Biological Activity and Applications of Natural Compounds

A special issue of Applied Sciences (ISSN 2076-3417). This special issue belongs to the section "Applied Biosciences and Bioengineering".

Deadline for manuscript submissions: closed (29 February 2020) | Viewed by 75840

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Guest Editor
cE3c—Centre for Ecology, Evolution and Environmental Changes, Azorean Biodiversity Group, University of Azores, Rua Mãe de Deus, 9501-801 Ponta Delgada, Portugal
Interests: bioactive natural compounds; secondary metabolites; chromatographic techniques; spectroscopic techniques; natural compounds
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Guest Editor
Departamento de Bioquímica, Microbiología, Genética y Biologia Celular, Facultad de Farmacia, Universidad de La Laguna, La Laguna, Spain
Interests: antimicrobial activity; secondary metabolites; biological evaluation; cytotoxic activity; mechanism of action

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Guest Editor
Research Institution “Chinese-Tajik Innovation Center for Natural Products”, Academy of Sciences of the Republic of Tajikistan, Rudaki Avenue 33, Dushanbe, Tajikistan
Interests: Natural products; medicinal plants; isolation active compounds; essential oils; biological activity; cytotoxicity; antioxidants; chromatography; sorption; adsorbents; drug discovery.

Special Issue Information

Dear Colleagues,

Natural compounds, also known as secondary metabolites, obtained from terrestrial or marine species, are a research focal point, both from the point of view of isolation and structural characterization of new molecules that can be valuable scaffolds, as well as from the point of view of applications of these molecules in the pharmaceutical (e.g., to treat cancer, cardiovascular and infectious), food (e.g. as additive), cosmetic (e.g. as proposal of smart-aging), and environmental industries, among others.

As Guest Editors of this Special Issue of Applied Sciences “Biological Activity and Applications of Natural Compounds”, we invite you to provide original research contributions, as well as review articles, related with pure and completely characterized secondary metabolites from plants, seaweed, and sponges. Specifically, this issue will focus on the potential of these metabolites as therapeutic agents (due to their in vitro and in vivo antitumor, antioxidant, anti-inflammatory, anti-neurodegenerative, antimicrobial, and anti-aging activities) as well as environmental health agents and nutraceuticals.

We look forward to receiving your contributions to this Special Issue.

Prof. Dr. Ana M. L Seca
Prof. Dr. Laila M. Moujir
Prof. Dr. Farukh Sharopov
Guest Editors

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Keywords

  • Natural compounds
  • bioactivities
  • industrial applications
  • drug discovery
  • nutraceutical
  • environmental health
  • anticancer
  • antioxidant
  • anti-aging
  • structure-activity relationship

Published Papers (13 papers)

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Editorial

Jump to: Research, Review

8 pages, 259 KiB  
Editorial
Natural Compounds: A Dynamic Field of Applications
by Ana M. L. Seca and Laila Moujir
Appl. Sci. 2020, 10(11), 4025; https://doi.org/10.3390/app10114025 - 10 Jun 2020
Cited by 5 | Viewed by 2838
Abstract
Nature represents an amazing source of inspiration since it produces a great diversity of natural compounds selected by evolution, which exhibit multiple biological activities and applications. A large and very active research field is dedicated to identifying biosynthesized compounds, to improve/develop new methodologies [...] Read more.
Nature represents an amazing source of inspiration since it produces a great diversity of natural compounds selected by evolution, which exhibit multiple biological activities and applications. A large and very active research field is dedicated to identifying biosynthesized compounds, to improve/develop new methodologies to produce/reuse natural compounds and to assess their potential for pharmaceutical, cosmetic and food industries, among others, and also to understand their mechanism of action. Here, the main results presented in each work are highlighted. The applications suggested are mostly related to pharmacological uses and involve mainly pure natural compounds and essential oils. These works are significant contributions and reinforce the dynamic field of natural products applications. Full article
(This article belongs to the Special Issue Biological Activity and Applications of Natural Compounds)

