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Bioactive Natural Compounds: Protecting Plants and Promoting Human Health

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 (20 September 2024) | Viewed by 12874

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Guest Editor
Research Centre for Vegetables and Ornamental Crops, Council for Agricultural Research and Economics (CREA), Via dei Fiori 8, 51017 Pescia, Italy
Interests: glucosinolate; isothiocyanate; myrosinase; Brassicales; nutraceuticals; biopesticides; biostimulants
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Special Issue Information

Dear Colleagues,

Recently, interest in natural resources, e.g., plants, biomass processing coproducts, microorganisms and algae, as the source of bioactive compounds, has been booming worldwide. Climate, economic and social change are the main drivers challenging the scientific community to find effective and sustainable bio-based products to meet new legislations and consumer choices. Bioactive natural compounds offer a wide variety of possible applications, ranging from plant protection to human-health-promoting effects. The knowledge about the broad diversity of natural compounds is continuously evolving and gathering the effort of scientists of several disciplines involved in multidisciplinary research projects.

This Special Issue on “Bioactive Natural Compounds: Protecting Plants and Promoting Human Health” welcomes original research and reviews covering several aspects of natural compounds including, but not limited to, the following: their discovery in and from different sources; their extraction, isolation and characterization; their biotechnological production and chemical modification; the evaluation of their in vitro and in vivo bioactivity; their role at a molecular level and the elucidation of their mechanism of action; and the investigation of their stability and functionality for potential practical application in plant protection and human health.

Dr. Gina Rosalinda De Nicola
Guest Editor

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Keywords

  • natural products
  • molecular biology
  • chemical characterization
  • bioactivity
  • mechanism of action
  • plant protection
  • human health promotion
  • antioxidant
  • anti-inflammation
  • biopesticides
  • biostimulants
  • nutraceuticals

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Published Papers (9 papers)

