Submit to Pharmaceuticals Review for Pharmaceuticals Propose a Special Issue

Journal Menu

Journal Browser

► Journal Browser

Plant-Derived Natural Compounds as Bioactive Molecules with Beneficial Effects on Human Health

Print Special Issue Flyer
Special Issue Editors
Special Issue Information
Keywords
Benefits of Publishing in a Special Issue
Published Papers

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

Deadline for manuscript submissions: closed (25 January 2025) | Viewed by 26170

Share This Special Issue

Special Issue Editor

Dr. Diego Morales

E-Mail Website
Guest Editor

Departmental Section of Galenic Pharmacy and Food Technology, Veterinary Faculty, Complutense University of Madrid, 28040 Madrid, Spain
Interests: bioactive compounds; supercritical fluids; bioactivities; HPLC; food; volatile component
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

A strong correlation between natural compounds and health status has been assumed by modern populations. Moreover, the use of non-synthetic drugs can, in some cases, avoid certain disadvantages linked to conventional pharmaceuticals, such as adverse reactions or side effects and lack of specificity. Accordingly, research on vegetal compounds (e.g., peptides, phenolic compounds, lipids, polysaccharides/fibers, etc.) has exponentially increased over the last few decades. These investigations must cover raw materials selection (including by-product revalorization), extraction, analytical and biochemical techniques (following, to the greatest extent possible, the principles of sustainability and green chemistry), and biological activity tests that include in vitro and animal models but also require validation through clinical trials. Numerous plant-based nutraceuticals and drugs have been designed and evaluated, encouraging further investigation to finally integrate these products with conventional medicaments and thus obtain healthy alternatives. Therefore, the aim of this Special Issue is to investigate the latest findings and insights related to the study of vegetal bioactives, plant nutraceuticals, and drugs (including extraction and biochemical and biological activity analyses); identify current limitations; and elucidate future perspectives.

Dr. Diego Morales
Guest Editor

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. Pharmaceuticals 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 2900 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

plant bioactives
bioactive compounds
gut microbiome
immune-modulatory
antioxidant
hypocholesterolemic
antihypertensive
clinical trials

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.
Reprint: MDPI Books provides the opportunity to republish successful Special Issues in book format, both online and in print.

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

Published Papers (10 papers)

Download All Papers

Order results

Result details

Show export options Show export options

Select all

Export citation of selected articles as:

Research

Jump to: Review

20 pages, 2897 KiB

Open AccessArticle

Behavioral and Biochemical Insights into the Therapeutic Potential of Mitocurcumin in a Zebrafish–Pentylenetetrazole (PTZ) Epilepsy Model

by Alin Dumitru Ciubotaru, Carmen-Ecaterina Leferman, Bogdan-Emilian Ignat, Anton Knieling, Irina Mihaela Esanu, Delia Lidia Salaru, Liliana Georgeta Foia, Bogdan Minea, Luminita Diana Hritcu, Cristina Daniela Dimitriu, Laura Stoica, Ioan-Adrian Ciureanu, Alin Stelian Ciobica, Andrei Neamtu, Bogdan Alexandru Stoica and Cristina Mihaela Ghiciuc

Pharmaceuticals 2025, 18(3), 382; https://doi.org/10.3390/ph18030382 - 7 Mar 2025

Cited by 1 | Viewed by 804

Abstract

Background/Objectives: Epilepsy is a complex neurological disorder with a strong link to oxidative stress, which contributes to seizure susceptibility and neuronal damage. This study aims to investigate the effects of curcumin (Cur), sodium valproate (VPA), and mitocurcumin (MitoCur), a mitochondria-targeted curcumin, on behavioral and oxidative stress parameters in a zebrafish model of pentylenetetrazole (PTZ)-induced seizures. Methods: Adult zebrafish were exposed to two concentrations (0.25 and 0.5 µM for Cur and MitoCur; 0.25 and 0.5 mM for VPA). Behavioral assessments, including locomotion, spatial exploration, and directional movement, were conducted using EthoVision XT tracking software. Oxidative stress markers, including superoxide dismutase (SOD), malondialdehyde (MDA), glutathione peroxidase (GPx), and total antioxidant status (TAS), were analyzed in brain homogenates. Results: Behavioral analyses indicated dose-dependent effects, with higher doses generally reducing activity. MitoCur at 0.25 µM enhanced antioxidant defenses and reduced oxidative damage, while higher doses exhibited a pro-oxidant shift. VPA at 0.25 mM improved TAS without significantly altering MDA levels. Conclusions: These findings emphasize the importance of dose optimization in antioxidant-based epilepsy treatments and highlight the potential of MitoCur as a targeted therapeutic option. Full article

