Abstract

Microalgae have been shown to be excellent producers of lipids, pigments, carbohydrates, and a plethora of secondary metabolites with possible applications in the pharmacological, nutraceutical, and cosmeceutical sectors. Recently, various microalgal raw extracts have been found to have anti-inflammatory properties. In this study, we performed the fractionation of raw extracts of the diatom Cylindrotheca closterium, previously shown to have anti-inflammatory properties, obtaining five fractions. Fractions C and D were found to significantly inhibit tumor necrosis factor alpha (TNF-⍺) release in LPS-stimulated human monocyte THP-1 cells. A dereplication analysis of these two fractions allowed the identification of their main components. Our data suggest that lysophosphatidylcholines and a breakdown product of chlorophyll, pheophorbide a, were probably responsible for the observed anti-inflammatory activity. Pheophorbide a is known to have anti-inflammatory properties. We tested and confirmed the anti-inflammatory activity of 1-palmitoyl-sn-glycero-3-phosphocholine, the most abundant lysophosphatidylcholine found in fraction C. This study demonstrated the importance of proper dereplication of bioactive extracts and fractions before isolation of compounds is commenced.

Highlights

  • Inflammation is a complex set of interactions among soluble factors and cells that can arise in any tissue helping to protect the host from systemic infection and to restore tissue homeostasis after injury, infection, and irritation [1,2,3]

  • We investigated the capacity of extracts of C. closterium to inhibit the release of one of the main effectors of inflammation, TNF-α [3], in LPS-stimulated human THP-1 monocytic leukemia cells

  • Previous studies have shown that raw extracts of the diatom C. closterium had anti-inflammatory properties [12]

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Summary

Introduction

Inflammation is a complex set of interactions among soluble factors and cells (e.g., chemokines, cytokines, adhesion molecules, recruitment, and activation of leukocytes) that can arise in any tissue helping to protect the host from systemic infection and to restore tissue homeostasis after injury, infection, and irritation [1,2,3]. Inflammation has important pathogenic roles in several pathologies, such as asthma, atherosclerosis, atopic dermatitis, Crohn’s disease, multiple sclerosis, cystic fibrosis, psoriasis, neurodegenerative diseases, as well as cancer [1,4]. Oceans account for 71% of the earth’s surface and represent a huge, relatively untapped, reservoir of new compounds for drug discovery [5]. One such source is the Phytoplankton, photosynthetic

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