Search for Articles:
Title / Keyword
Author / Affiliation / Email
Journal
Article Type
 
 
Advanced Search
 
Section
Special Issue
Volume
Issue
Number
Page
 
9.4
4.8
Journals
Biomolecules
Special Issues
Recent Advances in the Isolation, Chemical and Biological Characterization and...
share announcement

Recent Advances in the Isolation, Chemical and Biological Characterization and Synthesis of Bioactive Metabolites from Plants

A special issue of Biomolecules (ISSN 2218-273X). This special issue belongs to the section "Natural and Bio-derived Molecules".

Deadline for manuscript submissions: 31 August 2025 | Viewed by 7018

Special Issue Editors

Prof. Dr. Antonio Evidente

E-Mail Website
Guest Editor
Institute of Sciences of Food Production, National Research Council, Via Amendola 122/O, 70125 Bari, Italy
Interests: chemistry of natural substance; spectroscopy; biosynthesis; structure activity relationships
Special Issues, Collections and Topics in MDPI journals
Prof. Dr. Stefano Superchi

E-Mail Website
Guest Editor
Department of Sciences, University of Basilicata, Viale Ateneo Lucano 10, 85100 Potenza, Italy
Interests: stereochemical characterization of chiral molecules via chiroptical spectroscopy; the total synthesis of bioactive natural products; enantioselective catalysis

Special Issue Information

Dear Colleagues,

Although thousands of compounds have been discovered and often studied in depth, plants still constitute an almost inexhaustible reserve for the discovery of new bioactive metabolites with potential agricultural, medicinal, nutraceutical, and cosmetic applications. These metabolites belong to all classes of natural compounds such as alkaloids, amino acids, peptides, poliketides, phenyl propanoids, terpenes, etc., and often show original structures that overcome resistance developed by pathogens responsible for serious diseases of plants, animals and humans. Unfortunately, the quantities of these metabolites isolated from plants are not sufficient for their industrial production and thus for their practical use in different fields. Therefore, their enantioselective total synthesis represents a fundamental tool for their large-scale production using convenient and eco-friendly strategies. A fundamental prerequisite for developing such synthetic processes is the determination of the absolute configuration of the metabolites of interest due to its close relationship with their biological activity. The use of specific reactions also allows researchers to prepare derivatives of natural metabolites with increased and more specific biological activity for studying the structure–activity correlation and mechanism of action using synthetic intermediates.

Prof. Dr. Antonio Evidente
Prof. Dr. Stefano Superchi
Guest Editors

Manuscript Submission Information

Manuscripts should be submitted online at www.mdpi.com by registering and logging in to this website. Once you are registered, click here to go to the submission form. Manuscripts can be submitted until the deadline. All submissions that pass pre-check are peer-reviewed. Accepted papers will be published continuously in the journal (as soon as accepted) and will be listed together on the special issue website. Research articles, review articles as well as short communications are invited. For planned papers, a title and short abstract (about 100 words) can be sent to the Editorial Office for announcement on this website.

Submitted manuscripts should not have been published previously, nor be under consideration for publication elsewhere (except conference proceedings papers). All manuscripts are thoroughly refereed through a single-blind peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. Biomolecules is an international peer-reviewed open access monthly journal published by MDPI.

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

  • plants
  • bioactive metabolite
  • natural analogues
  • chemical and biological characterization
  • synthesis
  • synthetic intermediates and derivatives

Benefits of Publishing in a Special Issue

  • Ease of navigation: Grouping papers by topic helps scholars navigate broad scope journals more efficiently.
  • Greater discoverability: Special Issues support the reach and impact of scientific research. Articles in Special Issues are more discoverable and cited more frequently.
  • Expansion of research network: Special Issues facilitate connections among authors, fostering scientific collaborations.
  • External promotion: Articles in Special Issues are often promoted through the journal's social media, increasing their visibility.
  • e-Book format: Special Issues with more than 10 articles can be published as dedicated e-books, ensuring wide and rapid dissemination.

