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Plant- , Microbial- and Marine-Derived Natural Product Research in Drug Discovery: Strengths and Perspectives

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

Deadline for manuscript submissions: 20 May 2024 | Viewed by 23493

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Dr. Noelia Duarte

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iMed.ULisboa—Research Institute for Medicines, Faculty of Pharmacy, University of Lisbon, Avenida Prof. Gama Pinto, 1649-019 Lisbon, Portugal
Interests: natural products; bioactive compounds; terpenes; phenolics; plant derived compounds; medicinal plants; natural products chemistry; mass spectrometry; multidrug resistance; medicinal chemistry
Special Issues, Collections and Topics in MDPI journals

Dr. Isabel Ribeiro

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Faculty of Pharmacy, iMed.ULisboa - Research Institute for Medicines, University of Lisbon, Avenida Prof. Gama Pinto, 1649-019 Lisbon, Portugal
Interests: biosynthesis of antimicrobial compounds (e.g., antimicrobial glycolipids) and their LC-MS characterization; functionalization of biomaterial surfaces with biological active molecules; characterization of innovative biomaterials with pharmaceutical/biomedical applications; infections related to the design of platforms to prevent the use of medical devices (e.g., catheters, implants)
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Natural products play an essential role in traditional medicine, which is the basis of primary healthcare systems, particularly in developing countries. They are also vital in drug discovery and development, despite the reduced investments from many pharmaceutical companies in research projects in this area.

With the increasing need to develop new, effective, safe, and affordable drugs, we have recently witnessed a renewed interest in natural product research from the scientific and pharmaceutical communities. In fact, the vast majority of global biodiversity (plants, marine organisms, and microorganisms) is yet to be explored. Moreover, compared to synthetic molecules, the various chemical structures of secondary metabolites, along with the presence of chirality and functionality, represents an extremely rich biogenetic resource for the discovery of novel drugs, providing leading compounds for rational drug design.

This Special Issue, entitled “Plant-, Marine-, and Microbial-Derived Natural Product Research in Drug Discovery: Strengths and Perspectives 2023”, aims to collate both original articles and comprehensive reviews related to natural product research, including natural products of microbial origin, and focuses on their vital role in drug discovery, and possible application in medicine. Topics of consideration include, but are not limited to the following: isolation and structural elucidation of bioactive compounds, in vitro or in vivo biological activities of secondary metabolites, along with their mechanism of action and/or possible applications, anti-biofilm activity, antimicrobial activity, synthetic strategies, hemi-synthesis of natural product derivatives with improved bioactivity, biological, pharmacological and technological applications, and essential oils with pharmaceutical interest.

Dr. Noelia Duarte
Dr. Isabel Ribeiro
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. 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

natural products
plant-derived compounds
marine-derived compounds
microbial-derived compounds
in vitro and in vivo biological activity
anti-biofilm activity
biosynthesis
drug discovery
medicinal and technological applications

Published Papers (10 papers)

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Research

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19 pages, 5214 KiB

Open AccessArticle

Outlining the Phytoconstituents of Greek Clover Herb Extract and Assessment of Its Effect against Foodborne Infections Caused by Salmonella typhimurium

by Jawaher Alqahtani, Walaa A. Negm, Engy Elekhnawy, Moneerah J. Alqahtani, Ehssan Moglad, Sarah Ibrahim and Suzy A. El-Sherbeni

Pharmaceuticals 2024, 17(2), 259; https://doi.org/10.3390/ph17020259 - 18 Feb 2024

Viewed by 786

Abstract

Owing to the spread of resistance between pathogenic bacteria, searching for novel compounds with antibacterial activity is essential. Here, we investigated the potential antibacterial activity of Greek clover or Trigonella foenum-graecum herb extract on Salmonella typhimurium clinical isolates. The chemical profile of the herb was initially determined using LC-ESI-MS/MS, which explored 36 different compounds. Interestingly, the fenugreek extract possessed antibacterial action in vitro with minimum inhibitory concentrations of 64 to 512 µg/mL. The potential mechanism of action was studied by elucidating the effect of the fenugreek extract on the membrane properties of S. typhimurium bacteria, including the inner and outer membrane permeability and membrane integrity. Remarkably, the fenugreek extract had detrimental effects on the membrane properties in 40–60% of the isolates. Moreover, the in vivo antibacterial action was studied using a gastrointestinal infection model with S. typhimurium bacteria. Interestingly, the fenugreek extract (200 mg/kg) improved the infection outcomes in the tested mice. This was represented by the noteworthy decrease (p < 0.05) in the bacterial count in the small intestine and caecum tissues. The survival rate of the fenugreek-extract-treated mice significantly increased compared to the S. typhimurium-infected group. Additionally, there was an improvement in the histological and immunohistochemical features of tumor necrosis factor-alpha. In addition, using an ELISA and qRT-PCR, there was an improvement in the proinflammatory and oxidative stress markers in the fenugreek-extract-treated group. Consequently, fenugreek extract should be investigated further on other food pathogens. Full article