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Research

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18 pages, 2476 KiB  
Article
Study of Pentacyclic Triterpenes from Lyophilised Aguaje: Anti-Inflammatory and Antioxidant Properties
by Luis Apaza Ticona, Javier Sánchez Sánchez-Corral, Natalia Montoto Lozano, Pablo Prieto Ramos and Ángel Rumbero Sánchez
Int. J. Mol. Sci. 2024, 25(17), 9615; https://doi.org/10.3390/ijms25179615 - 5 Sep 2024
Viewed by 693
Abstract
Mauritia flexuosa (M. flexuosa), commonly known as Aguaje or Moriche palm, is traditionally recognised in South America for its medicinal properties, particularly for its anti-inflammatory and antioxidant effects. However, the bioactive compounds responsible for these effects have not been thoroughly investigated. This [...] Read more.
Mauritia flexuosa (M. flexuosa), commonly known as Aguaje or Moriche palm, is traditionally recognised in South America for its medicinal properties, particularly for its anti-inflammatory and antioxidant effects. However, the bioactive compounds responsible for these effects have not been thoroughly investigated. This study aims to isolate and characterise pentacyclic triterpenoid compounds from M. flexuosa and to evaluate their therapeutic potential. Using various chromatographic and spectroscopic techniques including Nuclear Magnetic Resonance (NMR) and Mass Spectrometry (MS), three pentacyclic triterpenoid compounds were successfully isolated. Among them, compound 1 (3,11-dioxours-12-en-28-oic acid) exhibited notable bioactivity, significantly inhibiting the activation of Nuclear Factor kappa-light-chain-enhancer of activated B cells (NF-κB) (IC50 = 7.39–8.11 μM) and of Nitric Oxide (NO) (IC50 = 4.75–6.59 μM), both of which are key processes in inflammation. Additionally, compound 1 demonstrated potent antioxidant properties by activating the antioxidant enzyme Superoxide Dismutase (SOD) (EC50 = 1.87 μM) and the transcription factor Nuclear factor erythroid 2-related factor 2 (Nrf2) (EC50 = 243–547.59 nM), thus showing its potential in combating oxidative stress. This study is the first to isolate and characterise the three compounds from M. flexuosa, suggesting that compound 1 could be a promising candidate for the development of safer and more effective therapies for inflammatory and oxidative stress-related diseases. Full article
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16 pages, 2620 KiB  
Article
Design, Synthesis, and Nematocidal Evaluation of Waltherione A Derivatives: Leveraging a Structural Simplification Strategy
by Zhan Hu, Bin Yang, Shuai Zheng, Ke Zhao, Kaifeng Wang and Ranfeng Sun
Int. J. Mol. Sci. 2024, 25(17), 9209; https://doi.org/10.3390/ijms25179209 - 25 Aug 2024
Viewed by 782
Abstract
Southern root-knot nematodes are among the most pernicious phytoparasites; they are responsible for substantial yield losses in agricultural crops worldwide. The limited availability of nematicides for the prevention and control of plant-parasitic nematodes necessitates the urgent development of novel nematicides. Natural products have [...] Read more.
Southern root-knot nematodes are among the most pernicious phytoparasites; they are responsible for substantial yield losses in agricultural crops worldwide. The limited availability of nematicides for the prevention and control of plant-parasitic nematodes necessitates the urgent development of novel nematicides. Natural products have always been a key source for the discovery of pesticides. Waltherione A, an alkaloid, exhibits potent nematocidal activity. In this study, we designed and synthesized a series of quinoline and quinolone derivatives from Waltherione A, leveraging a strategy of structural simplification. Bioassays have revealed that the quinoline derivatives exhibit better activity than quinolone derivatives in terms of both nematocidal and fungicidal activities. Notably, compound D1 demonstrated strong nematocidal activity, with a 72 h LC50 of 23.06 μg/mL, and it effectively controlled the infection of root-knot nematodes on cucumbers. The structure–activity relationship suggests that the quinoline moiety is essential for the nematocidal efficacy of Waltherione A. Additionally, compound D1 exhibited broad-spectrum fungicidal activity, with an EC50 of 2.98 μg/mL against Botrytis cinerea. At a concentration of 200 μg/mL, it significantly inhibited the occurrence of B. cinerea on tomato fruits, with an inhibitory effect of 96.65%, which is slightly better than the positive control (90.30%). Full article
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24 pages, 6270 KiB  
Article
Antioxidant Properties of Lippia alba Essential Oil: A Potential Treatment for Oxidative Stress-Related Conditions in Plants and Cancer Cells
by Ilaria Borromeo, Anastasia De Luca, Fabio Domenici, Cristiano Giordani, Luisa Rossi and Cinzia Forni
Int. J. Mol. Sci. 2024, 25(15), 8276; https://doi.org/10.3390/ijms25158276 - 29 Jul 2024
Viewed by 1132
Abstract
Lippia alba (Mill.) N.E.Br. ex Britton and P. Wilson is used in folk medicine of Central and South America for its biological activities: i.e., antifungal, antibacterial, antiviral, and anti-inflammatory. Based on ethnopharmacological information and the increasing interest in this species, this work aimed [...] Read more.
