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Research of Bioactive Substances in Plant Extracts
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Research of Bioactive Substances in Plant Extracts

A special issue of Plants (ISSN 2223-7747). This special issue belongs to the section "Phytochemistry".

Deadline for manuscript submissions: closed (28 February 2022) | Viewed by 72420

Special Issue Editor

Dr. Francesca Pintus

E-Mail Website1 Website2
Guest Editor
Department of Sciences of Life and Environment, University of Cagliari, Monserrato, Cagliari, Italy
Interests: plant extracts; bioactive compounds; enzymes; enzyme inhibition; protein purification and characterization
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Plant natural compounds represent an ever-increasing topic of research interest. Most of them are bioactive molecules with a broad range of biological properties. These include anticancer, antimicrobial, antiviral, anti-amyloidogenic, anti-inflammatory, and other biological activities.

To exert their effect, they could bind to specific enzymes and modulate their activity. Due to the important role of enzymes in several diseases’ pathogenesis, they represent targets for therapeutic intervention strategies. Thus, discovery of enzyme modulators is an interesting research area in the biochemistry and drug design field. Several plant extracts or plant-derived compounds are already reported to be inhibitors of tyrosinase, cyclooxygenases, MAOs, cholinesterases, amylase, and glycosidase, which are involved in pigmentation, inflammation, Alzheimer’s disease or diabetes.

The aim of this Special Issue is to highlight the newest discoveries in plant extract products and focus attention on the beneficial biological effects of plant extracts or plant-isolated compounds; their potential application in disease treatment and health promotion will also be of particular interest.

Dr. Francesca Pintus
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. Plants 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

  • plants extracts
  • bioactive compounds
  • enzyme inhibition
  • essential oils
  • anti-inflammatory
  • antiviral activity
  • antimicrobial activity
  • pharmaceutical potential
  • health benefit

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Published Papers (18 papers)

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18 pages, 1003 KiB  
Article
Antioxidation, Anti-Inflammation, and Regulation of SRD5A Gene Expression of Oryza sativa cv. Bue Bang 3 CMU Husk and Bran Extracts as Androgenetic Alopecia Molecular Treatment Substances
by Chiranan Khantham, Pichchapa Linsaenkart, Tanakarn Chaitep, Pensak Jantrawut, Chuda Chittasupho, Pornchai Rachtanapun, Kittisak Jantanasakulwong, Yuthana Phimolsiripol, Sarana Rose Sommano, Chanakan Prom-u-thai, Sansanee Jamjod, Chaiwat Arjin, Korawan Sringarm, Houda Berrada, Francisco J. Barba, Francisco David Carmona, Wutigri Nimlamool and Warintorn Ruksiriwanich
Plants 2022, 11(3), 330; https://0-doi-org.brum.beds.ac.uk/10.3390/plants11030330 - 26 Jan 2022
Cited by 10 | Viewed by 5166
Abstract
Androgenetic alopecia (AGA), a hair loss disorder, is a genetic predisposition to sensitive androgens, inflammation, and oxidative stress. Unfortunately, current treatments with synthetic medicines contain a restricted mechanism along with side effects, whereas the bioactive constituents of plant extracts are multifunctional, with fewer [...] Read more.
Androgenetic alopecia (AGA), a hair loss disorder, is a genetic predisposition to sensitive androgens, inflammation, and oxidative stress. Unfortunately, current treatments with synthetic medicines contain a restricted mechanism along with side effects, whereas the bioactive constituents of plant extracts are multifunctional, with fewer side effects. The massive amounts of rice husk and bran are agricultural wastes that may cause pollution and environmental problems. Owing to these rationales, the local rice variety, Bue Bang 3 CMU (BB3CMU), which is grown in northern Thailand, was evaluated for the valuable utilization of rice by-products, husk (BB3CMU-H) and bran (BB3CMU-RB) extracts, for AGA treatment regarding antioxidant, anti-inflammatory, anti-androgenic activities, and the characterization of bioactive compounds. Our study verified that BB3CMU-H had the highest level of polyphenols, contributing to its greater antioxidant activity. Conversely, BB3CMU-RB was the predominant source of tocopherols, resulting in better anti-androgenic activities regarding the downregulation of steroid 5α-reductase genes (SRD5A). Notably, anti-inflammation via the attenuation of nitric oxide productions was observed in BB3CMU-H (0.06 ± 0.13 μM) and BB3CMU-RB (0.13 ± 0.01 μM), which were significantly comparable to diclofenac sodium salt (0.13 ± 0.19 μM). Therefore, the combination of BB3CMU-H and BB3CMU-RB could be utilized in cosmeceutical and pharmaceutical applications for AGA patients. Full article
(This article belongs to the Special Issue Research of Bioactive Substances in Plant Extracts)
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18 pages, 3424 KiB  
Article
Digalloyl Glycoside: A Potential Inhibitor of Trypanosomal PFK from Euphorbia abyssinica J.F. Gmel
by Seham S. El-Hawary, Rabab Mohammed, Nadia M. Lithy, Sameh Fekry AbouZid, Mostafa A. Mansour, Suliman A. Almahmoud, Bader Huwaimel and Elham Amin
Plants 2022, 11(2), 173; https://0-doi-org.brum.beds.ac.uk/10.3390/plants11020173 - 10 Jan 2022
Cited by 5 | Viewed by 2119
Abstract
Human African trypanosomiasis is an endemic infectious disease caused by Trypanosoma brucei via the bite of tsetse-fly. Most of the drugs used for the treatment, e.g., Suramin, have shown several problems, including the high level of toxicity. Accordingly, the discovery of anti-trypanosomal drugs [...] Read more.
