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The Use of In Vitro and In Vivo Models for Research on Bioactive Compounds

A special issue of International Journal of Molecular Sciences (ISSN 1422-0067). This special issue belongs to the section "Bioactives and Nutraceuticals".

Deadline for manuscript submissions: closed (30 April 2023) | Viewed by 10257

Special Issue Editors

Dr. Raúl Domínguez-Perles

E-Mail Website
Guest Editor
Research Group on Quality, Safety, and Bioactivity of Plant Foods, Department of Food Science and Technology, Centro de Edafología y Biología Aplicada del Segura, Spanish National Research Council (CEBAS-CSIC), University Campus of Espinardo, Edif. 25, 30100 Murcia, Spain
Interests: lipidomics; plant oxylipins; bioaccessibility; bioavailability; bioactivity; structure-activity relationship (SAR); in vitro models of biological activity; inflammation; oxidative stress; immune system
Special Issues, Collections and Topics in MDPI journals
Dr. Diego A. Moreno

E-Mail Website
Guest Editor
Laboratorio de Fitoquímica y Alimentos Saludables (LabFAS), CEBAS, CSIC, Campus Universitario de Espinardo—25, E-30100 Espinardo, Murcia, Spain
Interests: phytochemicals; inflammation; obesity; health-centered agri-foods
Special Issues, Collections and Topics in MDPI journals
Dr. Antonio J. Ruiz-Alcaraz

E-Mail Website
Guest Editor
Department of Biochemistry, Molecular Biology B and Immunology, School of Medicine, University of Murcia, Regional Campus of International Excellence “Campus Mare Nostrum”, 30100 Murcia, Spain
Interests: inmune response; inflammation; immunonutrition; chronic diseases
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

To address the current challenges in the scientific validation of the functionality of bioactive compounds for health and well-being, there is a need for novel approaches and research results focused on the clarification, elucidation, and investigation of the structure–function relationships and the design of better dietary and clinical interventions to back up their potential functionality. Therefore, in this Special Issue of IJMS, we aim to assemble a topical collection of publications, communications, insightful and critical information, research results, and opinions on the state-of-the-art investigations using in vitro and in vivo models as preclinical research stages for the investigation of potentially bioactive compounds.

Moreover, we aim to provide an ideal platform for the discussion of the findings of epidemiological and clinical studies lacking this necessary preclinical information to foster future validation of functionalities. Many clinical results are lacking enough strength to validate a “functional” compound, ingredient, or food because of the gap of knowledge on the structure–function relationship due to insufficient bioactivity demonstration, and this Topical Collection aims to make results that fill this gap available in open access so that the research community worldwide may benefit.

We welcome the submission of studies considering the development, establishment, and validation of in vitro and in vivo models for the study of health-promoting bioactive compounds at the physiological, biochemical, and molecular levels in order to find the connection between the compounds in their natural matrices (extracted, purified, or formulated) and the potential effects on health and well-being through improvements in bioaccessibility, bioavailability, metabolism, and bioactivity.

Dr. Diego A. Moreno
Dr. Raúl Domínguez-Perles
Dr. Antonio J. Ruiz-Alcaraz
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. International Journal of Molecular Sciences is an international peer-reviewed open access semimonthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. There is an Article Processing Charge (APC) for publication in this open access journal. For details about the APC please see here. 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

  • cell assay
  • animal models
  • preclinical
  • bioavailability
  • metabolism
  • bioactivity
  • toxicology
  • in silico models
  • immune system
  • inflammation
  • pathology
  • structure
  • function
  • molecule
  • biomarker
  • therapeutic

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

Published Papers (3 papers)