Further information on MDPI's Special Issue policies can be found here.

Published Papers (5 papers)

Download All Papers
Order results
Result details
Show export options expand_more Show export options expand_less
Select all
Export citation of selected articles as:

Research

Jump to: Review

12 pages, 989 KiB  
Communication
Synthesis and Antiproliferative Effects of Grossheimin-Derived Aminoanalogues
by Meruyert Ashimbayeva, Zsolt Szakonyi, Sergazy M. Adekenov, Nikoletta Szemerédi, Gabriella Spengler and Tam Minh Le
Biomolecules 2025, 15(4), 578; https://doi.org/10.3390/biom15040578 - 14 Apr 2025
Viewed by 264
Abstract
Grossheimin, a guaiane-type sesquiterpene lactone, displayed a diverse range of biological activities, including anticancer, anti-inflammatory and antimicrobial effects. Various amino analogues of grossheimin were prepared through a Michael addition at its highly active α-methylene-γ-lactone motif. On the other hand, grossheimin was reduced to [...] Read more.
Grossheimin, a guaiane-type sesquiterpene lactone, displayed a diverse range of biological activities, including anticancer, anti-inflammatory and antimicrobial effects. Various amino analogues of grossheimin were prepared through a Michael addition at its highly active α-methylene-γ-lactone motif. On the other hand, grossheimin was reduced to diol, which was then subjected to nucleophilic addition or acetylation to introduce heteroatoms associated with oxygen, sulfur or nitrogen functionalities. All of the synthesised Michael and acetylated adducts were evaluated for their in vitro cytotoxic action on human colon adenocarcinoma lines, including Colo205 and Colo320. The bioassay results indicated that the acetylated adducts displayed a potent cytotoxic effect compared to grossheimin, the parent molecule. A docking study was also performed to exploit the observed results. Full article
(This article belongs to the Special Issue Recent Advances in the Isolation, Chemical and Biological Characterization and Synthesis of Bioactive Metabolites from Plants)
►▼ Show Figures

Figure 1

20 pages, 1322 KiB  
Article
Chemical Profiling of Polar Lipids and the Polyphenolic Fraction of Commercial Italian Phaseolus Seeds by UHPLC-HRMS and Biological Evaluation
by Vadym Samukha, Francesca Fantasma, Gilda D’Urso, Ester Colarusso, Anna Schettino, Noemi Marigliano, Maria Giovanna Chini, Gabriella Saviano, Vincenzo De Felice, Gianluigi Lauro, Francesco Maione, Giuseppe Bifulco, Agostino Casapullo and Maria Iorizzi
Biomolecules 2024, 14(10), 1336; https://doi.org/10.3390/biom14101336 - 20 Oct 2024
Viewed by 1474
Abstract
The common bean (Phaseolus vulgaris L.) is one of the oldest food crops in the world. In this study, the ultra-high-performance liquid chromatography high-resolution mass spectrometry (UHPLC-MS/MS) technique was used to characterize the polar lipid composition and polyphenolic fraction of five bean [...] Read more.
The common bean (Phaseolus vulgaris L.) is one of the oldest food crops in the world. In this study, the ultra-high-performance liquid chromatography high-resolution mass spectrometry (UHPLC-MS/MS) technique was used to characterize the polar lipid composition and polyphenolic fraction of five bean varieties commonly consumed in Italy: Cannellino (PVCA), Controne (PVCO), Borlotti (PVBO), Stregoni (PVST), and Vellutina (PVVE). Lipid content represents a minor fraction of the whole metabolome in dry beans, and little is known about their polar lipids, which could be potentially bioactive components. Thirty-three compounds were detected through UHPLC-MS/MS, including oxylipins, phospholipids, N-acyl glycerolipids, and several fatty acids. The dichloromethane extracts were subjected to principal component analysis (PCA), with the results showing greater differentiation for the Borlotti variety. Moreover, 27 components belonging to different polyphenol classes, such as phenolic acids, flavonoids, catechins, anthocyanins and their glycosides, and some saponins, were identified in the hydroalcoholic seed extracts. In addition, the mineral content of the beans was determined. Considering the high number of compounds in the five apolar seed extracts, all samples were examined to determine their in vitro inhibitory activity against the enzyme cyclooxygenase-2 (COX-2), which is inducible in inflammatory cells and mediates inflammatory responses. Only PVCO showed the best inhibition of the COX-2 enzyme with an IC50 = 31.15 ± 2.16 µg/mL. In light of these results, the potential anti-inflammatory properties of PVCO were evaluated in the LPS-stimulated murine macrophage cell line J774A.1. Herein, we demonstrate, for the first time, that PVCO at 30 µg/mL can significantly reduce the release of TNF-α, with a less significant anti-inflammatory effect being observed in terms of IL-6 release. Full article
(This article belongs to the Special Issue Recent Advances in the Isolation, Chemical and Biological Characterization and Synthesis of Bioactive Metabolites from Plants)
►▼ Show Figures

