molecules-logo

Journal Browser

Journal Browser

From Ethnobotany to Ecopharmacognosy: Chemical Characterization and Bioactivity Evaluation of Medicinal and Aromatic Plants

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

Deadline for manuscript submissions: closed (15 February 2021) | Viewed by 90454

Special Issue Editor


E-Mail Website1 Website2
Guest Editor
Department of Life Sciences and Biotechnology (SVeB), University of Ferrara, Ferrara, Italy
Interests: medicinal plants; extractions and chemical characterization; bioactivities; plants secondary metabolites

Special Issue Information

Dear Colleagues,

Like never before, the study of medicinal plants today represents a paradigmatic model of multidisciplinary research. First of all, ethnobotanical studies of ancient traditional uses of medicinal plants and crude drugs help to better understand their modern uses, driving research and playing a pivotal role as a source of new natural or semisynthetic drugs and lead compounds for treating different kinds of ancient and new disorders, and pathologies. Moreover, plants, as resilient organisms, interact in different ways with the environment in relation to biotic and abiotic conditions, changing their secondary metabolites profile that characterizes them for medicinal uses. For these reasons, it is of crucial importance to know the ethnobotanical cultural roots of medicinal plants, including their geographic botanical areal, the crude drugs, and the different ways to prepare them obtaining traditional preparations and, first of all, the chemical characterization of these traditional preparations to find putative bioactive compounds associated with health benefits. Starting from these premises, the modern uses of medicinal plants need the application of bio-guided oriented extraction strategies that combine efficiency and sustainability of the processes, to obtain extracts rich in those compounds responsible for the health properties, under a pharmacological and toxicological point of view. To reach this goal, distillation with its different assets, ultrasound-assisted extraction (UAE), microwave-assisted extraction (MAE), pressurized fluid extraction (PFE), and supercritical fluid extraction (SFE), enzyme-assisted extraction (EAE) could represent the technical link between ancient and modern uses, laying the foundation for future applications of medicinal plants. In this context, the chemical characterization both in its preliminary and most analytical expression, through thin layer chromatography (TLC), high-performance liquid chromatography (HPLC) coupled with different detectors and/or mass spectrometer (MS), gas chromatography coupled to mass spectrometry (GC-MS), and NMR, together with biological activity assays, may support extraction optimization under an efficiency and sustainability point of view. In fact, it is undoubtable that the modern production of health products (extracts) from medicinal plants needs the application of strategies inspired by green chemistry, linking sustainable productions (e.g., low environmental impact) with efficient extraction processes (e.g., extracts enriched of functional compounds). Finally, this multidisciplinary research approach on medicinal plants leads to the so-called ecopharmacognosy, that is, the study of natural drugs obtained from by-products of production chains of cultivated plants (e.g., agro-food chain), medicinal plants included.

Based on these research strategies, this Special Issue will focus on more recent studies dealing with extraction and chemical characterization of medicinal plants’ secondary metabolites and their in vitro or in vivo biological properties. To this end, original research articles, reviews, and short communications are welcome.

Prof. Gianni Sacchetti
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

  • Ethnobotany
  • Extraction strategies
  • Distillation
  • Ultrasound-assisted extraction
  • Microwave-assisted extraction
  • Pressurized fluid extraction
  • Supercritical fluid extraction
  • Enzyme-assisted extraction
  • Chromatography
  • Spectroscopy
  • Bioactivity assays (bio-autographic, in vitro, in vivo)
  • Ecopharmacognosy

Published Papers (18 papers)

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

Research

Jump to: Review

21 pages, 10223 KiB  
Article
β-Sitosterol Circumvents Obesity Induced Inflammation and Insulin Resistance by down-Regulating IKKβ/NF-κB and JNK Signaling Pathway in Adipocytes of Type 2 Diabetic Rats
by Selvaraj Jayaraman, Nalini Devarajan, Ponnulakshmi Rajagopal, Shyamaladevi Babu, Senthil Kumar Ganesan, Vishnu Priya Veeraraghavan, Chella Perumal Palanisamy, Bo Cui, Vijayalakshmi Periyasamy and Kirubhanand Chandrasekar
Molecules 2021, 26(7), 2101; https://doi.org/10.3390/molecules26072101 - 6 Apr 2021
Cited by 50 | Viewed by 5876
Abstract
β-sitosterol (SIT), the most abundant bioactive component of vegetable oil and other plants, is a highly potent antidiabetic drug. Our previous studies show that SIT controls hyperglycemia and insulin resistance by activating insulin receptor and glucose transporter 4 (GLUT-4) in the adipocytes of [...] Read more.
β-sitosterol (SIT), the most abundant bioactive component of vegetable oil and other plants, is a highly potent antidiabetic drug. Our previous studies show that SIT controls hyperglycemia and insulin resistance by activating insulin receptor and glucose transporter 4 (GLUT-4) in the adipocytes of obesity induced type 2 diabetic rats. The current research was undertaken to investigate if SIT could also exert its antidiabetic effects by circumventing adipocyte induced inflammation, a key driving factor for insulin resistance in obese individuals. Effective dose of SIT (20 mg/kg b.wt) was administered orally for 30 days to high fat diet and sucrose induced type-2 diabetic rats. Metformin, the conventionally used antidiabetic drug was used as a positive control. Interestingly, SIT treatment restores the elevated serum levels of proinflammatory cytokines including leptin, resistin, tumor necrosis factor-α (TNF-α) and interleukin-6 (IL-6) to normalcy and increases anti-inflammatory adipocytokines including adiponectin in type 2 diabetic rats. Furthermore, SIT decreases sterol regulatory element binding protein-1c (SREBP-1c) and enhances Peroxisome Proliferator–activated receptor-γ (PPAR-γ) gene expression in adipocytes of diabetic rats. The gene and protein expression of c-Jun-N-terminal kinase-1 (JNK1), inhibitor of nuclear factor kappa-B kinase subunit beta (IKKβ) and nuclear factor kappa B (NF-κB) were also significantly attenuated in SIT treated groups. More importantly, SIT acts very effectively as metformin to circumvent inflammation and insulin resistance in diabetic rats. Our results clearly show that SIT inhibits obesity induced insulin resistance by ameliorating the inflammatory events in the adipose tissue through the downregulation of IKKβ/NF-κB and c-Jun-N-terminal kinase (JNK) signaling pathway. Full article
Show Figures