Research

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20 pages, 3225 KiB  
Article
A Quick, Green and Simple Ultrasound-Assisted Extraction for the Valorization of Antioxidant Phenolic Acids from Moroccan Almond Cold-Pressed Oil Residues
by Duangjai Tungmunnithum, Ahmed Elamrani, Malika Abid, Samantha Drouet, Reza Kiani, Laurine Garros, Atul Kabra, Mohamed Addi and Christophe Hano
Appl. Sci. 2020, 10(9), 3313; https://doi.org/10.3390/app10093313 - 10 May 2020
Cited by 27 | Viewed by 4233
Abstract
Almond (Prunus dulcis (Mill.) D.A. Webb) is one of the most important nut crops both in terms of area and production. Over the last few decades, an important part of the beneficial actions for health associated with their consumption was attributed to [...] Read more.
Almond (Prunus dulcis (Mill.) D.A. Webb) is one of the most important nut crops both in terms of area and production. Over the last few decades, an important part of the beneficial actions for health associated with their consumption was attributed to the phenolic compounds, mainly accumulated in almond skin. Interestingly, after cold-pressed oil extraction, most of these antioxidant phenolic compounds are retained in a skin-enriched by-product, a so-called almond cold-pressed oil residue. In Morocco, the fifth highest ranking producer in the world, this production generates an important part of this valuable byproduct. In the present study, using a multivariate Box–Behnken design, an ultrasound-assisted extraction method of phenolic compounds from Moroccan almond cold-pressed oil residue was developed and validated. Response surface methodology resulted in the optimal extraction conditions: the use of aqueous ethanol 53.0% (v/v) as a green solvent, applying an ultrasound frequency of 27.0 kHz for an extraction duration of 29.4 min. The present ultrasound-assisted extraction allowed substantial gains in terms of extraction efficiency compared to conventional heat reflux extraction. Applied to three different local Beldi genotypes growing at three different experimental sites, the optimal conditions for ultrasound-assisted extraction led to a total phenolic content of 13.86 mg/g dry weight. HPLC analysis revealed that the main phenolic compounds from this valuable byproduct were: chlorogenic acid followed by protocatechuic acid, p-hydroxybenzoic acid, and p-coumaric acid. The accumulation of these phenolic compounds appeared to be more dependent on the genetic background than on the environmental impact here represented by the three experimental culture sites. Both in vitro cell free and cellular antioxidant assays were performed, and revealed the great potential of these extracts. In particular, correlation analysis provided evidence of the prominent roles of chlorogenic acid, protocatechuic acid, and p-hydroxybenzoic acid. To summarize, the validated ultrasound-assisted extraction method presented here is a quick, green, simple and efficient for the possible valorization of antioxidant phenolic compounds from Moroccan almond cold-pressed oil residues, making it possible to generate extracts with attractive antioxidant activities for future nutraceutical and/or cosmetic applications. Full article
(This article belongs to the Special Issue Biological Activity and Applications of Natural Compounds)
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14 pages, 34636 KiB  
Article
Evaluation of the In Vitro Wound-Healing Activity and Phytochemical Characterization of Propolis and Honey
by Alexandra M. Afonso, Joana Gonçalves, Ângelo Luís, Eugenia Gallardo and Ana Paula Duarte
Appl. Sci. 2020, 10(5), 1845; https://doi.org/10.3390/app10051845 - 07 Mar 2020
Cited by 22 | Viewed by 4350
Abstract
Honey and propolis are natural substances produced by Apis mellifera that contain flavonoids, phenolic acids, and several other phytochemicals. The aim of this study was to phytochemically characterize three different types of honey and propolis, both separately and mixed, and to evaluate their [...] Read more.
