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Pharmaceuticals
Special Issues
Plant Phytochemicals on Drug Development
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Plant Phytochemicals on Drug Development

A special issue of Pharmaceuticals (ISSN 1424-8247).

Deadline for manuscript submissions: closed (31 March 2019)

Special Issue Editors

Prof. Dr. Natália Cruz-Martins

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Guest Editor
1. Faculty of Medicine, University of Porto, 4099-002 Porto, Portugal
2. Institute for Research and Inovation in Health (i3S), University of Porto, 4099-002 Porto, Portugal
Interests: evidence-based medicine; phytochemistry; phytopharmacology; drug discovery; natural products biochemistry; bioactive molecules; functional foods; nutraceuticals; fungal and bacterial infections; resistance to antimicrobials
Special Issues, Collections and Topics in MDPI journals
Dr. Javad Sharifi-Rad

E-Mail Website
Guest Editor
Phytochemistry Research Center, Shahid Beheshti University of Medical Sciences, Tehran, Iran
Interests: natural product chemistry; natural product isolation; natural product pharmacology; natural product drug discovery; phytochemical analysis
Special Issues, Collections and Topics in MDPI journals
Dr. Bahare Salehi

E-Mail Website
Guest Editor
Student Research Committee, School of Medicine, Bam University of Medical Sciences, Bam, Iran
Interests: natural products; bioactive food components; phytotherapy; bioavailability of bioactive compounds; antioxidant capacities; natural products chemistry
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

The journals Pharmaceuticals and Plants will jointly be publishing a Special Issue on plant phytochemicals. Plant-derived products and their corresponding metabolites have garnered huge interest at the clinical, pharmacological, cosmetic and even industrial levels. Indeed, natural products are extremely rich sources of biomolecules useful for a multitude of applications. Nonetheless, and with regard to the pharmacological approach, it is of utmost importance to highlight that natural products are not drugs, but instead are a pool of phytochemicals for drug development. In the last decades, a wide variety of methods/techniques have been used to assess the renowned historical significance of natural products, also emphasizing their potential as a source of novel compounds that can be directly applied as therapeutic agents, and even as a source of inspiration for medicinal chemists generating new synthetic organic compounds. On the other hand, with regard to the high demand by consumers for healthy products, a wide variety of plant-derived foodstuffs have also been introduced into worldwide markets, contributing to shelf-life extension, the maintenance and even improvement of organoleptic and nutritional attributes, the formulation of functional products, among other biotechnological approaches. In this context, and considering that most secondary metabolites are produced for the protection of the own plant, some of the bioactive constituents have also been increasingly screened for crop protection, including biocide formulation. Thus, considering the high interest in plant-derived secondary metabolites as an emerging challenge for modern drug development, crop protection and biotechnological processes, this Special Issue will cover a wide variety of areas, aiming to contribute to the overall knowledge of medicinal plants from several aspects.

You may choose our Joint Special Issue in Plants.

Dr. Natália Martins
Dr. Javad Sharifi-Rad
Dr. Bahare Salehi
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

  • Phytopharmacology
  • Phytochemistry
  • Naturally-derived products
  • Functional products
  • Drug discovery
  • Bioavailability
  • Bioefficacy

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Published Papers (6 papers)