Figure 1

11 pages, 538 KiB  
Article
Phytochemical Characterization, In Vitro Anti-Inflammatory, Anti-Diabetic, and Cytotoxic Activities of the Edible Aromatic Plant; Pulicaria jaubertii
by Hamdoon A. Mohammed, Mohammed F. Abdelwahab, El-Sayed M. El-Ghaly and Ehab A. Ragab
Molecules 2021, 26(1), 203; https://doi.org/10.3390/molecules26010203 - 3 Jan 2021
Cited by 10 | Viewed by 2865
Abstract
Pulicaria jaubertii is a medicinal herb that alleviates inflammations and fever. Chromatographic separation, phytochemical characterization, and in vitro biological activities of the plant n-hexane extract were conducted for the first time in this study. Six compounds were isolated for the first time [...] Read more.
Pulicaria jaubertii is a medicinal herb that alleviates inflammations and fever. Chromatographic separation, phytochemical characterization, and in vitro biological activities of the plant n-hexane extract were conducted for the first time in this study. Six compounds were isolated for the first time from the n-hexane fraction of Pulicaria jaubertii aerial parts and were identified on the bases of NMR and MS analyses as pseudo-taraxaterol (1), pseudo-taraxasterol acetate (2), 3β-acetoxytaraxaster-20-en-30-aldehyde (3), calenduladiol-3-O-palmitate (4), stigmasterol (5), and α-tocospiro B (6). Compound (6) was a rare tocopherol-related compound and was isolated for the first time from family Asteraceae, while compound (3) was isolated for the first time from genus Pulicaria. The total alcoholic extract and n-hexane fraction were tested for their anti-inflammatory, antidiabetic, and cytotoxic activities. The n-hexane fraction has dose dependent red blood cells (RBCs) membrane stabilization and inhibition of histamine release activities with IC50: 60.8 and 72.9 µg/mL, respectively. As antidiabetic activity, the alcoholic extract exerted the most inhibition on the activity of yeast α-glucosidase, with an IC50: 76.8 µg/mL. The n-hexane fraction showed cytotoxic activity against hepatocarcinoma (HepG-2), breast carcinoma (MCF-7), and prostate carcinoma (PC-3) cell lines with IC50: 51.8, 90.8 and 62.2 µg/mL, respectively. In conclusion, the anti-inflammatory effect of Pulicaria jaubertii might be attributed to the triterpenoid constituents of the n-hexane extract of the plant. Full article
Show Figures

Figure 1

12 pages, 1059 KiB  
Article
A Novel Chemical Profile of a Selective In Vitro Cholinergic Essential Oil from Clinopodium taxifolium (Kunth) Govaerts (Lamiaceae), a Native Andean Species of Ecuador
by Sandra Espinosa, Nicole Bec, Christian Larroque, Jorge Ramírez, Barbara Sgorbini, Carlo Bicchi, Nixon Cumbicus and Gianluca Gilardoni
Molecules 2021, 26(1), 45; https://doi.org/10.3390/molecules26010045 - 23 Dec 2020
Cited by 13 | Viewed by 2629
Abstract
A novel chemical profile essential oil, distilled from the aerial parts of Clinopodium taxifolium (Kunth) Govaerts (Lamiaceae), was analysed by Gas Chromatography-Mass Spectrometry (GC-MS, qualitative analysis) and Gas Chromatography with Flame Ionization Detector (GC-FID, quantitative analysis), with both polar and non-polar stationary phase [...] Read more.
A novel chemical profile essential oil, distilled from the aerial parts of Clinopodium taxifolium (Kunth) Govaerts (Lamiaceae), was analysed by Gas Chromatography-Mass Spectrometry (GC-MS, qualitative analysis) and Gas Chromatography with Flame Ionization Detector (GC-FID, quantitative analysis), with both polar and non-polar stationary phase columns. The chemical composition mostly consisted of sesquiterpenes and sesquiterpenoids (>70%), the main ones being (E)-β-caryophyllene (17.8%), α-copaene (10.5%), β-bourbonene (9.9%), δ-cadinene (6.6%), cis-cadina-1(6),4-diene (6.4%) and germacrene D (4.9%), with the non-polar column. The essential oil was then submitted to enantioselective GC analysis, with a diethyl-tert-butyldimethylsilyl-β-cyclodextrin diluted in PS-086 chiral selector, resulting in the following enantiomeric excesses for the chiral components: (1R,5S)-(−)-α-thujene (67.8%), (1R,5R)-(+)-α-pinene (85.5%), (1S,5S)-(−)-β-pinene (90.0%), (1S,5S)-(−)-sabinene (12.3%), (S)-(−)-limonene (88.1%), (S)-(+)-linalool (32.7%), (R)-(−)-terpinen-4-ol (9.3%), (S)-(−)-α-terpineol (71.2%) and (S)-(−)-germacrene D (89.0%). The inhibition activity against acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) of C. taxifolium essential oil was then tested, resulting in selective activity against BChE with an IC50 value of 31.3 ± 3.0 μg/mL (positive control: donepezil, IC50 = 3.6 μg/mL). Full article
Show Figures

