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Biomolecules
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Natural Bioactives as Leading Molecules for Drug Development
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Natural Bioactives as Leading Molecules for Drug Development

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 December 2025 | Viewed by 5059

Special Issue Editors

Dr. Chang Liu

E-Mail Website
Guest Editor
Department of Biomedical and Pharmaceutical Sciences, College of Pharmacy, University of Rhode Island, Kingston, RI, USA
Interests: natural products; drug discovery; proteomics; cancer immunotherapy; immune checkpoints; immune checkpoint regulation
Special Issues, Collections and Topics in MDPI journals
Dr. Hang Ma

E-Mail Website
Guest Editor
Department of Biomedical and Pharmaceutical Sciences, College of Pharmacy, University of Rhode Island, 7 Greenhouse Rd, Kingston, RI 02881, USA
Interests: bioactive natural products; anti-aging; nutraceuticals; cosmeceuticals
Special Issues, Collections and Topics in MDPI journals
Dr. Ang Cai

E-Mail Website
Guest Editor
College of Pharmacy, University of Rhode Island, 7 Greenhouse Rd, Kingston, RI 02881, USA
Interests: natural products; DNA modification
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Natural bioactives have played a crucial role in drug development, regulating key pathophysiological processes such as inflammation, fibrosis, hypoxia, oxidative stress, cell proliferation, angiogenesis, migration, and metabolism linked to human diseases. The isolation and identification of these compounds, alongside their therapeutic applications, have consistently drawn the attention of researchers. Traditional extraction methods, however, are often labor-intensive and time-consuming. To overcome these challenges, innovative techniques, including green and solvent-free methods, are increasingly being employed. Omics methods are also extensively applied to explore potential targets and mechanisms of action for these bioactives. This Special Issue invites submissions on the development of natural bioactives as promising drug candidates, the application of novel techniques for their isolation and identification, and new insights into their bioactivities. Additionally, we welcome studies integrating omics with traditional assays for comprehensive evaluation

Dr. Chang Liu
Dr. Hang Ma
Dr. Ang Cai
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

  • drug discovery
  • natural products
  • leading molecules
  • isolation and identification
  • phytochemical investigation
  • omics approaches

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Published Papers (4 papers)