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Research

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8 pages, 1054 KiB  
Communication
Phenolic Plant Extracts Versus Penicillin G: In Vitro Susceptibility of Staphylococcus aureus Isolated from Bovine Mastitis
by Fernanda Gomes, Maria Elisa Rodrigues, Natália Martins, Isabel C.F.R. Ferreira and Mariana Henriques
Pharmaceuticals 2019, 12(3), 128; https://doi.org/10.3390/ph12030128 - 31 Aug 2019
Cited by 8 | Viewed by 3786
Abstract
Antibiotics are the elective drugs in bovine mastitis (BM) treatment, despite their low rates of efficiency and effectiveness and increasing risk of pathogen resistance. In this sense, it is urgent to discover new and effective antimicrobial agents to apply in BM control and [...] Read more.
Antibiotics are the elective drugs in bovine mastitis (BM) treatment, despite their low rates of efficiency and effectiveness and increasing risk of pathogen resistance. In this sense, it is urgent to discover new and effective antimicrobial agents to apply in BM control and even treatment. Plant extracts have been widely recognized as a rich source of phytochemicals with antimicrobial potential. Thus, the present work aims to compare the bioactivity of Eucalyptus globulus and Juglans regia extracts against Staphylococcus aureus bovine mastitis strains with penicillin G. At non-toxic concentrations, E. globulus exerted a bacteriostatic effect in planktonic cells and J. regia had no antimicrobial activity. Penicillin G, at minimum inhibitory concentration (MIC), demonstrated bactericidal activity, but just for S. aureus 3, 5, 6 and ATCC 25923, while the other strains seem to have acquired resistance. On the other hand, E. globulus and penicillin G in combination demonstrated synergy, being the most effective approach against S. aureus 1, 2 and 4. Thus, penicillin alone and in combination with E. globulus or J. regia seems to be promissory strategies to control bovine mastitis infections. Full article
(This article belongs to the Special Issue Plant Phytochemicals on Drug Development)
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10 pages, 286 KiB  
Article
Chemical Profile and Biological Activities of Essential Oil from Artemisia vulgaris L. Cultivated in Brazil
by Sonia Malik, Ludmilla Santos Silva de Mesquita, Carolina Rocha Silva, José Wilson Carvalho de Mesquita, Emmeline de Sá Rocha, Jayakumar Bose, Rambod Abiri, Patricia de Maria Silva Figueiredo and Livio M. Costa-Júnior
Pharmaceuticals 2019, 12(2), 49; https://doi.org/10.3390/ph12020049 - 01 Apr 2019
Cited by 39 | Viewed by 8136
Abstract
Essential oil from the leaves of Artemisia vulgaris L. (Compositae) cultivated in Brazil was investigated for its chemical composition and biological activities including antibacterial, antifungal, and anthelmintic. The constituents of essential oils isolated by hydro-distillation were examined by GC-MS and a total of [...] Read more.
Essential oil from the leaves of Artemisia vulgaris L. (Compositae) cultivated in Brazil was investigated for its chemical composition and biological activities including antibacterial, antifungal, and anthelmintic. The constituents of essential oils isolated by hydro-distillation were examined by GC-MS and a total of 18 components were identified. The essential oil was dominated by oxygenated sesquiterpenes (44.4%), sesquiterpene hydrocarbons (33.3%), and oxygenated monoterpenes (16.6%). Caryophyllene (37.45%), germacrene D (16.17%), and humulene (13.66%) were the major components. The essential oils from A. vulgaris showed bactericidal and fungicidal properties against Staphylococcus aureus and Candida albicans, respectively. Anthelmintic activity against Haemonchus contortus was absent in this essential oil. Altogether above results indicate that essential oils from A. vulgaris can be used for various medicinal purposes. Full article
(This article belongs to the Special Issue Plant Phytochemicals on Drug Development)
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11 pages, 1162 KiB  
Article
Curcumin and (−)- Epigallocatechin-3-Gallate Protect Murine MIN6 Pancreatic Beta-Cells against Iron Toxicity and Erastin-Induced Ferroptosis
by Tugba Kose, Mayra Vera-Aviles, Paul A. Sharp and Gladys O. Latunde-Dada
Pharmaceuticals 2019, 12(1), 26; https://doi.org/10.3390/ph12010026 - 06 Feb 2019
Cited by 84 | Viewed by 9019
Abstract
Ferroptosis is a form of programmed cell death that is characterized by lipid peroxidation and is inducible by iron and the accumulation of reactive oxygen species (ROS). It is triggered by erastin but inhibited by antioxidants such as α-tocopherol, β-carotene, polyphenols, and iron [...] Read more.
Ferroptosis is a form of programmed cell death that is characterized by lipid peroxidation and is inducible by iron and the accumulation of reactive oxygen species (ROS). It is triggered by erastin but inhibited by antioxidants such as α-tocopherol, β-carotene, polyphenols, and iron chelators such as deferoxamine (DFO), nitrilotriacetic acid (NTA), and ethylenediaminetetraacetic acid (EDTA). This study investigated the protective effects of two polyphenols, curcumin and (−)- epigallocatechin-3-gallate (EGCG), against iron loading and erastin-mediated ferroptosis in MIN6 cells. Cells were treated with polyphenols before exposure to iron-induced oxidative stress comprising of 20 μmol/L of 8-hydroxyquinoline (8HQ) and 50 μmol/L of ferric ammonium citrate, (FAC) (8HQ+FAC) or Fenton reaction substrate (FS) (30 μmol/L of FeSO4 and 0.5 of mmol/L H2O2) and 20 μmol/L erastin. Cell viability was determined by 3-(4,5-dimethyl-2-thiazolyl)-2,5-diphenyltetrazolium bromide (MTT) assay, iron levels were measured by inductively-coupled plasma mass spectrometry (ICP-MS), glutathione and lipid peroxidation were assayed with commercially-available kits. Curcumin and EGCG both significantly protected pancreatic cells against iron-induced oxidative damage. Moreover, both compounds also protected against erastin-induced ferroptosis in pancreatic cells. The polyphenols enhanced cell viability in erastin-treated MIN6 cells in a dose- and time-dependent manner. Furthermore, MIN6 cells exposed to erastin alone showed elevated levels of iron, glutathione (GSH) depletion, glutathione peroxidase 4 (GPX4) degradation and lipid peroxidation (p < 0.05) compared to cells that were protected by pre-treatment with curcumin or EGCG. Taken together, the data identify curcumin and EGCG as novel ferroptosis inhibitors, which might exert their protective effects by acting as iron chelators and preventing GSH depletion, GPX4 inactivation, and lipid peroxidation in MIN6 cells. The implications of the findings on the effects of iron overload and ferroptosis represent a potential therapeutic strategy against iron-related diseases. Full article