Figure 1

16 pages, 2898 KiB  
Article
Evaluation of Cholinesterase Inhibitory Potential of Different Genotypes of Ziziphus nummularia, Their HPLC-UV, and Molecular Docking Analysis
by Nisar Uddin, Niaz Ali, Zia Uddin, Nausheen Nazir, Muhammad Zahoor, Umer Rashid, Riaz Ullah, Ali S. Alqahtani, Abdulaziz M. Alqahtani, Fahd A. Nasr, Mengjun Liu and Mohammad Nisar
Molecules 2020, 25(21), 5011; https://doi.org/10.3390/molecules25215011 - 29 Oct 2020
Cited by 17 | Viewed by 3356
Abstract
Ziziphus nummularia is an important source of valuable phytoconstituents, which are widely used in traditional medicine system of Indo-Pak sub-continent. In this study we investigated the distribution of phenolic compounds in the fruit pericarps of six different genotypes (ZNP01-06) of Z. nummularia growing [...] Read more.
Ziziphus nummularia is an important source of valuable phytoconstituents, which are widely used in traditional medicine system of Indo-Pak sub-continent. In this study we investigated the distribution of phenolic compounds in the fruit pericarps of six different genotypes (ZNP01-06) of Z. nummularia growing in the unexplored hilly areas of Pakistan. The methanolic extracts of these genotypes were screened for total phenolic content (TPC), total flavonoid content (TFC), antioxidant, and cholinesterase inhibitory potentials. The observed biological potentials were explained in terms of the outcome of molecular docking and HPLC analyses. Among them, genotype ZNP02 displayed high TPC (88.50 ± 1.23 μg/mL) and showed potent scavenging activity against DPPH (67.03 ± 1.04 μg/mL) and ABTS (65.3 ± 1.74 μg/mL) in comparison to ascorbic acid (68.7 ± 0.47 μg/mL). Moreover, genotypes ZNP01, ZNP02, and ZNP04 displayed potent inhibition against acetyl and butyryl cholinesterases (AChE and BChE) with IC50 values of 21.2, 20.5, and 23.7 μg/mL (AChE) and 22.7, 24.4, and 33.1 μg/mL (BChE), respectively. Furthermore, the individual compounds in the most potent species ZNP01 responsible for potent enzyme inhibition (identified through HPLC-UV analysis), were computed via docking simulation software to the enzyme structures. Among these compounds rutin exhibited significant binding affinity with value of −9.20 kcal/mol. The differences amongst the phytochemical compositions of the selected genotypes highlighted the genotypic variations in them. Based on our results it was concluded that the selected plant can be used as remedy of oxidative stress and neurodegenerative diseases. However, further studies are needed to isolate responsible compounds and test the observed potential in vivo, along with toxicological evaluations in animal models. Full article
Show Figures

Graphical abstract

12 pages, 14723 KiB  
Article
Aromadendrin Inhibits T Cell Activation via Regulation of Calcium Influx and NFAT Activity
by Hyun-Su Lee and Gil-Saeng Jeong
Molecules 2020, 25(19), 4590; https://doi.org/10.3390/molecules25194590 - 8 Oct 2020
Cited by 14 | Viewed by 3874
Abstract
The objective of this study was to assess the inhibitory effect of the flavonoid aromadendrin on T cell activity to identify a non-cytotoxic immunosuppressive reagent. Conventional and qualitative PCR, MTT assays, flow cytometry and Western blotting were used to evaluate the effect of [...] Read more.
The objective of this study was to assess the inhibitory effect of the flavonoid aromadendrin on T cell activity to identify a non-cytotoxic immunosuppressive reagent. Conventional and qualitative PCR, MTT assays, flow cytometry and Western blotting were used to evaluate the effect of aromadendrin on the activity, cell viability and confluency, and proximal signal transduction of activated T cells. Aromadendrin effectively regulated IL-2 and IFNγ production in vitro from activated Jurkat T cells without cytotoxicity. Pre-treatment with aromadendrin also suppressed the expression levels of surface molecules CD69, CD25, and CD40L. Reduced calcium (Ca2+) influx in activated T cells pre-treated with aromadendrin was observed. Western blotting revealed that aromadendrin blocked the dephosphorylation of nuclear factor of activated T (NFAT) cells and its nuclear translocation. Involvement of the NFκB and MAPK pathways in the inhibitory effect of aromadendrin was also demonstrated. Results obtained demonstrated the suppressive effect of aromadendrin on T cell activation by Ca2+ influx regulation through NFAT activity suppression of the activated T cells. Full article
Show Figures

