editorial Board Member
Current Clinical Pharmacology An Overview of Cardenolides in Digitalis - More Than a Cardiotonic Compound
Current Pharmaceutical Design The Interplay between the Gut Immune System and Microbiota in Health and Disease: Nutraceutical Intervention for Restoring Intestinal Homeostasis
Current Pharmaceutical Design