Human African trypanosomiasis is an endemic infectious disease caused by Trypanosoma brucei via the bite of tsetse-fly. Most of the drugs used for the treatment, e.g., Suramin, have shown several problems, including the high level of toxicity. Accordingly, the discovery of anti-trypanosomal drugs from natural sources has become an urgent requirement. In our previous study on the anti-trypanosomal potential of Euphorbia species, Euphorbia abyssinica displayed significant anti-trypanosomal activity. Therefore, a phytochemical investigation of the methanolic extract of E. abyssinica was carried out. Twelve compounds, including two triterpenes (1, 2); one sterol-glucoside (4); three ellagic acid derivatives (3, 9, 11); three gallic acid derivatives (5, 6, 10); and three flavonoids (7, 8, 12), were isolated. The structures of isolated compounds were determined through different spectroscopic techniques. Compound (10) was obtained for the first time from genus Euphorbia while all other compounds except compound (4), were firstly reported in E. abyssinica. Consequently, an in silico study was used to estimate the anti-trypanosomal activity of the isolated compounds. Several compounds displayed interesting activity where 1,6-di-O-galloyl-d-glucose (10) appeared as the most potent inhibitor of trypanosomal phosphofructokinase (PFK). Moreover, molecular dynamics (MD) simulations and ADMET calculations were performed for 1,6-di-O-galloyl-d-glucose. In conclusion, 1,6-di-O-galloyl-d-glucose revealed high binding free energy as well as desirable molecular dynamics and pharmacokinetic properties; therefore, it could be suggested for further in vitro and in vivo studies for trypanosomiasis. Full article
(This article belongs to the Special Issue Research of Bioactive Substances in Plant Extracts)
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12 pages, 950 KiB  
Article
Phytochemical Analyses, Antioxidant and Anticancer Activities of Ethanolic Leaf Extracts of Moringa oleifera Lam. Varieties
by Bilques Farooq, Bhupendra Koul, Deveshi Mahant and Dhananjay Yadav
Plants 2021, 10(11), 2348; https://0-doi-org.brum.beds.ac.uk/10.3390/plants10112348 - 30 Oct 2021
Cited by 5 | Viewed by 2615
Abstract
Moringa oleifera Lam. (Moringaceae) is revered as s ‘miracle tree’ due to its remarkable nutritional, medicinal and industrial uses. In our study, a comparative analysis of the nutritional parameters (antioxidant activity, sugar content—TSS, total soluble proteins—TSP and mineral contents), phytochemicals (HPLC analysis of [...] Read more.
Moringa oleifera Lam. (Moringaceae) is revered as s ‘miracle tree’ due to its remarkable nutritional, medicinal and industrial uses. In our study, a comparative analysis of the nutritional parameters (antioxidant activity, sugar content—TSS, total soluble proteins—TSP and mineral contents), phytochemicals (HPLC analysis of four anticancer compounds), and cytotoxicity of M. oleifera leaf extracts (MLEs) of five selected varieties (conventional, PKM-1, PKM-2, ODC, and Jaffna), was performed. Jaffna variety possessed the highest antioxidant activity (FRAP) followed by other four varieties. The trend observed was: Jaffna (9.47 µg/mL, 18.48 µg/mL, 29.39 µg/mL, and 35.37 µg/mL) > PKM-1 (4.82 µg/mL, 7.63 µg/mL, 22.33 µg/mL, and 27.71 µg/mL) > PKM-2 (2.10 µg/mL, 7.04 µg/mL, 13.18 µg/mL, and 21.78 µg/mL) > ODC (0.17 µg/mL, 2.10 µg/mL, 4.41 µg/mL and 13.94 µg/mL) > Conventional (0.05 µg/mL, 1.08 µg/mL, 2.86 µg/mL, and 5.40 µg/mL), total soluble proteins (TSP) [0.69 ± 0.01 and 0.94 ± 0.01 µg/mL (young and mature stage, respectively)], sugar content (TSS) [0.39 ± 0.01 and 0.51 ± 0.01 µg/mL (young and mature stage, respectively)], chlorophyll content [1.07 ± 0.01 (plantlet stage), 1.36 ± 0.003 (vegetative-stage), 0.82 ± 0.004 (reproductive stage) mg/g], followed by the other four varieties. The trend observed for cytotoxic activities of ethanolic MLEs on HepG2 cell line, based on the IC50 values, was conventional (1.22 mg/mL) > ODC (0.90 mg/mL) > PKM-2 (0.65 mg/mL) > PKM-1 (0.35 mg/mL) > Jaffna (0.15 mg/mL). The results of HPLC quantification of anticancer compounds [beta-sitosterol (0.244%), quercetin (0.216%), kaempferol (0.013%), and moringin (0.063%)] was also in consonance with that of MTT assay. In summary, the trend observed in all the parameters tested was Jaffna > PKM-1 > PKM-2 > ODC > conventional. Thus, Jaffna variety has a better potential to combat malnutrition and cancer and must be recommended for commercial plantations. Full article
(This article belongs to the Special Issue Research of Bioactive Substances in Plant Extracts)
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10 pages, 1834 KiB  
Communication
A Natural Botanical Product, Resveratrol, Effectively Suppresses Vesicular Stomatitis Virus Infection In Vitro
by Shih-Chao Lin, Xiang Zhang, Caitlin W. Lehman, Han-Chi Pan, Ya Wen and Shiow-Yi Chen
Plants 2021, 10(6), 1231; https://0-doi-org.brum.beds.ac.uk/10.3390/plants10061231 - 17 Jun 2021
Cited by 2 | Viewed by 1996
Abstract
Numerous natural phytochemicals such as resveratrol are acknowledged as potent botanical agents in regulating immune responses. However, it is less understood whether such immunomodulatory phytochemicals are appropriate for use as direct treatments in veterinary viral diseases. In the present study, we investigated the [...] Read more.