Figure 1

19 pages, 2493 KiB  
Article
Hair Growth Activity of Three Plants of the Polynesian Cosmetopoeia and Their Regulatory Effect on Dermal Papilla Cells
by Kristelle Hughes, Raimana Ho, Stéphane Greff, Edith Filaire, Edwige Ranouille, Claire Chazaud, Gaëtan Herbette, Jean-François Butaud, Jean-Yves Berthon and Phila Raharivelomanana
Molecules 2020, 25(19), 4360; https://doi.org/10.3390/molecules25194360 - 23 Sep 2020
Cited by 5 | Viewed by 5095
Abstract
Hair loss is becoming increasingly prevalent as dietary and living habits change. The search for natural products to limit hair loss has led to tapping into traditional cosmetic knowledge. We studied three plants of the Polynesian cosmetopoeia, Bidens pilosa, Calophyllum inophyllum and [...] Read more.
Hair loss is becoming increasingly prevalent as dietary and living habits change. The search for natural products to limit hair loss has led to tapping into traditional cosmetic knowledge. We studied three plants of the Polynesian cosmetopoeia, Bidens pilosa, Calophyllum inophyllum and Fagraea berteroana, to determine their ability to promote hair growth. Their chemical content was characterized by liquid chromatography coupled to mass spectrometry (LC-MS). Their proliferative activity on dermal papilla cells (DPCs) was assessed via MTT assay and molecular targets were evaluated by RT-qPCR analysis of seven factors involved in the modulation of the hair cycle, CCND1, LEF1, DKK1, WNT5A PPARD, TGFΒ1, PPARD and RSPO2. Our results show that our extracts significantly increased proliferation of dermal papilla cells. Furthermore, LC-MS/MS analysis revealed a diversity of molecules, flavonoids, iridoids and organic acids, some known for hair-inducing properties. Finally, specific extracts and fractions of all three plants either upregulated CCND1, LEF1 and PPARD involved in stimulating hair follicle proliferation and/or lowered the gene expression levels of hair growth inhibiting factors, DKK1 and TGFB1. Our findings suggest that extracts from B. pilosa, C. inophyllum and F. berteroana are interesting candidates to stimulate hair growth. Full article
Show Figures

Graphical abstract

29 pages, 1240 KiB  
Article
Using Medicinal Plants in Valmalenco (Italian Alps): From Tradition to Scientific Approaches
by Martina Bottoni, Fabrizia Milani, Lorenzo Colombo, Kevin Nallio, Paola Sira Colombo, Claudia Giuliani, Piero Bruschi and Gelsomina Fico
Molecules 2020, 25(18), 4144; https://doi.org/10.3390/molecules25184144 - 10 Sep 2020
Cited by 21 | Viewed by 4809
Abstract
This ethnobotanical survey was carried out in Caspoggio (Valmalenco, SO, Italy) with the purpose of investigating the traditional uses of medicinal plants. Moreover, a bibliographic research meant to validate or refute the uses, focusing on the potentially responsible compounds, was performed. Fifty-nine species, [...] Read more.
This ethnobotanical survey was carried out in Caspoggio (Valmalenco, SO, Italy) with the purpose of investigating the traditional uses of medicinal plants. Moreover, a bibliographic research meant to validate or refute the uses, focusing on the potentially responsible compounds, was performed. Fifty-nine species, attributable to 30 families (Asteraceae, Pinaceae, Malvaceae, and Lamiaceae the most cited), were mentioned. Arnica montana, anti-inflammatory for traumas and musculoskeletal pains; Pinus mugo, expectorant; Malva sylvestris, anti-inflammatory and soothing; Achillea moschata, digestive. The compounds, responsible for the therapeutic activities, are often polyphenols and terpenoids: helenanin in A. montana, α-pinene, δ-3-carene, and limonene in P. mugo, gossypin and malvin in M. sylvestris, luteolin and apigenin in A. moschata. Scientific evidence for at least one of the traditional activities described was found for 50 species but only in 26 out of 196 works consulted, it is possible to make a comparison between investigated extracts and traditional preparations. This study is thus a stimulus to new phytochemical investigations, mimicking as much as possible the traditional preparations. This work is part of the European Interreg Italy-Switzerland B-ICE project, aimed at creating a management model for the ongoing climate change and searching for new sources of territory valorization as attractions for tourists. Full article
Show Figures

Graphical abstract

18 pages, 2112 KiB  
Article
Flavonoids and Terpenoids with PTP-1B Inhibitory Properties from the Infusion of Salvia amarissima Ortega
by Eric Salinas-Arellano, Araceli Pérez-Vásquez, Isabel Rivero-Cruz, Rafael Torres-Colin, Martín González-Andrade, Manuel Rangel-Grimaldo and Rachel Mata
Molecules 2020, 25(15), 3530; https://doi.org/10.3390/molecules25153530 - 1 Aug 2020
Cited by 16 | Viewed by 3851
Abstract
An infusion prepared from the aerial parts of Salvia amarissima Ortega inhibited the enzyme protein tyrosine phosphatase 1B (PTP-1B) (IC50~88 and 33 μg/mL, respectively). Phytochemical analysis of the infusion yielded amarisolide (1), 5,6,4′-trihydroxy-7,3′-dimethoxyflavone (2), 6-hydroxyluteolin (3 [...] Read more.
An infusion prepared from the aerial parts of Salvia amarissima Ortega inhibited the enzyme protein tyrosine phosphatase 1B (PTP-1B) (IC50~88 and 33 μg/mL, respectively). Phytochemical analysis of the infusion yielded amarisolide (1), 5,6,4′-trihydroxy-7,3′-dimethoxyflavone (2), 6-hydroxyluteolin (3), rutin (4), rosmarinic acid (5), isoquercitrin (6), pedalitin (7) and a new neo-clerodane type diterpenoid glucoside, named amarisolide G (8a,b). Compound 8a,b is a new natural product, and 26 are reported for the first time for the species. All compounds were tested for their inhibitory activity against PTP-1B; their IC50 values ranged from 62.0 to 514.2 μM. The activity was compared to that of ursolic acid (IC50 = 29.14 μM). The most active compound was pedalitin (7). Docking analysis predicted that compound 7 has higher affinity for the allosteric site of the enzyme. Gas chromatography coupled to mass spectrometry analyses of the essential oils prepared from dried and fresh materials revealed that germacrene D (15) and β-selinene (16), followed by β-caryophyllene (13) and spathulenol (17) were their major components. An ultra-high performance liquid chromatography coupled to mass spectrometry method was developed and validated to quantify amarisolide (1) in the ethyl acetate soluble fraction of the infusion of S. amarissima. Full article
Show Figures

