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Biologically Active Plant-Derived Pharmaceuticals: Recent Advances and Future Prospects
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Biologically Active Plant-Derived Pharmaceuticals: Recent Advances and Future Prospects

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

Deadline for manuscript submissions: closed (30 September 2023) | Viewed by 11262

Special Issue Editor

Prof. Dr. Karim Hosni

E-Mail Website
Guest Editor
Laboratoire des Substance Naturelles, Institut National de Recherche et d'Analyse Physico-chimique (INRAP), sidi Thabet, Tunisia
Interests: phytochemistry; secondary metabolites; lipids; functional foods; nutraceuticals

Special Issue Information

Dear Colleagues,

Plant-derived bioactive compounds are gaining momentum because of their intriguing pharmacological properties, low toxicity and economic viability. They encompass a plethora of active ingredients including alkaloids, terpenes, phenolics, glycosinolates, polysaccharides, lipids and minerals, among others.  Owing to these characteristics, extensive researches have been directed toward the extraction, characterization, and application of plant-derived bioactive metabolites. These efforts have led to the discovery and development of a wide array of drugs (i.e. quinine from Peruvian bark cinchoa, cocaine from cocoa, salicin from willow tree, taxol from common yew, vinblastine from Madagascar periwinkle, sanguinarin from bloodwort, etc.). Although the considerable technical and analytical advancements in drug development and biological evaluation, research on plant-derived pharmaceuticals (pharmacons) still represent a hot topic.

This special issue will provide a timely update of recent advances and emerging technologies on the pharmacological aspects of natural plant-derived pharmaceuticals. A special attention will be paid to the following (but not limited) facets:

  • Emerging technologies on extraction, purification and structural elucidation of plant-derived pharmaceuticals.
  • Structural diversity and natural variation of plant-derived pharmaceuticals.
  • Biomedical applications (metabolic syndrome, oxidative and inflammatory diseases, neurological disorders, cancer, cardiovascular diseases, skin diseases, etc.) of plant-derived pharmaceuticals.
  • Structure-Activity Relationship (SAR) of plant-derived pharmaceuticals
  • Computational approaches in pharmacon-based drug discovery and designing
  • Innovative approaches for the development of efficient carriers and pharmacon- delivery systems
  • High-throughput approaches for pharmacon-based drug synthesis and semi-synthesis

Prof. Dr. Karim Hosni
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. 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

  • plant-derived pharmaceuticals
  • biomedical applications
  • Structure-Activity Relationship
  • innovative technologies
  • drug-delivery systems

Published Papers (5 papers)