Honey and propolis are natural substances produced by Apis mellifera that contain flavonoids, phenolic acids, and several other phytochemicals. The aim of this study was to phytochemically characterize three different types of honey and propolis, both separately and mixed, and to evaluate their wound-healing activity. Total phenolic compounds and flavonoids were determined using the Folin–Ciocalteu’s and aluminum chloride colorimetric methods, respectively. The antioxidant activity was evaluated by both the DPPH free radical scavenging assay and β-carotene bleaching test, and the anti-inflammatory activity was determined by a protein denaturation method. To evaluate the wound-healing activity of the samples, NHDF cells were subjected to a wound scratch assay. The obtained results showed that dark-brown honey presents a higher concentration of phenolic compounds and flavonoids, as well as higher antioxidant and anti-inflammatory activities. Propolis samples had the highest concentrations in bioactive compounds. Examining the microscopic images, it was possible to verify that the samples promote cell migration, demonstrating the wound-healing potential of honey and propolis. Full article
(This article belongs to the Special Issue Biological Activity and Applications of Natural Compounds)
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9 pages, 1662 KiB  
Article
Analysis and Identification of Active Compounds from Salviae miltiorrhizae Radix Toxic to HCT-116 Human Colon Cancer Cells
by Bohyung Kang, Sullim Lee, Chang-Seob Seo, Ki Sung Kang and You-Kyung Choi
Appl. Sci. 2020, 10(4), 1304; https://doi.org/10.3390/app10041304 - 14 Feb 2020
Cited by 4 | Viewed by 2286
Abstract
Colorectal cancer is one of the most frequently diagnosed cancers worldwide. The aim of the present study was to simultaneously analyze compounds of Salviae miltiorrhizae Radix (SMR) and determine their cytotoxic effects on HCT-116 human colorectal cancer cells. We established a simultaneous analysis [...] Read more.
Colorectal cancer is one of the most frequently diagnosed cancers worldwide. The aim of the present study was to simultaneously analyze compounds of Salviae miltiorrhizae Radix (SMR) and determine their cytotoxic effects on HCT-116 human colorectal cancer cells. We established a simultaneous analysis method of five compounds (salvianic acid A, salvianolic acid B, caffeic acid, tanshinone IIA, and rosmarinic acid) contained in SMR, and found that among the various compounds in SMR, tanshinone IIA significantly decreased cell viability in a concentration-dependent manner. Hoechst staining also showed that both SMR and tanshinone IIA increased nuclear condensation, suggesting induction of apoptosis. By Western blotting, we found that tanshinone IIA induced apoptotic cell death, significantly increased Bax, but decreased Bcl-2 in the course of apoptosis. Tanshinone IIA increased the expression of cleaved caspases-7 and -8. Tanshinone IIA was shown to be an active ingredient of SMR that may be a useful chemotherapeutic strategy for patients with colorectal cancer. Full article
(This article belongs to the Special Issue Biological Activity and Applications of Natural Compounds)
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11 pages, 2497 KiB  
Article
Antibiotic Potential and Chemical Composition of the Essential Oil of Piper caldense C. DC. (Piperaceae)
by José Weverton Almeida Bezerra, Felicidade Caroline Rodrigues, Rafael Pereira da Cruz, Luiz Everson da Silva, Wanderlei do Amaral, Ricardo Andrade Rebelo, Ieda Maria Begnini, Camila Fonseca Bezerra, Marcello Iriti, Elena Maria Varoni, Henrique Douglas Melo Coutinho and Maria Flaviana Bezerra Morais-Braga
Appl. Sci. 2020, 10(2), 631; https://doi.org/10.3390/app10020631 - 15 Jan 2020
Cited by 20 | Viewed by 2645
Abstract
Infections by multiresistant microorganisms have led to a continuous investigation of substances acting as modifiers of this resistance. By following this approach, the chemical composition of the essential oil from Piper caldense leaf and its antimicrobial potential were investigated. The antimicrobial activity was [...] Read more.
Infections by multiresistant microorganisms have led to a continuous investigation of substances acting as modifiers of this resistance. By following this approach, the chemical composition of the essential oil from Piper caldense leaf and its antimicrobial potential were investigated. The antimicrobial activity was determined by broth microdilution method providing values for minimum inhibitory concentration (MIC), IC50, and minimum fungicidal concentration (MFC). The essential oil was tested as a modulator for several antibiotics, and its effect on the morphology of Candida albicans (CA) strains was also investigated. The chemical characterization revealed an oil composed mainly of sesquiterpenes. Among them are caryophyllene oxide (13.9%), spathulenol (9.1%), δ-cadinene (7.6%) and bicyclogermacrene (6.7%) with the highest concentrations. The essential oil showed very low activity against the strains of CA with the lowest values for IC50 and MFC of 1790 μg/mL and 8192 μg/mL, respectively. The essential oil modulated the activity of fluconazole against CA URM 4387 strain, which was demonstrated by the lower IC50 obtained, 2.7 μg/mL, whereas fluconazole itself presented an IC50 of 7.76 μg/mL. No modulating effect was observed in the MFC bioassays. The effect on fungal morphology was observed for both CA INCQS 40006 and URM 4387 strains. The hyphae projection was completely inhibited at 4096 μg/mL and 2048 μg/mL, respectively. Thus, the oil has potential as an adjuvant in antimicrobial formulations. Full article