(This article belongs to the Special Issue Plant Phytochemicals on Drug Development)
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18 pages, 728 KiB  
Article
Cereus jamacaru D.C. Hydroalcoholic Extract Promotes Anti-Cytotoxic and Antitumor Activity
by Jean Carlos Vencioneck Dutra, Jean Moisés Ferreira, Paula Roberta Costalonga Pereira, Judá Ben-Hur de Oliveira, Suiany Vitorino Gervásio, Mirieli Bernardes Xavier, Mainã Mantovanelli da Mota, Anny Carolyne da Luz, Irany Rodrigues Pretti, Hildegardo Seibert França, Claudia Masrouah Jamal and Maria do Carmo Pimentel Batitucci
Pharmaceuticals 2018, 11(4), 130; https://doi.org/10.3390/ph11040130 - 23 Nov 2018
Cited by 15 | Viewed by 4808
Abstract
Cereus jamacaru D.C. (mandacaru) is a cactus used as food and in the traditional medicine. In the present study, hydroalcoholic extract of C. jamacaru was evaluated for its chemical composition, antioxidant activity, cytotoxic and anti-cytotoxic effects in human lymphocytes and sarcoma 180 cells [...] Read more.
Cereus jamacaru D.C. (mandacaru) is a cactus used as food and in the traditional medicine. In the present study, hydroalcoholic extract of C. jamacaru was evaluated for its chemical composition, antioxidant activity, cytotoxic and anti-cytotoxic effects in human lymphocytes and sarcoma 180 cells in vitro by MTT assay and antitumoral, mutagenic and cytotoxic effects on mice sarcoma-induced in vivo. Phytochemical characterization showed positive reactions for coumarin, flavanol and tyramine and total flavonoid content of 0.51 µg/mL. C. jamacaru showed antioxidant activity following DPPH (EC50 = 427.74 µg/mL), ABTS (EC50 = 270.57 µg/mL) and Fe2+ chelating ions assays (EC50 = 41.18 µg/mL). C. jamacaru induced significant decrease of sarcoma 180 viability at 24 h and 48 h of treatment, did not induce cytotoxicity in human lymphocytes and inhibits the cytotoxicity of cisplatin in vitro. Following in vivo assays, C. jamacaru promoted tumor reduction (86.07% of tumor inhibition), without inducing mutagenic or cytotoxic damage on mice blood cells. We propose that phenolic and alkaloid compounds in the extract are related to antioxidant activity, increasing its ability in metal chelating activity and promoting anti-cytotoxic activity against cisplatin, as well as these compounds may act on the cell cycle of the tumor cells in vitro and in vivo, leading to anticancer effects and tumor reduction. Full article
(This article belongs to the Special Issue Plant Phytochemicals on Drug Development)
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18 pages, 3399 KiB  
Article
Effects of Boswellia Serrata Roxb. and Curcuma longa L. in an In Vitro Intestinal Inflammation Model Using Immune Cells and Caco-2
by Paolo Governa, Maddalena Marchi, Veronica Cocetta, Bianca De Leo, Philippa T. K. Saunders, Daniela Catanzaro, Elisabetta Miraldi, Monica Montopoli and Marco Biagi
Pharmaceuticals 2018, 11(4), 126; https://doi.org/10.3390/ph11040126 - 20 Nov 2018
Cited by 32 | Viewed by 9936
Abstract
Inflammatory bowel diseases, which consist of chronic inflammatory conditions of the colon and the small intestine, are considered a global disease of our modern society. Recently, the interest toward the use of herbal therapies for the management of inflammatory bowel diseases has increased [...] Read more.
Inflammatory bowel diseases, which consist of chronic inflammatory conditions of the colon and the small intestine, are considered a global disease of our modern society. Recently, the interest toward the use of herbal therapies for the management of inflammatory bowel diseases has increased because of their effectiveness and favourable safety profile, compared to conventional drugs. Boswellia serrata Roxb. and Curcuma longa L. are amongst the most promising herbal drugs, however, their clinical use in inflammatory bowel diseases is limited and little is known on their mechanism of action. The aim of this work was to investigate the effects of two phytochemically characterized extracts of B. serrata and C. longa in an in vitro model of intestinal inflammation. Their impact on cytokine release and reactive oxygen species production, as well as the maintenance of the intestinal barrier function and on intestinal mucosa immune cells infiltration, has been evaluated. The extracts showed a good protective effect on the intestinal epithelium at 1 µg/mL, with TEER values increasing by approximately 1.5 fold, compared to LPS-stimulated cells. C. longa showed an anti-inflammatory mechanism of action, reducing IL-8, TNF-α and IL-6 production by approximately 30%, 25% and 40%, respectively, compared to the inflammatory stimuli. B. serrata action was linked to its antioxidant effect, with ROS production being reduced by 25%, compared to H2O2-stimulated Caco-2 cells. C. longa and B. serrata resulted to be promising agents for the management of inflammatory bowel diseases by modulating in vitro parameters which have been identified in the clinical conditions. Full article
(This article belongs to the Special Issue Plant Phytochemicals on Drug Development)
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Review

