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Biological Properties of Plant Bioactive Compounds

A special issue of International Journal of Molecular Sciences (ISSN 1422-0067). This special issue belongs to the section "Bioactives and Nutraceuticals".

Deadline for manuscript submissions: closed (15 September 2022) | Viewed by 21936

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Guest Editor
Institute of Crop Sciences, Chinese Academy of Agricultural Sciences, Beijing 100081, China
Interests: minor crop; bioactive compounds; gene regulation; biosynthesis pathways
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

In recent years, demand has increased for plants and so they have attracted the attention of nutritional and medical scientists due to their bioactive compounds and high efficacy as functional foods and medicines with healing effects over chronic diseases, exhibiting antitumor, anti-inflammatory and anti-diabetic activities, etc. Additionally, these bioactive compounds also play important roles in mediating plant–plant, plant–microorganism or plant–environment interactions to maintain ecological and environmental sustainable development.

In this Special Issue for IJMS, we will focus on the important roles of bioactive compounds from plants in human health and disease, as well as in plant–environment interactions and their potential for maintaining ecological balances. Research papers and up-to-date review articles are welcome

Dr. Meiliang Zhou
Prof. Dr. Milen I. Georgiev
Guest Editors

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Keywords

  • plants
  • bioactive compounds
  • biological properties

Published Papers (12 papers)

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Research

21 pages, 1946 KiB  
Article
Genomic, Molecular, and Phenotypic Characterization of Arthrobacter sp. OVS8, an Endophytic Bacterium Isolated from and Contributing to the Bioactive Compound Content of the Essential Oil of the Medicinal Plant Origanum vulgare L.
by Giulia Semenzato, Sara Del Duca, Alberto Vassallo, Angela Bechini, Carmela Calonico, Vania Delfino, Fabiola Berti, Francesco Vitali, Stefano Mocali, Angela Frascella, Giovanni Emiliani and Renato Fani
Int. J. Mol. Sci. 2023, 24(5), 4845; https://0-doi-org.brum.beds.ac.uk/10.3390/ijms24054845 - 02 Mar 2023
Cited by 3 | Viewed by 1900
Abstract
Medicinal plants play an important role in the discovery of new bioactive compounds with antimicrobial activity, thanks to their pharmacological properties. However, members of their microbiota can also synthesize bioactive molecules. Among these, strains belonging to the genera Arthrobacter are commonly found associated [...] Read more.
Medicinal plants play an important role in the discovery of new bioactive compounds with antimicrobial activity, thanks to their pharmacological properties. However, members of their microbiota can also synthesize bioactive molecules. Among these, strains belonging to the genera Arthrobacter are commonly found associated with the plant’s microenvironments, showing plant growth-promoting (PGP) activity and bioremediation properties. However, their role as antimicrobial secondary metabolite producers has not been fully explored. The aim of this work was to characterize the Arthrobacter sp. OVS8 endophytic strain, isolated from the medicinal plant Origanum vulgare L., from molecular and phenotypic viewpoints to evaluate its adaptation and influence on the plant internal microenvironments and its potential as a producer of antibacterial volatile molecules (VOCs). Results obtained from the phenotypic and genomic characterization highlight its ability to produce volatile antimicrobials effective against multidrug-resistant (MDR) human pathogens and its putative PGP role as a producer of siderophores and degrader of organic and inorganic pollutants. The outcomes presented in this work identify Arthrobacter sp. OVS8 as an excellent starting point toward the exploitation of bacterial endophytes as antibiotics sources. Full article
(This article belongs to the Special Issue Biological Properties of Plant Bioactive Compounds)
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15 pages, 3902 KiB  
Article
Effects of Ascorbic Acid on Physiological Characteristics during Somatic Embryogenesis of Fraxinus mandshurica
by Xue Cheng, Tianyi Xie, Ling Yang and Hailong Shen
Int. J. Mol. Sci. 2023, 24(1), 289; https://0-doi-org.brum.beds.ac.uk/10.3390/ijms24010289 - 24 Dec 2022
Cited by 1 | Viewed by 1169
Abstract
Fraxinus mandshurica is one of the precious tree species in northeast China and has important economic and ecological value. Ascorbic acid (ASA) is a strong antioxidant that can significantly improve plant photosynthetic efficiency and stress resistance and participate widely in plant growth and [...] Read more.
