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Bioactive Compounds in Natural Products: Extraction, Analysis and In Vitro Studies

A special issue of Molecules (ISSN 1420-3049). This special issue belongs to the section "Natural Products Chemistry".

Deadline for manuscript submissions: closed (31 October 2023) | Viewed by 2116

Special Issue Editors


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Guest Editor
Instituto de Biologia Experimental e Tecnológica, Apartado 12, 2781-901 Oeiras, Portugal
Interests: analytical chemistry; food quality; phytochemicals; phenolic compounds; bioacessibility; bioavailability; bioactivity

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Guest Editor
Instituto de Biologia Experimental e Tecnológica, Apartado 12, 2781-901 Oeiras, Portugal
Interests: natural bioactives; bioactivity; cell-based assays; human intervention studies; anticancer effect
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Guest Editor Assistant
Instituto de Biologia Experimental e Tecnológica, Apartado 12, 2781-901 Oeiras, Portugal
Interests: waste valorization; deep eutectic solvents; pressurized co2 extraction; microwave-assisted extraction; natural bioactives
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Natural products are an important source of bioactive compounds. The diversity of molecules as well as their varying concentration and bioactivity make this study a real challenge.

The methodologies used to extract the different families of bioactive compounds must be chosen according to the characteristics of the matrices under study and the compounds to be evaluated. Moreover, the methodologies used for chemical characterization purposes must be carefully chosen based on sensitivity and selectivity criteria.

In recent years, there has been great development in the procedures used for extraction, characterization, and the evaluation of in vitro bioactivity.

Environmentally friendly and efficient strategies should be developed for the recovery of bioactive compounds from natural matrices. Solid–liquid extraction methods using alternative solvents, such as deep eutectic or pressurized solvents, as well as intensified extractions (e.g., microwaves or ultrasounds assisted), have recently been described.

Advances in sample preparation methodologies, as well as separation techniques, detection modes, and mass spectrometry, have contributed to important advances in the characterization of new molecules and their quantitation in different matrices.

In vitro studies are essential tools to elucidate the possible human-health-promoting effects of natural bioactive compounds. Bioactivity studies range from chemical assays, enzymatic methods, and cell-based assays. More recently, the use of 3D cell models has been applied using advanced analytical tools (omics) in the food and nutrition field to unveil the mechanisms of action of bioactive compounds in health/disease.

Alternative processes of extraction, applications describing new approaches or methodologies to improve the quality of results, recent advances in sample characterization, and applications describing new methodologies to evaluate bioactivity are welcome in this Special Issue.

Dr. Maria Rosário Bronze
Dr. Teresa Serra
Guest Editors

Dr. Naiara Fernández
Guest Editor Assistant

Manuscript Submission Information

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Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 2700 CHF (Swiss Francs). Submitted papers should be well formatted and use good English. Authors may use MDPI's English editing service prior to publication or during author revisions.

Keywords

  • bioactive
  • extraction
  • characterization
  • bioactivity

Published Papers (2 papers)