(This article belongs to the Special Issue Plant- , Microbial- and Marine-Derived Natural Product Research in Drug Discovery: Strengths and Perspectives)

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24 pages, 4036 KiB

Open AccessArticle

Nanophytosomal Gel of Heydotis corymbosa (L.) Extract against Psoriasis: Characterisation, In Vitro and In Vivo Biological Activity

by Neelam Singh, Ayaz Mukarram Shaikh, Puneet Gupta, Béla Kovács, Mohammed F. Abuzinadah, Aftab Ahmad, Radha Goel, Swapnil Singh and Chaitanya Vinayak

Pharmaceuticals 2024, 17(2), 213; https://doi.org/10.3390/ph17020213 - 06 Feb 2024

Viewed by 993

Abstract

The current study was conducted to examine the possible advantages of Heydotis corymbosa (L.) Lam. extract nanogel as a perspective for enhanced permeation and extended skin deposition in psoriasis-like dermatitis. Optimised nanophytosomes (NPs) were embedded in a pluronic gel base to obtain nanogel and tested ex vivo (skin penetration and dermatokinetics) and in vivo. The optimised NPs had a spherical form and entrapment efficiency of 73.05 ± 1.45% with a nanosized and zeta potential of 86.11 nm and −10.40 mV, respectively. Structural evaluations confirmed encapsulation of the drug in the NPs. Topical administration of prepared nanogel to a rat model of psoriasis-like dermatitis revealed its specific in vivo anti-psoriatic efficacy in terms of drug activity compared to the control and other formulations. Nanogel had improved skin integrity and downregulation of inflammatory cytokines. These findings suggest that developed phytoconstituent-based nanogel has the potential to alleviate psoriasis-like dermatitis with better skin retention and effectiveness. Full article

(This article belongs to the Special Issue Plant- , Microbial- and Marine-Derived Natural Product Research in Drug Discovery: Strengths and Perspectives)

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14 pages, 2551 KiB

Open AccessArticle

Cytotoxic Activity of Wild Plant and Callus Extracts of Ageratina pichinchensis and 2,3-Dihydrobenzofuran Isolated from a Callus Culture

by Mariana Sánchez-Ramos, José Guillermo Encarnación-García, Silvia Marquina-Bahena, Jessica Nayelli Sánchez-Carranza, Antonio Bernabé-Antonio, Valeri Domínguez-Villegas, Emmanuel Cabañas-García and Francisco Cruz-Sosa

Pharmaceuticals 2023, 16(10), 1400; https://doi.org/10.3390/ph16101400 - 03 Oct 2023

Viewed by 1234

Abstract

Ageratina pichinchensis (Kunth) R.M. King & H. Rob. belongs to the Asteraceae family and is a plant native to Mexico to which several biological properties are attributed. In this study, the cytotoxic effect of four extracts from the wild plants and two extracts from A. pichinchensis callus culture were evaluated against carcinogenic cell lines including prostate carcinoma, cervical cancer, hepatocellular carcinoma, hepatoma human, lung cancer, and cellular keratinocytes. The extracts were obtained with ethyl acetate and methanol using both leaves and stems or the callus. Only the ethyl acetate extract of the callus culture influenced the cervical cancer cell line (HeLa) with an IC₅₀ of 94.79 ± 2.0 µg/mL. From the ethyl acetate callus extract, 2,3-dihydrobenzofuran was isolated and purified and also evaluated against cancer cells. The cytotoxic evaluation of this compound showed a significant effect against the HeLa cell line with an IC₅₀ of 23.86 ± 2.5 µg/mL. Our results contribute to the development of biotechnological alternatives and extraction processes to produce compounds with possible potential against certain types of human cancer. Full article

(This article belongs to the Special Issue Plant- , Microbial- and Marine-Derived Natural Product Research in Drug Discovery: Strengths and Perspectives)