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Research

15 pages, 1558 KiB  
Article
Resveratrol-Loaded Attalea funifera Oil Organogel Nanoparticles: A Potential Nanocarrier against A375 Human Melanoma Cells
by Douglas Dourado, Fabiana Pacheco Reis Batista, Biane Oliveira Philadelpho, Myla Lôbo de Souza, Mariana Barros de Cerqueira e Silva, Rone Aparecido de Grandis, Priscila Anjos Miranda, Nelson Barros Colauto, Daniel T. Pereira, Fabio Rocha Formiga, Eduardo Maffud Cilli, Fernando Rogério Pavan, Carolina Oliveira de Souza and Ederlan de Souza Ferreira
Int. J. Mol. Sci. 2023, 24(15), 12112; https://doi.org/10.3390/ijms241512112 - 28 Jul 2023
Cited by 3 | Viewed by 1768
Abstract
This study aimed to evaluate Attalea funifera seed oil with or without resveratrol entrapped in organogel nanoparticles in vitro against A375 human melanoma tumor cells. Organogel nanoparticles with seed oil (SON) or with resveratrol entrapped in the seed oil (RSON) formed functional organogel [...] Read more.
This study aimed to evaluate Attalea funifera seed oil with or without resveratrol entrapped in organogel nanoparticles in vitro against A375 human melanoma tumor cells. Organogel nanoparticles with seed oil (SON) or with resveratrol entrapped in the seed oil (RSON) formed functional organogel nanoparticles that showed a particle size <100 nm, polydispersity index <0.3, negative zeta potential, and maintenance of electrical conductivity. The resveratrol entrapment efficiency in RSON was 99 ± 1%. The seed oil and SON showed no cytotoxicity against human non-tumor cells or tumor cells. Resveratrol at 50 μg/mL was cytotoxic for non-tumor cells, and was cytotoxic for tumor cells at 25 μg/mL. Resveratrol entrapped in RSON showed a decrease in cytotoxicity against non-tumor cells and cytotoxic against tumor cells at 50 μg/mL. Thus, SON is a potential new platform for the delivery of resveratrol with selective cytotoxic activity in the treatment of melanoma. Full article
(This article belongs to the Special Issue The Use of In Vitro and In Vivo Models for Research on Bioactive Compounds)
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13 pages, 7260 KiB  
Article
Evidence on the Bioaccessibility of Glucosinolates and Breakdown Products of Cruciferous Sprouts by Simulated In Vitro Gastrointestinal Digestion
by Ángel Abellán, Raúl Domínguez-Perles, Cristina García-Viguera and Diego A. Moreno
Int. J. Mol. Sci. 2021, 22(20), 11046; https://doi.org/10.3390/ijms222011046 - 13 Oct 2021
Cited by 19 | Viewed by 2712
Abstract
Cruciferous vegetables are gaining importance as nutritious and sustainable foods, rich in phytochemical compounds such as glucosinolates (GSLs). However, the breakdown products of these sulfur-based compounds, mainly represented by isothiocyanates (ITC) and indoles, can contribute to human health. In the human digestive system, [...] Read more.
Cruciferous vegetables are gaining importance as nutritious and sustainable foods, rich in phytochemical compounds such as glucosinolates (GSLs). However, the breakdown products of these sulfur-based compounds, mainly represented by isothiocyanates (ITC) and indoles, can contribute to human health. In the human digestive system, the formation of these compounds continues to varying extents in the different stages of digestion, due to the contact of GSLs with different gastric fluids and enzymes under the physicochemical conditions of the gastrointestinal tract. Therefore, the aim of the present work was to uncover the effect of gastrointestinal digestion on the release of glucosinolates and their transformation into their bioactive counterparts by applying a simulated in vitro static model on a range of brassica (red radish, red cabbage, broccoli, and mustard) sprouts. In this sense, significantly higher bioaccessibility of ITC and indoles from GSLs of red cabbage sprouts was observed in comparison with broccoli, red radish, and mustard sprouts, due to the aliphatic GSLs proportion present in the different sprouts. This indicates that the bioaccessibility of GSLs from Brasicaceae sprouts is not exclusively associated with the initial content of these compounds in the plant material (almost negligible), but also with the release of GSLs and the ongoing breakdown reactions during the gastric and intestinal phases of digestion, respectively. Additionally, aliphatic GSLs provided higher bioaccessibility of their corresponding ITC in comparison to indolic and aromatic GSLs. Full article
(This article belongs to the Special Issue The Use of In Vitro and In Vivo Models for Research on Bioactive Compounds)
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9 pages, 1500 KiB  
Article
Trans-Cinnamaldehyde Exhibits Synergy with Conventional Antibiotic against Methicillin-Resistant Staphylococcus aureus
by Shu Wang, Ok-Hwa Kang and Dong-Yeul Kwon
Int. J. Mol. Sci. 2021, 22(5), 2752; https://doi.org/10.3390/ijms22052752 - 9 Mar 2021
Cited by 26 | Viewed by 3022
Abstract
Methicillin-resistant Staphylococcus aureus (MRSA) is a major nosocomial pathogen worldwide and has acquired multiple resistance to a wide range of antibiotics. Hence, there is a pressing need to explore novel strategies to overcome the increase in antimicrobial resistance. The present study aims to [...] Read more.
Methicillin-resistant Staphylococcus aureus (MRSA) is a major nosocomial pathogen worldwide and has acquired multiple resistance to a wide range of antibiotics. Hence, there is a pressing need to explore novel strategies to overcome the increase in antimicrobial resistance. The present study aims to investigate the efficacy and mechanism of plant-derived antimicrobials, trans-cinnamaldehyde (TCA) in decreasing MRSA’s resistance to eight conventional antibiotics. A checkerboard dilution test and time–kill curve assay are used to determine the synergistic effects of TCA combined with the antibiotics. The results indicated that TCA increased the antibacterial activity of the antibiotics by 2-16-fold. To study the mechanism of the synergism, we analyzed the mecA transcription gene and the penicillin-binding protein 2a level of MRSA treated with TCA by quantitative RT-PCR or Western blot assay. The gene transcription and the protein level were significantly inhibited. Additionally, it was verified that TCA can significantly inhibit the biofilm, which is highly resistant to antibiotics. The expression of the biofilm regulatory gene hld of MRSA after TCA treatment was also significantly downregulated. These findings suggest that TCA maybe is an exceptionally potent modulator of antibiotics. Full article
(This article belongs to the Special Issue The Use of In Vitro and In Vivo Models for Research on Bioactive Compounds)
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