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Research

16 pages, 945 KiB  
Article
Sesquiterpene Lactones and Flavonoid from the Leaves of Basin Big Sagebrush (Artemisia tridentata subsp. tridentata): Isolation, Characterization and Biological Activities
by Rosemary Anibogwu, Karl De Jesus, Samjhana Pradhan, Shanae Van Leuven and Kavita Sharma
Molecules 2024, 29(4), 802; https://doi.org/10.3390/molecules29040802 - 09 Feb 2024
Viewed by 797
Abstract
This research is an exploratory study on the sesquiterpenes and flavonoid present in the leaves of Artemisia tridentata subsp. tridentata. The leaf foliage was extracted with 100% chloroform. Thin-layer chromatography (TLC) analysis of the crude extract showed four bands. Each band was [...] Read more.
This research is an exploratory study on the sesquiterpenes and flavonoid present in the leaves of Artemisia tridentata subsp. tridentata. The leaf foliage was extracted with 100% chloroform. Thin-layer chromatography (TLC) analysis of the crude extract showed four bands. Each band was purified by column chromatography followed by recrystallization. Three sesquiterpene lactones (SLs) were isolated—leucodin, matricarin and desacetylmatricarin. Of these, desacetylmatricarin was the major component. In addition, a highly bio-active flavonoid, quercetagetin 3,6,4′-trimethyl ether (QTE), was also isolated. This is the first report on the isolation of this component from the leaves of Artemisia tridentata subsp. tridentata. All the components were identified and isolated by TLC, high-performance liquid chromatography (HPLC) and mass spectrometry (MS) techniques. Likewise, the structure and stereochemistry of the purified components were characterized by extensive spectroscopic analysis, including 1D and 2D nuclear magnetic resonance (NMR) and Fourier transform infrared spectroscopy (FTIR) studies. The antioxidant activities of crude extract were analyzed, and their radical-scavenging ability was determined by Ferric reducing antioxidant power (FRAP) and 2,2-diphenyl-1-picrylhydrazyl (DPPH) assay. The crude extract showed antioxidant activity of 18.99 ± 0.51 and 11.59 ± 0.38 µmol TEg−1 FW for FRAP and DPPH assay, respectively, whereas the activities of matricarin, leucodin, desacetylmatricarin and QTE were 13.22, 13.03, 14.90 and 15.02 µmol TEg−1 FW, respectively, for the FRAP assay. The antitumor properties were probed by submitting the four isolated compounds to the National Cancer Institute (NCI) for NCI-60 cancer cell line screening. Overall, the results of the one-dose assay for each SL were unremarkable. However, the flavonoid’s one-dose mean graph demonstrated significant growth inhibition and lethality, which prompted an evaluation of this compound against the 60-cell panel at a five-dose assay. Tests from two separate dates indicate a lethality of approximately 75% and 98% at the log−4 concentration when tested against the melanoma cancer line SK-Mel 5. This warrants further testing and derivatization of the bioactive components from sagebrush as a potential source for anticancer properties. Full article
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13 pages, 2646 KiB  
Article
Active Components of Leontopodium alpinum Callus Culture Extract for Blue Light Damage in Human Foreskin Fibroblasts
by Haodong Li, Xianyao Meng, Ying Zhang, Miaomiao Guo and Li Li
Molecules 2023, 28(21), 7319; https://doi.org/10.3390/molecules28217319 - 28 Oct 2023
Viewed by 1021
Abstract
Leontopodium alpinum is a source of raw material for food additives and skin health. The purpose of this study was to investigate the application of Leontopodium alpinum callus culture extract (LACCE) to prevent blue light damage to the skin. We screened and identified [...] Read more.
Leontopodium alpinum is a source of raw material for food additives and skin health. The purpose of this study was to investigate the application of Leontopodium alpinum callus culture extract (LACCE) to prevent blue light damage to the skin. We screened and identified the blue light-damage-protecting activities and mechanisms of ten components of LACCE, including chlorogenic acid (A), isoquercitrin (B), isochlorogenic acid A (C), cynaroside (D), syringin (E), isochlorogenic acid (F), cynarin (G), rutin (H), leontopodic acid A (I), and leontopodic acid B (J), using a novel blue light-induced human foreskin fibroblast (HFF-1) cell injury model. The study examined the cytotoxicity of ten ingredients using the cell counting kit-8 (CCK-8) assay, and selecting concentrations of 5, 10, and 20 μM for experiments with a cell viability above 65%. We explored the effects and mechanisms of action of these LACCE components in response to blue light injury using Western blotting and an enzyme-linked immunosorbent assay. We also measured ROS secretion and Ca2+ influx. Our study revealed that leontopodic acid A effectively boosted COI-1 expression, hindered MMP-1 expression, curbed ROS and Ca2+ endocytosis, and reduced OPN3 expression. These results provide theoretical support for the development of new raw materials for the pharmaceutical and skincare industries. Full article
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