(This article belongs to the Special Issue Biological Activity and Applications of Natural Compounds)
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7 pages, 1018 KiB  
Communication
Synthesis and Evaluation of the Lifespan-Extension Properties of Oleracones D–F, Antioxidative Flavonoids from Portulaca oleracea L.
by Jeong A Yoon, Changjin Lim, Dong Seok Cha and Young Taek Han
Appl. Sci. 2019, 9(19), 4014; https://doi.org/10.3390/app9194014 - 25 Sep 2019
Cited by 6 | Viewed by 2369
Abstract
Plant-derived antioxidants have been widely used as supplementary health foods, as well as having been regarded as drug candidates for aging and aging-associated diseases. Oleracones, a novel series of flavonoids isolated from Portulaca oleracea L., possess potent antioxidative activities and are expected to [...] Read more.
Plant-derived antioxidants have been widely used as supplementary health foods, as well as having been regarded as drug candidates for aging and aging-associated diseases. Oleracones, a novel series of flavonoids isolated from Portulaca oleracea L., possess potent antioxidative activities and are expected to exhibit therapeutic potential on the aging process. The current paper describes the concise sequential synthesis of oleracones D–F. Oleracones D and F were efficiently synthesized via selective intramolecular oxa-Michael addition from oleracone E. In addition, we investigated their possible lifespan-extension properties using Caenorhabditis elegans, which is excellently suited as an experimental model to study aging. A significant longevity effect was observed when nematodes were grown with 20 μM of oleracone E. Full article
(This article belongs to the Special Issue Biological Activity and Applications of Natural Compounds)
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8 pages, 241 KiB  
Article
Essential Oil Compositions and Antifungal Activity of Sunflower (Helianthus) Species Growing in North Alabama
by Sims K. Lawson, Layla G. Sharp, Chelsea N. Powers, Robert L. McFeeters, Prabodh Satyal and William N. Setzer
Appl. Sci. 2019, 9(15), 3179; https://doi.org/10.3390/app9153179 - 05 Aug 2019
Cited by 16 | Viewed by 5092
Abstract
Helianthus species are North American members of the Asteraceae, several of which have been used as traditional medicines by Native Americans. The aerial parts of two cultivars of Helianthus annuus, “Chianti” and “Mammoth”, and wild-growing H. strumosus, were collected from locations [...] Read more.
Helianthus species are North American members of the Asteraceae, several of which have been used as traditional medicines by Native Americans. The aerial parts of two cultivars of Helianthus annuus, “Chianti” and “Mammoth”, and wild-growing H. strumosus, were collected from locations in north Alabama. The essential oils were obtained by hydrodistillation and analyzed by gas chromatography—mass spectrometry. The Helianthus essential oils were dominated by monoterpene hydrocarbons, in particular α-pinene (50.65%, 48.91%, and 58.65%, respectively), sabinene (6.81%, 17.01%, and 1.91%, respectively), β-pinene (5.79%, 3.27%, and 4.52%, respectively), and limonene (7.2%, 7.1%, and 3.8%, respectively). The essential oils were screened against three opportunistic pathogenic fungal species, Aspergillus niger, Candida albicans, and Cryptococcus neoformans. The most sensitive fungus was C. neoformans with minimum inhibitory concentration (MIC) values of 78, 156, and 78 μg/mL, respectively. Full article
(This article belongs to the Special Issue Biological Activity and Applications of Natural Compounds)
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11 pages, 2157 KiB  
Article
Structural Requirements for Antimicrobial Activity of Phenolic Nor-Triterpenes from Celastraceae Species
by Laila Moujir, Manuel R. López, Carolina P. Reyes, Ignacio A. Jiménez and Isabel L. Bazzocchi