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Research

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16 pages, 2427 KiB  
Article
Hot-Melt Extrusion as an Effective Technique for Obtaining an Amorphous System of Curcumin and Piperine with Improved Properties Essential for Their Better Biological Activities
by Kamil Wdowiak, Robert Pietrzak, Ewa Tykarska and Judyta Cielecka-Piontek
Molecules 2023, 28(9), 3848; https://doi.org/10.3390/molecules28093848 - 1 May 2023
Cited by 8 | Viewed by 1967
Abstract
Poor bioavailability hampers the use of curcumin and piperine as biologically active agents. It can be improved by enhancing the solubility as well as by using bioenhancers to inhibit metabolic transformation processes. Obtaining an amorphous system of curcumin and piperine can lead to [...] Read more.
Poor bioavailability hampers the use of curcumin and piperine as biologically active agents. It can be improved by enhancing the solubility as well as by using bioenhancers to inhibit metabolic transformation processes. Obtaining an amorphous system of curcumin and piperine can lead to the overcoming of these limitations. Hot-melt extrusion successfully produced their amorphous systems, as shown by XRPD and DSC analyses. Additionally, the presence of intermolecular interactions between the components of the systems was investigated using the FT-IR/ATR technique. The systems were able to produce a supersaturation state as well as improve the apparent solubilities of curcumin and piperine by 9496- and 161-fold, respectively. The permeabilities of curcumin in the GIT and BBB PAMPA models increased by 12578- and 3069-fold, respectively, whereas piperine’s were raised by 343- and 164-fold, respectively. Improved solubility had a positive effect on both antioxidant and anti-butyrylcholinesterase activities. The best system suppressed 96.97 ± 1.32% of DPPH radicals, and butyrylcholinesterase activity was inhibited by 98.52 ± 0.87%. In conclusion, amorphization remarkably increased the dissolution rate, apparent solubility, permeability, and biological activities of curcumin and piperine. Full article
(This article belongs to the Special Issue Biologically Active Plant-Derived Pharmaceuticals: Recent Advances and Future Prospects)
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14 pages, 9251 KiB  
Article
Phenotypic and Target-Directed Screening Yields New Acaricidal Alternatives for the Control of Ticks
by Tatiana Saporiti, Mauricio Cabrera, Josefina Bentancur, María Elisa Ferrari, Nallely Cabrera, Ruy Pérez-Montfort, Francisco J. Aguirre-Crespo, Jorge Gil, Ulises Cuore, Dimitris Matiadis, Marina Sagnou and Guzmán Alvarez
Molecules 2022, 27(24), 8863; https://doi.org/10.3390/molecules27248863 - 13 Dec 2022
Cited by 1 | Viewed by 1618
Abstract
Rhipicephalus microplus, the “common cattle tick”, is the most important ectoparasite in livestock worldwide due to the economic and health losses it produces. This tick is a vector for pathogens of several tick-borne diseases. In Latin American countries, damages reach approximately USD [...] Read more.
Rhipicephalus microplus, the “common cattle tick”, is the most important ectoparasite in livestock worldwide due to the economic and health losses it produces. This tick is a vector for pathogens of several tick-borne diseases. In Latin American countries, damages reach approximately USD 500 million annually due to tick infections, as well as tick-borne diseases. Currently, resistant populations for every chemical group of acaricides have been reported, posing a serious problem for tick control. This study aims to find new alternatives for controlling resistant ticks with compounds derived from small synthetic organic molecules and natural origins. Using BME26 embryonic cells, we performed phenotypic screening of 44 natural extracts from 10 Mexican plants used in traditional medicine, and 33 compounds selected from our chemical collection. We found 10 extracts and 13 compounds that inhibited cell growth by 50% at 50 µg/mL and 100 µM, respectively; the dose-response profile of two of them was characterized, and these compounds were assayed in vitro against different life stages of Rhipicephalus microplus. We also performed a target-directed screening of the activity of triosephosphate isomerase, using 86 compounds selected from our chemical collection. In this collection, we found the most potent and selective inhibitor of tick triosephosphate isomerase reported until now. Two other compounds had a potent acaricidal effect in vitro using adults and larvae when compared with other acaricides such as ivermectin and Amitraz. Those compounds were also selective to the ticks compared with the cytotoxicity in mammalian cells like macrophages or bovine spermatozoids. They also had a good toxicological profile, resulting in promising acaricidal compounds for tick control in cattle raising. Full article
(This article belongs to the Special Issue Biologically Active Plant-Derived Pharmaceuticals: Recent Advances and Future Prospects)
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18 pages, 2072 KiB  
Article
Essential Oil Stabilisation by Response Surface Methodology (RSM): Nanoemulsion Formulation, Physicochemical, Microbiological, and Sensory Investigations
by Mariem BenJemaa, Fatma Zohra Rahali, Hanen Falleh, Raja Beji-Serairi, Wided Megdiche-Ksouri, Ibtissem Hamrouni, Majdi Hammami, Ralph Nehme, Renato B. Pereira, Sonia Andrés, Said Bouhallab, David M. Pereira, Fabrizio Ceciliani, Latifa Abdennebi-Najar and Riadh Ksouri
Molecules 2022, 27(21), 7330; https://doi.org/10.3390/molecules27217330 - 28 Oct 2022
Cited by 3 | Viewed by 2216
Abstract
This manuscript aimed to optimise the encapsulation of Thymus capitatus essential oil into nanoemulsion. Response Surface Methodology results were best fitted into polynomial models with regression coefficient values of more than 0.95. The optimal nanoemulsion showed nanometer-sized droplets (380 nm), a polydispersity index [...] Read more.
This manuscript aimed to optimise the encapsulation of Thymus capitatus essential oil into nanoemulsion. Response Surface Methodology results were best fitted into polynomial models with regression coefficient values of more than 0.95. The optimal nanoemulsion showed nanometer-sized droplets (380 nm), a polydispersity index less than 0.5, and a suitable Zeta potential (−10.3 mV). Stability results showed that nanoemulsions stored at 4 °C were stable with the lowest d3,2, PolyDispersity Index (PDI), and pH (day 11). Significant ameliorations in the capacity to neutralise DPPH radical after the encapsulation of the antimicrobial efficacy of thyme essential oil were recorded. S. typhimurium growth inhibition generated by nanoencapsulated thyme essential oil was 17 times higher than by bulk essential oil. The sensory analysis highlighted that the encapsulation of thyme essential oil improved enriched milk’s sensory appreciation. Indeed, 20% of the total population attributed a score of 4 and 5 on the scale used for milk enriched with nanoemulsion. In comparison, only 11% attributed the same score to milk enriched with bulk essential oil. The novel nanometric delivery system presents significant interest for agroalimentary industries. Full article
(This article belongs to the Special Issue Biologically Active Plant-Derived Pharmaceuticals: Recent Advances and Future Prospects)
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Review

