Abstract
DNA is a valid drug target for development of target-based therapeutics against cancer. Screening DNA-targeted anticancer drugs is a key process for the research and development of new anticancer drugs. The traditional anticancer drug screening methods, including animal experiments and cell-based screening assays, have unavoidable drawbacks. In this contribution, the new instrument-based screening assay for DNA-targeted anticancer drugs in vitro using resonance light scattering (RLS) technique was proposed. The experiments suggested that the increment of RLS intensity was directly proportional to the antitumor effect of anticancer drugs. Therefore, it was intuitive to obtain the sequence of the antitumor activity of four anticancer drugs without data processing as follows: mitoxantrone (MIT) > pirarubicin (PIR) > daunorubicin (DAU) > doxorubicin (DOX) by RLS screening spectra. Moreover, the apparent equilibrium constant (K) was 1.23 x 104, 2.22 x 104, 4.66 x 104 L/mol for DOX, DAU, and PIR, respectively. The inhibitory concentration 50 (IC50) was 0.148, 0.102, 0.025, 0.013 μmol/L for DOX, DAU, PIR, MIT, respectively. Therefore, the antitumor effect of four drugs was as follows: MIT > PIR > DAU > DOX, which was in good agreement with the result obtained from RLS screening assays. The mechanism between DNA and anthracycline drugs was investigated using UV-vis spectroscopy, fluorescence spectroscopy, and electrophoresis experiments. The proposed assay is a rapid, intuitive, and easy-to-conduct bioassay with good accuracy and reproducibility.
Keywords: Instrument-based screening, resonance light scattering, DNA-targeted, anticancer drug, anthracycline, apparent equilibrium constant, inhibitory concentration 50
Combinatorial Chemistry & High Throughput Screening
Title: An Instrument-Based Screening Assay for DNA-Targeted Anticancer Drugs Using Resonance Light Scattering
Volume: 13 Issue: 5
Author(s): Zhanguang Chen, Guoliang Liu, Maohuai Chen, Xi Chen, Mingyao Wu and Xingtong Chen
Affiliation:
Keywords: Instrument-based screening, resonance light scattering, DNA-targeted, anticancer drug, anthracycline, apparent equilibrium constant, inhibitory concentration 50
Abstract: DNA is a valid drug target for development of target-based therapeutics against cancer. Screening DNA-targeted anticancer drugs is a key process for the research and development of new anticancer drugs. The traditional anticancer drug screening methods, including animal experiments and cell-based screening assays, have unavoidable drawbacks. In this contribution, the new instrument-based screening assay for DNA-targeted anticancer drugs in vitro using resonance light scattering (RLS) technique was proposed. The experiments suggested that the increment of RLS intensity was directly proportional to the antitumor effect of anticancer drugs. Therefore, it was intuitive to obtain the sequence of the antitumor activity of four anticancer drugs without data processing as follows: mitoxantrone (MIT) > pirarubicin (PIR) > daunorubicin (DAU) > doxorubicin (DOX) by RLS screening spectra. Moreover, the apparent equilibrium constant (K) was 1.23 x 104, 2.22 x 104, 4.66 x 104 L/mol for DOX, DAU, and PIR, respectively. The inhibitory concentration 50 (IC50) was 0.148, 0.102, 0.025, 0.013 μmol/L for DOX, DAU, PIR, MIT, respectively. Therefore, the antitumor effect of four drugs was as follows: MIT > PIR > DAU > DOX, which was in good agreement with the result obtained from RLS screening assays. The mechanism between DNA and anthracycline drugs was investigated using UV-vis spectroscopy, fluorescence spectroscopy, and electrophoresis experiments. The proposed assay is a rapid, intuitive, and easy-to-conduct bioassay with good accuracy and reproducibility.