Appl. Sci. 2019, 9(15), 2957; https://doi.org/10.3390/app9152957 - 24 Jul 2019
Cited by 6 | Viewed by 2404
Abstract
The emergence of pathogenic bacteria-resistant strains is a major public health issue. In this regard, natural product scaffolds offer a promising source of new antimicrobial drugs. In the present study, we report the antimicrobial activity against Gram-positive and Gram-negative bacteria and the yeast [...] Read more.
The emergence of pathogenic bacteria-resistant strains is a major public health issue. In this regard, natural product scaffolds offer a promising source of new antimicrobial drugs. In the present study, we report the antimicrobial activity against Gram-positive and Gram-negative bacteria and the yeast Candida albicans of five phenolic nor-triterpenes (15) isolated from Maytenus blepharodes and Maytenus canariensis in addition to four derivatives (69), three of them reported for the first time. Their stereostructures have been elucidated on the basis of spectroscopic analysis, including one-dimensional (1D) and two-dimensional (2D) NMR techniques, spectrometric methods, and comparison with data reported in the literature. To understand the structural basis for the antimicrobial activity of this type of compounds, we have performed an in-depth study of the structure–activity relationship (SAR) of a series of previously reported phenolic nor-triterpenes. The SAR analysis was based on the skeleton framework, oxidation degree, functional groups, and regiosubstitution patterns, revealing that these aspects modulate the antimicrobial activity. Full article
(This article belongs to the Special Issue Biological Activity and Applications of Natural Compounds)
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17 pages, 1704 KiB  
Article
Chalcones and Flavanones Bearing Hydroxyl and/or Methoxyl Groups: Synthesis and Biological Assessments
by Gonçalo P. Rosa, Ana M. L. Seca, Maria do Carmo Barreto, Artur M. S. Silva and Diana C. G. A. Pinto
Appl. Sci. 2019, 9(14), 2846; https://doi.org/10.3390/app9142846 - 17 Jul 2019
Cited by 27 | Viewed by 5155
Abstract
Chalcones and flavanones are isomeric structures and also classes of natural products, belonging to the flavonoid family. Moreover, their wide range of biological activities makes them key scaffolds for the synthesis of new and more efficient drugs. In this work, the synthesis of [...] Read more.
Chalcones and flavanones are isomeric structures and also classes of natural products, belonging to the flavonoid family. Moreover, their wide range of biological activities makes them key scaffolds for the synthesis of new and more efficient drugs. In this work, the synthesis of hydroxy and/or methoxychalcones was studied using less common bases, such as sodium hydride (NaH) and lithium bis(trimethylsilyl)amide (LiHMDS), in the aldol condensation. The results show that the use of NaH was more effective for the synthesis of 2′-hydroxychalcone derivatives, while LiHMDS led to the synthesis of polyhydroxylated chalcones in a one-pot process. During this study, it was also possible to establish the conditions that favor their isomerization into flavanones, allowing at the same time the synthesis of hydroxy and/or methoxyflavanones. The chalcones and flavanones obtained were evaluated to disclose their antioxidant, anticholinesterasic, antibacterial and antitumor activities. 2′,4′,4-Trihydroxychalcone was the most active compound in terms of antioxidant, anti-butyrylcholinesterase (IC50 26.55 ± 0.55 μg/mL, similar to control drug donepezil, IC50 28.94 ± 1.76 μg/mL) and antimicrobial activity. 4′,7-Dihydroxyflavanone presented dual inhibition, that is, the ability to inhibit both cholinesterases. 4′-Hydroxy-5,7-dimethoxyflavanone and 2′-hydroxy-4-methoxychalcone were the compounds with the best antitumor activity. The substitution pattern and the biological assay results allowed the establishment of some structure/activity relationships. Full article
(This article belongs to the Special Issue Biological Activity and Applications of Natural Compounds)
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17 pages, 1918 KiB  
Article
Volatile Secondary Metabolites with Potent Antidiabetic Activity from the Roots of Prangos pabularia Lindl.—Computational and Experimental Investigations
by Sodik Numonov, Farukh S. Sharopov, Sunbula Atolikhshoeva, Abduahad Safomuddin, Mahinur Bakri, William N. Setzer, Azizullo Musoev, Mizhgona Sharofova, Maidina Habasi and Haji Akber Aisa
Appl. Sci. 2019, 9(11), 2362; https://doi.org/10.3390/app9112362 - 10 Jun 2019
