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Pharmaceuticals
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Exploring Natural Metabolites to Identify Novel Potential Therapeutic Agents
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Exploring Natural Metabolites to Identify Novel Potential Therapeutic Agents

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

Deadline for manuscript submissions: closed (20 June 2024) | Viewed by 10079

Special Issue Editor

Dr. Francesca Alessandra Ambrosio

E-Mail Website
Guest Editor
Department of Health Sciences, University “Magna Græcia” of Catanzaro, Viale Europa, 88100 Catanzaro, Italy
Interests: natural products; drug discovery; medicinal chemistry; anticancer and antiviral drug design; in silico studies

Special Issue Information

Dear Colleagues,

Historically, natural products have played a crucial role in drug discovery, especially for cancer and infectious diseases, but also in other therapeutic areas, including cardiovascular diseases, inflammation, and neurological disorders.

Today, many drugs on the market were discovered from natural sources, and in this context a key role is represented by plant secondary metabolites and microorganisms, which represent fascinating and unique sources of bioactive compounds with a wide range of activity.

These secondary metabolites are active compounds that are biosynthetically derived from primary metabolites. Many plant secondary metabolites are constitutive, and their common roles in plants are in defense and adaptation to the environment, and many of them are repellent or toxic to herbivores and pathogens, and thus protect plants from their attacks. Microbial secondary metabolites are low-molecular-mass molecules with heterogeneous structures produced during the late growth phase of microorganisms.

Based on their chemical nature, these metabolites can be classified into different categories: terpenoids and steroids, alkaloids, non-ribosomal polypeptides, fatty-acid-derived substances and polyketides, and shikimate-derived compounds. All these compounds have different bioactivities, and have always been studied for their pharmaceutical efficacy on human health, and have constantly played a pivotal role in the design and development of powerful therapeutic agents.

In summary, natural metabolites play a significant role in the design and development of novel powerful therapeutic agents because of their functions and unique structures, because of which they can be considered the cornerstone of drug discovery.

This Special Issue, “Exploring natural metabolites to identify novel potential therapeutic agents”, aims to collect papers concerning the identification, discovery, analysis and/or activity of new biologically active metabolites from microorganisms and plants; in addition, a particular focus on new achievements in the field will be appreciated. Reviews and future perspectives are also welcome.

Dr. Francesca Alessandra Ambrosio
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

  • hit identification
  • marine microorganisms
  • computational approaches
  • in vivo/in vitro assays
  • active metabolites
  • fungi
  • drug discovery
  • natural products
  • functional foods

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Published Papers (5 papers)

