A cell-based assay for screening lipoxygenase inhibitors |
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| Affiliation: | 1. School of Medicine, University of Adelaide, Adelaide, SA, Australia;2. Centre for Heart Rhythm Disorders, University of Adelaide, Adelaide, SA, Australia;3. Heart Health Theme, South Australian Health and Medical Research Institute, Adelaide, SA, Australia;4. Department of Cardiology, Central Adelaide Local Health Network, Adelaide, SA, Australia;1. Chair of Pharmaceutical/Medicinal Chemistry, Institute of Pharmacy, Friedrich Schiller University Jena, Philosophenweg 14, D-07743 Jena, Germany;2. Department of Pharmacy, University of Naples Federico II, 80131 Naples, Italy;3. Institute of Transfusion Medicine, University Hospital Jena, 07743 Jena, Germany;4. Jena Center for Soft Matter (JCSM), Friedrich Schiller University Jena, Philosophenweg 7, 07743 Jena, Germany;5. Laboratory of Organic and Macromolecular Chemistry (IOMC), Friedrich Schiller University Jena, Humboldtstrasse 10, D-07743 Jena, Germany;6. Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Gazi University, Etiler, 06330 Yenimahalle, Ankara, Turkey;1. Department of Medicinal Chemistry, Faculty of Pharmacy, University of Mansoura, Mansoura 35516, Egypt;2. Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Delta University for Science and Technology, Gamasa City, Egypt;3. Department of Pharmacology, College of Pharmacy, King Saud University, Riyadh 11451, Saudi Arabia;4. Department of Pharmacology, Faculty of Pharmacy, University of Mansourua, Mansoura 35516, Egypt;5. Department of Pharmaceutical Chemistry, College of Pharmacy, King Saud University, Riyadh 11451, Saudi Arabia;1. Department of Nutritional Science, Okayama Prefectural University, 111 Kuboki, Soja, Okayama, 719-1197, Japan;2. Department of Nutrition and Life Science, Fukuyama University, Sanzo, Gakuen-cho 1, Fukuyama, Hiroshima, 729-0292, Japan;3. Laboratory of Microenvironmental and Metabolic Health Sciences, Center for Disease Biology and Integrative Medicine, Faculty of Medicine, The University of Tokyo, 7-3-1 Hongo, Bunkyo-ku, Tokyo, 113-8655, Japan;4. Graduate School of Technology, Industrial and Social Science, Tokushima University, 2-1, Minami-jyosanjima-cho, Tokushima, 770-8513, Japan;1. Applied Organic Chemistry Department, National Research Centre, Cairo, Egypt;2. Faculty of Science and Arts, Mohail Asser, King Khalid University, Saudi Arabia;3. Organometallic and Organometalloid Chemistry Department, National Research Centre, Cairo, Egypt;4. Chemistry Department, Faculty of Science, Al-Azhar University (Boys), Cairo, Egypt;5. Department of Chemistry, College of Science, United Arab Emirates University, P.O. Box 15551, Al-Ain, United Arab Emirates;6. Department of Pharmaceutical Organic Chemistry, Faculty of Pharmacy, Mansoura University, Mansoura, Egypt;7. Department of Pharmacology and Toxicology, Faculty of Pharmacy, Mansoura University, Mansoura, Egypt;8. Department of Medicinal Chemistry, Faculty of Pharmacy, Mansoura University, Mansoura, Egypt |
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| Abstract: | Lipoxygenases (LOX) form a family of lipid peroxidizing enzymes within the plant and animal kingdoms. In humans, six functional lipoxygenase isoforms have been identified. 5-LOX, “platelet-type” 12-LOX (p12-LOX) and 15-LOX type 1 (15-LOX1), originally identified in leukocytes, platelets, and reticulocytes, respectively, generate lipid mediators involved in host cellular functions and in the pathophysiology of asthma, cardiovascular diseases, and cancer. The pharmaceutical industry has reinvigorated their programs to develop novel LOX inhibitors in view of recent findings. However, high throughput LOX screening assays to test novel agents against these intracellular enzymes are limited. We describe a cell-based 96-well microplate fluorescence assay tested against several existing LOX inhibitors, and validate the assay by comparing known IC50 values and HPLC analysis, which may provide a useful screen for novel LOX inhibitors. |
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