Cited by 7 | Viewed by 3463
Abstract
(1) Background: Almost 500 million people worldwide are suffering from diabetes. Since ancient times, humans have used medicinal plants for the treatment of diabetes. Medicinal plants continue to serve as natural sources for the discovery of antidiabetic compounds. Prangos pabularia Lindl. is a [...] Read more.
(1) Background: Almost 500 million people worldwide are suffering from diabetes. Since ancient times, humans have used medicinal plants for the treatment of diabetes. Medicinal plants continue to serve as natural sources for the discovery of antidiabetic compounds. Prangos pabularia Lindl. is a widely distributed herb with large reserves in Tajikistan. Its roots and fruits have been used in Tajik traditional medicine. To our best knowledge, there are no previously published reports concerning the antidiabetic activity and the chemical composition of the essential oil obtained from roots of P. pabularia. (2) Methods: The volatile secondary metabolites were obtained by hydrodistillation from the underground parts of P. pabularia growing wild in Tajikistan and were analyzed by gas chromatography (GC) and gas chromatography-mass spectrometry (GC-MS). Protein tyrosine phosphatase 1B (PTP-1B) inhibition assay and molecular docking analysis were carried out to evaluate the potential antidiabetic activity of the P. pabularia essential oil. (3) Results: The main constituents of the volatile oil of P. pabularia were 5-pentylcyclohexa-1,3-diene (44.6%), menthone (12.6%), 1-tridecyne (10.9%), and osthole (6.0%). PTP-1B inhibition assay of the essential oil and osthole resulted in significant inhibitory activity with an IC50 value of 0.06 ± 0.01 and 0.93 ± 0.1 μg/mL. Molecular docking analysis suggests volatile compounds such as osthole inhibit PTP-1B, and the results are also in agreement with experimental investigations. (4) Conclusions: Volatile secondary metabolites and the pure isolated compound (osthole) from the roots of P. pabularia exhibited potent antidiabetic activity, twenty-five and nearly two times more than the positive control (3-(3,5-dibromo-4-hydroxybenzoyl)-2-ethylbenzofuran-6-sulfonic acid-(4-(thiazol-2-ylsulfamyl)-phenyl)-amide)) with an IC50 value of 1.46 ± 0.4 μg/mL, respectively. Full article
(This article belongs to the Special Issue Biological Activity and Applications of Natural Compounds)
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11 pages, 2617 KiB  
Article
The Antifungal Potential of Carvacrol against Penicillium Digitatum through 1H-NMR Based Metabolomics Approach
by Chunpeng Wan, Yuting Shen, Muhammad Farrukh Nisar, Wenwen Qi, Chuying Chen and Jinyin Chen
Appl. Sci. 2019, 9(11), 2240; https://doi.org/10.3390/app9112240 - 30 May 2019
Cited by 18 | Viewed by 2953
Abstract
Carvacrol (5-Isopropyl-2-methylphenol), a volatile oil constituent, mainly exists in Labiaceae family plants. Carvacrol has long been studied for its natural antifungal potential and food preservative potential. However, its exact mode of action, especially against Penicillium digitatum (P. digitatum), remains unexplored. Herein, [...] Read more.
Carvacrol (5-Isopropyl-2-methylphenol), a volatile oil constituent, mainly exists in Labiaceae family plants. Carvacrol has long been studied for its natural antifungal potential and food preservative potential. However, its exact mode of action, especially against Penicillium digitatum (P. digitatum), remains unexplored. Herein, a 1H-NMR-based metabolomic technique was used to investigate the antifungal mechanism of carvacrol against P. digitatum. The metabolomic profiling data showed that alanine, aspartate, glutamate, and glutathione metabolism were imbalanced in the fungal hyphae. A strong positive correlation was seen between aspartate, glutamate, alanine, and glutamine, with a negative correlation among glutathione and lactate. These metabolic changes revealed that carvacrol-induced oxidative stress had disturbed the energy production and amino acid metabolism of P. digitatum. The current study will improve the understanding of the metabolic changes posed by plant-based fungicides in order to control citrus fruit green mold caused by P. digitatum. Moreover, the study will provide a certain experimental and theoretical basis for the development of novel citrus fruit preservatives. Full article
(This article belongs to the Special Issue Biological Activity and Applications of Natural Compounds)
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Review

