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Molecules
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Pharmacological and Biological Activities of Bioactive Compounds in Natural Products
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Pharmacological and Biological Activities of Bioactive Compounds in Natural Products

A special issue of Molecules (ISSN 1420-3049). This special issue belongs to the section "Natural Products Chemistry".

Deadline for manuscript submissions: 30 April 2024 | Viewed by 7184

Special Issue Editors

Dr. Josiana A. Vaz

E-Mail Website
Guest Editor
Mountain Research Center (CIMO), Polytechnic Institute of Bragança, Santa Apolónia Campus, 5300-253 Bragança, Portugal
Interests: nutraceuticals and functional foods; development of nutraceuticals and innovative food formulations with functional properties
Dr. Paula Coutinho

E-Mail Website
Guest Editor
1. CPIRN-UDI-IPG–Research Unit for Inland Development, Center for Potential and Innovation of Natural Resources, Polytechnic of Guarda, Av. Dr. Francisco Sá Carneiro, 506300-559 Guarda, Portugal
2. Health Sciences Research Centre (CICS-UBI), Beira Interior University, Av. Infante D. Henrique, 6201-506 Covilhã, Portugal
Interests: microalgae; bioactive compounds as health promotors; bioactivity
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Natural products are an important source of bioactive compounds with remarkable pharmacological action. Global challenges such as bacterial resistance to a high number of “classic” antibiotics led to the progressive and emergent search for natural antimicrobials to be used as an alternative or as co-adjuvants in the treatment of infections. Moreover, bioactive compounds extracted from natural and diverse sources present other potential pharmacological actions namely considering the antitumoral, antiaging, healing, antioxidant, antihyperglycemic, analgesic, anticoagulant, antihypertensive and anti-inflammatory effects, reason why can be used not only in clinics, but also as active ingredients in pharmaceutical industry or as additives in food industry. Further, several compounds identified as promising are also the object of new applications, and through the application of advanced technologies like micro-and nano-encapsulation to be used in new pharmaceutical and cosmetics formulations or new biomaterials for tissue engineering.

Despite of the important amount of research that has been carried out on natural compounds, the potential of tive compounds is leading to a wide number of new applications, which we expect will be covered in this issue.

Thus, this Special Issue will cover, but not be limited to:

  • natural antitumoral compounds
  • natural anti-inflammatory compounds
  • natural antimicrobial compounds
  • natural antioxidants compounds
  • natural antihyperglycemic compounds
  • natural analgesic compounds
  • natural anticoagulant compounds
  • natural antihypertensive compounds
  • natural antiageing compounds
  • natural UV-protection
  • food applications
  • pharmacological and cosmetic applications
  • new formulation

Dr. Josiana A. Vaz
Dr. Paula Coutinho
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. Molecules is an international peer-reviewed open access semimonthly 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

  • natural bioactive compounds
  • microorganisms
  • plants
  • animals
  • natural-based products
  • pharmacological actions
  • cosmetics
  • food products
  • pharmaceual industry

Published Papers (3 papers)