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16 pages, 1733 KiB  
Review
Pharmacological Effects of Astragaloside IV: A Review
by Yutong Liang, Biqiong Chen, Di Liang, Xiaoxiao Quan, Ruolan Gu, Zhiyun Meng, Hui Gan, Zhuona Wu, Yunbo Sun, Shuchen Liu and Guifang Dou
Molecules 2023, 28(16), 6118; https://doi.org/10.3390/molecules28166118 - 18 Aug 2023
Cited by 14 | Viewed by 3060
Abstract
Astragaloside IV (AS-IV) is one of the main active components extracted from the Chinese medicinal herb Astragali and serves as a marker for assessing the herb’s quality. AS-IV is a tetracyclic triterpenoid saponin in the form of lanolin ester alcohol and exhibits various [...] Read more.
Astragaloside IV (AS-IV) is one of the main active components extracted from the Chinese medicinal herb Astragali and serves as a marker for assessing the herb’s quality. AS-IV is a tetracyclic triterpenoid saponin in the form of lanolin ester alcohol and exhibits various biological activities. This review article summarizes the chemical structure of AS-IV, its pharmacological effects, mechanism of action, applications, future prospects, potential weaknesses, and other unexplored biological activities, aiming at an overall analysis. Papers were retrieved from online electronic databases, such as PubMed, Web of Science, and CNKI, and data from studies conducted over the last 10 years on the pharmacological effects of AS—IV as well as its impact were collated. This review focuses on the pharmacological action of AS-IV, such as its anti-inflammatory effect, including suppressing inflammatory factors, increasing T and B lymphocyte proliferation, and inhibiting neutrophil adhesion-associated molecules; antioxidative stress, including scavenging reactive oxygen species, cellular scorching, and regulating mitochondrial gene mutations; neuroprotective effects, antifibrotic effects, and antitumor effects. Full article
(This article belongs to the Special Issue Biologically Active Plant-Derived Pharmaceuticals: Recent Advances and Future Prospects)
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13 pages, 1101 KiB  
Review
Towards Better Sinomenine-Type Drugs to Treat Rheumatoid Arthritis: Molecular Mechanisms and Structural Modification
by Cuili Zhang, Shujie Zhang, Jingjing Liao, Zipeng Gong, Xin Chai and Haining Lyu
Molecules 2022, 27(24), 8645; https://doi.org/10.3390/molecules27248645 - 7 Dec 2022
Cited by 7 | Viewed by 1687
Abstract
Sinomenine is the main component of the vine Sinomenium acutum. It was first isolated in the early 1920s and has since attracted special interest as a potential anti-rheumatoid arthritis (RA) agent, owing to its successful application in traditional Chinese medicine for the [...] Read more.
Sinomenine is the main component of the vine Sinomenium acutum. It was first isolated in the early 1920s and has since attracted special interest as a potential anti-rheumatoid arthritis (RA) agent, owing to its successful application in traditional Chinese medicine for the treatment of neuralgia and rheumatoid diseases. In the past few decades, significant advances have broadened our understanding of the molecular mechanisms through which sinomenine treats RA, as well as the structural modifications necessary for improved pharmacological activity. In this review, we summarize up-to-date reports on the pharmacological properties of sinomenine in RA treatment, document their underlying mechanisms, and provide an overview of promising sinomenine derivatives as potential RA drug therapies. Full article
(This article belongs to the Special Issue Biologically Active Plant-Derived Pharmaceuticals: Recent Advances and Future Prospects)
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