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Editorial Board Members’ Collection Series: Natural Products as Sources of New Approved Drugs

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

Deadline for manuscript submissions: closed (30 September 2024) | Viewed by 18462

Special Issue Editors

Prof. Dr. Maria Camilla Bergonzi

E-Mail Website
Guest Editor
Department of Chemistry, University of Florence, Sesto Fiorentino, 50019 Florence, Italy
Interests: natural products; drug delivery; liposomes; lipid nanocarriers; micro and nanoemulsions; nanoparticles; solubility; stability; bioefficacy; oral, brain and skin delivery; PAMPA test
Special Issues, Collections and Topics in MDPI journals
Prof. Dr. Souvik Kusari

E-Mail Website
Guest Editor
Institute of Biology and Ecology, Department of Genetics, Faculty of Science, University of Pavol Jozef Šafárik, Košice, Slovakia
Interests: plant-microbe interactions; chemical ecology; metabolomics; epigenetic engineering; natural product chemistry; natural product biotechnology; ai-guided drug discovery; endophytes; biologics
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

We are pleased to announce this Collection titled "Editorial Board Members’ Collection Series: Natural Products as Sources of New Approved Drugs”. This issue will be a collection of papers from researchers invited by the Editorial Board Members.

Natural products are fascinating molecules for drug discovery due to their exciting structural variability and their interactions with various biological targets, which represent the best approach to develop successful medications for many diseases. Due to an increasing demand for chemical diversity in pharmaceutical screening programs, the identification of novel therapeutic drugs from natural sources represents an interesting approach. Indeed, plants are extremely rich sources of bioactive molecules with a multitude of applications in biomedicine, cosmetics, and the food industry.

Contributions to this Special Issue may cover all research related to the extraction, identification, and characterization of bioactive molecules from plants, the evaluation of their biological activities that could potentially contribute to the development of new drugs, and their formulation using classical and innovative delivery systems to increase their bioavailability. 

Original research papers and review articles are welcome.

Prof. Dr. Maria Camilla Bergonzi
Dr. Souvik Kusari
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 compounds
  • bioactive molecules
  • pharmacological properties
  • in vitro and in vivo test
  • clinical investigations
  • formulations development

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Published Papers (5 papers)