Fraxinus mandshurica is one of the precious tree species in northeast China and has important economic and ecological value. Ascorbic acid (ASA) is a strong antioxidant that can significantly improve plant photosynthetic efficiency and stress resistance and participate widely in plant growth and development. In this study, we investigated the development process of mature zygotic embryos of F. mandshurica under different concentrations of ASA and found that 100 mg·L−1 exogenous ASA was the optimal concentration and that the induction rate of somatic embryos (SEs) was the highest at 72.89%, which was 7.13 times higher than that of the control group. The polyphenol content, peroxidase (POD) activity, nitric oxide (NO) content, nitrate reductase (NR) activity, total ascorbic acid (T-ASA) content, ASA content, ASA/Dehydroascorbic acid (DHA) ratio, GSH/GSSG ratio, and ascorbate peroxidase (APX) activity were significantly increased under the application of exogenous ASA in explants, whereas the polyphenol oxidase (PPO) activity, phenylalanine ammonia-lyase (PAL) activity, superoxide dismutase (SOD) activity, and catalase (CAT) activity, malondialdehyde (MDA) content and nitric oxide synthase (NOS) activity were decreased. At the same time, the content of T-ASA and ASA, T-GSH and GSSG, and PAL and SOD had the same change pattern in the control group and the treatment group. These results suggested that high or low concentrations of ASA could not promote the somatic embryogenesis of F. mandshurica and that exogenous ASA had significant effects on the physiology of F. mandshurica explants. ASA was also highly related to somatic embryogenesis and the explant browning of F. mandshurica. Our results could provide a reference for further study on the browning mechanism of F. mandshurica explants and lay the foundation for optimizing the condition of somatic embryogenesis in F. mandshurica. Full article
(This article belongs to the Special Issue Biological Properties of Plant Bioactive Compounds)
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11 pages, 4409 KiB  
Communication
Bioassay-Guided Isolation of Anthelmintic Components from Semen pharbitidis, and the Mechanism of Action of Pharbitin
by Maoxuan Liu, Jing-Guang Lu, Ming-Rong Yang, Zhi-Hong Jiang, Xiaochun Wan and Walter Luyten
Int. J. Mol. Sci. 2022, 23(24), 15739; https://0-doi-org.brum.beds.ac.uk/10.3390/ijms232415739 - 12 Dec 2022
Cited by 2 | Viewed by 1311
Abstract
Parasitic helminths continue to pose problems in human and veterinary medicine, as well as in agriculture. Semen pharbitidis, the seeds of Pharbitis nil (Linn.) Choisy (Convolvulaceae), is a well-known traditional Chinese medicinal botanical preparation widely used for treating intestinal parasites in China [...] Read more.
Parasitic helminths continue to pose problems in human and veterinary medicine, as well as in agriculture. Semen pharbitidis, the seeds of Pharbitis nil (Linn.) Choisy (Convolvulaceae), is a well-known traditional Chinese medicinal botanical preparation widely used for treating intestinal parasites in China owing to its desirable efficacy. However, the anthelmintic compounds in Semen pharbitidis and their mechanism of action have not been investigated yet. This study aimed to identify the compounds active against helminths from Semen pharbitidis, and to establish the mechanism of action of these active compounds. Bioassay-guided fractionation was used to identify the anthelmintic compounds from Semen pharbitidis. The anthelmintic assay was performed by monitoring Caenorhabditis elegans (C. elegans) motility with a WMicrotracker instrument. Active compounds were identified by high-resolution mass spectrometry. Several (analogues of) fragments of the anthelmintic compounds were purchased and tested to explore the structure–activity relationship, and to find more potent