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Research

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13 pages, 4528 KiB  
Article
New Insights for Polyphenolic Compounds as Naturally Inspired Proteasome Inhibitors
by Emanuela Marchese, Maria Eugenia Gallo Cantafio, Francesca Alessandra Ambrosio, Roberta Torcasio, Ilenia Valentino, Francesco Trapasso, Giuseppe Viglietto, Stefano Alcaro, Giosuè Costa and Nicola Amodio
Pharmaceuticals 2023, 16(12), 1712; https://doi.org/10.3390/ph16121712 - 11 Dec 2023
Cited by 2 | Viewed by 1491
Abstract
Polyphenols, an important class of natural products, are widely distributed in plant-based foods. These compounds are endowed with several biological activities and exert protective effects in various physiopathological contexts, including cancer. We herein investigated novel potential mechanisms of action of polyphenols, focusing on [...] Read more.
Polyphenols, an important class of natural products, are widely distributed in plant-based foods. These compounds are endowed with several biological activities and exert protective effects in various physiopathological contexts, including cancer. We herein investigated novel potential mechanisms of action of polyphenols, focusing on the proteasome, which has emerged as an attractive therapeutic target in cancers such as multiple myeloma. We carried out a structure-based virtual screening study using the DrugBank database as a repository of FDA-approved polyphenolic molecules. Starting from 86 polyphenolic compounds, based on the theoretical binding affinity and the interactions established with key residues of the chymotrypsin binding site, we selected 2 promising candidates, namely Hesperidin and Diosmin. The further assessment of the biologic activity highlighted, for the first time, the capability of these two molecules to inhibit the β5-proteasome activity and to exert anti-tumor activity against proteasome inhibitor-sensitive or resistant multiple myeloma cell lines. Full article
(This article belongs to the Special Issue Exploring Natural Metabolites to Identify Novel Potential Therapeutic Agents)
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16 pages, 6034 KiB  
Article
Hyperhalophilic Diatom Extract Protects against Lead-Induced Oxidative Stress in Rats and Human HepG2 and HEK293 Cells
by Wassim Guermazi, Saoussan Boukhris, Neila Annabi-Trabelsi, Tarek Rebai, Alya Sellami-Kamoun, Waleed Aldahmash, Gabriel Ionut Plavan, Abdel Halim Harrath and Habib Ayadi
Pharmaceuticals 2023, 16(6), 875; https://doi.org/10.3390/ph16060875 - 13 Jun 2023
Cited by 2 | Viewed by 1932
Abstract
This work investigated the protective effects of microalga Halamphora sp. extract (HExt), a nutraceutical and pharmacological natural product, on human lead-intoxicated liver and kidney cells in vitro and in vivo in Wistar rats. The human hepatocellular carcinoma cell line HepG2 and the human [...] Read more.
This work investigated the protective effects of microalga Halamphora sp. extract (HExt), a nutraceutical and pharmacological natural product, on human lead-intoxicated liver and kidney cells in vitro and in vivo in Wistar rats. The human hepatocellular carcinoma cell line HepG2 and the human embryonic kidney cell line HEK293 were used for the in vitro study. The analysis of the fatty acid methyl esters in the extract was performed via GC/MS. The cells were pretreated with HExt at 100 µg mL−1, followed by treatment with different concentrations of lead acetate, ranging from 25 to 200 µM for 24 h. The cultures were incubated (5% CO, 37 °C) for 24 h. Four groups, each containing six rats, were used for the in vivo experiment. The rats were exposed to subchronic treatment with a low dose of lead acetate (5 mg kg−1 b.w. per day). Pretreating HepG2 and HEK293 cells with the extract (100 µg mL−1) significantly (p < 0.05) protected against the cytotoxicity induced by lead exposure. For the in vivo experiment, the biochemical parameters in serum—namely, the level of malondialdehyde (MDA), and the activities of superoxide dismutase (SOD), catalase (CAT), and glutathione peroxidase (GPx)—were measured in the organ homogenate supernatants. HExt was found to be rich in fatty acids, mainly palmitic and palmitoleic acids (29.464% and 42.066%, respectively). In both the in vitro and in vivo experiments, cotreatment with HExt protected the liver and kidney cell structures and significantly preserved the normal antioxidant and biochemical parameters in rats. This study discovered the possible protective effect of HExt, which could be beneficial for Pb-intoxicated cells. Full article
(This article belongs to the Special Issue Exploring Natural Metabolites to Identify Novel Potential Therapeutic Agents)
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14 pages, 4591 KiB  
Communication
Antimetastatic Activity of Apoptolidin A by Upregulation of N-Myc Downstream-Regulated Gene 1 Expression in Human Colorectal Cancer Cells
by Kay Zin Kyaw, Jiyoon Park, Seung Ho Oh, Ji Yun Lee, Eun Seo Bae, Hyen Joo Park, Dong-Chan Oh and Sang Kook Lee
Pharmaceuticals 2023, 16(4), 491; https://doi.org/10.3390/ph16040491 - 26 Mar 2023
Viewed by 1959
Abstract
Colorectal cancer (CRC) is one of the most prevalent tumors with high metastatic potential; consequently, finding new drug candidates that suppress tumor metastasis is essential. Apoptolidin A is a macrocyclic lactone produced by Amycolatopsis sp. DW02G. It exhibits significant cytotoxicity against several cancer [...] Read more.
Colorectal cancer (CRC) is one of the most prevalent tumors with high metastatic potential; consequently, finding new drug candidates that suppress tumor metastasis is essential. Apoptolidin A is a macrocyclic lactone produced by Amycolatopsis sp. DW02G. It exhibits significant cytotoxicity against several cancer cell lines, but its effects on CRC cells remain unknown. Therefore, the present study investigated the antiproliferative and antimetastatic activities of apoptolidin A and its underlying molecular mechanisms in CRC cells. Apoptolidin A effectively inhibited CRC cell growth and colony formation. The induction of G0/G1 phase cell cycle arrest was associated with the downregulation of cyclin D1 and CDK4/6 expression. Long-term exposure to apoptolidin A also induced apoptosis as confirmed by the downregulation and upregulation of Bcl-2 and Bax expression, respectively. Moreover, apoptolidin A effectively upregulated the suppressed expression of N-Myc downstream-regulated gene 1 (NDRG1), a tumor suppressor gene, in a concentration-dependent manner in CRC cells. The antimetastatic potential of apoptolidin A was also correlated with the expression of epithelial–mesenchymal transition (EMT) biomarkers, including the upregulation of E-cadherin and downregulation of N-cadherin, vimentin, snail, and MMP9 in CRC cells. These findings suggest that apoptolidin A exerts antiproliferative and antimetastatic activities by regulating the NDRG1-activated EMT pathway in CRC cells. Full article
(This article belongs to the Special Issue Exploring Natural Metabolites to Identify Novel Potential Therapeutic Agents)
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25 pages, 7076 KiB  
Article
Profiling of Secondary Metabolites of Optimized Ripe Ajwa Date Pulp (Phoenix dactylifera L.) Using Response Surface Methodology and Artificial Neural Network
by Fanar Alshammari, Md Badrul Alam, Marufa Naznin, Ahsan Javed, Sunghwan Kim and Sang-Han Lee
Pharmaceuticals 2023, 16(2), 319; https://doi.org/10.3390/ph16020319 - 20 Feb 2023
Cited by 6 | Viewed by 2767
Abstract
The date palm (Phoenix dactylifera L.) is a popular edible fruit consumed all over the world and thought to cure several chronic diseases and afflictions. The profiling of the secondary metabolites of optimized ripe Ajwa date pulp (RADP) extracts is scarce. The [...] Read more.
The date palm (Phoenix dactylifera L.) is a popular edible fruit consumed all over the world and thought to cure several chronic diseases and afflictions. The profiling of the secondary metabolites of optimized ripe Ajwa date pulp (RADP) extracts is scarce. The aim of this study was to optimize the heat extraction (HE) of ripe Ajwa date pulp using response surface methodology (RSM) and artificial neural network (ANN) modeling to increase its polyphenolic content and antioxidant activity. A central composite design was used to optimize HE to achieve the maximum polyphenolic compounds and antioxidant activity of target responses as a function of ethanol concentration, extraction time, and extraction temperature. From RSM estimates, 75.00% ethanol and 3.7 h (extraction time), and 67 °C (extraction temperature) were the optimum conditions for generating total phenolic content (4.49 ± 1.02 mgGAE/g), total flavonoid content (3.31 ± 0.65 mgCAE/g), 2,2-diphenyl-1-picrylhydrazyl (11.10 ± 0.78 % of inhibition), and cupric-reducing antioxidant capacity (1.43 µM ascorbic acid equivalent). The good performance of the ANN was validated using statistical metrics. Seventy-one secondary metabolites, including thirteen new bioactive chemicals (hebitol II, 1,2-di-(syringoyl)-hexoside, naringin dihydrochalcone, erythron-guaiacylglycerol-β-syringaresinol ether hexoside, erythron-1-(4′-O-hexoside-3,5-dimethoxyphenyl)-2-syrngaresinoxyl-propane-1,3-diol, 2-deoxy-2,3-dehydro-N-acetyl-neuraminic acid, linustatin and 1-deoxynojirimycin galactoside), were detected using high-resolution mass spectroscopy. The results revealed a significant concentration of phytoconstituents, making it an excellent contender for the pharmaceutical and food industries. Full article
(This article belongs to the Special Issue Exploring Natural Metabolites to Identify Novel Potential Therapeutic Agents)
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Review