Numerous natural phytochemicals such as resveratrol are acknowledged as potent botanical agents in regulating immune responses. However, it is less understood whether such immunomodulatory phytochemicals are appropriate for use as direct treatments in veterinary viral diseases. In the present study, we investigated the efficacy of resveratrol in suppressing vesicular stomatitis virus (VSV) infection. Outbreaks of VSV can cause massive economic loss in poultry and livestock husbandry farming, and VSV treatment is in need of therapeutic development. We utilized a recombinant VSV that expresses green fluorescent protein (GFP) to measure viral replication in cells treated with resveratrol. Our findings revealed that resveratrol treatment affords a protective effect, shown by increased viability and reduced viral replication, as indicated by a reduction in fluorescent signals. Additionally, we found that resveratrol inhibition of VSV infection occurs via suppression of the caspase cascade. Structural analysis also indicated that resveratrol potentially interacts with the active sites of caspase-3 and -7, facilitating antiviral activity. The potential effect of resveratrol on reducing VSV infection in vitro suggests that resveratrol should be further investigated as a potential veterinary therapeutic or prophylactic agent. Full article
(This article belongs to the Special Issue Research of Bioactive Substances in Plant Extracts)
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13 pages, 1373 KiB  
Article
Water Extract of Rubus coreanus Prevents Inflammatory Skin Diseases In Vitro Models
by Sumin Pyeon, Ok-Kyung Kim, Ho-Geun Yoon, Shintae Kim, Kyung-Chul Choi, Yoo-Hyun Lee, Jeongmin Lee, Jeongjin Park and Woojin Jun
Plants 2021, 10(6), 1230; https://0-doi-org.brum.beds.ac.uk/10.3390/plants10061230 - 17 Jun 2021
Cited by 3 | Viewed by 2397
Abstract
Atopic dermatitis (AD) is a chronic inflammatory skin disease caused by immune hypersensitivity reaction. The cause of AD is unclear, but its symptoms have a negative effect on quality of life; various treatment methods to alleviate these symptoms are underway. In the present [...] Read more.
Atopic dermatitis (AD) is a chronic inflammatory skin disease caused by immune hypersensitivity reaction. The cause of AD is unclear, but its symptoms have a negative effect on quality of life; various treatment methods to alleviate these symptoms are underway. In the present study, we aimed to evaluate in vitro antioxidant and anti-inflammatory effects of Rubus coreanus water extract (RCW) on AD. Total phenolic compounds and flavonoid content of RCW were 4242.40 ± 54.84 mg GAE/g RCE and 1010.99 ± 14.75 mg CE/g RCW, respectively. RCW reduced intracellular reactive oxygen species level and increased the action of antioxidant enzymes, such as catalase, superoxide dismutase, and glutathione peroxidase in tumor necrosis factor-α (TNF-α)/interferon-γ (IFN-γ)-stimulated HaCaT cells. Moreover, mRNA expression of the pro-inflammatory cytokines, including TNF-α, interleukin-1β, and interleukin-6, was downregulated by RCW in the TNF-α/IFN-γ-stimulated cells. The levels of inflammatory chemokines (thymus- and activation-regulated chemokine; eotaxin; macrophage-derived chemokine; regulated on activation, normal T-cell expressed and secreted; and granulocyte-macrophage colony-stimulating factor) and intercellular adhesion molecule-1 were decreased in the TNF-α/IFN-γ-stimulated HaCaT cells after RCW treatment. Additionally, the mRNA expression levels of filaggrin and involucrin, proteins that form the skin, were increased by RCW. Furthermore, RCW inhibited the nuclear factor kappa-light-chain-enhancer of the activated B cells pathway in the TNF-α/IFN-γ-stimulated HaCaT cells. Collectively, the present investigation indicates that RCW is a potent substance that inhibits AD. Full article
(This article belongs to the Special Issue Research of Bioactive Substances in Plant Extracts)
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11 pages, 2527 KiB  
Article
Inhibition of Solar UV-Induced Matrix Metalloproteinase (MMP)-1 Expression by Non-Enzymatic Softening Cherry Blossom (Prunus yedoensis) Extract
by Yeong-A Jung, Ji-Yoon Lee, Pomjoo Lee, Han-Seung Shin and Jong-Eun Kim
Plants 2021, 10(5), 1016; https://0-doi-org.brum.beds.ac.uk/10.3390/plants10051016 - 19 May 2021
Cited by 3 | Viewed by 2604
Abstract
Cherry blossom (Prunus yedoensis) petals are used as ingredients in many cosmetics. However, despite their use in numerous products, the exact function of cherry blossom petals in cosmetics is unclear. Therefore, we need evidence-based studies to support the labeling claims that [...] Read more.