compounds. A panel of C. elegans mutant strains resistant to major currently used anthelmintic drugs was used to explore the mechanism of action of the active compounds. The bioassay-guided isolation from an ethanol extract of Semen pharbitidis led to a group of glycosides, namely pharbitin (IC50: 41.0 ± 9.4 μg/mL). Hit expansion for pharbitin fragments yielded two potent analogues: 2-bromohexadecanoic acid (IC50: 1.6 ± 0.7 μM) and myristoleic acid (IC50: 35.2 ± 7.6 μM). One drug-resistant mutant ZZ37 unc-63 (x37) demonstrated a ~17-fold increased resistance to pharbitin compared with wild-type worms. Collectively, we provide further experimental scientific evidence to support the traditional use of Semen pharbitidis for the treatment of intestinal parasites. The anthelmintic activity of Semen pharbitidis is due to pharbitin, whose target could be UNC-63 in C. elegans. Full article
(This article belongs to the Special Issue Biological Properties of Plant Bioactive Compounds)
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10 pages, 1157 KiB  
Communication
Phytochemical and Antioxidant Profile of the Medicinal Plant Melia azedarach Subjected to Water Deficit Conditions
by Maria Celeste Dias, Diana C. G. A. Pinto, Maria Costa, Márcia Araújo, Conceição Santos and Artur M. S. Silva
Int. J. Mol. Sci. 2022, 23(21), 13611; https://0-doi-org.brum.beds.ac.uk/10.3390/ijms232113611 - 06 Nov 2022
Viewed by 1536
Abstract
Environmental stress triggered by climate change can alter the plant’s metabolite profile, which affects its physiology and performance. This is particularly important in medicinal species because their economic value depends on the richness of their phytocompounds. We aimed to characterize how water deficit [...] Read more.
Environmental stress triggered by climate change can alter the plant’s metabolite profile, which affects its physiology and performance. This is particularly important in medicinal species because their economic value depends on the richness of their phytocompounds. We aimed to characterize how water deficit modulated the medicinal species Melia azedarach’s lipophilic profile and antioxidant status. Young plants were exposed to water deficit for 20 days, and lipophilic metabolite profile and the antioxidant capacity were evaluated. Leaves of M. azedarach are rich in important fatty acids and oleamide. Water deficit increased the radical scavenging capacity, total phenol, flavonoids, and catechol pools, and the accumulation of β-sitosterol, myo-inositol, succinic acid, sucrose, d-glucose and derivatives, d-psicofuranose, d-(+)-fructofuranose, and the fatty acids stearic, α-linolenic, linoleic and palmitic acids. These responses are relevant to protecting the plant against climate change-related stress and also increase the nutritional and antioxidant quality of M. azedarach leaves. Full article
(This article belongs to the Special Issue Biological Properties of Plant Bioactive Compounds)
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16 pages, 3515 KiB  
Article
Deodorized Garlic Decreases Oxidative Stress Caused by Lipopolysaccharide in Rat Heart through Hydrogen Sulfide: Preliminary Findings
by Israel Pérez-Torres, Linaloe Manzano-Pech, Verónica Guarner-Lans, María Elena Soto, Vicente Castrejón-Téllez, Ricardo Márquez-Velasco, Álvaro Vargas-González, Raúl Martínez-Memije, Leonardo Del Valle-Mondragón, Julieta Anabell Díaz-Juárez, María Sánchez-Aguilar and Juan Carlos Torres-Narváez
Int. J. Mol. Sci. 2022, 23(20), 12529; https://0-doi-org.brum.beds.ac.uk/10.3390/ijms232012529 - 19 Oct 2022
Cited by 3 | Viewed by 1368
Abstract
Deodorized garlic (DG) may favor the activity of the antioxidant enzymes and promote the synthesis of hydrogen sulfide (H2S). The objective was to test if DG favors an increase in H2S and if it decreases the oxidative stress caused [...] Read more.
