title: Head-to-Head Comparison of Anti-Inflammatory Performance of Known Natural Products In Vitro.
abstract: Inflammation is an important therapeutic target. Due to their potency, steroidal drugs dominate the current treatment of inflammatory disorders. However, steroidal drugs can also exert a broad range of side effects and appear not always effective. This calls for the development of alternative drugs with a different mechanism of action, which are likely to be found in the field of natural products (NPs). For many NPs strong anti-inflammatory effects have been described, but usually investigating a single compound in a single assay. In this study, eight promising NPs were selected and tested against the strong anti-inflammatory drug prednisolone. For this head-to-head comparison, in vitro assays were used which represent different pathways of the inflammatory response: TNF-α and IL-6 expression by macrophages, IL-8 expression by colon epithelial cells, ROS production in polymorphonuclear leukocytes and platelet activation in whole blood. Performance profiles were established which allowed us to identify curcumin, berberine chloride and epigallocatechin gallate as potential alternatives for prednisolone or other glucocorticoids in inflammation.
authors.affiliation: Department of Biomaterials Science and Technology, University of Twente, Enschede, The Netherlands.
authors.forename: Iris E
authors.initials: IE
authors.lastname: Allijn
authors.affiliation: Technology & Innovation, Innovative testing in Life Sciences and Chemistry, University of Applied Sciences Utrecht, Utrecht, The Netherlands.
authors.forename: Stefan F C
authors.initials: SF
authors.lastname: Vaessen
authors.affiliation: Medicinal Chemistry & Chemical Biology - Biomolecular Analysis, Department of Pharmaceutical Sciences, Utrecht University, Utrecht, The Netherlands.
authors.forename: Linda C
authors.initials: LC
authors.lastname: Quarles van Ufford
authors.affiliation: Medicinal Chemistry & Chemical Biology - Biomolecular Analysis, Department of Pharmaceutical Sciences, Utrecht University, Utrecht, The Netherlands.|PhytoGeniX BV, Bunnik, The Netherlands.
authors.forename: Kees J
authors.initials: KJ
authors.lastname: Beukelman
authors.affiliation: Department of Medical Biochemistry, Academic Medical Center, Amsterdam, The Netherlands.
authors.forename: Menno P J
authors.initials: MP
authors.lastname: de Winther
authors.affiliation: Department of Biomaterials Science and Technology, University of Twente, Enschede, The Netherlands.|Department of Pharmaceutics, Utrecht University, Utrecht, The Netherlands.
authors.forename: Gert
authors.initials: G
authors.lastname: Storm
authors.affiliation: Clinical Chemistry and Haematology, University Medical Centre, Utrecht, The Netherlands.
authors.forename: Raymond M
authors.initials: RM
authors.lastname: Schiffelers
mesh_terms: D000098:Acetophenones / Q000494:pharmacology; D000818:Animals; D000893:Anti-Inflammatory Agents / Q000494:pharmacology*; D001599:Berberine / Q000494:pharmacology*; D001688:Biological Products / Q000494:pharmacology*; D001792:Blood Platelets / Q000166:cytology / Q000187:drug effects / Q000276:immunology; D018938:Caco-2 Cells; D002392:Catechin / Q000031:analogs & derivatives* / Q000494:pharmacology; D002460:Cell Line; D003474:Curcumin / Q000494:pharmacology*; D006801:Humans; D015850:Interleukin-6 / Q000096:biosynthesis / Q000276:immunology; D016209:Interleukin-8 / Q000037:antagonists & inhibitors / Q000096:biosynthesis / Q000276:immunology; D008264:Macrophages / Q000166:cytology / Q000187:drug effects / Q000276:immunology; D051379:Mice; D009504:Neutrophils / Q000166:cytology / Q000187:drug effects* / Q000276:immunology; D015539:Platelet Activation / Q000187:drug effects; D017035:Pravastatin / Q000494:pharmacology; D011239:Prednisolone / Q000494:pharmacology; D061251:Primary Cell Culture; D017382:Reactive Oxygen Species / Q000037:antagonists & inhibitors / Q000276:immunology / Q000378:metabolism; D013267:Stilbenes / Q000494:pharmacology; D014409:Tumor Necrosis Factor-alpha / Q000037:antagonists & inhibitors / Q000096:biosynthesis / Q000276:immunology; D000093242:Interleukin-6 Inhibitors
chemical_list: D000098:Acetophenones; D000893:Anti-Inflammatory Agents; D001599:Berberine; D001688:Biological Products; D002392:Catechin; D003474:Curcumin; D015850:Interleukin-6; D016209:Interleukin-8; D017035:Pravastatin; D011239:Prednisolone; D017382:Reactive Oxygen Species; D013267:Stilbenes; D014409:Tumor Necrosis Factor-alpha; D000093242:Interleukin-6 Inhibitors; C508600:IL6 protein, human; C107773:pterostilbene; C013638:paeonol; C056165:acetovanillone; C045651:epigallocatechin gallate