Cherry blossom (Prunus yedoensis) petals are used as ingredients in many cosmetics. However, despite their use in numerous products, the exact function of cherry blossom petals in cosmetics is unclear. Therefore, we need evidence-based studies to support the labeling claims that are made in cherry blossom products in the cosmetics industry. We investigated the skin anti-aging potential of non-enzymatic softening cherry blossom extract (NES-CBE) in this study. The extract desalinated, to improve its quality such that it can be used as a functional material for the skin. The anti-wrinkle effect of NES-CBE was investigated on human keratinocytes (HaCaT cells) under solar UV (sUV) light exposure. We found that NES-CBE reduced the sUV-induced matrix metalloproteinase (MMP)-1 expression and modulated the transactivation of the activator protein (AP)-1. Furthermore, NES-CBE suppressed the phosphorylation of MEK1/2 and ERK proteins, indicating its regulation of sUV-induced MAPK signaling. Additionally, we observed NES-CBE reduced MMP-1 protein expression in a human skin equivalent model. Taken together, these results suggest that NES-CBE reduces sUV-induced MMP-1 protein expression through reducing AP-1 transactivation via regulation of the MEK1/2-ERK pathway. Full article
(This article belongs to the Special Issue Research of Bioactive Substances in Plant Extracts)
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30 pages, 3376 KiB  
Article
Antiinflammatory Medicinal Plants from the Ugandan Greater Mpigi Region Act as Potent Inhibitors in the COX-2/PGH2 Pathway
by Fabien Schultz, Ogechi Favour Osuji, Barbara Wack, Godwin Anywar and Leif-Alexander Garbe
Plants 2021, 10(2), 351; https://0-doi-org.brum.beds.ac.uk/10.3390/plants10020351 - 12 Feb 2021
Cited by 19 | Viewed by 5654
Abstract
Our study investigates 16 medicinal plants via assessment of inhibition of proinflammatory enzymes such as cyclooxygenases (COX). The plants are used by traditional healers in the Greater Mpigi region in Uganda to treat inflammation and related disorders. We present results of diverse in [...] Read more.
Our study investigates 16 medicinal plants via assessment of inhibition of proinflammatory enzymes such as cyclooxygenases (COX). The plants are used by traditional healers in the Greater Mpigi region in Uganda to treat inflammation and related disorders. We present results of diverse in vitro experiments performed with 76 different plant extracts, namely, (1) selective COX-2 and COX-1 inhibitor screening; (2) 15-LOX inhibition screening; (3) antibacterial resazurin assay against multidrug-resistant Staphylococcus aureus, Listeria innocua, Listeria monocytogenes, and Escherichia coli K12; (4) DPPH assay for antioxidant activity; and (5) determination of the total phenolic content (TPC). Results showed a high correlation between traditional use and pharmacological activity, e.g., extracts of 15 out of the 16 plant species displayed significant selective COX-2 inhibition activity in the PGH2 pathway. The most active COX-2 inhibitors (IC50 < 20 µg/mL) were nine extracts from Leucas calostachys, Solanum aculeastrum, Sesamum calycinum subsp. angustifolium, Plectranthus hadiensis, Morella kandtiana, Zanthoxylum chalybeum, and Warburgia ugandensis. There was no counteractivity between COX-2 and 15-LOX inhibition in these nine extracts. The ethyl acetate extract of Leucas calostachys showed the lowest IC50 value with 0.66 µg/mL (COX-2), as well as the most promising selectivity ratio with 0.1 (COX-2/COX-1). The TPCs and the EC50 values for DPPH radical scavenging activity showed no correlation with COX-2 inhibitory activity. This led to the assumption that the mechanisms of action are most likely not based on scavenging of reactive oxygen species and antioxidant activities. The diethyl ether extract of Harungana madagascariensis stem bark displayed the highest growth inhibition activity against S. aureus (MIC value: 13 µg/mL), L. innocua (MIC value: 40 µg/mL), and L. monocytogenes (MIC value: 150 µg/mL). This study provides further evidence for the therapeutic use of the previously identified plants used medicinally in the Greater Mpigi region. Full article
(This article belongs to the Special Issue Research of Bioactive Substances in Plant Extracts)
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17 pages, 4687 KiB  
Article
Resveratrol Inhibits Venezuelan Equine Encephalitis Virus Infection by Interfering with the AKT/GSK Pathway
by Caitlin W. Lehman, Kylene Kehn-Hall, Megha Aggarwal, Nicole R. Bracci, Han-Chi Pan, Lauren Panny, Robert A. Lamb and Shih-Chao Lin
Plants 2021, 10(2), 346; https://0-doi-org.brum.beds.ac.uk/10.3390/plants10020346 - 12 Feb 2021
Cited by 7 | Viewed by 2739
Abstract
The host proteins Protein Kinase B (AKT) and glycogen synthase kinase-3 (GSK-3) are associated with multiple neurodegenerative disorders. They are also important for the replication of Venezuelan equine encephalitis virus (VEEV), thereby making the AKT/GSK-3 pathway an attractive target for developing anti-VEEV therapeutics. [...] Read more.