Export Options
About this article
Cite this article as:
Chen Zhanguang, Liu Guoliang, Chen Maohuai, Chen Xi, Wu Mingyao and Chen Xingtong, An Instrument-Based Screening Assay for DNA-Targeted Anticancer Drugs Using Resonance Light Scattering, Combinatorial Chemistry & High Throughput Screening 2010; 13 (5) . https://dx.doi.org/10.2174/138620710791292949
DOI https://dx.doi.org/10.2174/138620710791292949 |
Print ISSN 1386-2073 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5402 |
Call for Papers in Thematic Issues
Artificial Intelligence Methods for Biomedical, Biochemical and Bioinformatics Problems
Recently, a large number of technologies based on artificial intelligence have been developed and applied to solve a diverse range of problems in the areas of biomedical, biochemical and bioinformatics problems. By utilizing powerful computing resources and massive amounts of data, methods based on artificial intelligence can significantly improve the ...read more
Eco-friendly Agents for Biological Control of Pathogenic Diseases
The discovery of an alternative biological approach to disease management includes work on medicinal products derived from natural sources as a starting point for the development of eco-friendly agents for these diseases and the injuries they cause, as well as reducing human contact with hazardous chemicals and their residues. We ...read more
Emerging trends in diseases mechanisms, noble drug targets and therapeutic strategies: focus on immunological and inflammatory disorders
Recently infectious and inflammatory diseases have been a key concern worldwide due to tremendous morbidity and mortality world Wide. Recent, nCOVID-9 pandemic is a good example for the emerging infectious disease outbreak. The world is facing many emerging and re-emerging diseases out breaks at present however, there is huge lack ...read more
Exploring Spectral Graph Theory in Combinatorial Chemistry
Scope of the Thematic Issue: Combinatorial chemistry involves the synthesis and analysis of a large number of diverse compounds simultaneously. Traditional methods rely on brute force experimentation, which can be time-consuming and resource-intensive. Spectral Graph Theory, a branch of mathematics dealing with the properties of graphs in relation to the ...read more
- 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
-
Silencing Human Cancer: Identification and Uses of MicroRNAs
Recent Patents on Anti-Cancer Drug Discovery The p53-Estrogen Receptor Loop in Cancer
Current Molecular Medicine Editorial (Thematic Issue: Combined Cancer Therapy)
Current Pharmaceutical Design A Review on Fruit Juice Probiotication: Pomegranate
Current Nutrition & Food Science Insulin-Like Growth Factor 2 - The Oncogene and its Accomplices
Current Pharmaceutical Design Targeting Cellular Proapoptotic Molecules for Developing Anticancer Agents from Marine Sources
Current Drug Targets Activation of the dsRNA-Activated Protein Kinase PKR in Mitochondrial Dysfunction and Inflammatory Stress in Metabolic Syndrome
Current Pharmaceutical Design Dendrimers: A Class of Polymers in the Nanotechnology for the Delivery of Active Pharmaceuticals
Current Pharmaceutical Design Carbonic Anhydrase Inhibitors and the Management of Cancer
Current Topics in Medicinal Chemistry The Evaluation of Potential Cytotoxic Effect of Different Proton Pump Inhibitors on Different Human Cancer Cell Lines
Anti-Cancer Agents in Medicinal Chemistry Overview of Flaxseed Patent Applications for the Reduction of Cholesterol Levels
Recent Patents on Food, Nutrition & Agriculture Patent Selections
Recent Patents on Inflammation & Allergy Drug Discovery Drug Delivery Systems with Modified Release for Systemic and Biophase Bioavailability
Current Clinical Pharmacology Ovarian Cancer Biomarkers: Headway Towards Early Diagnosis
Current Chemical Biology TNF alpha Inhibition as Treatment Modality for Certain Rheumatologic and Gastrointestinal Diseases
Endocrine, Metabolic & Immune Disorders - Drug Targets Nongenomic Actions of Retinoids: Role of Nur77 and RXR in the Regulation of Apoptosis and Inflammation
Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry Natural Medicine:The Genus Angelica
Current Medicinal Chemistry microRNAs in Cancer: Lessons from Melanoma
Current Pharmaceutical Design TNFα as Therapeutic Target: New Drugs, More Applications
Current Drug Targets - Inflammation & Allergy Oncomirs: From Tumor Biology to Molecularly Targeted Anticancer Strategies
Mini-Reviews in Medicinal Chemistry