New Advances in Natural Products in Drug Discovery

A special issue of Biomolecules (ISSN 2218-273X). This special issue belongs to the section "Natural and Bio-inspired Molecules".

Deadline for manuscript submissions: closed (31 May 2023) | Viewed by 18808

Special Issue Editors

Faculty of Pharmacy, King Abdulaziz University, P.O. Box 80260, Jeddah 21589, Saudi Arabia
Interests: marine natural products; marine invertebrates and associated microbes; cyanobacteria; structural determinations; marine macrolides and toxins; compounds with actin-disruption effects; antitumors and antibiotics; marine chemical ecology
Special Issues, Collections and Topics in MDPI journals
Suez Canal University Hospital, Suez Canal University, Ismailia 41522, Egypt
Interests: marine natural products; marine biodiscovery; invertebrates; cyanobacteria; marine microbes; structure determinations; marine alkaloids; antitumor and antibiotics
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Drugs from natural sources may fall into one of three categories of compounds: those that were isolated from biological organisms, those that are modified versions of natural products, and those that are completely synthetic, yet based upon models of natural origin. Today, natural products are responsible for about half of the approved drugs that are currently available. The percentage is even higher for treatment of infection or cancer, as natural products for those illnesses accounted for approximately 60% of the drugs either in use or awaiting FDA approval between 1989 and 1995.

Misuse and overuse of antibiotics in human and veterinary medicine and agriculture, and unsuitable waste management, resulted in a substantially increased antimicrobial-resistance-associated bacterial persistence. This is of major public concern, since most areas of modern medicine are unthinkable without access to effective treatment with antibiotics. Furthermore, an overlooked aspect of concern with the COVID-19 pandemic is the significant cases of secondary infections, associated with multidrug-resistant bacteria, which are observed in hospitalized patients and those with already compromised immune systems. Associated with this problem is the massive use of antibiotics as a COVID-19 (co)treatment worldwide, which is predicted to add to the ongoing emergence of antimicrobial resistance.

The discovery of antibiotics and antiviral agents represents the major focus of chemists and pharmacologists in the area of marine biodiscovery.

This Special Issue aims to incorporate original research articles on the discovery of secondary metabolites of natural sources with different bioactivities, such as antimicrobial, antiviral, antioxidant, etc., and recent reviews on previously reported classes of natural compounds with different activities, as well as diverse applications of these compounds in drug development, as agrochemicals, and other applications.

Keywords:

  • Natural compounds
  • Bioassay-guided purification of hits
  • Structure determination
  • Antimicrobial
  • Antifungal
  • Antibiotics
  • Antivirals
  • Antioxidants
  • Docking
  • Quorum-sensing inhibition
  • Inhibition of microbial biofilm formation
  • Pharmaceutical application
  • Network pharmacology

Prof. Dr. Diaa Youssef
Dr. Lamiaa Shaala
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. Biomolecules 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 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 products
  • bioactivity
  • in vitro screening
  • in vivo studies
  • computational approaches
  • network pharmacology
  • antitumors
  • cytotoxic

Published Papers (6 papers)

Order results
Result details
Select all
Export citation of selected articles as:

