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Antioxidant Plant Metabolites in Disease and Health

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

Deadline for manuscript submissions: closed (31 March 2024) | Viewed by 2410

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Dear Colleagues,

Medicinal plants have historically played an important role as a source of new drugs. Renewed scientific interest in plant secondary metabolites for drug discovery and for treating important pathologies is evident from the analysis of publication trends in several scientific databases and from the impact on the public health policies.

In this scenario, the study of the biological activity of plant derivatives, often due to the synergistic interactions of several active molecules, becomes crucial in the fight against serious diseases, such as cancer, whose cause is always multi-factorial.

In light of these premises, this Special Issue aims to collect contributions on the potential of plant secondary metabolites for health applications, through the chemical characterization of standardized extracts, single compounds and their mixtures, their biological activities, such as cytotoxicity against microorganisms and human cell lines, antimicrobial, antifungal, antioxidant, anti-inflammatory effect and safety properties, such as genotoxicity and/or geno-protection.

Dr. Alessandra Guerrini
Guest Editor

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Keywords

plant secondary metabolites
chemical characterization
cytotoxicity
biological effects
antioxidant

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16 pages, 2481 KiB

Open AccessArticle

In Vitro Anti-Inflammatory Activity of Methyl Derivatives of Flavanone

by Małgorzata Kłósek, Agnieszka Krawczyk-Łebek, Edyta Kostrzewa-Susłow, Ewelina Szliszka, Joanna Bronikowska, Dagmara Jaworska, Grażyna Pietsz and Zenon P. Czuba

Molecules 2023, 28(23), 7837; https://doi.org/10.3390/molecules28237837 - 29 Nov 2023

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Abstract

Inflammation plays an important role in the immune defense against injury and infection agents. However, the inflammatory chronic process may lead to neurodegenerative diseases, atherosclerosis, inflammatory bowel diseases, or cancer. Flavanones present in citrus fruits exhibit biological activities, including anti-oxidative and anti-inflammatory properties. The beneficial effects of flavanones have been found based on in vitro cell cultures and animal studies. A suitable in vitro model for studying the inflammatory process are macrophages (RAW264.7 cell line) because, after stimulation using lipopolysaccharide (LPS), they release inflammatory cytokines involved in the immune response. We determined the nitrite concentration in the macrophage cell culture and detected ROS using chemiluminescence. Additionally, we measured the production of selected cytokines using the Bio-Plex Magnetic Luminex Assay and the Bio-PlexTM 200 System. For the first time, we have shown that methyl derivatives of flavanone inhibit NO and chemiluminescence generated via LPS-stimulated macrophages. Moreover, the tested compounds at 1–20 µM dose-dependently modulate proinflammatory cytokine production (IL-1β, IL-6, IL-12p40, IL-12p70, and TNF-α) in stimulated RAW264.7 cells. The 2′-methylflavanone (5B) and the 3′-methylflavanone (6B) possess the strongest anti-inflammatory activity among all the tested flavanone derivatives. These compounds reduce the concentration of IL-6, IL-12p40, and IL12p70 compared to the core flavanone structure. Moreover, 2′-methylflavanone reduces TNF-α, and 3′-methylflavanone reduces IL-1β secreted by RAW264.7 cells. Full article

(This article belongs to the Special Issue Antioxidant Plant Metabolites in Disease and Health)

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17 pages, 9031 KiB

Open AccessArticle

Antioxidant and Anti-Aging Phytoconstituents from Faucaria tuberculosa: In Vitro and In Silico Studies

by Hayam S. Ahmed, Hala Abouzeid, Mostafa A. Mansour, Asmaa I. Owis, Elham Amin, Hany W. Darwish, Ashwag S. Alanazi, Ibrahim A. Naguib and Naglaa Afifi

Molecules 2023, 28(19), 6895; https://doi.org/10.3390/molecules28196895 - 30 Sep 2023

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Abstract

Research targeting natural cosmeceuticals is now increasing due to the safety and/or limited side effects of natural products that are highly valued in cosmetology. Within a research program exploring botanical sources for valuable skincare antioxidant components, the current study investigated the phytochemical content and the biological potential of Faucaria tuberculosa. Phytochemical investigation of F. tuberculosa extract resulted in purification and characterization of six phytoconstituents, including a new one. The structure of the new constituent was elucidated as (-) catechin-(2→1′,4→2′)-phloroglucinol (4). The structural identity of all isolated compounds were confirmed on the basis of extensive physical and spectral (1D, 2D-NMR and HRESIMS) investigations. The ethanolic extract exhibits a rich content of total phenolics (TPC) and total flavonoids (TFC), estimated as 32 ± 0.034 mg GAE/g and 43 ± 0.004 mg RE/g, respectively. In addition, the antioxidant (ABTS and FRAP), antihyaluronidase and antityrosinase activities of all purified phytoconstituents were evaluated. The results noted (-) catechin-(2→1′,4→2′) phloroglucinol (4) and phloroglucinol (1) for their remarkable antioxidant activity, while isorhamnetin 3-O-rutinoside (3) and 3,5-dihydroxyphenyl β-D-glucopyranoside (2) achieved the most potent inhibitory activity against tyrosinase (IC₅₀ 22.09 ± 0.7 µM and 29.96 ± 0.44 µM, respectively) and hyaluronidase enzymes (IC₅₀ 49.30 ± 1.57 µM and 62.58 ± 0.92, respectively) that remarkably exceeds the activity of the standard drugs kojic acid (IC₅₀ = 65.21 ± 0.47 µM) and luteolin, (IC₅₀ = 116.16 ± 1.69 µM), respectively. A molecular docking study of the two active compounds (3 and 2) highlighted their high potential to bind to the active sites of the two enzymes involved in the study. Full article

(This article belongs to the Special Issue Antioxidant Plant Metabolites in Disease and Health)

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