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17 pages, 3701 KiB  
Review
Unearthing the Potential Therapeutic Effects of Oxyresveratrol Based on Intrinsic Links between Pharmacological Effects: Implications for the Gut–Liver–Brain Axis
by Lijuan Zhao, Yan Duan, Zhaoxing Li, Juan Li and Shunxiang Li
Pharmaceuticals 2024, 17(8), 1063; https://doi.org/10.3390/ph17081063 - 13 Aug 2024
Viewed by 1058
Abstract
Oxyresveratrol is a stilbene compound with a simple chemical structure and various therapeutic potentials. This study summarized and analyzed the multiple pharmacological effects and mechanisms of oxyresveratrol, identifying its prominent performance in neuroprotection, hepatoprotection, and anti-inflammatory activities in the intestines. By integrating the [...] Read more.
Oxyresveratrol is a stilbene compound with a simple chemical structure and various therapeutic potentials. This study summarized and analyzed the multiple pharmacological effects and mechanisms of oxyresveratrol, identifying its prominent performance in neuroprotection, hepatoprotection, and anti-inflammatory activities in the intestines. By integrating the pharmacological effects of oxyresveratrol with insights from the network pharmacology and molecular docking of its interactions with targets linked to gut–liver–brain axis disorders, it has been shown that oxyresveratrol may hold promise for the treatment of gut–liver–brain axis-related disorders. The synergistic effect between various mechanisms has inspired further research and the development of oxyresveratrol’s application value. Full article
(This article belongs to the Special Issue Exploring Natural Metabolites to Identify Novel Potential Therapeutic Agents)
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