Phytochemicals and Analogues as Sources of Bioactive Substances of Pharmacological and Industrial Interest

A special issue of Pharmaceuticals (ISSN 1424-8247). This special issue belongs to the section "Natural Products".

Deadline for manuscript submissions: 10 September 2024 | Viewed by 4073

Special Issue Editors


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Guest Editor
1. Associate Laboratory i4HB—Institute for Health and Bioeconomy, University Institute of Health Sciences—CESPU, 4585-116 Gandra, Portugal
2. UCIBIO—Applied Molecular Biosciences Unit, Translational Toxicology Research Laboratory, University Institute of Health Sciences (1H-TOXRUN, IUCS-CESPU), 4585-116 Gandra, Portugal
Interests: organic chemistry; analytical chemistry; mass spectrometry; heterocyclic compounds
Special Issues, Collections and Topics in MDPI journals

E-Mail Website
Guest Editor
1. Associate Laboratory i4HB—Institute for Health and Bioeconomy, University Institute of Health Sciences—CESPU, 4585-116 Gandra, Portugal
2. UCIBIO—Applied Molecular Biosciences Unit, Translational Toxicology Research Laboratory, University Institute of Health Sciences (1H-TOXRUN, IUCS-CESPU), 4585-116 Gandra, Portugal
Interests: chromatography; chiral drugs; pharmaceuticals; environmental contaminants
Special Issues, Collections and Topics in MDPI journals

E-Mail Website
Guest Editor
1. Laboratory of Organic and Pharmaceutical Chemistry, Department of Chemical Sciences, Faculty of Pharmacy, University of Porto, Porto, Portugal
2. CIIMAR—Interdisciplinary Centre of Marine and Environmental Research, Edifício do Terminal de Cruzeiros do Porto de Leixões, Av. General Norton de Matos s/n, 4050-208 Matosinhos, Portugal
3. Associate Laboratory i4HB—Institute for Health and Bioeconomy, University Institute of Health Sciences—CESPU, 4585-116 Gandra, Portugal
4. UCIBIO—Applied Molecular Biosciences Unit, Translational Toxicology Research Laboratory, University Institute of Health Sciences (1H-TOXRUN, IUCS-CESPU), 4585-116 Gandra, Portugal
Interests: organic and pharmaceutical chemistry; chromatography; chirality; organic environmental pollutants
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Phytochemicals as bioactive compounds are of great value as they have important applications in various fields. Indeed, the so called "secondary metabolites” or “plant-based chemicals” are the subject of continuous research for the development and design of new drugs, cosmetics, food additives or preservatives, pesticides, and other products.

Many phytochemicals have recognized pharmacological properties, including antioxidant, anti-inflammatory, antimicrobial, and anticancer effects. The classical example is the compound artemisinin, found in the plant Artemisia annua, used as an antimalarial drug. Flavonoids, common in many fruits and vegetables, have been shown to have antioxidant, anti-inflammatory and anticancer properties. Another example is the use of certain plant extracts in skin care products for their anti-aging or anti-inflammatory properties.

Overall, the pharmacological interest of phytochemicals lies in their potential to provide a direct benefit for society by providing new and innovative products in industries related with the sustainable development of drugs, pesticides (food and agriculture), cosmetics and personal cares products, etc.

This Special Issue, “Phytochemicals and Analogues as Sources of Bioactive Substances of pharmacological and Industrial Interest”, invites authors to contribute review or original research articles dedicated to the most recent advances in the discovery of plant-based phytochemicals. Contributions may include the discovery of new compounds and their structural elucidation or synthetic analogues as well as the assessment of the pharmacological properties. Structure–activity studies directing toward eco-friendly methodologies for the synthesis of more bioactive derivatives are also welcomed.

Prof. Dr. Eduarda M. P. Silva
Dr. Cláudia Maria Rosa Ribeiro
Dr. Maria Elizabeth Tiritan
Guest Editors

Manuscript Submission Information

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Keywords

  • Natural products
  • Phytochemical
  • Biologically active
  • Secondary metabolites

Published Papers (2 papers)