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24 pages, 1045 KiB

Open AccessArticle

Analysis of Safety Concerns on Herbal Products with Assumed Phytoestrogenic Activity

by A. Marije Tjeerdsma, Florence P. A. M. van Hunsel, Sonja van de Koppel, Corine Ekhart, Annabella Vitalone and Herman J. Woerdenbag

Pharmaceuticals 2023, 16(8), 1137; https://doi.org/10.3390/ph16081137 - 10 Aug 2023

Viewed by 1831

Abstract

Phytoestrogens (PEs) are plant-based compounds that can interact with estrogen receptors and are mainly used to treat menopausal complaints. However, the safety of products with assumed phytoestrogenic activity is not fully understood. This study aimed to identify plant species with assumed phytoestrogenic activity, review existing literature on their use and safety, and critically evaluate adverse reaction (AR) reports of single-herb, multi-herb, and mixed-multiple products, as submitted to the Netherlands Pharmacovigilance Centre Lareb and to VigiBase of the World Health Organization (WHO). In the Lareb database, the most commonly reported plant species to cause ARs (total of 67 reports) were Actaea racemosa L. (black cohosh) (47.8%), Humulus lupulus L. (hops) (32.8%), and Glycine max (L.) Merr. (soybean) (22.4%). In the VigiBase database (total of 21,944 reports), the top three consisted of Glycine max (L.) Merr. (71.4%), Actaea racemosa L. (11.6%), and Vitex agnus-castus L. (chaste tree) (6.4%). In the scoping review (total of 73 articles), Actaea racemosa L. (30.1%), Glycine max (L.) Merr. (28.8%), and Trifolium pratense L. (13.7%) were the most frequently mentioned plant species. ARs were most frequently reported in the system organ classes “gastrointestinal disorders”, “skin and subcutaneous tissue disorders”, “reproductive system and breast disorders”, and “general disorders and administration site conditions”. Furthermore, from the scoping review, it appeared that the use of products with assumed phytoestrogenic activity was associated with postmenopausal bleeding. It was concluded that, while the potential benefits of products with assumed phytoestrogenic activity have been extensively pursued, the potential occurrence of ARs after using these products is less well understood. This study highlights the need for further investigation and careful monitoring of these products to better understand their effects and ensure the safety and well-being of individuals using them. Full article

(This article belongs to the Special Issue Plant- , Microbial- and Marine-Derived Natural Product Research in Drug Discovery: Strengths and Perspectives)

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22 pages, 1219 KiB

Open AccessArticle

Structure–Activity Relationship Studies of Indolglyoxyl-Polyamine Conjugates as Antimicrobials and Antibiotic Potentiators

by Melissa M. Cadelis, Tim Liu, Kenneth Sue, Florent Rouvier, Marie-Lise Bourguet-Kondracki, Jean Michel Brunel and Brent R. Copp

Pharmaceuticals 2023, 16(6), 823; https://doi.org/10.3390/ph16060823 - 31 May 2023

Cited by 3 | Viewed by 1164

Abstract

Antibiotic resistance is a growing global health threat, requiring urgent attention. One approach to overcome antibiotic resistance is to discover and develop new antibiotic enhancers, molecules that work with legacy antibiotics to enhance their efficacy against resistant bacteria. Our previous screening of a library of purified marine natural products and their synthetic analogues led to the discovery of an indolglyoxyl-spermine derivative that exhibited intrinsic antimicrobial properties and was also able to potentiate the action of doxycycline towards the difficult to treat, Gram-negative bacterium Pseudomonas aeruginosa. A set of analogues have now been prepared, exploring the influence of indole substitution at the 5- and 7- positions and length of the polyamine chain on biological activity. While limiting cytotoxicity and/or hemolytic activities were observed for many analogues, two 7-methyl substituted analogues (23b and 23c) were found to exhibit strong activity towards Gram-positive bacteria with no detectable cytotoxicity or hemolytic properties. Different molecular attributes were required for antibiotic enhancing properties, with one example identified, a 5-methoxy-substitiuted analogue (19a), as being a non-toxic, non-hemolytic enhancer of the action of two tetracycline antibiotics, doxycycline and minocycline, towards P. aeruginosa. These results provide further stimulation for the search for novel antimicrobials and antibiotic enhancers amongst marine natural products and related synthetic analogues. Full article