Deodorized garlic (DG) may favor the activity of the antioxidant enzymes and promote the synthesis of hydrogen sulfide (H2S). The objective was to test if DG favors an increase in H2S and if it decreases the oxidative stress caused by lipopolysaccharide (LPS) in rat hearts. A total of 24 rats were divided into 4 groups: Group 1 control (C), Group 2 LPS, Group 3 DG, and Group 4 LPS plus DG. The cardiac mechanical performance (CMP), coronary vascular resistance (CVR), and oxidative stress markers, such as total antioxidant capacity (TAC), glutathione (GSH), selenium (Se), lipid peroxidation (LPO), thiols, hydrogen sulfide (H2S), and the activities and expressions of thioredoxin reductase (TrxR), glutathione peroxidase (GPx), and glutathione-S-transferase (GST), cystathionine synthetase (CBS), cystathionine γ-lyase (CTH), iNOS, and eNOS-p, were analyzed in the heart. Infarct zones in the cardiac tissue were present (p = 0.01). The CMP and CVR decreased and increased (p ≤ 0.05), TAC, GSH, H2S, NO, thiols, and GST activity (p ≤ 0.01) decreased, and LPO and iNOS increased (p ≤ 0.05). The activities and expressions of TrxR, GPx, eNOS-p, CTH, and CBS (p ≤ 0.05) decreased with the LPS treatment; however, DG normalized this effect. DG treatment decreases heart damage caused by LPS through the cross-talk between the H2S and NO systems. Full article
(This article belongs to the Special Issue Biological Properties of Plant Bioactive Compounds)
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20 pages, 3514 KiB  
Article
Diversity and Biological Activities of Endophytic Fungi from the Flowers of the Medicinal Plant Vernonia anthelmintica
by Litao Niu, Nigora Rustamova, Huxia Ning, Paiziliya Paerhati, Chunfang Lu and Abulimiti Yili
Int. J. Mol. Sci. 2022, 23(19), 11935; https://0-doi-org.brum.beds.ac.uk/10.3390/ijms231911935 - 08 Oct 2022
Cited by 8 | Viewed by 2105
Abstract
Secondary metabolites produced by endophytic fungi are an important source of biologically active compounds. The current research was focused on the biological activities of ethyl acetate extracts of fungi, isolated and identified from Vernonia anthelmintica flowers for the first time. In addition, an [...] Read more.
Secondary metabolites produced by endophytic fungi are an important source of biologically active compounds. The current research was focused on the biological activities of ethyl acetate extracts of fungi, isolated and identified from Vernonia anthelmintica flowers for the first time. In addition, an investigation of the non-polar chemical composition of dichloromethane-ethyl acetate extracts of the most active fungal strain was carried out. The isolates included Ovatospora senegalensis NR-03, Chaetomium globosum NR-04, Thielavia subthermophila NR-06, Aspergillus calidoustus NR-10, Aspergillus keveii XJF-23 and Aspergillus terreus XJF-3 species. Strains were identified by 18S rRNA gene sequencing methods and were registered in GenBank. Crude extracts of the fungi displayed in vitro biological activities, including antimicrobial and cytotoxic activities. A melanin content assay was performed on murine B16 cells. An ethyl acetate extract of O. senegalensis NR-03 showed high anticancer and antimicrobial activity; therefore, we also studied the non-polar chemical composition of the dichloromethane-ethyl acetate fraction and identified 52 non-polar compounds with the different medium. This investigation discovered that the secondary metabolites of the total extract of endophytic fungi could be a potential source of alternative natural antimicrobial, cytotoxic and melanin synthesis activity in their host plant, and the isolation of bioactive metabolites may provide a lead to new compounds of pharmaceutical significance. Full article
(This article belongs to the Special Issue Biological Properties of Plant Bioactive Compounds)
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14 pages, 3410 KiB  
Article
The Isolation and Preparation of Samwinol from Dracocephalum heterophyllum and Prevention on Aβ25–35-Induced Neuroinflammation in PC-12 Cells
by Chengzhao Li, Jun Dang, Yue Lv, Yan Fang, Chengjun Ma, Qilan Wang and Gang Li
Int. J. Mol. Sci. 2022, 23(19), 11572; https://0-doi-org.brum.beds.ac.uk/10.3390/ijms231911572 - 30 Sep 2022
Cited by 2 | Viewed by 1362
Abstract
Dracocephalum heterophyllum (D. heterophyllum) is a traditional Chinese Tibetan medicine that has been used for the treatment of lymphitis, hepatitis, and bronchitis. However, only a few selected chemical components are currently obtained from D. heterophyllum, which limits its further [...] Read more.