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Research

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16 pages, 2820 KiB  
Article
Olea europaea L. Leaves as a Source of Anti-Glycation Compounds
by Marzia Vasarri, Maria Camilla Bergonzi, Emilija Ivanova Stojcheva, Anna Rita Bilia and Donatella Degl’Innocenti
Molecules 2024, 29(18), 4368; https://doi.org/10.3390/molecules29184368 - 14 Sep 2024
Cited by 3 | Viewed by 1436
Abstract
High concentrations of advanced glycation end products (AGEs) have been linked to diseases, including diabetic complications. The pathophysiological effects of AGEs are mainly due to oxidative stress and inflammatory processes. Among the proteins most affected by glycation are albumin, the most abundant circulating [...] Read more.
High concentrations of advanced glycation end products (AGEs) have been linked to diseases, including diabetic complications. The pathophysiological effects of AGEs are mainly due to oxidative stress and inflammatory processes. Among the proteins most affected by glycation are albumin, the most abundant circulating protein, and collagen, which has a long biological half-life and is abundant in the extracellular matrix. The potential cellular damage caused by AGEs underscores the importance of identifying and developing natural AGE inhibitors. Indeed, despite initial promise, many synthetic inhibitors have been withdrawn from clinical trials due to issues such as cytotoxicity and poor pharmacokinetics. In contrast, natural products have shown significant potential in inhibiting AGE formation. Olea europaea L. leaves, rich in bioactive compounds like oleuropein and triterpenoids, have attracted scientific interest, emphasizing the potential of olive leaf extracts in health applications. This study investigates the anti-glycation properties of two polyphenol-rich extracts (OPA40 and OPA70) and a triterpene-enriched extract (TTP70) from olive leaves. Using in vitro protein glycation methods with bovine serum albumin (BSA)–glucose and gelatin–glucose systems, this study assesses AGE formation inhibition by these extracts through native polyacrylamide gel electrophoresis (N-PAGE) and autofluorescence detection. OPA40 and OPA70 exhibited strong, dose-dependent anti-glycation effects. These effects were corroborated by electrophoresis and further supported by similar results in a gelatin–glucose system. Additionally, TTP70 showed moderate anti-glycation activity, with a synergistic effect of its components. The results support the real possibility of using olive leaf bioproducts in ameliorating diabetic complications, contributing to sustainable bio-economy practices. Full article
(This article belongs to the Special Issue Editorial Board Members’ Collection Series: Natural Products as Sources of New Approved Drugs)
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26 pages, 18661 KiB  
Article
Antimicrobial, Antidiabetic, Antioxidant, and Anticoagulant Activities of Cupressus sempervirens In Vitro and In Silico
by Aisha M. H. Al-Rajhi, Marwah M. Bakri, Husam Qanash, Hassan Y. Alzahrani, Haneen Halawani, Meaad A. Algaydi and Tarek M. Abdelghany
Molecules 2023, 28(21), 7402; https://doi.org/10.3390/molecules28217402 - 2 Nov 2023
Cited by 15 | Viewed by 2569
Abstract
In the last decade, the urgent need to explore medicinal plants or drug development has increased enormously around the world to overcome numerous health problems. In the present investigation, HPLC indicated the existence of 18 phenolic and flavonoid compounds in the Cupressus sempervirens [...] Read more.
In the last decade, the urgent need to explore medicinal plants or drug development has increased enormously around the world to overcome numerous health problems. In the present investigation, HPLC indicated the existence of 18 phenolic and flavonoid compounds in the Cupressus sempervirens extract. Hesperetin represents the greatest concentration (25,579.57 µg/mL), while other compounds, such as pyro catechol, rutin, gallic acid, chlorogenic acid, naringenin, and quercetin, were recognized in concentrations of 2922.53 µg/mL, 1313.26 µg/mL, 1107.26 µg/mL, 389.09 µg/mL, 156.53 µg/mL, and 97.56 µg/mL, respectively. The well diffusion method documented the antibacterial/antifungal activity of C. sempervirens extract against E. faecalis, E. coli, C. albicans, S. typhi, S.aureus, and M. circinelloid with 35, 33, 32, 25, 23, and 21 mm inhibition zones, respectively, more than the standard antibiotic/antifungal agent. Low values ranging from 7.80 to 15.62 µg/mL of MIC and MBC were recorded for E. faecalis, E. coli, and C. albicans. From the 1- diphenyl-2-picryl hydrazyl (DPPH) assay, promising antioxidant activity was recorded for C. sempervirens extract with IC50 of an 8.97 µg/mL. Moreover, ferric reducing antioxidant power (FRAP) and total antioxidant capacity assays (TAC) confirmed the antioxidant activity of the extract, which was expressed as the ascorbic acid equivalent (AAE) of 366.9 ± 0.2 µg/mg and 102 ± 0.2 µg/mg of extracts, respectively. α-amylase and α-glucosidase inhibition % were determined to express the antidiabetic activity of the extract in vitro, with promising IC50 value (27.01 µg/mL) for α-amylase compared to that of acarbose (50.93 µg/mL), while IC50 value of the extract for α-glucosidase was 19.21µg/mL compared to that of acarbose 4.13 µg/mL. Prothrombin time (PT) and activated partial thromboplastin time (APTT) revealed the role of C. sempervirens extract as an anticoagulant agent if compared with the activity of heparin. Binding interactions of hesperetin and gallic acid were examined via the Molecular Operating Environment (MOE) Dock software against E. faecalis (PDB ID: 3CLQ), C. albicans (PDB ID: 7RJC), α-amylase (PDB ID: 4W93), and α-glucosidase (PDB ID: 3TOP). The obtained results shed light on how molecular modeling methods might inhibit the tested compounds, which have the potential to be useful in the treatment of target proteins. Full article
(This article belongs to the Special Issue Editorial Board Members’ Collection Series: Natural Products as Sources of New Approved Drugs)
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Review

