Abstract
Many flavonoids, as eminent phenolic compounds, have been commercialized and consumed as dietary supplements due to their incredible human health benefits. In the present study, a bioactive flavone glycoside linarin (LN) was designated to comprehensively overview its phytochemical and biological properties. LN has been characterized abundantly in the Cirsium, Micromeria, and Buddleja species belonging to Asteraceae, Lamiaceae, and Scrophulariaceae families, respectively. Biological assessments exhibited promising activities of LN, particularly, the remedial effects on central nervous system (CNS) disorders, whereas the remarkable sleep enhancing and sedative effects as well as AChE (acetylcholinesterase) inhibitory activity were highlighted. Of note, LN has indicated promising anti osteoblast proliferation and differentiation, thus a bone formation effect. Further biological and pharmacological assessments of LN and its optimized semi-synthetic derivatives, specifically its therapeutic characteristics on osteoarthritis and osteoporosis, might lead to uncovering potential drug candidates.
Highlights
Apart from a qualification study, in which the LN content was determined in the flower methanolic extract of C. indicum [32], hydro-ethanolic partition (95%) of the flower and bud parts contained 48.3 mg/g, whilst acetonitrile and water in HPLC-DAD was used as the solvent system [30]
The hydro-ethanolic (70%) fractions extracted from the inflorescence part of Coptis chinensis Franch. (Ranunculaceae family) were assessed via HPLC-MS and LN was identified as the main compounds [71]
The osteoarthritis mechanism of action of C. zawadskii var. latilobum extract revealed that the matrix metalloproteinases-1 (MMP-1), MMP-3, MMP-9 and MMP-13 expressions were inhibited by the dose-dependent extract, while expressions of the ECM synthetic genes, COL2A1 and ACAN, and the transcription factor SOX9 were increased to normal condition by the extract treatment dose-dependently
Summary
Publisher’s Note: MDPI stays neutral with regard to jurisdictional claims in published maps and institutional affiliations. The study of plant constituents has led to the discovery of secondary metabolites (phytochemicals) as the major compounds responsible for the bioactivities. Based on the chemical structures, these compounds are divided into six main subclasses: flavones, flavanones, flavonols, flavan-3-ols, isoflavones, and Pharmaceuticals 2021, 14, 1104. Even though the phytochemical and biological characteristics of these compounds are being studied [11,12], they are still interesting target molecules to be explored. 1), has been identified from various plant species mainly these compounds are being studied [11,12], they are still interesting target molecules to be belonging to the Asteraceae and Lamiaceae families. Among the 13 plant families containing linarin within (LN), Asteraceae and Lamipapers The most LN contents have been reported in various Cirsium spp.; this compound has been isolated from the genus
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