Graphical abstract

17 pages, 3054 KiB  
Article
A Herbal Mixture from Propolis, Pomegranate, and Grape Pomace Endowed with Anti-Inflammatory Activity in an In Vivo Rheumatoid Arthritis Model
by Valentina Parisi, Antonio Vassallo, Claudio Pisano, Giacomo Signorino, Francesco Cardile, Milena Sorrentino, Fabiana Colelli, Alessandra Fucci, Egildo Luca D’Andrea, Nunziatina De Tommasi, Alessandra Braca and Marinella De Leo
Molecules 2020, 25(9), 2255; https://doi.org/10.3390/molecules25092255 - 11 May 2020
Cited by 20 | Viewed by 4021
Abstract
Rheumatoid arthritis (RA) is a chronic inflammatory autoimmune disease characterized by the production of inflammatory factors. In order to overcome the side effects of currently used anti-inflammatory drugs, several attempts have been made to identify natural products capable of relieving RA symptoms. In [...] Read more.
Rheumatoid arthritis (RA) is a chronic inflammatory autoimmune disease characterized by the production of inflammatory factors. In order to overcome the side effects of currently used anti-inflammatory drugs, several attempts have been made to identify natural products capable of relieving RA symptoms. In this work, a herbal preparation consisting of propolis, pomegranate peel, and Aglianico grape pomace (PPP) extracts (4:1:1) was designed and evaluated for its effect on a murine collagen-induced arthritis (CIA) model. Firstly, the chemical contents of four different Italian propolis collected in the Campania region (Italy) were here reported for the first time. LC-MS analyses showed the presence of 38 constituents, identified in all propolis extracts, belonging to flavonoids and phenolic acids classes. The Pietradefusi extract was the richest one and thus was selected to design the PPP preparation for the in vivo assay. Our results highlight the impact of PPP on RA onset and progression. By using in vivo CIA models, the treatment with PPP resulted in a delayed onset of the disease and alleviated the severity of the clinical symptoms. Furthermore, we demonstrated that early PPP treatment was associated with a reduction in serum levels of IL-17, IL-1b, and IL-17–triggering cytokines. Full article
Show Figures

Figure 1

19 pages, 1633 KiB  
Article
Reconsidering Hydrosols as Main Products of Aromatic Plants Manufactory: The Lavandin (Lavandula × intermedia) Case Study in Tuscany
by Matteo Politi, Luigi Menghini, Barbara Conti, Stefano Bedini, Priscilla Farina, Pier Luigi Cioni, Alessandra Braca and Marinella De Leo
Molecules 2020, 25(9), 2225; https://doi.org/10.3390/molecules25092225 - 9 May 2020
Cited by 37 | Viewed by 4949
Abstract
The present work evaluates for the first time two Lavandin (Lavandula × intermedia Emeric ex Loisel.) aromatic waters obtained from different plant organs, the flowers and the stems. Both extracts were analysed by GC-MS, which indicates semi-quantitative differences between the major metabolites [...] Read more.
The present work evaluates for the first time two Lavandin (Lavandula × intermedia Emeric ex Loisel.) aromatic waters obtained from different plant organs, the flowers and the stems. Both extracts were analysed by GC-MS, which indicates semi-quantitative differences between the major metabolites including linalool, 1,8-cineole, camphor, linalyl acetate and 4-terpineol. 1H-NMR and LC-MS investigation confirmed the presence of these compounds. Moreover, behavioural tests with the food insect pest Tribolium confusum (Coleoptera Tenebrionidae) showed a good repellency for both hydrosols extracts with RD50 values of 3.6 and 3.3 µL·cm−2 for the flowers and stems, respectively; at the higher concentrations, however, the hydrosol extract from the flowers is expected to be more effective than the one from the stems. The effect of the flowers and stems aromatic water of Lavandin on seed germination of Raphanus sativus was also evaluated. Results showed that seed germination was completely inhibited by flowers hydrolate, having a possible application as natural herbicide. The overall experience with these Lavandin extracts indicates the potential of improved hydrolates to become the main distillation products, rather than by-products, of the aromatic plants manufacturing; this stimulates further discussions about the potential positive impacts that such a shift could have in the context of ecopharmacognosy. Full article
Show Figures