Lippia alba (Mill.) N.E.Br. ex Britton and P. Wilson is used in folk medicine of Central and South America for its biological activities: i.e., antifungal, antibacterial, antiviral, and anti-inflammatory. Based on ethnopharmacological information and the increasing interest in this species, this work aimed to test a possible wide use of its essential oil (EO) in pharmaceutical and horticultural applications. Therefore, we focused the attention on the antioxidant activity of the oil as a possible tool to overcome the oxidative stress in both applications. For this purpose, we have chosen three aggressive breast cancer cell lines and two horticultural species (Solanum lycopersicum L. and Phaseolus acutifolius L.) that are very sensitive to salt stress. We determined the antioxidant activity of L. alba EO through the quantification of phenols and flavonoids. Regarding tomato and bean plants under salt stress, L. alba EO was used for the first time as a seed priming agent to enhance plant salt tolerance. In this case, the seed treatment enhanced the content of phenolic compounds, reduced power and scavenger activity, and decreased membrane lipid peroxidation, thus mitigating the oxidative stress induced by salt. While in breast cancer cells the EO treatment showed different responses according to the cell lines, i.e., in SUM149 and MDA-MB-231 the EO decreased proliferation and increased antioxidant activity and lipid peroxidation, showing high cytotoxic effects associated with the release of lactate dehydrogenase, vice versa no effect was observed in MDA-MB-468. Such antioxidant activity opens a new perspective about this essential oil as a possible tool to counteract proliferation in some cancer cell lines and in horticulture as a seed priming agent to protect from oxidative damage in crops sensitive to salinity. Full article
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13 pages, 565 KiB  
Article
Biofunctional Textiles: Antioxidant and Antibacterial Finishings of Cotton with Propolis and Honey
by Ana Sofia Freitas, Rui Oliveira, Alice Ribeiro and Cristina Almeida-Aguiar
Int. J. Mol. Sci. 2024, 25(15), 8034; https://doi.org/10.3390/ijms25158034 - 23 Jul 2024
Viewed by 1090
Abstract
The growing activity in the textile industry has been demanding the search for new and innovative technologies to meet consumers’ needs regarding more sustainable and ecological processes, with functionality receiving more attention. Bee products are known for their wide spectra of properties, including [...] Read more.
The growing activity in the textile industry has been demanding the search for new and innovative technologies to meet consumers’ needs regarding more sustainable and ecological processes, with functionality receiving more attention. Bee products are known for their wide spectra of properties, including antioxidant and antibacterial activities. Propolis and honey are the most popular and used since ancient times for the most diverse applications due to their health benefits. With the increasing need for safer and more sustainable practices, the use of natural products for the functional finishing process can be a suitable alternative due to their safety and eco-friendly nature. For that, a biosolution, composed of a mixture of propolis and honey in water, was used to perform the functional finishing of cotton knits, both in the presence and in the absence of potassium alum as a chemical mordant. The fastness strength was also evaluated after three washing cycles. The antioxidant potential of the biosolution, assessed with the in vitro ABTS scavenging assay, provided textiles with the capacity to reduce more than 90% of the ABTS radical, regardless of the mordant presence and even after three washing cycles. Furthermore, biofunctional textiles decreased the growth of Bacillus subtilis, Propionibacterium acnes, Escherichia coli, and, particularly, Staphylococcus aureus cultures after 24 h of incubation with an increase in antibacterial activity when potassium alum was used. These findings show that bee products are promising and effective alternatives to be used in the textile industry to confer antioxidant and antibacterial properties to cotton textiles, thereby enhancing human health. Full article
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16 pages, 3556 KiB  
Article
Onion (Allium cepa L.) Flavonoid Extract Ameliorates Osteoporosis in Rats Facilitating Osteoblast Proliferation and Differentiation in MG-63 Cells and Inhibiting RANKL-Induced Osteoclastogenesis in RAW 264.7 Cells
by Danyang Zhang, Xiaoyu Wang, Kezhuo Sun, Jianli Guo, Jia Zhao, Yuesheng Dong and Yongming Bao
Int. J. Mol. Sci. 2024, 25(12), 6754; https://doi.org/10.3390/ijms25126754 - 19 Jun 2024
Cited by 1 | Viewed by 1248
Abstract
Osteoporosis, a prevalent chronic health issue among the elderly, is a global bone metabolic disease. Flavonoids, natural active compounds widely present in vegetables, fruits, beans, and cereals, have been reported for their anti-osteoporotic properties. Onion is a commonly consumed vegetable rich in flavonoids [...] Read more.