The host proteins Protein Kinase B (AKT) and glycogen synthase kinase-3 (GSK-3) are associated with multiple neurodegenerative disorders. They are also important for the replication of Venezuelan equine encephalitis virus (VEEV), thereby making the AKT/GSK-3 pathway an attractive target for developing anti-VEEV therapeutics. Resveratrol, a natural phytochemical, has been shown to substantially inhibit the AKT pathway. Therefore, we attempted to explore whether it exerts any antiviral activity against VEEV. In this study, we utilized green fluorescent protein (GFP)- and luciferase-encoding recombinant VEEV to determine the cytotoxicity and antiviral efficacy via luciferase reporter assays, flow cytometry, and immunofluorescent assays. Our results indicate that resveratrol treatment is capable of inhibiting VEEV replication, resulting in increased viability of Vero and U87MG cells as well as reduced virion production and viral RNA contents within host cells for at least 48 h with a single treatment. Furthermore, the suppression of apoptotic signaling adaptors, caspase-3, caspase-7, and annexin V may also be implicated in resveratrol-mediated antiviral activity. We found that decreased phosphorylation of the AKT/GSK-3 pathway, mediated by resveratrol, can be triggered during the early stages of VEEV infection, suggesting that resveratrol disrupts the viral replication cycle and consequently promotes cell survival. Finally, molecular docking and dynamics simulation studies revealed that resveratrol can directly bind to VEEV glycoproteins, which may interfere with virus attachment and entry. In conclusion, our results suggest that resveratrol exerts inhibitory activity against VEEV infection and upon further modification could be a useful compound to study in neuroprotective research and veterinary sciences. Full article
(This article belongs to the Special Issue Research of Bioactive Substances in Plant Extracts)
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12 pages, 3924 KiB  
Article
Effects of Extra Virgin Olive Oil Polyphenols on Beta-Cell Function and Survival
by Nicola Marrano, Rosaria Spagnuolo, Giuseppina Biondi, Angelo Cignarelli, Sebastio Perrini, Leonardo Vincenti, Luigi Laviola, Francesco Giorgino and Annalisa Natalicchio
Plants 2021, 10(2), 286; https://0-doi-org.brum.beds.ac.uk/10.3390/plants10020286 - 03 Feb 2021
Cited by 18 | Viewed by 2718
Abstract
Extra virgin olive oil (EVOO) is a major component of the Mediterranean diet and is appreciated worldwide because of its nutritional benefits in metabolic diseases, including type 2 diabetes (T2D). EVOO contains significant amounts of secondary metabolites, such as phenolic compounds (PCs), that [...] Read more.
Extra virgin olive oil (EVOO) is a major component of the Mediterranean diet and is appreciated worldwide because of its nutritional benefits in metabolic diseases, including type 2 diabetes (T2D). EVOO contains significant amounts of secondary metabolites, such as phenolic compounds (PCs), that may positively influence the metabolic status. In this study, we investigated for the first time the effects of several PCs on beta-cell function and survival. To this aim, INS-1E cells were exposed to 10 μM of the main EVOO PCs for up to 24 h. Under these conditions, survival, insulin biosynthesis, glucose-stimulated insulin secretion (GSIS), and intracellular signaling activation (protein kinase B (AKT) and cAMP response element-binding protein (CREB)) were evaluated. Hydroxytyrosol, tyrosol, and apigenin augmented beta-cell proliferation and insulin biosynthesis, and apigenin and luteolin enhanced the GSIS. Conversely, vanillic acid and vanillin were pro-apoptotic for beta-cells, even if they increased the GSIS. In addition, oleuropein, p-coumaric, ferulic and sinapic acids significantly worsened the GSIS. Finally, a mixture of hydroxytyrosol, tyrosol, and apigenin promoted the GSIS in human pancreatic islets. Apigenin was the most effective compound and was also able to activate beneficial intracellular signaling. In conclusion, this study shows that hydroxytyrosol, tyrosol, and apigenin foster beta-cells’ health, suggesting that EVOO or supplements enriched with these compounds may improve insulin secretion and promote glycemic control in T2D patients. Full article
(This article belongs to the Special Issue Research of Bioactive Substances in Plant Extracts)
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9 pages, 835 KiB  
Article
Study of Bio-Pharmaceutical and Antimicrobial Properties of Pomegranate (Punica granatum L.) Leathery Exocarp Extract
by Hazem S. Elshafie, Lucia Caputo, Laura De Martino, Shimaa H. Sakr, Vincenzo De Feo and Ippolito Camele
Plants 2021, 10(1), 153; https://0-doi-org.brum.beds.ac.uk/10.3390/plants10010153 - 14 Jan 2021
Cited by 33 | Viewed by 4011
Abstract
Pomegranate (Punica granatum L.) fruits are important sources of vitamins and minerals and widely used in the dietary supplement industry. An aqueous extract of its leathery exocarp (LEP) was obtained by a solid-phase micro-extraction method. The antifungal activity was examined against the [...] Read more.