Figure 1

21 pages, 930 KiB  
Article
Composition and Antibacterial Activity of Aronia melanocarpa (Michx.) Elliot, Cornus mas L. and Chaenomeles superba Lindl. Leaf Extracts
by Magdalena Efenberger-Szmechtyk, Agnieszka Nowak, Agata Czyżowska, Alicja Z. Kucharska and Izabela Fecka
Molecules 2020, 25(9), 2011; https://doi.org/10.3390/molecules25092011 - 25 Apr 2020
Cited by 35 | Viewed by 4065
Abstract
The purpose of this study was to investigate the composition of leaf extracts from Aronia melanocarpa, Chaenomeles superba, and Cornus mas, and their antimicrobial activity against typical spoilage-causing and pathogenic bacteria found in meat and meat products. The highest total [...] Read more.
The purpose of this study was to investigate the composition of leaf extracts from Aronia melanocarpa, Chaenomeles superba, and Cornus mas, and their antimicrobial activity against typical spoilage-causing and pathogenic bacteria found in meat and meat products. The highest total phenolic content (TPC) was detected in C. superba extract, followed by C. mas and A. melanocarpa extracts. The antioxidant capacity of the extracts was measured by DPPH and ABTS assays. The lowest IC50 values were found for C. superba extract, followed by C. mas and A. melanocarpa extracts. LC-MS and HPLC analysis revealed that A. melanocarpa and C. superba extracts contained hydroxycinnamic acid derivatives and flavonoids (mainly flavonols). Hydroxycinnamic acid derivatives were detected in the C. mas extract, as well as flavonols, ellagitannins, and iridoids. The antibacterial activity of the plant extracts was tested against Gram-negative bacteria (Moraxella osloensis, Pseudomonas fragi, Acinetobacter baumanii, Escherichia coli, Enterobacter aerogenes, Salmonella enterica) and Gram-positive bacteria (Enterococcus faecium, Staphylococcus aureus, Brochothrix thermosphacta, Lactobacillus sakei, Listeria monocytogenes) using the microculture method. The extracts acted as bacteriostatic agents, decreasing the growth rate (µmax) and extending the lag phase (tlag). C. mas showed most potent antibacterial activity, as confirmed by principal component analysis (PCA). Full article
Show Figures

Figure 1

22 pages, 4454 KiB  
Article
The Anti-Inflammatory and Antimicrobial Potential of Selected Ethnomedicinal Plants from Sri Lanka
by Mayuri Napagoda, Jana Gerstmeier, Hannah Butschek, Sudhara De Soyza, Simona Pace, Sybille Lorenz, Mallique Qader, Sanjeeva Witharana, Ajith Nagahawatte, Gaya Wijayaratne, Aleš Svatoš, Lalith Jayasinghe, Andreas Koeberle and Oliver Werz
Molecules 2020, 25(8), 1894; https://doi.org/10.3390/molecules25081894 - 20 Apr 2020
Cited by 8 | Viewed by 4591
Abstract
Traditional folk medicine in Sri Lanka is mostly based on plants and plant-derived products, however, many of these medicinal plant species are scientifically unexplored. Here, we evaluated the anti-inflammatory and antimicrobial potency of 28 different extracts prepared from seven popular medicinal plant species [...] Read more.
Traditional folk medicine in Sri Lanka is mostly based on plants and plant-derived products, however, many of these medicinal plant species are scientifically unexplored. Here, we evaluated the anti-inflammatory and antimicrobial potency of 28 different extracts prepared from seven popular medicinal plant species employed in Sri Lanka. The extracts were subjected to cell-based and cell-free assays of 5-lipoxygenase (5-LO), microsomal prostaglandin E2 synthase (mPGES)-1, and nitric oxide (NO) scavenging activity. Moreover, antibacterial and disinfectant activities were assessed. Characterization of secondary metabolites was achieved by gas chromatography coupled to mass spectrometric (GC-MS) analysis. n-Hexane- and dichloromethane-based extracts of Garcinia cambogia efficiently suppressed 5-LO activity in human neutrophils (IC50 = 0.92 and 1.39 µg/mL), and potently inhibited isolated human 5-LO (IC50 = 0.15 and 0.16 µg/mL) and mPGES-1 (IC50 = 0.29 and 0.49 µg/mL). Lipophilic extracts of Pothos scandens displayed potent inhibition of mPGES-1 only. A methanolic extract of Ophiorrhiza mungos caused significant NO scavenging activity. The lipophilic extracts of G. cambogia exhibited prominent antibacterial and disinfectant activities, and GC-MS analysis revealed the presence of fatty acids, sesquiterpenes and other types of secondary metabolites. Together, our results suggest the prospective utilization of G. cambogia as disinfective agent with potent anti-inflammatory properties. Full article
Show Figures

Graphical abstract

17 pages, 12899 KiB  
Article
Chemical Composition and Biological Activities of Essential Oils from Peels of Three Citrus Species
by Lucia Caputo, Laura Cornara, Miriam Bazzicalupo, Clara De Francesco, Vincenzo De Feo, Domenico Trombetta and Antonella Smeriglio
Molecules 2020, 25(8), 1890; https://doi.org/10.3390/molecules25081890 - 19 Apr 2020
Cited by 34 | Viewed by 6686
Abstract
Background: Fruit peels are generally underutilized byproducts of the food industry, although they are valuable sources of bioactive compounds. The aim of this study is to evaluate a new application for three Citrus peel EOs as bio-herbicides. Methods: After a micro-morphological evaluation of [...] Read more.
Background: Fruit peels are generally underutilized byproducts of the food industry, although they are valuable sources of bioactive compounds. The aim of this study is to evaluate a new application for three Citrus peel EOs as bio-herbicides. Methods: After a micro-morphological evaluation of Citrus peels by SEM analysis, the phytochemical composition of the EOs of Citrus × bergamia Risso & Poit., Citrus × myrtifolia Raf., and Citrus limon (L.) Osbeck was characterized by GC/FID and GC/MS analyses. The in vitro phytotoxicity against germination and initial radical elongation of several crop and weed species was evaluated. Furthermore, the eco-compatibility of these EOs has been assessed by the brine shrimp (Artemia salina) lethality assay. Results: SEM analysis highlighted the morphometric differences of the schizolysigenous pockets among the peels of the three Citrus species. Oxygenated monoterpenes are the main constituents in C. × bergamia (51.09%), whereas monoterpene hydrocarbons represent the most abundant compounds in C. × myrtifolia (82.15%) and C. limon (80.33%) EOs. They showed marked and selective phytotoxic activity in vitro, often at very low concentration (0.1 μg/mL) against all plant species investigated, without showing any toxicity on Artemia salina, opening the perspective of their use as safe bio-herbicides. Full article
Show Figures