(This article belongs to the Special Issue Plant-Derived Natural Compounds as Bioactive Molecules with Beneficial Effects on Human Health)

► Show Figures

Figure 1

18 pages, 4829 KiB

Open AccessArticle

Identification of Two Flavonoids as New and Safe Inhibitors of Kynurenine Aminotransferase II via Computational and In Vitro Study

by Redouane Rebai, Luc Jasmin and Abdennacer Boudah

Pharmaceuticals 2025, 18(1), 76; https://doi.org/10.3390/ph18010076 - 10 Jan 2025

Cited by 2 | Viewed by 757

Abstract

Background/Objectives: Kynurenine aminotransferase II (KAT-II) is a target for treating several diseases characterized by an excess of kynurenic acid (KYNA). Although KAT-II inactivators are available, they often lead to adverse side effects due to their irreversible inhibition mechanism. This study aimed to identify potent and safe inhibitors of KAT-II using computational and in vitro approaches. Methods: Virtual screening, MM/GBSA, and molecular dynamics simulations were conducted to identify the top drug candidates, followed by kinetic measurements and in vitro cytotoxicity evaluation. Results: The study showed that two compounds, herbacetin and (-)-Epicatechin exhibited the best scores. Their Glide docking scores are −8.66 kcal/mol and −8.16 kcal/mol, respectively, and their MM/GBSA binding energies are −50.30 kcal/mol and −51.35 kcal/mol, respectively. These scores are superior to those of the standard inhibitor, PF-04859989, which has docking scores of −7.12 kcal/mol and binding energy of −38.41 kcal/mol. ADMET analysis revealed that the selected compounds have favorable pharmacokinetic parameters, moderate bioavailability, and a safe toxicity profile, which supports their potential use. Further, the kinetic study showed that herbacetin and (-)-Epicatechin are reversible KAT-II inhibitors and exhibit a competitive inhibition mechanism. Their half-maximal inhibitory concentrations (IC50) are 5.98 ± 0.18 µM and 8.76 ± 0.76 µM, respectively. The MTT assay for cell toxicity indicated that the two compounds do not affect HepG2 cell viability at the necessary concentration for KAT-II inhibition. Conclusions: These results suggest that herbacetin and (-)-Epicatechin are suitable for KAT-II inhibition and are promising candidates for further development of KAT-II inhibitors. Full article

(This article belongs to the Special Issue Plant-Derived Natural Compounds as Bioactive Molecules with Beneficial Effects on Human Health)

► Show Figures

Figure 1

15 pages, 2719 KiB

Open AccessArticle

Evaluation of Cytotoxicity and Acute Oral Toxicity of Saline Extract and Protein-Rich Fraction from Moringa oleifera Lam. Leaves

by Robson Raion de Vasconcelos Alves, Alisson Macário de Oliveira, Gabryella Borges dos Prazeres, Abdênego Rodrigues da Silva, Franciele Florencio Costa, Bárbara Rafaela da Silva Barros, Talita Giselly dos Santos Souza, Luana Cassandra Breintenbach Barroso Coelho, Cristiane Moutinho Lagos de Melo, Magda Rhayanny Assunção Ferreira, Luiz Alberto Lira Soares, Cristiano Aparecido Chagas, Maria Lígia Rodrigues Macedo, Thiago Henrique Napoleão, Mariana Pinheiro Fernandes and Patrícia Maria Guedes Paiva

Pharmaceuticals 2024, 17(8), 1045; https://doi.org/10.3390/ph17081045 - 8 Aug 2024

Cited by 1 | Viewed by 1680 | Correction

Abstract

Moringa oleifera Lam. (horseradish tree) leaves demonstrate high nutritional value, are rich in proteins, and are widely used in folk medicine and food. This study investigated the presence of secondary metabolites and antinutritional proteins in leaf extract (LE) and the protein-rich fraction (PRF) derived from M. oleifera leaves, as well as the cytotoxicity to human cells, hemolytic activity, and in vivo acute toxicity and genotoxicity in mice. The flavonoids rutin and vitexin as well as trypsin inhibitors and lectins were detected in LE and PRF. Neither sample demonstrated toxicity against human peripheral blood mononuclear cells and both showed low hemolytic action. In vivo, LE and PRF did not show antinutritional effects and caused no death. The hematological parameters of the animals in the treated group were similar to those of the control. A significant increase in the serum levels of alanine aminotransferase and a discrete leukocyte infiltration with cytoplasmic vacuolization of the hepatocytes in the liver were detected in LE-treated animals. The preparations were not genotoxic or mutagenic. This study shows that LE and PRF are not antinutritional agents and presented low acute toxicity and no genotoxicity or mutagenicity. The present study contributes to the determination of the safety of using M. oleifera leaf proteins. Full article