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18 pages, 672 KiB  
Review
The Therapeutic Potential of Naringenin: A Review of Clinical Trials
by Bahare Salehi, Patrick Valere Tsouh Fokou, Mehdi Sharifi-Rad, Paolo Zucca, Raffaele Pezzani, Natália Martins and Javad Sharifi-Rad
Pharmaceuticals 2019, 12(1), 11; https://doi.org/10.3390/ph12010011 - 10 Jan 2019
Cited by 461 | Viewed by 20771
Abstract
Naringenin is a flavonoid belonging to flavanones subclass. It is widely distributed in several Citrus fruits, bergamot, tomatoes and other fruits, being also found in its glycosides form (mainly naringin). Several biological activities have been ascribed to this phytochemical, among them antioxidant, antitumor, [...] Read more.
Naringenin is a flavonoid belonging to flavanones subclass. It is widely distributed in several Citrus fruits, bergamot, tomatoes and other fruits, being also found in its glycosides form (mainly naringin). Several biological activities have been ascribed to this phytochemical, among them antioxidant, antitumor, antiviral, antibacterial, anti-inflammatory, antiadipogenic and cardioprotective effects. Nonetheless, most of the data reported have been obtained from in vitro or in vivo studies. Although some clinical studies have also been performed, the main focus is on naringenin bioavailability and cardioprotective action. In addition, these studies were done in compromised patients (i.e., hypercholesterolemic and overweight), with a dosage ranging between 600 and 800 μM/day, whereas the effect on healthy volunteers is still debatable. In fact, naringenin ability to improve endothelial function has been well-established. Indeed, the currently available data are very promising, but further research on pharmacokinetic and pharmacodynamic aspects is encouraged to improve both available production and delivery methods and to achieve feasible naringenin-based clinical formulations. Full article
(This article belongs to the Special Issue Plant Phytochemicals on Drug Development)
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