Research

Jump to: Review

15 pages, 1565 KiB  
Article
Epithelial-Immune Cell Crosstalk Determines the Activation of Immune Cells In Vitro by the Human Cathelicidin LL-37 at Low Physiological Concentrations
by Ivan V. Bogdanov, Maria A. Streltsova, Elena I. Kovalenko, Alexander M. Sapozhnikov, Pavel V. Panteleev and Tatiana V. Ovchinnikova
Biomolecules 2023, 13(9), 1316; https://doi.org/10.3390/biom13091316 - 28 Aug 2023
Cited by 1 | Viewed by 940
Abstract
The only human cathelicidin, LL-37, is a host defense antimicrobial peptide with antimicrobial activities against protozoans, fungi, Gram(+) and Gram(−) bacteria, and enveloped viruses. It has been shown in experiments in vitro that LL-37 is able to induce the production of various inflammatory [...] Read more.
The only human cathelicidin, LL-37, is a host defense antimicrobial peptide with antimicrobial activities against protozoans, fungi, Gram(+) and Gram(−) bacteria, and enveloped viruses. It has been shown in experiments in vitro that LL-37 is able to induce the production of various inflammatory and anti-inflammatory cytokines and chemokines by different human cell types. However, it remains an open question whether such cytokine induction is physiologically relevant, as LL-37 exhibited its immunomodulatory properties at concentrations that are much higher (>20 μg/mL) than those observed in non-inflamed tissues (1–5 μg/mL). In the current study, we assessed the permeability of LL-37 across the Caco-2 polarized monolayer and showed that this peptide could pass through the Caco-2 monolayer with low efficiency, which predetermined its low absorption in the gut. We showed that LL-37 at low physiological concentrations (<5 μg/mL) was not able to directly activate monocytes. However, in the presence of polarized epithelial monolayers, LL-37 is able to activate monocytes through the MAPK/ERK signaling pathway and induce the production of cytokines, as assessed by a multiplex assay at the protein level. We have demonstrated that LL-37 is able to fulfill its immunomodulatory action in vivo in non-inflamed tissues at low physiological concentrations. In the present work, we revealed a key role of epithelial-immune cell crosstalk in the implementation of immunomodulatory functions of the human cathelicidin LL-37, which might shed light on its physiological action in vivo. Full article
(This article belongs to the Special Issue New Advances in Natural Products in Drug Discovery)
Show Figures

Figure 1

13 pages, 5296 KiB  
Article
Inhibitory Potential of Synthetic Amino Acid Derivatives against Digestive Enzymes as Promising Hypoglycemic and Anti-Obesity Agents
by Franciane Campos da Silva, Bruna Celeida Silva Santos, Pedro Pôssa de Castro, Giovanni Wilson Amarante and Orlando Vieira de Sousa
Biomolecules 2023, 13(6), 953; https://doi.org/10.3390/biom13060953 - 07 Jun 2023
Viewed by 1225
Abstract
Over the last decades, the increased incidence of metabolic disorders, such as type two diabetes and obesity, has motivated researchers to investigate new enzyme inhibitors. In this study, the inhibitory effects of synthetic amino acid derivatives (PPC80, PPC82, PPC84, PPC89, and PPC101) on [...] Read more.
Over the last decades, the increased incidence of metabolic disorders, such as type two diabetes and obesity, has motivated researchers to investigate new enzyme inhibitors. In this study, the inhibitory effects of synthetic amino acid derivatives (PPC80, PPC82, PPC84, PPC89, and PPC101) on the activity of digestive enzymes were assessed using in vitro assays. The inhibitory effect was determined by the inhibition percentage and the 50% inhibitory concentration (IC50), and the mechanism of action was investigated using kinetic parameters and Lineweaver–Burk plots. PPC80, PPC82, and PPC84 inhibited pancreatic lipase (IC50 of 167–1023 µM) via competitive or mixed mechanisms. The activity of pancreatic α-amylase was suppressed by PPC80, PPC82, PPC84, PPC89, and PPC101 (IC50 of 162–519 µM), which acted as competitive or mixed inhibitors. Finally, PPC84, PPC89, and PPC101 also showed potent inhibitory effects on α-glucosidase (IC50 of 51–353 µM) as competitive inhibitors. The results suggest that these synthetic amino acid derivatives have inhibitory potential against digestive enzymes and may be used as therapeutic agents to control metabolic disorders. Full article
(This article belongs to the Special Issue New Advances in Natural Products in Drug Discovery)
Show Figures