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Research

17 pages, 2255 KiB  
Article
Antioxidant Properties of Maqui Berry Extract (Aristotelia chilensis (Mol.) Stuntz) and Its Potential Photoprotective Role on Human Skin Fibroblasts
by Marta Wacewicz-Muczyńska, Justyna Moskwa, Anna Puścion-Jakubik, Sylwia K. Naliwajko, Marek Niczyporuk and Katarzyna Socha
Molecules 2023, 28(23), 7802; https://doi.org/10.3390/molecules28237802 - 27 Nov 2023
Viewed by 1211
Abstract
Maqui berry (Aristotelia chilensis) is characterized by antioxidant and anti-inflammatory properties. The aim of this study was to evaluate the effect of maqui berry extracts on human skin fibroblasts (NHSFs) exposed to ultraviolet radiation (UVB). The photoprotective properties of the extracts [...] Read more.
Maqui berry (Aristotelia chilensis) is characterized by antioxidant and anti-inflammatory properties. The aim of this study was to evaluate the effect of maqui berry extracts on human skin fibroblasts (NHSFs) exposed to ultraviolet radiation (UVB). The photoprotective properties of the extracts were investigated via the determination of the total polyphenolic content (TPC) and antioxidant capacity (DPPH), and the chemical composition was assessed. The chemical purity of the extracts was studied via the evaluation of the toxic elements level. The water extract (MWE 57.75 ± 0.44 mg GAE/g) had the highest mean polyphenol content. The water (MWE) and ethanol (MEE70) extracts had the highest inhibitory activities against DPPH radical formation (283.63 ± 7.29 and 284.60 ± 4.31 mg Tx/L, respectively). The analyzed extracts were found to be safe in terms of toxic elements (arsenic, cadmium, lead). The tested extracts of maqui berry did not cause a cytotoxic effect on NHSF cells after 24, 48, and 72 h of incubation. When the NHSF cells were exposed to UVB radiation in the presence of maqui extracts, their viability was increased or maintained. The maqui berry extracts had a slightly protective effect against skin damage caused by UVB radiation. These were preliminary studies that require further research to determine which maqui compounds correspond with the photoprotective activity. Full article
(This article belongs to the Special Issue Pharmacological and Biological Activities of Bioactive Compounds in Natural Products)
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19 pages, 15683 KiB  
Article
Antidiabetic Activity, Molecular Docking, and ADMET Properties of Compounds Isolated from Bioactive Ethyl Acetate Fraction of Ficus lutea Leaf Extract
by Oyinlola O. Olaokun and Muhammad S. Zubair
Molecules 2023, 28(23), 7717; https://doi.org/10.3390/molecules28237717 - 22 Nov 2023
Cited by 2 | Viewed by 1305
Abstract
Diabetes contributes to the rising global death rate. Despite scientific advancements in understanding and managing diabetes, no single therapeutic agent has been identified to effectively treat and prevent its progression. Consequently, the exploration for new antidiabetic therapeutics continues. This study aimed to investigate [...] Read more.
Diabetes contributes to the rising global death rate. Despite scientific advancements in understanding and managing diabetes, no single therapeutic agent has been identified to effectively treat and prevent its progression. Consequently, the exploration for new antidiabetic therapeutics continues. This study aimed to investigate the antidiabetic bioactive ethyl acetate fraction of F. lutea at the molecular level to understand the molecular interactions and ligand-protein binding. To do this, the fraction underwent column chromatography fractionation to yield five compounds: lupeol, stigmasterol, α-amyrin acetate, epicatechin, and epiafzelechin. These compounds were evaluated in vitro through α-glucosidase inhibition and glucose utilization assays in C2C12 muscle and H-4-11-E liver cells using standard methods. In silico analysis was conducted using molecular docking and ADMET studies. Epicatechin exhibited the most potent α-glucosidase inhibition (IC50 = 5.72 ± 2.7 µg/mL), while epiafzelechin stimulated superior glucose utilization in C2C12 muscle cells (33.35 ± 1.8%) and H-4-11-E liver cells (46.7 ± 1.2%) at a concentration of 250 µg/mL. The binding energies of the isolated compounds for glycogen phosphorylase (1NOI) and α-amylase (1OSE) were stronger (<−8.1) than those of the positive controls. Overall, all tested compounds exhibited characteristics indicative of their potential as antidiabetic agents; however, toxicity profiling predicted epiafzelechin and epicatechin as better alternatives. The ethyl acetate fraction and its compounds, particularly epiafzelechin, showed promise as antidiabetic agents. However, further comprehensive studies are necessary to validate these findings. Full article
(This article belongs to the Special Issue Pharmacological and Biological Activities of Bioactive Compounds in Natural Products)
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27 pages, 7692 KiB  
Article
Anti-Inflammatory Effects of Minor Cannabinoids CBC, THCV, and CBN in Human Macrophages
by Esmaeel Ghasemi Gojani, Bo Wang, Dong-Ping Li, Olga Kovalchuk and Igor Kovalchuk
Molecules 2023, 28(18), 6487; https://doi.org/10.3390/molecules28186487 - 07 Sep 2023
Cited by 2 | Viewed by 3812
Abstract
Inflammation is a natural response of the body to signals of tissue damage or infection caused by pathogens. However, when it becomes imbalanced, it can lead to various disorders such as cancer, obesity, cardiovascular problems, neurological conditions, and diabetes. The endocannabinoid system, which [...] Read more.
Inflammation is a natural response of the body to signals of tissue damage or infection caused by pathogens. However, when it becomes imbalanced, it can lead to various disorders such as cancer, obesity, cardiovascular problems, neurological conditions, and diabetes. The endocannabinoid system, which is present throughout the body, plays a regulatory role in different organs and influences functions such as food intake, pain perception, stress response, glucose tolerance, inflammation, cell growth and specialization, and metabolism. Phytocannabinoids derived from Cannabis sativa can interact with this system and affect its functioning. In this study, we investigate the mechanisms underlying the anti-inflammatory effects of three minor phytocannabinoids including tetrahydrocannabivarin (THCV), cannabichromene (CBC), and cannabinol (CBN) using an in vitro system. We pre-treated THP-1 macrophages with different doses of phytocannabinoids or vehicle for one hour, followed by treating the cells with 500 ng/mL of LPS or leaving them untreated for three hours. To induce the second phase of NLRP3 inflammasome activation, LPS-treated cells were further treated with 5 mM ATP for 30 min. Our findings suggest that the mitigation of the PANX1/P2X7 axis plays a significant role in the anti-inflammatory effects of THCV and CBC on NLRP3 inflammasome activation. Additionally, we observed that CBC and THCV could also downregulate the IL-6/TYK-2/STAT-3 pathway. Furthermore, we discovered that CBN may exert its inhibitory impact on the assembly of the NLRP3 inflammasome by reducing PANX1 cleavage. Interestingly, we also found that the elevated ADAR1 transcript responded negatively to THCV and CBC in LPS-macrophages, indicating a potential involvement of ADAR1 in the anti-inflammatory effects of these two phytocannabinoids. THCV and CBN inhibit P-NF-κB, downregulating proinflammatory gene transcription. In summary, THCV, CBC, and CBN exert anti-inflammatory effects by influencing different stages of gene expression: transcription, post-transcriptional regulation, translation, and post-translational regulation. Full article
(This article belongs to the Special Issue Pharmacological and Biological Activities of Bioactive Compounds in Natural Products)
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