Dracocephalum heterophyllum (D. heterophyllum) is a traditional Chinese Tibetan medicine that has been used for the treatment of lymphitis, hepatitis, and bronchitis. However, only a few selected chemical components are currently obtained from D. heterophyllum, which limits its further pharmacological applications. In this study, we have obtained samwinol from D. heterophyllum by medium- and high-pressure liquid chromatography separation for the first time. Thereafter, we investigated the protective actions of samwinol against amyloid beta protein fragment 25–35 (Aβ25–35) induced neurotoxicity in cultured rat pheochromocytoma PC-12 cells and explored its underlying mechanisms of action. The results indicated that samwinol could increase cell viability and inhibit the production of reactive oxygen species (ROS) and mitochondria-derived ROS, as assessed by MTT assay, Giemsa staining, and flow cytometry assay. Through Western blot analysis, it was found that samwinol substantially inhibited the phosphorylation of ERK(1/2) and promoted the expression of HO-1 and Nrf2. The data obtained from molecular docking were also consistent with the above conclusions. All of these results showed that samwinol from D. heterophyllum can display significant anti-neuroinflammatory and antioxidant activities in vitro, which are associated with the suppression of ERK/AKT phosphorylation and the activation of the Nrf2/HO-1 signaling pathway. In the future, additional in-depth mechanism studies will be carried out to provide more evidence for the potential of samwinol in the treatment of Alzheimer’s disease. Full article
(This article belongs to the Special Issue Biological Properties of Plant Bioactive Compounds)
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11 pages, 1671 KiB  
Article
Pharmacokinetics of Myo-Inositol in a Wistar Rat Animal Model
by Tomasz Antonowski, Adam Osowski, Damian Szczesny, Joanna Szablińska-Piernik, Jerzy Juśkiewicz, Lesław Lahuta, Andrzej Rynkiewicz and Joanna Wojtkiewicz
Int. J. Mol. Sci. 2022, 23(19), 11246; https://0-doi-org.brum.beds.ac.uk/10.3390/ijms231911246 - 24 Sep 2022
Cited by 1 | Viewed by 1613
Abstract
Myo-inositol is the most popular inositol in living organisms, where it is present as a sugar alcohol, in a free form, and can also be described as a lipid. The aim of this study was to check the concentration change of a [...] Read more.
Myo-inositol is the most popular inositol in living organisms, where it is present as a sugar alcohol, in a free form, and can also be described as a lipid. The aim of this study was to check the concentration change of a myo-inositol solution from the time of oral administration and over a 48 h period in Wistar-type rats. All rats received 2 g/kg of inositol as a solution in distilled water by oral gavage. Estimated parameters were based on the serum concentration of myo-inositol observed in nine individual rats with regard to time. Observations were described as a one-compartment pharmacokinetic model with first-order absorption and zero-order endogenous input of checked inositol. The highest myo-inositol concentration was observed in the first hour after oral administration in the serum of all tested rats. Then, the concentration began decreasing immediately after the maximal peak. The inositol concentration continued to decrease, but after 24 h its level was still higher than before the administration. The plasma profile of the myo-inositol concentration showed a rapid decline over time, possibly due to the metabolism of this compound. Full article
(This article belongs to the Special Issue Biological Properties of Plant Bioactive Compounds)
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15 pages, 5133 KiB  
Article
Studies on the Phytochemical Profile of Ocimum basilicum var. minimum (L.) Alef. Essential Oil, Its Larvicidal Activity and In Silico Interaction with Acetylcholinesterase against Aedes aegypti (Diptera: Culicidae)
by Anderson de Santana Botelho, Oberdan Oliveira Ferreira, Mozaniel Santana de Oliveira, Jorddy Neves Cruz, Sandro Henrique dos Reis Chaves, Alejandro Ferraz do Prado, Lidiane Diniz do Nascimento, Geilson Alcantara da Silva, Cristine Bastos do Amarante and Eloisa Helena de Aguiar Andrade
Int. J. Mol. Sci. 2022, 23(19), 11172; https://0-doi-org.brum.beds.ac.uk/10.3390/ijms231911172 - 22 Sep 2022
Cited by 3 | Viewed by 1658
Abstract
Aedes aegypti L. (Diptera: Culicidae) is an important transmitter of diseases in tropical countries and controlling the larvae of this mosquito helps to reduce cases of diseases such as dengue, zika and chikungunya. Thus, the present study aimed to evaluate the larvicidal potential [...] Read more.