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21 pages, 6221 KiB  
Review
Principal Bioactive Properties of Oleanolic Acid, Its Derivatives, and Analogues
by Fatin Jannus, Juan Sainz and Fernando J. Reyes-Zurita
Molecules 2024, 29(14), 3291; https://doi.org/10.3390/molecules29143291 - 12 Jul 2024
Cited by 5 | Viewed by 3470
Abstract
Natural products have always played an important role in pharmacotherapy, helping to control pathophysiological processes associated with human disease. Thus, natural products such as oleanolic acid (OA), a pentacyclic triterpene that has demonstrated important activities in several disease models, are in high demand. [...] Read more.
Natural products have always played an important role in pharmacotherapy, helping to control pathophysiological processes associated with human disease. Thus, natural products such as oleanolic acid (OA), a pentacyclic triterpene that has demonstrated important activities in several disease models, are in high demand. The relevant properties of this compound have motivated re-searchers to search for new analogues and derivatives using the OA as a scaffold to which new functional groups have been added or modifications have been realized. OA and its derivatives have been shown to be effective in the treatment of inflammatory processes, triggered by chronic diseases or bacterial and viral infections. OA and its derivatives have also been found to be effective in diabetic disorders, a group of common endocrine diseases characterized by hyperglycemia that can affect several organs, including the liver and brain. This group of compounds has been reported to exhibit significant bioactivity against cancer processes in vitro and in vivo. In this review, we summarize the bioactive properties of OA and its derivatives as anti-inflammatory, anti-bacterial, antiviral, anti-diabetic, hepatoprotective, neuroprotective, and anticancer agents. Full article
(This article belongs to the Special Issue Editorial Board Members’ Collection Series: Natural Products as Sources of New Approved Drugs)
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17 pages, 738 KiB  
Review
Hirudin in the Treatment of Chronic Kidney Disease
by Sai-Ji Liu, Yi-Ling Cao and Chun Zhang
Molecules 2024, 29(5), 1029; https://doi.org/10.3390/molecules29051029 - 27 Feb 2024
Cited by 5 | Viewed by 3469
Abstract
Chronic kidney disease (CKD) is a common public health concern. The global burden of CKD is increasing due to the high morbidity and mortality associated with it, indicating the shortcomings of therapeutic drugs at present. Renal fibrosis is the common pathology of CKD, [...] Read more.
Chronic kidney disease (CKD) is a common public health concern. The global burden of CKD is increasing due to the high morbidity and mortality associated with it, indicating the shortcomings of therapeutic drugs at present. Renal fibrosis is the common pathology of CKD, which is characterized by glomerulosclerosis, renal tubular atrophy, and renal interstitial fibrosis. Natural hirudin is an active ingredient extracted from Hirudo medicinalis, which has been found to be the strongest natural specific inhibitor of thrombin. Evidence based on pharmacological data has shown that hirudin has important protective effects in CKD against diabetic nephrology, nephrotic syndrome, and renal interstitial fibrosis. The mechanisms of hirudin in treating CKD are mainly related to inhibiting the inflammatory response, preventing apoptosis of intrinsic renal cells, and inhibiting the interactions between thrombin and protease-activated receptors. In this review, we summarize the function and beneficial properties of hirudin for the treatment of CKD, and its underlying mechanisms. Full article
(This article belongs to the Special Issue Editorial Board Members’ Collection Series: Natural Products as Sources of New Approved Drugs)
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21 pages, 1427 KiB  
Review
Cannabis as a Source of Approved Drugs: A New Look at an Old Problem
by Adi Gabarin, Ludmila Yarmolinsky, Arie Budovsky, Boris Khalfin and Shimon Ben-Shabat
Molecules 2023, 28(23), 7686; https://doi.org/10.3390/molecules28237686 - 21 Nov 2023
Cited by 12 | Viewed by 6132
Abstract
Cannabis plants have been used in medicine since ancient times. They are well known for their anti-diabetic, anti-inflammatory, neuroprotective, anti-cancer, anti-oxidative, anti-microbial, anti-viral, and anti-fungal activities. A growing body of evidence indicates that targeting the endocannabinoid system and various other receptors with cannabinoid [...] Read more.
Cannabis plants have been used in medicine since ancient times. They are well known for their anti-diabetic, anti-inflammatory, neuroprotective, anti-cancer, anti-oxidative, anti-microbial, anti-viral, and anti-fungal activities. A growing body of evidence indicates that targeting the endocannabinoid system and various other receptors with cannabinoid compounds holds great promise for addressing multiple medical conditions. There are two distinct avenues in the development of cannabinoid-based drugs. The first involves creating treatments directly based on the components of the cannabis plant. The second involves a singular molecule strategy, in which specific phytocannabinoids or newly discovered cannabinoids with therapeutic promise are pinpointed and synthesized for future pharmaceutical development and validation. Although the therapeutic potential of cannabis is enormous, few cannabis-related approved drugs exist, and this avenue warrants further investigation. With this in mind, we review here the medicinal properties of cannabis, its phytochemicals, approved drugs of natural and synthetic origin, pitfalls on the way to the widespread clinical use of cannabis, and additional applications of cannabis-related products. Full article
(This article belongs to the Special Issue Editorial Board Members’ Collection Series: Natural Products as Sources of New Approved Drugs)
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