Pomegranate (Punica granatum L.) fruits are important sources of vitamins and minerals and widely used in the dietary supplement industry. An aqueous extract of its leathery exocarp (LEP) was obtained by a solid-phase micro-extraction method. The antifungal activity was examined against the phytopathogenic fungi, Fusarium oxysporum, Phytophthora cinnamomi, Penicillium digitatum and Botrytis cinerea, and the antibacterial activity was evaluated against Escherichia coli, Xanthomonas campestris,Bacillus megaterium and Clavibacter michiganensis. The antimicrobial assays showed, in some cases, a promising antimicrobial effect compared to the synthetic drugs. The possible anti-acetylcholinesterase and antioxidant activities of the LEP extract were investigated by the Ellman’s assay and 2,2-diphenyl-1-picrylhydrazyl (DPPH) test, respectively, and their results showed that the LEP extract has an effective anti-acetylcholinesterase inhibitory effect and an antioxidant activity. Thus, the LEP extract could be valid as a candidate for further studies on the use of pomegranate in neurodegenerative diseases as a food preservative and a suitable substitute to control several phytopathogens. Full article
(This article belongs to the Special Issue Research of Bioactive Substances in Plant Extracts)
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12 pages, 1859 KiB  
Article
Anti-Aging Potential of Extracts from Washingtonia filifera Seeds
by Benedetta Era, Sonia Floris, Valeria Sogos, Clara Porcedda, Alessandra Piras, Rosaria Medda, Antonella Fais and Francesca Pintus
Plants 2021, 10(1), 151; https://0-doi-org.brum.beds.ac.uk/10.3390/plants10010151 - 14 Jan 2021
Cited by 18 | Viewed by 3157
Abstract
The aim of this study was to test the inhibitory effect of fruit extracts from Washingtonia filifera on skin aging-related enzymes. The pulp extracts did not exert a significant enzyme inhibition while seed extracts from W. filifera exhibit anti-elastase, anti-collagenase, and anti-tyrosinase activities. [...] Read more.
The aim of this study was to test the inhibitory effect of fruit extracts from Washingtonia filifera on skin aging-related enzymes. The pulp extracts did not exert a significant enzyme inhibition while seed extracts from W. filifera exhibit anti-elastase, anti-collagenase, and anti-tyrosinase activities. Tyrosinase was mildly inhibited while a stronger effect was observed with respect to elastase and collagenase inhibition. Alcoholic extracts provided better results than aqueous extracts. Among them, methanol extracts showed the prominent enzyme inhibitory activities being IC50 value for elastase and collagenase comparable and even better than the reference compound. The inhibition mode of the most active extracts was investigated by Lineweaver-Burk plot analysis. Seed extracts from W. filifera were also investigated for their photo-protective effect by Mansur equation and the antioxidant activity of W. filifera extract was evaluated in oxidative-stressed cells. To evaluate the safety of the extract, the effect on cell viability of human keratinocytes cells was analyzed. Methanol extract presented the best photo-protective effect and exerted an antioxidant activity in a cellular system with no cytotoxic effect. The overall results demonstrate that W. filifera extracts are promising sources of bioactive compounds that could be used in cosmetic and pharmaceutical preparation. Full article
(This article belongs to the Special Issue Research of Bioactive Substances in Plant Extracts)
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17 pages, 10136 KiB  
Article
Alleviation of Collagen-Induced Arthritis by Crotonoside through Modulation of Dendritic Cell Differentiation and Activation
by Shih-Chao Lin, Chi-Chien Lin, Shiming Li, Wan-Yi Lin, Caitlin W. Lehman, Nicole R. Bracci and Sen-Wei Tsai
Plants 2020, 9(11), 1535; https://0-doi-org.brum.beds.ac.uk/10.3390/plants9111535 - 10 Nov 2020
Cited by 6 | Viewed by 2650
Abstract
Crotonoside, a guanosine analog originally isolated from Croton tiglium, is reported to be a potent tyrosine kinase inhibitor with immunosuppressive effects on immune cells. Due to its potential immunotherapeutic effects, we aimed to evaluate the anti-arthritic activity of crotonoside and explore its [...] Read more.
Crotonoside, a guanosine analog originally isolated from Croton tiglium, is reported to be a potent tyrosine kinase inhibitor with immunosuppressive effects on immune cells. Due to its potential immunotherapeutic effects, we aimed to evaluate the anti-arthritic activity of crotonoside and explore its immunomodulatory properties in alleviating the severity of arthritic symptoms. To this end, we implemented the treatment of crotonoside on collagen-induced arthritic (CIA) DBA/1 mice and investigated its underlying mechanisms towards pathogenic dendritic cells (DCs). Our results suggest that crotonoside treatment remarkably improved clinical arthritic symptoms in this CIA mouse model as indicated by decreased pro-inflammatory cytokine production in the serum and suppressed expression of co-stimulatory molecules, CD40, CD80, and MHC class II, on CD11c+ DCs from the CIA mouse spleens. Additionally, crotonoside treatment significantly reduced the infiltration of CD11c+ DCs into the synovial tissues. Our in vitro study further demonstrated that bone marrow-derived DCs (BMDCs) exhibited lower yield in numbers and expressed lower levels of CD40, CD80, and MHC-II when incubated with crotonoside. Furthermore, LPS-stimulated mature DCs exhibited limited capability to prime antigen-specific CD4+ and T-cell proliferation, cytokine secretions, and co-stimulatory molecule expressions when treated with crotonoside. Our pioneer study highlights the immunotherapeutic role of crotonoside in the alleviation of the CIA via modulation of pathogenic DCs, thus creating possible applications of crotonoside as an immunosuppressive agent that could be utilized and further explored in treating autoimmune disorders in the future. Full article
(This article belongs to the Special Issue Research of Bioactive Substances in Plant Extracts)
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Review

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14 pages, 527 KiB  
Review
Revisiting Trigonella foenum-graecum L.: Pharmacology and Therapeutic Potentialities
by Theysshana Visuvanathan, Leslie Thian Lung Than, Johnson Stanslas, Shu Yih Chew and Shalini Vellasamy
Plants 2022, 11(11), 1450; https://0-doi-org.brum.beds.ac.uk/10.3390/plants11111450 - 29 May 2022
Cited by 24 | Viewed by 4248
Abstract
Fenugreek (Trigonella foenum-graecum L.) is a medicinal plant that has been used as a food condiment as well as for its multiple therapeutic characteristics since ancient times. Fenugreek plant grows up to 60 cm in height, and its seeds are golden-yellow rhomboidal-shaped. [...] Read more.