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Research

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17 pages, 1315 KiB  
Article
Biological Activities of Essential Oils and Hydrolates from Different Parts of Croatian Sea Fennel (Crithmum maritimum L.)
by Livia Slišković, Nikolina Režić Mužinić, Olivera Politeo, Petra Brzović, Josip Tomaš, Ivana Generalić Mekinić and Marijana Popović
Biomolecules 2025, 15(5), 666; https://doi.org/10.3390/biom15050666 - 4 May 2025
Viewed by 254
Abstract
The traditional nutritional use of sea fennel (Crithmum maritimum L.) has been rediscovered and reestablished, making this halophyte plant a prominent ingredient in coastal cuisine and a subject of interest in various scientific disciplines, including pharmacy and medicine. The first objective of [...] Read more.
The traditional nutritional use of sea fennel (Crithmum maritimum L.) has been rediscovered and reestablished, making this halophyte plant a prominent ingredient in coastal cuisine and a subject of interest in various scientific disciplines, including pharmacy and medicine. The first objective of this study was to identify the volatile profiles of essential oils (EOs) and hydrolates derived from the leaves, flowers, and fruits of sea fennel using gas chromatography–mass spectrometry. A total of 25 different volatiles were identified in the EOs and 63 were identified in the hydrolates. Limonene was the most abundant component in the EOs (74.85%, 74.30%, and 67.41%, respectively), while in the hydrolates, it was terpinen-4-ol in the leaves (27.8%) and the flowers (36.7%) and (Z)-carveol in the fruits (11.4%). The second objective was to investigate the biological activities of the samples. The antioxidant and choline inhibitory activities of hydrolates were generally low, with the flower hydrolate providing the inhibition of both enzymes and the leaf hydrolate with the highest antiradical activity. The cytotoxic activities of the EOs and hydrolates were also investigated. The human breast adenocarcinoma cell line MDA-MB-23 was the most sensitive against EOs from the flowers and fruits, reaching the IC50 after 48 and 72 h, respectively. The leaf hydrolate exhibited cytotoxic activity after 72 h, while the flower hydrolate was effective after 48 h. The MCF-7 cell line was sensitive to the flower and fruit EOs, and the IC50 was reached at all the tested periods. Overall, the results highlight sea fennel as a rich source of bioactive compounds that have significant potential for greater utilization in the nutraceutical and pharmaceutical industries. Full article
(This article belongs to the Special Issue Natural Bioactives as Leading Molecules for Drug Development)
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21 pages, 3711 KiB  
Article
Metabolomic Profiling and In Vitro Evaluation of Cytotoxic, Genotoxic, and Antigenotoxic Effects of Staphylea pinnata L. Extract from Italian Flora
by Ghanya Al-Naqeb, Fabio Pietrolucci, Mauro Commisso, Aliki Kalmpourtzidou, Amanda Oldani, Sara Boussetta, Beatrice Maccarini, Rachele De Giuseppe and Hellas Cena
Biomolecules 2025, 15(3), 385; https://doi.org/10.3390/biom15030385 - 6 Mar 2025
Viewed by 896
Abstract
Staphylea pinnata L., (S. pinnata), has long been recognized in Europe as both a wild food source and a traditional medicinal. This study aimed to characterize the metabolomic profile of the leaf extract of S. pinnata and assess its cytotoxic, genotoxic, [...] Read more.
Staphylea pinnata L., (S. pinnata), has long been recognized in Europe as both a wild food source and a traditional medicinal. This study aimed to characterize the metabolomic profile of the leaf extract of S. pinnata and assess its cytotoxic, genotoxic, and antigenotoxic effects in vitro for the first time. The methanolic extract of the leaves was analyzed using Ultra-Performance Liquid Chromatography–High-Resolution Mass Spectrometry (UPLC-HRMS). To evaluate its cytotoxic, genotoxic, and antigenotoxic properties, the cytokinesis block micronucleus assay was performed on Chinese hamster ovarian K1 cells. The analysis revealed a wide variety of metabolites in the extract, with B-type procyanidins and prodelphinidins being the most abundant. The genotoxicity of the extract varied depending on its concentration; at the lowest concentration (75 μg/mL), it showed no genotoxic effects and exhibited antigenotoxic properties by reducing the frequency of micronuclei induced by mitomycin C. However, at the highest concentration (300 μg/mL), the extract demonstrated genotoxic effects. In conclusion, the S. pinnata extract displayed both genotoxic and antigenotoxic properties, which may be attributed to its phytochemical composition. These findings highlight the complex nature of the plant’s bioactive compounds, suggesting potential therapeutic applications with careful consideration of dosage. Additional research is necessary to understand the mechanisms underlying these properties. Full article
(This article belongs to the Special Issue Natural Bioactives as Leading Molecules for Drug Development)
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15 pages, 3803 KiB  
Article
Compound K Promotes Megakaryocytic Differentiation by NLRP3 Inflammasome Activation
by Seonhwa Hwang, Min-Seo Park, Anthony Junhoe Koo, Eunsoo Yoo, Seh-Hyon Song, Hye-Kyung Kim, Min-Hi Park and Jae-Seon Kang
Biomolecules 2024, 14(10), 1257; https://doi.org/10.3390/biom14101257 - 4 Oct 2024
Viewed by 1894
Abstract
Platelets are essential blood components that maintain hemostasis, prevent excessive bleeding, and facilitate wound healing. Reduced platelet counts are implicated in various diseases, including leukemia, hepatitis, cancer, and Alzheimer’s disease. Enhancing megakaryocytic differentiation is a promising strategy to increase platelet production. Compound K [...] Read more.
Platelets are essential blood components that maintain hemostasis, prevent excessive bleeding, and facilitate wound healing. Reduced platelet counts are implicated in various diseases, including leukemia, hepatitis, cancer, and Alzheimer’s disease. Enhancing megakaryocytic differentiation is a promising strategy to increase platelet production. Compound K (CK), a major bioactive metabolite of ginsenosides from Panax ginseng, has demonstrated anti-cancer and neuroprotective properties. In this study, we investigated the effects of CK on megakaryocytic differentiation and apoptosis in chronic myeloid leukemia (CML) cell lines K562 and Meg-01. CK treatment significantly upregulated the mRNA expression of key megakaryocytic differentiation markers, including CD61, CD41, and CD42a, and promoted the formation of large, multinucleated cells in K562 cells. Additionally, flow cytometry analysis revealed that CK at 5 µM induced apoptosis, a critical process in thrombocytopoiesis, in both K562 and Meg-01 cells. RT2 Profiler PCR array analysis further identified a marked increase in the expression of genes associated with the activation of the NLRP3 inflammasome in CK-treated K562 and Meg-01 cells. This study is the first to demonstrate that CK promotes megakaryocytic differentiation and apoptosis through the activation of the ERK/EGR1 and NLRP3 inflammasome pathways. These findings suggest that CK may enhance platelet production, indicating its potential as a therapeutic candidate for platelet-related disorders and other associated diseases. Full article
(This article belongs to the Special Issue Natural Bioactives as Leading Molecules for Drug Development)
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Review