Figure 1

Review

Jump to: Research

30 pages, 3108 KiB  
Review
Pharmacological Potential of Betulin as a Multitarget Compound
by Feyisayo O. Adepoju, Kingsley C. Duru, Erguang Li, Elena G. Kovaleva and Mikhail V. Tsurkan
Biomolecules 2023, 13(7), 1105; https://doi.org/10.3390/biom13071105 - 12 Jul 2023
Cited by 10 | Viewed by 2916
Abstract
Betulin is a natural triterpene, usually from birch bark, known for its potential wound-healing properties. Despite having a wide range of pharmacological targets, no studies have proposed betulin as a multitarget compound. Betulin has protective effects against cardiovascular and liver diseases, cancer, diabetes, [...] Read more.
Betulin is a natural triterpene, usually from birch bark, known for its potential wound-healing properties. Despite having a wide range of pharmacological targets, no studies have proposed betulin as a multitarget compound. Betulin has protective effects against cardiovascular and liver diseases, cancer, diabetes, oxidative stress, and inflammation. It reduces postprandial hyperglycemia by inhibiting α-amylase and α-glucosidase activity, combats tumor cells by inducing apoptosis and inhibiting metastatic proteins, and modulates chronic inflammation by blocking the expression of proinflammatory cytokines via modulation of the NFκB and MAPKs pathways. Given its potential to influence diverse biological networks with high target specificity, it can be hypothesized that betulin may eventually become a new lead for drug development because it can modify a variety of pharmacological targets. The summarized research revealed that the diverse beneficial effects of betulin in various diseases can be attributed, at least in part, to its multitarget anti-inflammatory activity. This review focuses on the natural sources, pharmacokinetics, pharmacological activity of betulin, and the multi-target effects of betulin on signaling pathways such as MAPK, NF-κB, and Nrf2, which are important regulators of the response to oxidative stress and inflammation in the body. Full article
(This article belongs to the Special Issue New Advances in Natural Products in Drug Discovery)
Show Figures

Figure 1

44 pages, 5181 KiB  
Review
Fungal Endophytes: Microfactories of Novel Bioactive Compounds with Therapeutic Interventions; A Comprehensive Review on the Biotechnological Developments in the Field of Fungal Endophytic Biology over the Last Decade
by Aditi Gupta, Vineet Meshram, Mahiti Gupta, Soniya Goyal, Kamal Ahmad Qureshi, Mariusz Jaremko and Kamlesh Kumar Shukla
Biomolecules 2023, 13(7), 1038; https://doi.org/10.3390/biom13071038 - 25 Jun 2023
Cited by 12 | Viewed by 4118
Abstract
The seminal discovery of paclitaxel from endophytic fungus Taxomyces andreanae was a milestone in recognizing the immense potential of endophytic fungi as prolific producers of bioactive secondary metabolites of use in medicine, agriculture, and food industries. Following the discovery of paclitaxel, the research [...] Read more.
The seminal discovery of paclitaxel from endophytic fungus Taxomyces andreanae was a milestone in recognizing the immense potential of endophytic fungi as prolific producers of bioactive secondary metabolites of use in medicine, agriculture, and food industries. Following the discovery of paclitaxel, the research community has intensified efforts to harness endophytic fungi as putative producers of lead molecules with anticancer, anti-inflammatory, antimicrobial, antioxidant, cardio-protective, and immunomodulatory properties. Endophytic fungi have been a valuable source of bioactive compounds over the last three decades. Compounds such as taxol, podophyllotoxin, huperzine, camptothecin, and resveratrol have been effectively isolated and characterized after extraction from endophytic fungi. These findings have expanded the applications of endophytic fungi in medicine and related fields. In the present review, we systematically compile and analyze several important compounds derived from endophytic fungi, encompassing the period from 2011 to 2022. Our systematic approach focuses on elucidating the origins of endophytic fungi, exploring the structural diversity and biological activities exhibited by these compounds, and giving special emphasis to the pharmacological activities and mechanism of action of certain compounds. We highlight the tremendous potential of endophytic fungi as alternate sources of bioactive metabolites, with implications for combating major global diseases. This underscores the significant role that fungi can play in the discovery and development of novel therapeutic agents that address the challenges posed by prevalent diseases worldwide. Full article
(This article belongs to the Special Issue New Advances in Natural Products in Drug Discovery)
Show Figures