Aedes aegypti L. (Diptera: Culicidae) is an important transmitter of diseases in tropical countries and controlling the larvae of this mosquito helps to reduce cases of diseases such as dengue, zika and chikungunya. Thus, the present study aimed to evaluate the larvicidal potential of the essential oil (EO) of Ocimum basilicum var. minimum (L.) Alef. The EO was extracted by stem distillation and the chemical composition was characterized by gas chromatography coupled with mass spectrometry (GC/MS and GC-FID). The larvicidal activity of EO was evaluated against third instar Ae. aegypti following World Health Organization (WHO) standard protocol and the interaction of the major compounds with the acetylcholinesterase (AChE) was evaluated by molecular docking. The predominant class was oxygenated monoterpenes with a concentration of 81.69% and the major compounds were limonene (9.5%), 1,8-cineole (14.23%), linalool (24.51%) and methyl chavicol (37.41%). The O. basilicum var. minimum EO showed unprecedented activity against third instar Ae. aegypti larvae at a dose-dependent relationship with LC50 of 69.91 (µg/mL) and LC90 of 200.62 (µg/mL), and the major compounds were able to interact with AChE in the Molecular Docking assay, indicating an ecological alternative for mosquito larvae control. Full article
(This article belongs to the Special Issue Biological Properties of Plant Bioactive Compounds)
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13 pages, 3794 KiB  
Article
Effects of Triterpene Soyasapogenol B from Arachis hypogaea (Peanut) on Differentiation, Mineralization, Autophagy, and Necroptosis in Pre-Osteoblasts
by Hyung-Mun Yun, Joon Yeop Lee, Soo Hyun Kim, Il Keun Kwon and Kyung-Ran Park
Int. J. Mol. Sci. 2022, 23(15), 8297; https://0-doi-org.brum.beds.ac.uk/10.3390/ijms23158297 - 27 Jul 2022
Cited by 3 | Viewed by 1488
Abstract
Triterpenes are a diverse group of natural compounds found in plants. Soyasapogenol B (SoyB) from Arachis hypogaea (peanut) has various pharmacological properties. This study aimed to elucidate the pharmacological properties and mechanisms of SoyB in bone-forming cells. In the present study, 1–20 μM [...] Read more.
Triterpenes are a diverse group of natural compounds found in plants. Soyasapogenol B (SoyB) from Arachis hypogaea (peanut) has various pharmacological properties. This study aimed to elucidate the pharmacological properties and mechanisms of SoyB in bone-forming cells. In the present study, 1–20 μM of SoyB showed no cell proliferation effects, whereas 30–100 μM of SoyB increased cell proliferation in MC3T3-E1 cells. Next, osteoblast differentiation was analyzed, and it was found that SoyB enhanced ALP staining and activity and bone mineralization. SoyB also induced RUNX2 expression in the nucleus with the increased phosphorylation of Smad1/5/8 and JNK2 during osteoblast differentiation. In addition, SoyB-mediated osteoblast differentiation was not associated with autophagy and necroptosis. Furthermore, SoyB increased the rate of cell migration and adhesion with the upregulation of MMP13 levels during osteoblast differentiation. The findings of this study provide new evidence that SoyB possesses biological effects in bone-forming cells and suggest a potentially beneficial role for peanut-based foods. Full article
(This article belongs to the Special Issue Biological Properties of Plant Bioactive Compounds)
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35 pages, 4202 KiB  
Article
The Phytotoxin Myrigalone A Triggers a Phased Detoxification Programme and Inhibits Lepidium sativum Seed Germination via Multiple Mechanisms including Interference with Auxin Homeostasis
by Kazumi Nakabayashi, Matthew Walker, Dianne Irwin, Jonathan Cohn, Stephanie M. Guida-English, Lucio Garcia, Iva Pavlović, Ondřej Novák, Danuše Tarkowská, Miroslav Strnad, Marta Pérez, Anne Seville, David Stock and Gerhard Leubner-Metzger
Int. J. Mol. Sci. 2022, 23(9), 4618; https://0-doi-org.brum.beds.ac.uk/10.3390/ijms23094618 - 21 Apr 2022
Cited by 6 | Viewed by 2374
Abstract
Molecular responses of plants to natural phytotoxins comprise more general and compound-specific mechanisms. How phytotoxic chalcones and other flavonoids inhibit seedling growth was widely studied, but how they interfere with seed germination is largely unknown. The dihydrochalcone and putative allelochemical myrigalone A (MyA) [...] Read more.