(This article belongs to the Special Issue Plant-Derived Natural Compounds as Bioactive Molecules with Beneficial Effects on Human Health)

► Show Figures

Graphical abstract

19 pages, 4938 KiB

Open AccessArticle

Inula salicina L.: Insights into Its Polyphenolic Constituents and Biological Activity

by Viktoria Ivanova, Paraskev Nedialkov, Petya Dimitrova, Tsvetelina Paunova-Krasteva and Antoaneta Trendafilova

Pharmaceuticals 2024, 17(7), 844; https://doi.org/10.3390/ph17070844 - 27 Jun 2024

Cited by 3 | Viewed by 2340

Abstract

In this study, UHPLC-HRMS analysis of the defatted methanol extract obtained from Inula salicina L. led to the identification of 58 compounds—hydroxycinnamic and hydroxybenzoic acids and their glycosides, acylquinic and caffeoylhexaric acids, and flavonoids and their glycosides. In addition, a new natural compound, N-(8-methylnepetin)-3-hydroxypiperidin-2-one was isolated and its structure was elucidated by NMR spectroscopy. The presence of a flavoalkaloid in genus Inula is described now for the first time. Chlorogenic acid was the main compound followed by 3,5-, 1,5- and 4,5-dicaffeoylquinic acids. The methanol extract was studied for its antioxidant potential by DPPH, ABTS, and FRAP assays and sun protective properties. In addition, a study was conducted to assess the effectiveness of the tested extract in inhibiting biofilm formation by Gram-positive and Gram-negative strains. Results from crystal violet tests revealed a notable decrease in biofilm mass due to the extract. The anti-biofilm efficacy was confirmed through the observation of the biofilm viability by live/dead staining. The obtained results showed that this plant extract could be used in the development of cosmetic products with antibacterial and sun protection properties. Full article

(This article belongs to the Special Issue Plant-Derived Natural Compounds as Bioactive Molecules with Beneficial Effects on Human Health)

► Show Figures

Graphical abstract

28 pages, 203516 KiB

Open AccessFeature PaperArticle

Cistus, Acacia, and Lemon verbena Valorization through Response Surface Methodology: Optimization Studies and Potential Application in the Pharmaceutical and Nutraceutical Industries

by Filipa A. Fernandes, Márcio Carocho, Tiane C. Finimundy, Miguel A. Prieto, Isabel C. F. R. Ferreira, Lillian Barros and Sandrina A. Heleno

Pharmaceuticals 2024, 17(5), 593; https://doi.org/10.3390/ph17050593 - 7 May 2024

Viewed by 1527

Abstract

Cistus ladanifer L., Acacia dealbata L., and Aloysia citrodora Paláu were subject to an optimization procedure for two extraction techniques (heat-assisted extraction (HAE) and ultrasound-assisted extraction (UAE)). The extracts were then analyzed by HPLC-DAD-ESI/MS for their phenolic profile (cistus—15 compounds, acacia—21 compounds, and lemon verbena—9 compounds). The response surface methodology was applied, considering four varying factors: ethanol percentage; extraction time; temperature/power; and S/L ratio, generating two responses (the major phenolic compound, or family of compounds, and the extraction yield). For cistus, both techniques optimized the extraction yield of punicalagins, with UAE proving to be the most efficient extraction method (3.22% ethanol, 22 min, 171 W, and 35 g/L). For acacia, HAE maximized the extraction of procyanidin (74% ethanol, 86 min, 24 °C, and 50 g/L), and UAE maximized the content of myricetin (65% ethanol, 8 min, 50 W, and 50 g/L). For lemon verbena, HAE favored the extraction of martynoside (13% ethanol, 96 min, 49 °C and 17 g/L) and forsythiaside UAE (94% ethanol, 25 min, 399 W, and 29 g/L). The optimal conditions for the extraction of compounds with high added value and potential for use in pharmaceuticals and nutraceuticals were defined. Full article

(This article belongs to the Special Issue Plant-Derived Natural Compounds as Bioactive Molecules with Beneficial Effects on Human Health)

► Show Figures

Graphical abstract

14 pages, 4519 KiB

Open AccessArticle

In Vivo Anti-Inflammatory and Antinociceptive Activities of Black Elder (Sambucus nigra L.) Fruit and Flower Extracts

by Daniela Seymenska, Desislava Teneva, Irina Nikolova, Niko Benbassat and Petko Denev