Fenugreek (Trigonella foenum-graecum L.) is a medicinal plant that has been used as a food condiment as well as for its multiple therapeutic characteristics since ancient times. Fenugreek plant grows up to 60 cm in height, and its seeds are golden-yellow rhomboidal-shaped. Though fenugreek is more commonly known for its seeds, the leaves and stem have also been reported to have medicinal uses. These properties exhibited are due to the content of the secondary metabolites, also known as phytochemicals, in the fenugreek plant. Such metabolites are alkaloids, saponins, tannins, phenols, and many others. Fenugreek has been used traditionally for numerous indications, such as aid in labour, lactation stimulant, and laxatives. In modern research, there have been several animal and clinical studies that have shown therapeutic effects of fenugreek when taken orally. Fenugreek is a suitable plant candidate with a high prospect of being used as a credible medicinal plant to derive new drugs. This review aims to summarize the physical and chemical properties of fenugreek and its bioactive compounds that have been isolated for medicinal purposes and discusses the traditional and pharmacological uses of fenugreek. Full article
(This article belongs to the Special Issue Research of Bioactive Substances in Plant Extracts)
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22 pages, 17084 KiB  
Review
Euphorbia characias: Phytochemistry and Biological Activities
by Antonella Fais, Giovanna Lucia Delogu, Sonia Floris, Benedetta Era, Rosaria Medda and Francesca Pintus
Plants 2021, 10(7), 1468; https://0-doi-org.brum.beds.ac.uk/10.3390/plants10071468 - 17 Jul 2021
Cited by 8 | Viewed by 3720
Abstract
The aim of this review is to summarize all the compounds identified and characterized from Euphorbia characias, along with the biological activities reported for this plant. Euphorbia is one of the greatest genera in the spurge family of Euphorbiaceae and includes different [...] Read more.
The aim of this review is to summarize all the compounds identified and characterized from Euphorbia characias, along with the biological activities reported for this plant. Euphorbia is one of the greatest genera in the spurge family of Euphorbiaceae and includes different kinds of plants characterized by the presence of milky latex. Among them, the species Euphorbia characias L. is an evergreen perennial shrub widely distributed in Mediterranean countries. E. characias latex and extracts from different parts of the plant have been extensively studied, leading to the identification of several chemical components such as terpenoids, sterol hydrocarbons, saturated and unsaturated fatty acids, cerebrosides and phenolic and carboxylic acids. The biological properties range between antioxidant activities, antimicrobial, antiviral and pesticidal activities, wound-healing properties, anti-aging and hypoglycemic properties and inhibitory activities toward target enzymes related to different diseases, such as cholinesterases and xanthine oxidase. The information available in this review allows us to consider the plant E. characias as a potential source of compounds for biomedical research. Full article
(This article belongs to the Special Issue Research of Bioactive Substances in Plant Extracts)
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17 pages, 3754 KiB  
Review
Pharmacological Exploration of Phenolic Compound: Raspberry Ketone—Update 2020
by Shailaja Rao, Mallesh Kurakula, Nagarjuna Mamidipalli, Papireddy Tiyyagura, Bhaumik Patel and Ravi Manne
Plants 2021, 10(7), 1323; https://0-doi-org.brum.beds.ac.uk/10.3390/plants10071323 - 29 Jun 2021
Cited by 13 | Viewed by 5803
Abstract
Raspberry ketone (RK) is an aromatic phenolic compound naturally occurring in red raspberries, kiwifruit, peaches, and apples and reported for its potential therapeutic and nutraceutical properties. Studies in cells and rodents have suggested an important role for RK in hepatic/cardio/gastric protection and as [...] Read more.
Raspberry ketone (RK) is an aromatic phenolic compound naturally occurring in red raspberries, kiwifruit, peaches, and apples and reported for its potential therapeutic and nutraceutical properties. Studies in cells and rodents have suggested an important role for RK in hepatic/cardio/gastric protection and as an anti-hyperlipidemic, anti-obesity, depigmentation, and sexual maturation agent. Raspberry ketone-mediated activation of peroxisome proliferator-activated receptor-α (PPAR-α) stands out as one of its main modes of action. Although rodent studies have demonstrated the efficacious effects of RK, its mechanism remains largely unknown. In spite of a lack of reliable human research, RK is marketed as a health supplement, at very high doses. In this review, we provide a compilation of scientific research that has been conducted so far, assessing the therapeutic properties of RK in several disease conditions as well as inspiring future research before RK can be considered safe and efficacious with limited side effects as an alternative to modern medicines in the treatment of major lifestyle-based diseases. Full article
(This article belongs to the Special Issue Research of Bioactive Substances in Plant Extracts)
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31 pages, 470 KiB  
Review
A Review on Cistus sp.: Phytochemical and Antimicrobial Activities
by Imane Zalegh, Mohamed Akssira, Mohammed Bourhia, Fouad Mellouki, Naima Rhallabi, Ahmad Mohammad Salamatullah, Mohammed Saeed Alkaltham, Heba Khalil Alyahya and Rajaa Ait Mhand
Plants 2021, 10(6), 1214; https://0-doi-org.brum.beds.ac.uk/10.3390/plants10061214 - 15 Jun 2021
Cited by 30 | Viewed by 6581
Abstract
Resistance to drugs is reaching alarming levels and is placing human health at risk. With the lack of new antimicrobials drugs, infectious diseases are becoming harder to treat. Hence, there is an increasing awareness of active phytochemicals with therapeutic functions. The tremendous research [...] Read more.