Graphical abstract

17 pages, 9639 KiB  
Article
Insights into the Metabolite Profiles of Two Camellia (Theaceae) Species in Yunnan Province through Metabolomic and Transcriptomic Analysis
by Miao Niu, Ranyang Li, Xiongyu Li, Hongyan Yang, Jianliang Ding, Xianxiu Zhou, Yuqi He, Yawen Xu, Qian Qu, Zhiwei Liu and Jiahua Li
Biomolecules 2024, 14(9), 1106; https://doi.org/10.3390/biom14091106 - 3 Sep 2024
Cited by 2 | Viewed by 1647
Abstract
Tea (Camellia sinensis) falls into the family Theaceae, is a valuable commercial crop, and tea products made from its buds and young leaves are favored by consumers all over the world. The more common Thea plant is Camellia sinensis (C. sinensis [...] Read more.
Tea (Camellia sinensis) falls into the family Theaceae, is a valuable commercial crop, and tea products made from its buds and young leaves are favored by consumers all over the world. The more common Thea plant is Camellia sinensis (C. sinensis), but its most important relative, Camellia taliensis (C. taliensis), is also utilized by locals in the area of cultivation to manufacture tea. In this investigation, C. taliensis (DL) and C. sinensis (QJZ) were characterized in terms of their agronomic traits, physicochemical indices, metabolomics, and transcriptomics. The leaf area of DL is larger than that of QJZ; the color of DL’s buds and leaves is yellowish-green, while that of QJZ’s is green. DL’s buds and leaves are more densely velvety than those of QJZ. The HPLC results indicated that the physicochemical contents varied considerably between the two samples, with DL having greater concentrations of EGCG and GABA than QJZ, while QJZ had remarkably higher concentrations of C, CA, and EGC than DL. A total of 2269 metabolites and 362,190,414 genes were positively identified, with the number of DAMs and DEGs being 1001 and 34,026, respectively. The flavonoids, phenolic acids, and alkaloid metabolites were dramatically different between the two tea group plants. Bioinformatics profiling revealed that the DAMs and DEGs of the two tea group plants interacted with each other and were involved in metabolic pathways, including “biosynthesis of secondary metabolites”, “biosynthesis of amino acids”, “biosynthesis of cofactors”, “phenylpropanoid biosynthesis”, and “flavonoid biosynthesis”. Overall, these results provide statistical support for germplasm conservation and production for both C. taliensis and C. sinensis. Full article
(This article belongs to the Special Issue Recent Advances in the Isolation, Chemical and Biological Characterization and Synthesis of Bioactive Metabolites from Plants)
►▼ Show Figures