Figure 1

20 pages, 2423 KiB  
Article
Chemical Composition, Antioxidant, Anti-Tyrosinase, Anti-Cholinesterase and Cytotoxic Activities of Essential Oils of Six Algerian Plants
by Kadour Cheraif, Boulanouar Bakchiche, Abdelaziz Gherib, Sanaa K. Bardaweel, Melek Çol Ayvaz, Guido Flamini, Roberta Ascrizzi and Mosad A. Ghareeb
Molecules 2020, 25(7), 1710; https://doi.org/10.3390/molecules25071710 - 8 Apr 2020
Cited by 55 | Viewed by 4846
Abstract
In this study, the essential oils (EOs) of six Algerian plants (Artemisia campestris L., Artemisia herba-alba Asso, Juniperus phoenicea L., Juniperus oxycedrus L., Mentha pulegium L. and Lavandula officinalis Chaix) were obtained by hydrodistillation, and their compositions determined by GC-MS and [...] Read more.
In this study, the essential oils (EOs) of six Algerian plants (Artemisia campestris L., Artemisia herba-alba Asso, Juniperus phoenicea L., Juniperus oxycedrus L., Mentha pulegium L. and Lavandula officinalis Chaix) were obtained by hydrodistillation, and their compositions determined by GC-MS and GC-FID. The antioxidant activity of the EOS was evaluated via 2,2′-diphenyl-1-picrylhydrazyl (DPPH), ferric-reducing/antioxidant power (FRAP) and 2,2′-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid (ABTS) assays. Moreover, their cytotoxic effect was evaluated—as well as their tyrosinase, acetyl- and butyryl-cholinesterase (AChE and BuChE) inhibitory activities. The chemical analyses detected 44, 45, 51, 53, 26 and 40 compounds in EOs of A. campestris, A. herba-alba, J. phoenicea, J. oxycedrus, M. pulegium and L. officinalis, respectively. A. campestris EO was mainly composed of β-pinene (20.7%), while A. herba-alba EO contained davanone D (49.5%) as the main component. α-Pinene (41.8%) was detected as the major constituent in both J. phoenicea (41.8%) and J. oxycedrus (37.8%) EOs. M. pulegium EO was characterized by pulegone as the most abundant (76.9%) compound, while linalool (35.8%) was detected as a major constituent in L. officinalis EO. The antioxidant power evaluation revealed IC50 values ranging from 2.61 to 91.25 mg/mL for DPPH scavenging activity, while the FRAP values ranged from 0.97–8.17 µmol Trolox equivalents (TX)/g sample. In the ABTS assay, the values ranged from 7.01 to 2.40 µmol TX/g sample. In the presence of 1 mg/mL of the samples, tyrosinase inhibition rates ranged from 11.35% to 39.65%, AChE inhibition rates ranged from 40.57% to 73.60% and BuChE inhibition rates ranged from 6.47% to 72.03%. A significant cytotoxic effect was found for A. herba-alba EO. The obtained results support some of the traditional uses of these species in food preservation and for protection against several diseases. Full article
Show Figures

Figure 1

17 pages, 1884 KiB  
Article
Grapevine Green Pruning Residues as a Promising and Sustainable Source of Bioactive Phenolic Compounds
by Stefano Acquadro, Silvia Appleton, Arianna Marengo, Carlo Bicchi, Barbara Sgorbini, Manuela Mandrone, Francesco Gai, Pier Giorgio Peiretti, Cecilia Cagliero and Patrizia Rubiolo
Molecules 2020, 25(3), 464; https://doi.org/10.3390/molecules25030464 - 22 Jan 2020
Cited by 15 | Viewed by 3812
Abstract
Green pruning residues (GPRs) and leaves from 16 red and white Vitis vinifera L. cultivars from Piedmont (Italy) were studied. The investigated samples were extracted by ultrasound-assisted extraction optimized by an experimental design, and quali- and quantitatively analyzed by HPLC-PDA-MS/MS. GPRs and leaves [...] Read more.
Green pruning residues (GPRs) and leaves from 16 red and white Vitis vinifera L. cultivars from Piedmont (Italy) were studied. The investigated samples were extracted by ultrasound-assisted extraction optimized by an experimental design, and quali- and quantitatively analyzed by HPLC-PDA-MS/MS. GPRs and leaves show a similar polyphenolic pattern, with quercetin 3-O-glucuronide, caftaric acid, and quercetin 3-O-glucoside as the main components, although in variable proportions. The HPLC results were related to the antioxidant activity, measured as total phenolic content and through DPPH and ABTS assays with similar results. Colorimetric in vitro assays, offline combined with HPLC-PDA analysis, determine which compounds contribute to the antioxidant activity in terms of radical scavenging abilities. Valorization of GPRs is a potential source of natural compounds that could be of interest in the health field, increasing their economic value together with a positive effect on the environment. Full article
Show Figures