Resistance to drugs is reaching alarming levels and is placing human health at risk. With the lack of new antimicrobials drugs, infectious diseases are becoming harder to treat. Hence, there is an increasing awareness of active phytochemicals with therapeutic functions. The tremendous research interest on the Cistus L. genus includes numerous plants used in traditional medicine by people living around the Mediterranean Sea, also resulted in some interesting discoveries and written literature. This review aimed at gathering scientific literature about Cistus species, describing phytochemical profiles and the various pharmacological activities. We also extensively reviewed the antimicrobial activities, including antiviral, antiparasitic, antifungal, and antibacterial potentials of Essential Oils (EO), raw extracts as well as isolated compounds. Mechanisms of action along with methods used are also investigated in this review. Considering the findings of the Cistus species extracts, this genus offers an adequate reserve of active phytochemicals since many have been used to create drugs. Therefore, this review work can serve society by providing a global view on Cistus L. sp. regarding pharmacological potentials and their chemical profiles. Full article
(This article belongs to the Special Issue Research of Bioactive Substances in Plant Extracts)
17 pages, 2873 KiB  
Review
Non-Cannabinoid Metabolites of Cannabis sativa L. with Therapeutic Potential
by Henry Lowe, Blair Steele, Joseph Bryant, Ngeh Toyang and Wilfred Ngwa
Plants 2021, 10(2), 400; https://0-doi-org.brum.beds.ac.uk/10.3390/plants10020400 - 20 Feb 2021
Cited by 45 | Viewed by 8321
Abstract
The cannabis plant (Cannabis sativa L.) produces an estimated 545 chemical compounds of different biogenetic classes. In addition to economic value, many of these phytochemicals have medicinal and physiological activity. The plant is most popularly known for its two most-prominent and most-studied [...] Read more.
The cannabis plant (Cannabis sativa L.) produces an estimated 545 chemical compounds of different biogenetic classes. In addition to economic value, many of these phytochemicals have medicinal and physiological activity. The plant is most popularly known for its two most-prominent and most-studied secondary metabolites—Δ9-tetrahydrocannabinol (Δ9-THC) and cannabidiol (CBD). Both Δ9-THC and CBD have a wide therapeutic window across many ailments and form part of a class of secondary metabolites called cannabinoids—of which approximately over 104 exist. This review will focus on non-cannabinoid metabolites of Cannabis sativa that also have therapeutic potential, some of which share medicinal properties similar to those of cannabinoids. The most notable of these non-cannabinoid phytochemicals are flavonoids and terpenes. We will also discuss future directions in cannabis research and development of cannabis-based pharmaceuticals. Caflanone, a flavonoid molecule with selective activity against the human viruses including the coronavirus OC43 (HCov-OC43) that is responsible for COVID-19, and certain cancers, is one of the most promising non-cannabinoid molecules that is being advanced into clinical trials. As validated by thousands of years of the use of cannabis for medicinal purposes, vast anecdotal evidence abounds on the medicinal benefits of the plant. These benefits are attributed to the many phytochemicals in this plant, including non-cannabinoids. The most promising non-cannabinoids with potential to alleviate global disease burdens are discussed. Full article
(This article belongs to the Special Issue Research of Bioactive Substances in Plant Extracts)
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53 pages, 1560 KiB  
Review
So Uncommon and so Singular, but Underexplored: An Updated Overview on Ethnobotanical Uses, Biological Properties and Phytoconstituents of Sardinian Endemic Plants
by Cinzia Sanna, Andrea Maxia, Giuseppe Fenu and Maria Cecilia Loi
Plants 2020, 9(8), 958; https://0-doi-org.brum.beds.ac.uk/10.3390/plants9080958 - 29 Jul 2020
Cited by 17 | Viewed by 3940
Abstract
The last decades have recorded an increase of plant-based drug discovery processes. Indeed, natural products possess a superior chemical diversity as compared to synthetic ones, leading to a renewal in searching for new therapeutic agents from the plant kingdom. In particular, since the [...] Read more.
The last decades have recorded an increase of plant-based drug discovery processes. Indeed, natural products possess a superior chemical diversity as compared to synthetic ones, leading to a renewal in searching for new therapeutic agents from the plant kingdom. In particular, since the structural variety of natural compounds reflects the biodiversity of their source organisms, regions of the world with high biodiversity and endemism deserve particular interest. In this context, Sardinia Island (Italy), with 290 endemic taxa (12% of the total flora), is expected to provide unique and structurally diverse phytochemicals for drug development. Several research groups built up a large program dedicated to the analysis of Sardinian endemic species, highlighting their peculiar features, both in respect of phytochemical and biological profiles. On this basis, the aim of this review is to provide an up-to-date and comprehensive overview on ethnobotanical uses, biological properties and phytoconstituents of Sardinian endemic plants in order to support their beneficial potential and to provide input for future investigations. We documented 152 articles published from 1965 to June 2020 in which a broad range of biological activities and the identification of previously undescribed compounds have been reported, supporting their great value as sources of therapeutic agents. Full article
(This article belongs to the Special Issue Research of Bioactive Substances in Plant Extracts)
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