Figure 1

31 pages, 2685 KiB  
Review
The Outstanding Chemodiversity of Marine-Derived Talaromyces
by Rosario Nicoletti, Rosa Bellavita and Annarita Falanga
Biomolecules 2023, 13(7), 1021; https://doi.org/10.3390/biom13071021 - 21 Jun 2023
Cited by 4 | Viewed by 1679
Abstract
Fungi in the genus Talaromyces occur in every environment in both terrestrial and marine contexts, where they have been quite frequently found in association with plants and animals. The relationships of symbiotic fungi with their hosts are often mediated by bioactive secondary metabolites, [...] Read more.
Fungi in the genus Talaromyces occur in every environment in both terrestrial and marine contexts, where they have been quite frequently found in association with plants and animals. The relationships of symbiotic fungi with their hosts are often mediated by bioactive secondary metabolites, and Talaromyces species represent a prolific source of these compounds. This review highlights the biosynthetic potential of marine-derived Talaromyces strains, using accounts from the literature published since 2016. Over 500 secondary metabolites were extracted from axenic cultures of these isolates and about 45% of them were identified as new products, representing a various assortment of chemical classes such as alkaloids, meroterpenoids, isocoumarins, anthraquinones, xanthones, phenalenones, benzofurans, azaphilones, and other polyketides. This impressive chemodiversity and the broad range of biological properties that have been disclosed in preliminary assays qualify these fungi as a valuable source of products to be exploited for manifold biotechnological applications. Full article
(This article belongs to the Special Issue New Advances in Natural Products in Drug Discovery)
Show Figures

Figure 1

34 pages, 5167 KiB  
Review
Targeting Apoptotic Pathway of Cancer Cells with Phytochemicals and Plant-Based Nanomaterials
by Atif Khurshid Wani, Nahid Akhtar, Tahir ul Gani Mir, Rattandeep Singh, Prakash Kumar Jha, Shyam Kumar Mallik, Shruti Sinha, Surya Kant Tripathi, Abha Jain, Aprajita Jha, Hari Prasad Devkota and Ajit Prakash
Biomolecules 2023, 13(2), 194; https://doi.org/10.3390/biom13020194 - 18 Jan 2023
Cited by 32 | Viewed by 6746
Abstract
Apoptosis is the elimination of functionally non-essential, neoplastic, and infected cells via the mitochondrial pathway or death receptor pathway. The process of apoptosis is highly regulated through membrane channels and apoptogenic proteins. Apoptosis maintains cellular balance within the human body through cell cycle [...] Read more.
Apoptosis is the elimination of functionally non-essential, neoplastic, and infected cells via the mitochondrial pathway or death receptor pathway. The process of apoptosis is highly regulated through membrane channels and apoptogenic proteins. Apoptosis maintains cellular balance within the human body through cell cycle progression. Loss of apoptosis control prolongs cancer cell survival and allows the accumulation of mutations that can promote angiogenesis, promote cell proliferation, disrupt differentiation, and increase invasiveness during tumor progression. The apoptotic pathway has been extensively studied as a potential drug target in cancer treatment. However, the off-target activities of drugs and negative implications have been a matter of concern over the years. Phytochemicals (PCs) have been studied for their efficacy in various cancer cell lines individually and synergistically. The development of nanoparticles (NPs) through green synthesis has added a new dimension to the advancement of plant-based nanomaterials for effective cancer treatment. This review provides a detailed insight into the fundamental molecular pathways of programmed cell death and highlights the role of PCs along with the existing drugs and plant-based NPs in treating cancer by targeting its programmed cell death (PCD) network. Full article
(This article belongs to the Special Issue New Advances in Natural Products in Drug Discovery)
Show Figures

Figure 1

Back to TopTop