Figure 1

Review

Jump to: Research

24 pages, 9257 KiB  
Review
Marrubium vulgare L.: A Phytochemical and Pharmacological Overview
by Milica Aćimović, Katarina Jeremić, Nebojša Salaj, Neda Gavarić, Biljana Kiprovski, Vladimir Sikora and Tijana Zeremski
Molecules 2020, 25(12), 2898; https://doi.org/10.3390/molecules25122898 - 24 Jun 2020
Cited by 46 | Viewed by 9412
Abstract
Marrubium vulgare is a plant with high bioactive potential. It contains marrubiin, a labdane diterpene that is characteristic for this genus, as well as a complex mixture of phenolic compounds. According to numerous studies, M. vulgare acts as a good antioxidant agent, and [...] Read more.
Marrubium vulgare is a plant with high bioactive potential. It contains marrubiin, a labdane diterpene that is characteristic for this genus, as well as a complex mixture of phenolic compounds. According to numerous studies, M. vulgare acts as a good antioxidant agent, and due to this, it could potentially be useful in treatments of cancer, diabetes mellitus, and liver diseases. In addition, its anti-inflammatory, wound-healing, antihypertensive, hypolipidemic, and sedative potential are discussed. Apart from that, its antimicrobial activity, especially against Gram+ bacteria, fungi, herpes simplex virus, and parasites such as Toxoplasma gondii, Trichomonas vaginalis, and Plasmodium berghei-berghei was recorded. Additionally, it could be used as a chicken lice repellent, herbicide, and natural insecticide against mosquito larvae and natural molluscicide. In veterinary medicine, M. vulgare can be used as an anthelmintic against the eggs and larvae of bovine strongyles parasites, and as an antibiotic against bovine mastitis caused by resistant bacterial strains. Due to the mentioned benefits, there is a tendency for the cultivation of M. vulgare in order to ensure high-quality raw material, but more firm scientific evidence and well-designed clinical trials are necessary for the well-established use of M. vulgare herb and its preparations. Full article
31 pages, 2136 KiB  
Review
Anti-Infective and Anti-Cancer Properties of the Annona Species: Their Ethnomedicinal Uses, Alkaloid Diversity, and Pharmacological Activities
by Ari Satia Nugraha, Yuvita Dian Damayanti, Phurpa Wangchuk and Paul A. Keller
Molecules 2019, 24(23), 4419; https://doi.org/10.3390/molecules24234419 - 3 Dec 2019
Cited by 51 | Viewed by 8179
Abstract
Annona species have been a valuable source of anti-infective and anticancer agents. However, only limited evaluations of their alkaloids have been carried out. This review collates and evaluates the biological data from extracts and purified isolates for their anti-infective and anti-cancer activities. An [...] Read more.
Annona species have been a valuable source of anti-infective and anticancer agents. However, only limited evaluations of their alkaloids have been carried out. This review collates and evaluates the biological data from extracts and purified isolates for their anti-infective and anti-cancer activities. An isoquinoline backbone is a major structural alkaloid moiety of the Annona genus, and more than 83 alkaloids have been isolated from this genus alone. Crude extracts of Annona genus are reported with moderate activities against Plasmodium falciparum showing larvicidal activities. However, no pure compounds from the Annona genus were tested against the parasite. The methanol extract of Annona muricata showed apparent antimicrobial activities. The isolated alkaloids from this genus including liriodenine, anonaine, asimilobine showed sensitivity against Staphylococcus epidermidis. Other alkaloids such as (+)-Xylopine and isocoreximine indicated significant anti-cancer activity against A549 and K-562 cell lines, respectively. This review revealed that the alkaloids from Annona genus are rich in structural diversity and pharmacological activities. Further exploration of this genus and their alkaloids has potential for developing novel anti-infective and anticancer drugs. Full article
Show Figures

Figure 1

19 pages, 2139 KiB  
Review
Corilagin in Cancer: A Critical Evaluation of Anticancer Activities and Molecular Mechanisms
by Ashutosh Gupta, Amit Kumar Singh, Ramesh Kumar, Risha Ganguly, Harvesh Kumar Rana, Prabhash Kumar Pandey, Gautam Sethi, Anupam Bishayee and Abhay K. Pandey
Molecules 2019, 24(18), 3399; https://doi.org/10.3390/molecules24183399 - 19 Sep 2019
Cited by 62 | Viewed by 6130
Abstract
Corilagin (β-1-O-galloyl-3,6-(R)-hexahydroxydiphenoyl-d-glucose), an ellagitannin, is one of the major bioactive compounds present in various plants. Ellagitannins belong to the hydrolyzable tannins, a group of polyphenols. Corilagin shows broad-spectrum biological, and therapeutic activities, such as antioxidant, anti-inflammatory, hepatoprotective, [...] Read more.
Corilagin (β-1-O-galloyl-3,6-(R)-hexahydroxydiphenoyl-d-glucose), an ellagitannin, is one of the major bioactive compounds present in various plants. Ellagitannins belong to the hydrolyzable tannins, a group of polyphenols. Corilagin shows broad-spectrum biological, and therapeutic activities, such as antioxidant, anti-inflammatory, hepatoprotective, and antitumor actions. Natural compounds possessing antitumor activities have attracted significant attention for treatment of cancer. Corilagin has shown inhibitory activity against the growth of numerous cancer cells by prompting cell cycle arrest at the G2/M phase and augmented apoptosis. Corilagin-induced apoptosis and autophagic cell death depends on production of intracellular reactive oxygen species in breast cancer cell line. It blocks the activation of both the canonical Smad and non-canonical extracellular-signal-regulated kinase/Akt (protein kinase B) pathways. The potential apoptotic action of corilagin is mediated by altered expression of procaspase-3, procaspase-8, procaspase-9, poly (ADP ribose) polymerase, and Bcl-2 Bax. In nude mice, corilagin suppressed cholangiocarcinoma growth and downregulated the expression of Notch1 and mammalian target of rapamycin. The aim of this review is to summarize the anticancer efficacy of corilagin with an emphasis on the molecular mechanisms involving various signaling pathways in tumor cells. Full article
Show Figures

Figure 1

Back to TopTop