Jump to: Editorial, Research

32 pages, 2000 KiB  
Review
Applications of Sesquiterpene Lactones: A Review of Some Potential Success Cases
by Laila Moujir, Oliver Callies, Pedro M. C. Sousa, Farukh Sharopov and Ana M. L. Seca
Appl. Sci. 2020, 10(9), 3001; https://doi.org/10.3390/app10093001 - 25 Apr 2020
Cited by 71 | Viewed by 12089
Abstract
Sesquiterpene lactones, a vast range of terpenoids isolated from Asteraceae species, exhibit a broad spectrum of biological effects and several of them are already commercially available, such as artemisinin. Here the most recent and impactful results of in vivo, preclinical and clinical studies [...] Read more.
Sesquiterpene lactones, a vast range of terpenoids isolated from Asteraceae species, exhibit a broad spectrum of biological effects and several of them are already commercially available, such as artemisinin. Here the most recent and impactful results of in vivo, preclinical and clinical studies involving a selection of ten sesquiterpene lactones (alantolactone, arglabin, costunolide, cynaropicrin, helenalin, inuviscolide, lactucin, parthenolide, thapsigargin and tomentosin) are presented and discussed, along with some of their derivatives. In the authors’ opinion, these compounds have been neglected compared to others, although they could be of great use in developing important new pharmaceutical products. The selected sesquiterpenes show promising anticancer and anti-inflammatory effects, acting on various targets. Moreover, they exhibit antifungal, anxiolytic, analgesic, and antitrypanosomal activities. Several studies discussed here clearly show the potential that some of them have in combination therapy, as sensitizing agents to facilitate and enhance the action of drugs in clinical use. The derivatives show greater pharmacological value since they have better pharmacokinetics, stability, potency, and/or selectivity. All these natural terpenoids and their derivatives exhibit properties that invite further research by the scientific community. Full article
(This article belongs to the Special Issue Biological Activity and Applications of Natural Compounds)
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23 pages, 1248 KiB  
Review
Therapeutic Potential of Rosmarinic Acid: A Comprehensive Review
by Muhammad Nadeem, Muhammad Imran, Tanweer Aslam Gondal, Ali Imran, Muhammad Shahbaz, Rai Muhammad Amir, Muhammad Wasim Sajid, Tahira Batool Qaisrani, Muhammad Atif, Ghulam Hussain, Bahare Salehi, Elise Adrian Ostrander, Miquel Martorell, Javad Sharifi-Rad, William C. Cho and Natália Martins
Appl. Sci. 2019, 9(15), 3139; https://doi.org/10.3390/app9153139 - 02 Aug 2019
Cited by 153 | Viewed by 24514
Abstract
Naturally occurring food-derived active ingredients have received huge attention for their chemopreventive and chemotherapy capabilities in several diseases. Rosmarinic acid (RA) is a caffeic acid ester and a naturally-occurring phenolic compound in a number of plants belonging to the Lamiaceae family, such as [...] Read more.
Naturally occurring food-derived active ingredients have received huge attention for their chemopreventive and chemotherapy capabilities in several diseases. Rosmarinic acid (RA) is a caffeic acid ester and a naturally-occurring phenolic compound in a number of plants belonging to the Lamiaceae family, such as Rosmarinus officinalis (rosemary) from which it was formerly isolated. RA intervenes in carcinogenesis through different ways, including in tumor cell proliferation, apoptosis, metastasis, and inflammation. On the other hand, it also exerts powerful antimicrobial, anti-inflammatory, antioxidant and even antidepressant, anti-aging effects. The present review aims to provide an overview on anticancer activities of RA and to deliberate its therapeutic potential against a wide variety of diseases. Given the current evidence, RA may be considered as part of the daily diet in the treatment of several diseases, with pre-determined doses avoiding cytotoxicity. Full article
(This article belongs to the Special Issue Biological Activity and Applications of Natural Compounds)
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