(This article belongs to the Special Issue Plant- , Microbial- and Marine-Derived Natural Product Research in Drug Discovery: Strengths and Perspectives)

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45 pages, 3569 KiB

Open AccessArticle

Comparative Study on the Effect of Phenolics and Their Antioxidant Potential of Freeze-Dried Australian Beach-Cast Seaweed Species upon Different Extraction Methodologies

by Vigasini Subbiah, Faezeh Ebrahimi, Osman T. Agar, Frank R. Dunshea, Colin J. Barrow and Hafiz A. R. Suleria

Pharmaceuticals 2023, 16(5), 773; https://doi.org/10.3390/ph16050773 - 22 May 2023

Cited by 6 | Viewed by 2622

Abstract

Brown seaweed is rich in phenolic compounds and has established health benefits. However, the phenolics present in Australian beach-cast seaweed are still unclear. This study investigated the effect of ultrasonication and conventional methodologies using four different solvents on free and bound phenolics of freeze-dried brown seaweed species obtained from the southeast Australian shoreline. The phenolic content and their antioxidant potential were determined using in vitro assays followed by identification and characterization by LC-ESI-QTOF-MS/MS and quantified by HPLC-PDA. The Cystophora sp. displayed high total phenolic content (TPC) and phlorotannin content (FDA) when extracted using 70% ethanol (ultrasonication method). Cystophora sp., also exhibited strong antioxidant potential in various assays, such as DPPH, ABTS, and FRAP in 70% acetone through ultrasonication. TAC is highly correlated to FRAP, ABTS, and RPA (p < 0.05) in both extraction methodologies. LC-ESI-QTOF-MS/MS analysis identified 94 and 104 compounds in ultrasound and conventional methodologies, respectively. HPLC-PDA quantification showed phenolic acids to be higher for samples extracted using the ultrasonication methodology. Our findings could facilitate the development of nutraceuticals, pharmaceuticals, and functional foods from beach-cast seaweed. Full article

(This article belongs to the Special Issue Plant- , Microbial- and Marine-Derived Natural Product Research in Drug Discovery: Strengths and Perspectives)

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Review

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35 pages, 1343 KiB

Open AccessReview

Bioactivity of the Genus Turnera: A Review of the Last 10 Years

by Aída Parra-Naranjo, Cecilia Delgado-Montemayor, Ricardo Salazar-Aranda and Noemí Waksman-Minsky

Pharmaceuticals 2023, 16(11), 1573; https://doi.org/10.3390/ph16111573 - 07 Nov 2023

Viewed by 1620

Abstract

Turnera is a genus of plants whose biological activity has been widely studied. The importance of this genus, particularly Turnera diffusa, as a source of treatment for various conditions is evidenced by the large number of new studies that have evaluated its biological activity. Accordingly, the objective of this review was to compile the information published in the last ten years concerning the biological activities reported for Turnera spp. The present work includes 92 publications that evaluate 29 bioactivities and toxicological and genotoxic information on five species of this genus. Among the pharmacological effects reported, the antioxidant, hepatoprotective, neuroprotective, hypoglycemic, and aphrodisiac activities seem more promising. Phytochemicals and standardized plant extracts could offer alternative therapeutic remedies for various diseases. Although several flavonoids, cyanogenic glycosides, monoterpenoids, triterpenoids, and fatty acids have been isolated for Turnera plants, future research should focus on the identification of the main active principles responsible for these pharmacological activities, as well as to perform clinical trials to support the laboratory results. Full article

(This article belongs to the Special Issue Plant- , Microbial- and Marine-Derived Natural Product Research in Drug Discovery: Strengths and Perspectives)

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30 pages, 4117 KiB

Open AccessReview

Ethnomedicinal Uses, Phytochemistry and Pharmacological Properties of Suregada Genus: A Review

by Mandisa Mangisa, Douglas Kemboi, Gerda Fouche, Rudzani Nthambeleni, Moses Kiprotich Langat, Clemence Tarirai, Martin Cheek, Odwa Gonyela and Vuyelwa Jacqueline Tembu

Pharmaceuticals 2023, 16(10), 1390; https://doi.org/10.3390/ph16101390 - 30 Sep 2023