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Research

21 pages, 2874 KiB  
Article
Comparative Assessment of Lignan Profiling and Biological Activities of Schisandra henryi Leaf and In Vitro PlantForm Bioreactor-Grown Culture Extracts
by Karolina Jafernik, Paweł Kubica, Michał Dziurka, Łukasz Kulinowski, Izabela Korona-Głowniak, Hosam O. Elansary, Piotr Waligórski, Krystyna Skalicka-Woźniak and Agnieszka Szopa
Pharmaceuticals 2024, 17(4), 442; https://0-doi-org.brum.beds.ac.uk/10.3390/ph17040442 - 29 Mar 2024
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Abstract
This research’s scope encompassed biotechnological, phytochemical, and biological studies of Schisandra henryi, including investigations into its in vitro microshoot culture grown in PlantForm bioreactors (temporary immersion systems, TISs), as well as extracts from leaves of the parent plant, focusing on anti-inflammatory, antioxidant, [...] Read more.
This research’s scope encompassed biotechnological, phytochemical, and biological studies of Schisandra henryi, including investigations into its in vitro microshoot culture grown in PlantForm bioreactors (temporary immersion systems, TISs), as well as extracts from leaves of the parent plant, focusing on anti-inflammatory, antioxidant, anticancer, and antimicrobial activities. The phytochemical analysis included the isolation and quantification of 17 compounds from dibenzocyclooctadiene, aryltetralin lignans, and neolignans using centrifugal partition chromatography (CPC), HPLC-DAD, and UHPLC-MS/MS tandem mass spectrometry with triple quadrupole mass filter methods. Higher contents of compounds were found in microshoots extracts (max. 543.99 mg/100 g DW). The major compound was schisantherin B both in the extracts from microshoots and the leaves (390.16 and 361.24 mg/100 g DW, respectively). The results of the anti-inflammatory activity in terms of the inhibition of COX-1, COX-2, sPLA2, and LOX-15 enzymes indicated that PlantForm microshoot extracts showed strong activity against COX-1 and COX-2 (for 177 mg/mL the inhibition percentage was 76% and 66%, respectively). The antioxidant potential assessed using FRAP, CUPRAC, and DPPH assays showed that extracts from microshoot cultures had 5.6, 3.8, and 3.3 times higher power compared to extracts from the leaves of the parent plant, respectively. The total polyphenol content (TPC) was 4.1 times higher in extracts from the in vitro culture compared to the leaves. The antiproliferative activity against T-cell lymphoblast line Jurkat, breast adenocarcinoma cultures (MCF-7), colon adenocarcinoma (HT-29), and cervical adenocarcinoma (HeLa), showed that both extracts have considerable effects on the tested cell lines. The antimicrobial activity tested against strains of Gram-positive and Gram-negative bacteria and fungi showed the highest activity towards H. pylori (MIC and MBC 0.625 mg/mL). Full article
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14 pages, 9800 KiB  
Article
Phytochemical Investigation of Equisetum arvense and Evaluation of Their Anti-Inflammatory Potential in TNFα/INFγ-Stimulated Keratinocytes
by Se Yun Jeong, Hyung-Seok Yu, Moon-Jin Ra, Sang-Mi Jung, Jeong-Nam Yu, Jin-Chul Kim and Ki Hyun Kim
Pharmaceuticals 2023, 16(10), 1478; https://0-doi-org.brum.beds.ac.uk/10.3390/ph16101478 - 16 Oct 2023
Cited by 1 | Viewed by 2011
Abstract
Equisetum arvense L. (Equisetaceae), widely known as ‘horsetail’, is a perennial plant found extensively across Asia. Extracts of E. arvense have been used in traditional medicine, particularly for the treatment of inflammatory disorders. This study aimed to determine the phytochemical compounds in E. [...] Read more.
Equisetum arvense L. (Equisetaceae), widely known as ‘horsetail’, is a perennial plant found extensively across Asia. Extracts of E. arvense have been used in traditional medicine, particularly for the treatment of inflammatory disorders. This study aimed to determine the phytochemical compounds in E. arvense ethanolic extract and their anti-inflammatory properties. Subsequently, we isolated and identified nine secondary metabolites, including kaempferol 3,7-di-O-β-D-glucopyranoside (1), icariside B2 (2), (Z)-3-hexenyl β-D-glucopyranoside (3), luteolin 5-O-β-D-glucopyranoside (4), 4-O-β-D-glucopyranosyl caffeic acid (5), clemastanin B (6), 4-O-caffeoylshikimic acid (7), (7S,8S)-threo-7,9,9′-trihydroxy-3,3′-dimethoxy-8-O-4′-neolignan-4-O-β-D-glucopyranoside (8), and 3-O-caffeoylshikimic acid (9). The chemical structures of the isolated compounds (1–9) were elucidated using HR-ESI-MS data, NMR spectra, and ECD data. Next, the anti-inflammatory effects of the isolates were evaluated in tumor necrosis factor (TNF)α/interferon (IFN)γ-induced HaCaT, a human keratinocyte cell line. Among the isolates, compound 3 showed the highest inhibitory effect on the expression of pro-inflammatory chemokines, followed by compounds 6 and 8. Correspondingly, the preceding isolates inhibited TNFα/IFNγ-induced activation of pro-inflammatory transcription factors, signal transducer and activator of transcription 1, and nuclear factor-κB. Collectively, E. arvense could be employed for the development of prophylactic or therapeutic agents for improving dermatitis. Full article
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