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The health benefits of food, plants, fruits, and seaweeds stem from the biological activities of their constituents—namely, secondary metabolites. The study of secondary metabolites and their potential to treat and/or prevent a number of diseases has become a research topic of growing interest for biologists, pharmacists, and chemists. Notably, in order to propose a compound as a potential new drug with pharmacological effects, the chemical structure of this compound and its biological activity against a given target must be well established. The Special Issue, “Isolation and Identification of Bioactive Secondary Metabolites”, considers species beyond their nutritional value and identifies instances of wider and more efficient use, thereby contributing to a more sustainable management of natural resources. The fifteen articles published in this Special Issue reflect the latest research trends, and consider the isolation, identification, and assessment of the beneficial effects of secondary metabolites from both edible and inedible species. Thus, these contributions collectively demonstrate that these compounds, and their plants of origin, should be valued beyond their nutritional benefits.

coumarins --- Lycium --- metabolomic --- HPLC-MS --- orbitrap --- secondary metabolites --- endemic plants --- olive leaves --- supercritical fluid extraction --- antioxidants --- hyperuricemia --- plant-based functional food --- xanthine oxidase --- adenosine deaminase --- uric acid transporter --- bioactive compound --- Piper pseudoarboreum --- bioassay-guided fractionation --- leishmanicidal activity --- alkamides --- (E)-piplartine --- Wedelia chinensis --- organic farming --- phytotoxic substances --- vanillic acid --- gallic acid --- Origanum subspecies --- morphological traits --- glandular trichomes --- essential oil composition --- rosmarinic acid --- sensory evaluation --- colored potato tubers --- total phenols --- anthocyanins --- saccharides --- nutrition --- microelements --- plants --- fungi --- food supplements --- cardiovascular diseases --- neurodegenerative diseases --- Alzheimer’s disease --- metabolic syndrome --- apocarotenoid --- caffeic acid derivative --- flavonoid --- Lactuca sativa --- lignan --- megastigmane --- sesquiterpene lactone --- 1,2,3,4-tetrahydro-β-carboline-3-carboxylic acid --- black chokeberry --- anthocyanin --- simulated moving bed --- antioxidant activity --- neuroprotection --- Artemisia --- clinical trials --- health effects --- adverse effects --- anticancer --- antiparasitic --- artemisinin --- santonin --- achillin --- tehranolide --- Aglaomorpha quercifolia --- GC-MS profile --- rhizome --- leaves --- n-hexane extract --- fatty acids --- terpenoids --- linolenic acid --- hop-16-ene --- cardiac glycosides --- secondary plant metabolites --- natural product isolation --- hyrcanoside --- deglucohyrcanoside --- ouabain --- cymarin --- digitoxin --- anticancer activity --- Na+/K+-ATPase inhibitors --- corn salad --- leafy vegetables --- phytochemicals --- liquid chromatography --- mass spectrometry --- celastrol --- Celastraceae --- antimicrobial activity --- mechanism of action --- Bacillus subtilis --- n/a --- Alzheimer's disease