Cited by 2 | Viewed by 926

Abstract

Plants of the Suregada Roxb. ex Rottler (formerly Gelonium Roxb. ex Willd) are utilized to treat various ailments, namely, hepatic, gum diseases, pyrexia, eczema, and venereal diseases. This review links the reported compounds to ethnomedicinal uses through pharmacological activities. The compounds possess anticancer, anti-allergic, antibacterial, anti-inflammatory, antioxidant, and anti-HIV properties. From the previous reports, 32 known species of the Suregada genus have been investigated morphologically, and nine were investigated for their phytochemistry and pharmacology. Phytochemistry, ethnomedicinal, and pharmacological uses of the other 23 Suregada species are not known and/or not reported. In this review, abietane diterpenoids are the main compounds expressed by the Suregada, accounting for 71 of the 114 reported compounds. Ten triterpenoids and sterols, one aliphatic, two lignans, five flavonoids, and twenty-one nitrogen-containing compounds have been reported from the genus. Full article

(This article belongs to the Special Issue Plant- , Microbial- and Marine-Derived Natural Product Research in Drug Discovery: Strengths and Perspectives)

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34 pages, 2681 KiB

Open AccessReview

Exploring the Benefits of Phycocyanin: From Spirulina Cultivation to Its Widespread Applications

by Raquel Fernandes, Joana Campos, Mónica Serra, Javier Fidalgo, Hugo Almeida, Ana Casas, Duarte Toubarro and Ana I. R. N. A. Barros

Pharmaceuticals 2023, 16(4), 592; https://doi.org/10.3390/ph16040592 - 14 Apr 2023

Cited by 22 | Viewed by 8690

Abstract

Large-scale production of microalgae and their bioactive compounds has steadily increased in response to global demand for natural compounds. Spirulina, in particular, has been used due to its high nutritional value, especially its high protein content. Promising biological functions have been associated with Spirulina extracts, mainly related to its high value added blue pigment, phycocyanin. Phycocyanin is used in several industries such as food, cosmetics, and pharmaceuticals, which increases its market value. Due to the worldwide interest and the need to replace synthetic compounds with natural ones, efforts have been made to optimize large-scale production processes and maintain phycocyanin stability, which is a highly unstable protein. The aim of this review is to update the scientific knowledge on phycocyanin applications and to describe the reported production, extraction, and purification methods, including the main physical and chemical parameters that may affect the purity, recovery, and stability of phycocyanin. By implementing different techniques such as complete cell disruption, extraction at temperatures below 45 °C and a pH of 5.5–6.0, purification through ammonium sulfate, and filtration and chromatography, both the purity and stability of phycocyanin have been significantly improved. Moreover, the use of saccharides, crosslinkers, or natural polymers as preservatives has contributed to the increased market value of phycocyanin. Full article

(This article belongs to the Special Issue Plant- , Microbial- and Marine-Derived Natural Product Research in Drug Discovery: Strengths and Perspectives)

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34 pages, 2828 KiB

Open AccessReview

Microorganism-Derived Molecules as Enzyme Inhibitors to Target Alzheimer’s Diseases Pathways

by Thi Hanh Nguyen, San-Lang Wang and Van Bon Nguyen

Pharmaceuticals 2023, 16(4), 580; https://doi.org/10.3390/ph16040580 - 12 Apr 2023

Cited by 6 | Viewed by 2415

Abstract

Alzheimer’s disease (AD) is the most common form of dementia. It increases the risk of other serious diseases and causes a huge impact on individuals, families, and socioeconomics. AD is a complex multifactorial disease, and current pharmacological therapies are largely based on the inhibition of enzymes involved in the pathogenesis of AD. Natural enzyme inhibitors are the potential sources for targeting AD treatment and are mainly collected from plants, marine organisms, or microorganisms. In particular, microbial sources have many advantages compared to other sources. While several reviews on AD have been reported, most of these previous reviews focused on presenting and discussing the general theory of AD or overviewing enzyme inhibitors from various sources, such as chemical synthesis, plants, and marine organisms, while only a few reviews regarding microbial sources of enzyme inhibitors against AD are available. Currently, multi-targeted drug investigation is a new trend for the potential treatment of AD. However, there is no review that has comprehensively discussed the various kinds of enzyme inhibitors from the microbial source. This review extensively addresses the above-mentioned aspect and simultaneously updates and provides a more comprehensive view of the enzyme targets involved in the pathogenesis of AD. The emerging trend of using in silico studies to discover drugs concerning AD inhibitors from microorganisms and perspectives for further experimental studies are also covered here. Full article

(This article belongs to the Special Issue Plant- , Microbial- and Marine-Derived Natural Product Research in Drug Discovery: Strengths and Perspectives)

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