Pharmaceuticals 2024, 17(4), 409; https://doi.org/10.3390/ph17040409 - 23 Mar 2024

Cited by 7 | Viewed by 2448

Abstract

Sambucus nigra L. (S. nigra, SN) or black elder is a traditional medicinal plant widely used worldwide for therapeutic and dietary purposes. The aim of the current study was to investigate the anti-inflammatory and antinociceptive activities of black elder fruit and flower extracts (SNFrE and SNFlE, respectively). The primary polyphenol constituents in the flower extract were flavonoids and phenolic acids, while anthocyanins were the main components in the fruit extract. SNFrE revealed pronounced and dose-dependent in vivo anti-inflammatory activity assessed by the cotton pellet-induced granuloma test. Doses of 10, 20, and 50 mg/kg BW of SNFrE reduced the weight of induced granuloma in rats by 20.3%, 20.5%, and 28.4%, respectively. At the highest dose (50 mg/kg BW), SNFrE had significant (p < 0.01) anti-inflammatory activity comparable to that of diclofenac, the reference compound used (10 mg/kg BW). In addition, the in vivo antinociceptive activity of the extracts in mice was estimated using the acetic-acid-induced writhing test. Both extracts at doses of 50 mg/kg BW inhibited the abdominal contractions induced by the acetic acid significantly comparing to the control group (p < 0.01). Our findings indicate that black elder extracts and particularly SNFrE possess anti-inflammatory and antinociceptive activities, providing experimental evidence for the use of S. nigra in traditional medicine. Full article

(This article belongs to the Special Issue Plant-Derived Natural Compounds as Bioactive Molecules with Beneficial Effects on Human Health)

► Show Figures

Figure 1

Review

Jump to: Research

15 pages, 3998 KiB

Open AccessReview

Plants with Potential Importance in Supporting the Treatment of Depression: Current Trends, and Research

by Renata Nurzyńska-Wierdak

Pharmaceuticals 2024, 17(11), 1489; https://doi.org/10.3390/ph17111489 - 6 Nov 2024

Viewed by 2705

Abstract

Depression is one of the most common diseases in the world, and it is also the most common mental disorder. Depressive disorders are a real threat not only to individuals, but also to the general population. This disease is a leading cause of disability and inability to work. Due to the numerous side effects of conventional drugs, attention is increasingly being paid to other solutions, including herbal medicines. Many plant species are known for their traditional uses in the treatment of anxiety, insomnia, and depression. The clinically proven effects of adaptogenic raw materials on depression symptoms are probably related to the positive impact of some secondary metabolites (terpenoids, alkaloids, glucosinolates, phenols). Currently, it is emphasized that in many cases the antioxidant and anti-inflammatory properties of plant substances play a protective role at the neurocellular level. Among the medicinal plants analyzed in clinical trials for the treatment of depression, the following seem to be particularly interesting: saffron (Crocus L.), turmeric (Curcuma L.), ginkgo (Ginkgo L.), St. John’s wort (Hypericum L.), and passionflower (Passiflora L.), which have broad and strong biological activity, well-documented history of action and use, and effectiveness in preventing and/or treating anxiety and depression. These plants are still in the sphere of biochemical and phytopharmaceutical research, the results of which are very promising. Full article

(This article belongs to the Special Issue Plant-Derived Natural Compounds as Bioactive Molecules with Beneficial Effects on Human Health)

► Show Figures

Graphical abstract

38 pages, 2368 KiB

Open AccessReview

Lignin: An Adaptable Biodegradable Polymer Used in Different Formulation Processes

by Andreea Creteanu, Claudiu N. Lungu and Mirela Lungu

Pharmaceuticals 2024, 17(10), 1406; https://doi.org/10.3390/ph17101406 - 21 Oct 2024

Cited by 2 | Viewed by 2429

Abstract

Introduction: LIG is a biopolymer found in vascular plant cell walls that is created by networks of hydroxylated and methoxylated phenylpropane that are randomly crosslinked. Plant cell walls contain LIG, a biopolymer with significant potential for usage in modern industrial and pharmaceutical applications. It is a renewable raw resource. The plant is mechanically protected by this substance, which may increase its durability. Because it has antibacterial and antioxidant qualities, LIG also shields plants from biological and chemical challenges from the outside world. Researchers have done a great deal of work to create new materials and substances based on LIG. Numerous applications, including those involving antibacterial agents, antioxidant additives, UV protection agents, hydrogel-forming molecules, nanoparticles, and solid dosage forms, have been made with this biopolymer. Methods: For this review, a consistent literature screening using the Pubmed database from 2019–2024 has been performed. Results: The results showed that there is an increase in interest in lignin as an adaptable biomolecule. The most recent studies are focused on the biosynthesis and antimicrobial properties of lignin-derived molecules. Also, the use of lignin in conjunction with nanostructures is actively explored. Conclusions: Overall, lignin is a versatile molecule with multiple uses in industry and medical science Full article