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25 pages, 2772 KiB  
Review
Natural Alternatives in the Treatment of Colorectal Cancer: A Mechanisms Perspective
by Karen Vanessa Fernandez-Muñoz, Cuauhtémoc Ángel Sánchez-Barrera, Marco Meraz-Ríos, Jose Luis Reyes, Eloy Andrés Pérez-Yépez, Maria Teresa Ortiz-Melo, Luis I. Terrazas and Monica Graciela Mendoza-Rodriguez
Biomolecules 2025, 15(3), 326; https://doi.org/10.3390/biom15030326 - 24 Feb 2025
Cited by 2 | Viewed by 1271
Abstract
Colorectal cancer (CRC) is one of the deadliest neoplasia. Intrinsic or acquired resistance is the main cause of failure of therapy regimens that leads to relapse and death in CRC patients. The widely used chemotherapeutic agent 5-fluorouracil (5-FU) remains the mainstay for therapeutic [...] Read more.
Colorectal cancer (CRC) is one of the deadliest neoplasia. Intrinsic or acquired resistance is the main cause of failure of therapy regimens that leads to relapse and death in CRC patients. The widely used chemotherapeutic agent 5-fluorouracil (5-FU) remains the mainstay for therapeutic combinations. Unfortunately, chemotherapeutic resistance and side effects are frequent events that compromise the success of these therapies; the dysregulation of enzymes that regulate 5-FU metabolism increases the expression and activity of efflux pumps. Additional tumor cell adaptations such as epithelial–mesenchymal transition (EMT), autophagy shaping of the tumor microenvironment, and inflammation contribute to chemoresistance. Finding new strategies and alternatives to enhance conventional chemotherapies has become necessary. Recently, the study of natural compounds has been gaining strength as an alternative to chemotherapeutics in different cancers. Curcumin, trimethylglycine, resveratrol, artemisinin, and some helminth-derived molecules, among others, are some natural compounds studied in the context of CRC. This review discusses the main benefits, mechanisms, advances, and dark side of conventional chemotherapeutics currently evaluated in CRC treatment. We also analyzed the landscape of alternative non-conventional compounds and their underlying mechanisms of action, which could, in the short term, provide fundamental knowledge to harness their anti-tumor effects and allow them to be used as alternative adjuvant therapies. Full article
(This article belongs to the Special Issue Natural Bioactives as Leading Molecules for Drug Development)
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