Figure 1

13 pages, 3021 KiB  
Article
Metabolites from Aerial Parts of Glycyrrhiza foetida as Modulators of Targets Related to Metabolic Syndrome
by Hekmat B. Al-Hmadi, Elena Serino, Arianna Pastore, Giuseppina Chianese, Saoussen Hammami, Mariano Stornaiuolo and Orazio Taglialatela-Scafati
Biomolecules 2024, 14(4), 467; https://doi.org/10.3390/biom14040467 - 11 Apr 2024
Cited by 1 | Viewed by 1523
Abstract
A detailed phytochemical investigation has been carried out on the aerial parts of G. foetida leading to the isolation of 29 pure compounds, mainly belonging to the amorfrutin and polyphenol classes. Among them, the new amorfrutin N (5) and exiguaflavone L [...] Read more.
A detailed phytochemical investigation has been carried out on the aerial parts of G. foetida leading to the isolation of 29 pure compounds, mainly belonging to the amorfrutin and polyphenol classes. Among them, the new amorfrutin N (5) and exiguaflavone L (21) were isolated and their structures elucidated by means of HR-ESIMS and NMR. All the isolated compounds were investigated for modulation of mitochondrial activity and stimulation of glucose uptake via GLUT transporters, two metabolic processes involved in intracellular glucose homeostasis, which, therefore, correlate with the incidence of metabolic syndrome. These experiments revealed that amorfrutins were active on both targets, with amorfrutin M (17) and decarboxyamorfrutin A (2) emerging as mitochondrial stimulators, and amorfrutin 2 (12) as a glucose uptake promoter. However, members of the rich chalcone/flavonoid fraction also proved to contribute to this activity. Full article
(This article belongs to the Special Issue Recent Advances in the Isolation, Chemical and Biological Characterization and Synthesis of Bioactive Metabolites from Plants)
►▼ Show Figures

Figure 1

Review

Jump to: Research

34 pages, 786 KiB  
Review
A Review of the Phytochemistry, Molecular Docking, Pharmacology, Toxicology, Ethnopharmacology, Botany, and Clinical Studies of Maytenus senegalensis (Lam.) Excell
by Thanyani Emelton Ramadwa and Stephen Meddows-Taylor
Biomolecules 2025, 15(2), 197; https://doi.org/10.3390/biom15020197 - 30 Jan 2025
Viewed by 1043
Abstract
Maytenus senegalensis (Lam.) Excell, also known as Gymnosporia senegalensis (Lam.) Loes, is distributed particularly in savannah regions of tropical Africa. It is used to treat malaria, tuberculosis, rheumatism and diarrhea, amongst other afflictions. The objective of this comprehensive review is to summarize studies [...] Read more.
Maytenus senegalensis (Lam.) Excell, also known as Gymnosporia senegalensis (Lam.) Loes, is distributed particularly in savannah regions of tropical Africa. It is used to treat malaria, tuberculosis, rheumatism and diarrhea, amongst other afflictions. The objective of this comprehensive review is to summarize studies on phytochemistry, molecular docking, pharmacology, toxicology, ethnopharmacology, botany, and clinical trials of M. senegalensis. Data on M. senegalensis were collected using different databases such as Google Scholar, Science Direct, Web of Science, Scopus, SciFinder, Wiley Online, etc. This review showed that 118 biomolecules from different parts of M. senegalensis were identified. A total of 46 compounds were tested for antiplasmodial, anti-inflammatory, and antiproliferative activities, and some in vivo studies were carried out on mice. Isomintlactone (31), pristimerin (24), and jacareubin (32) were analyzed for molecular docking. The crude extracts and fractions had pharmacological activities, including antiparasitic, antimycobacterial, anti-inflammatory, antiviral, antiproliferative, and antidiabetic, while showing low toxicity in mice. Clinical trial studies on the safety and tolerability of M. senegalensis ethanol root bark extracts in male volunteers showed its potential immunomodulatory effects. Another trial specifically evaluated the electrocardiographic effects of M. senegalensis in adult volunteers and showed its advantageous cardiac profile by improving the overall safety profile. Full article
(This article belongs to the Special Issue Recent Advances in the Isolation, Chemical and Biological Characterization and Synthesis of Bioactive Metabolites from Plants)
►▼ Show Figures

Figure 1

Show export options expand_more Show export options expand_less
Select all
Export citation of selected articles as:
 
Displaying articles 1-5
Back to TopTop