(This article belongs to the Special Issue Plant-Derived Natural Compounds as Bioactive Molecules with Beneficial Effects on Human Health)

► Show Figures

Figure 1

14 pages, 755 KiB

Open AccessReview

Icariin as a Treatment Proposal in Mammalian Reproduction

by Manuel Sánchez-Gutiérrez, Aleli Julieta Izquierdo-Vega, Eduardo Osiris Madrigal-Santillán, Claudia Velázquez-González and Jeannett Alejandra Izquierdo-Vega

Pharmaceuticals 2024, 17(9), 1104; https://doi.org/10.3390/ph17091104 - 23 Aug 2024

Cited by 1 | Viewed by 3178

Abstract

Icariin (ICA), one of the main active components of Herba Epimedii, is a natural prenylated flavonol glycoside that possesses a wide range of pharmacological effects, including antioxidant, antiosteoporotic, anti-aging, neuroprotective, immunomodulatory, antitumor, and aphrodisiac effects, and prevents numerous health disorders, such as cardiovascular diseases, osteoporosis, cancer, sexual dysfunction, menstrual disorders, neurodegenerative diseases, asthma, chronic inflammation, and diabetes. In the reproductive system, it has been observed that ICA may play a role in preserving fertility by regulating different signalling pathways, such as PI3K/AKT, which improves ovarian function, and ERα/Nrf2, which enhances testicular function and prevents ROS generation. In contrast, regulating the NF/kB signalling pathway causes anti-inflammatory effects, reducing spontaneous abortions. In this study, we review and examine the relevant literature on the therapeutic potential of ICA in reproduction, highlight the various mechanisms of action and limitations for the therapeutic applications of ICA, and summarise and highlight the existing preclinical research on its effects on male and female reproduction. Full article

(This article belongs to the Special Issue Plant-Derived Natural Compounds as Bioactive Molecules with Beneficial Effects on Human Health)

► Show Figures

Figure 1

29 pages, 1637 KiB

Open AccessReview

Potential Anti-Tumorigenic Properties of Diverse Medicinal Plants against the Majority of Common Types of Cancer

by Ghosoon Albahri, Adnan Badran, Zaher Abdel Baki, Mohamad Alame, Akram Hijazi, Anis Daou and Elias Baydoun

Pharmaceuticals 2024, 17(5), 574; https://doi.org/10.3390/ph17050574 - 30 Apr 2024

Cited by 9 | Viewed by 6960

Abstract

Globally, cancer is one of the primary causes of both morbidity and mortality. To prevent cancer from getting worse, more targeted and efficient treatment plans must be developed immediately. Recent research has demonstrated the benefits of natural products for several illnesses, and these products have played a significant role in the development of novel treatments whose bioactive components serve as both chemotherapeutic and chemo-preventive agents. Phytochemicals are naturally occurring molecules obtained from plants that have potential applications in both cancer therapy and the development of new medications. These phytochemicals function by regulating the molecular pathways connected to the onset and progression of cancer. Among the specific methods are immune system control, inducing cell cycle arrest and apoptosis, preventing proliferation, raising antioxidant status, and inactivating carcinogens. A thorough literature review was conducted using Google Scholar, PubMed, Scopus, Google Patent, Patent Scope, and US Patent to obtain the data. To provide an overview of the anticancer effects of several medicinal plants, including Annona muricata, Arctium lappa, Arum palaestinum, Cannabis sativa, Catharanthus roseus, Curcuma longa, Glycyrrhiza glabra, Hibiscus, Kalanchoe blossfeldiana, Moringa oleifera, Nerium oleander, Silybum marianum, Taraxacum officinale, Urtica dioica, Withania somnifera L., their availability, classification, active components, pharmacological activities, signaling mechanisms, and potential side effects against the most common cancer types were explored. Full article

(This article belongs to the Special Issue Plant-Derived Natural Compounds as Bioactive Molecules with Beneficial Effects on Human Health)

► Show Figures

Journal Menu

Journal Browser

Plant-Derived Natural Compounds as Bioactive Molecules with Beneficial Effects on Human Health

Share This Special Issue

Special Issue Editor

Special Issue Information

Keywords

Benefits of Publishing in a Special Issue

Published Papers (10 papers)

Research

Review

Further Information

Guidelines

MDPI Initiatives

Follow MDPI