Molecular responses of plants to natural phytotoxins comprise more general and compound-specific mechanisms. How phytotoxic chalcones and other flavonoids inhibit seedling growth was widely studied, but how they interfere with seed germination is largely unknown. The dihydrochalcone and putative allelochemical myrigalone A (MyA) inhibits seed germination and seedling growth. Transcriptome (RNAseq) and hormone analyses of Lepidium sativum seed responses to MyA were compared to other bioactive and inactive compounds. MyA treatment of imbibed seeds triggered the phased induction of a detoxification programme, altered gibberellin, cis-(+)-12-oxophytodienoic acid and jasmonate metabolism, and affected the expression of hormone transporter genes. The MyA-mediated inhibition involved interference with the antioxidant system, oxidative signalling, aquaporins and water uptake, but not uncoupling of oxidative phosphorylation or p-hydroxyphenylpyruvate dioxygenase expression/activity. MyA specifically affected the expression of auxin-related signalling genes, and various transporter genes, including for auxin transport (PIN7, ABCG37, ABCG4, WAT1). Responses to auxin-specific inhibitors further supported the conclusion that MyA interferes with auxin homeostasis during seed germination. Comparative analysis of MyA and other phytotoxins revealed differences in the specific regulatory mechanisms and auxin transporter genes targeted to interfere with auxin homestasis. We conclude that MyA exerts its phytotoxic activity by multiple auxin-dependent and independent molecular mechanisms. Full article
(This article belongs to the Special Issue Biological Properties of Plant Bioactive Compounds)
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20 pages, 3371 KiB  
Article
Ebola Entry Inhibitors Discovered from Maesa perlarius
by Nga Yi Tsang, Wan-Fei Li, Elizabeth Varhegyi, Lijun Rong and Hong-Jie Zhang
Int. J. Mol. Sci. 2022, 23(5), 2620; https://0-doi-org.brum.beds.ac.uk/10.3390/ijms23052620 - 27 Feb 2022
Cited by 2 | Viewed by 2175
Abstract
Ebola virus disease (EVD), a disease caused by infection with Ebola virus (EBOV), is characterized by hemorrhagic fever and a high case fatality rate. With limited options for the treatment of EVD, anti-Ebola viral therapeutics need to be urgently developed. In this study, [...] Read more.
Ebola virus disease (EVD), a disease caused by infection with Ebola virus (EBOV), is characterized by hemorrhagic fever and a high case fatality rate. With limited options for the treatment of EVD, anti-Ebola viral therapeutics need to be urgently developed. In this study, over 500 extracts of medicinal plants collected in the Lingnan region were tested against infection with Ebola-virus-pseudotyped particles (EBOVpp), leading to the discovery of Maesa perlarius as an anti-EBOV plant lead. The methanol extract (MPBE) of the stems of this plant showed an inhibitory effect against EBOVpp, with an IC50 value of 0.52 µg/mL, which was confirmed by testing the extract against infectious EBOV in a biosafety level 4 laboratory. The bioassay-guided fractionation of MPBE resulted in three proanthocyanidins (procyanidin B2 (1), procyanidin C1 (2), and epicatechin-(4β→8)-epicatechin-(4β→8)-epicatechin-(4β→8)-epicatechin (3)), along with two flavan-3-ols ((+)-catechin (4) and (−)-epicatechin (5)). The IC50 values of the compounds against pseudovirion-bearing EBOV-GP ranged from 0.83 to 36.0 µM, with 1 as the most potent inhibitor. The anti-EBOV activities of five synthetic derivatives together with six commercially available analogues, including EGCG ((−)-epigallocatechin-3-O-gallate (8)), were further investigated. Molecular docking analysis and binding affinity measurement suggested the EBOV glycoprotein could be a potential molecular target for 1 and its related compounds. Full article
(This article belongs to the Special Issue Biological Properties of Plant Bioactive Compounds)
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