Osteoporosis, a prevalent chronic health issue among the elderly, is a global bone metabolic disease. Flavonoids, natural active compounds widely present in vegetables, fruits, beans, and cereals, have been reported for their anti-osteoporotic properties. Onion is a commonly consumed vegetable rich in flavonoids with diverse pharmacological activities. In this study, the trabecular structure was enhanced and bone mineral density (BMD) exhibited a twofold increase following oral administration of onion flavonoid extract (OFE). The levels of estradiol (E2), calcium (Ca), and phosphorus (P) in serum were significantly increased in ovariectomized (OVX) rats, with effects equal to alendronate sodium (ALN). Alkaline phosphatase (ALP) and tartrate-resistant acid phosphatase (TRAP) levels in rat serum were reduced by 35.7% and 36.9%, respectively, compared to the OVX group. In addition, the effects of OFE on bone health were assessed using human osteoblast-like cells MG-63 and osteoclast precursor RAW 264.7 cells in vitro as well. Proliferation and mineralization of MG-63 cells were promoted by OFE treatment, along with increased ALP activity and mRNA expression of osteoprotegerin (OPG)/receptor activator of nuclear factor-kappaB ligand (RANKL). Additionally, RANKL-induced osteoclastogenesis and osteoclast activity were inhibited by OFE treatment through decreased TRAP activity and down-regulation of mRNA expression-related enzymes in RAW 264.7 cells. Overall findings suggest that OFE holds promise as a natural functional component for alleviating osteoporosis. Full article
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19 pages, 1138 KiB  
Article
Hesperidin as a Species-Specific Modifier of Aphid Behavior
by Katarzyna Stec, Bożena Kordan, Jan Bocianowski and Beata Gabryś
Int. J. Mol. Sci. 2024, 25(9), 4822; https://doi.org/10.3390/ijms25094822 - 28 Apr 2024
Cited by 1 | Viewed by 863
Abstract
Hesperidin is a highly bioactive natural flavonoid whose role in ecological interactions is poorly known. In particular, the effects of hesperidin on herbivores are rarely reported. Flavonoids have been considered as prospective biopesticides; therefore, the aim of the present study was to examine [...] Read more.
Hesperidin is a highly bioactive natural flavonoid whose role in ecological interactions is poorly known. In particular, the effects of hesperidin on herbivores are rarely reported. Flavonoids have been considered as prospective biopesticides; therefore, the aim of the present study was to examine the influence of hesperidin on the host plant selection behavior of three aphid (Hemiptera: Aphididae) species: Acyrthosiphon pisum Harrris, Rhopalosiphum padi (L.), and Myzus persicae (Sulz.). The aphid host plants were treated with 0.1% and 0.5% ethanolic solutions of hesperidin. Aphid probing behavior in the no-choice experiment was monitored using electropenetrography and aphid settling on plants in the choice experiment was recorded. The results demonstrated that hesperidin can be applied as a pre-ingestive, ingestive, and post-ingestive deterrent against A. pisum, as an ingestive deterrent against R. padi, and as a post-ingestive deterrent against M. persicae using the relatively low 0.1% concentration. While in A. pisum the deterrent effects of hesperidin were manifested as early as during aphid probing in peripheral plant tissues, in M. persicae, the avoidance of plants was probably the consequence of consuming the hesperidin-containing phloem sap. Full article
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15 pages, 3196 KiB  
Article
Biocontrol Potential of Streptomyces odonnellii SZF-179 toward Alternaria alternata to Control Pear Black Spot Disease
by Fei Zhang, Shaohua Wen, Beibei Wang, Zhe Zhang, Fang Liu, Ting Ye, Kaimei Wang, Hongju Hu, Xiaoping Yang and Wei Fang
Int. J. Mol. Sci. 2023, 24(24), 17515; https://doi.org/10.3390/ijms242417515 - 15 Dec 2023
Cited by 1 | Viewed by 1305
Abstract
Pear black spot disease, caused by Alternaria alternata, is a devastating disease in pears and leads to enormous economic losses worldwide. In this investigation, we isolated a Streptomyces odonnellii SZF-179 from the rhizosphere soil of pear plants in China. Indoor confrontation experiments results [...] Read more.
Pear black spot disease, caused by Alternaria alternata, is a devastating disease in pears and leads to enormous economic losses worldwide. In this investigation, we isolated a Streptomyces odonnellii SZF-179 from the rhizosphere soil of pear plants in China. Indoor confrontation experiments results showed that both SZF-179 and its aseptic filtrate had excellent inhibitory effects against A. alternata. Afterwards, the main antifungal compound of SZF-179 was identified as polyene, with thermal and pH stability in the environment. A microscopic examination of A. alternata mycelium showed severe morphological abnormalities caused by SZF-179. Protective studies showed that SZF-179 fermentation broth could significantly reduce the diameter of the necrotic lesions on pear leaves by 42.25%. Furthermore, the potential of fermentation broth as a foliar treatment to control black leaf spot was also evaluated. Disease indexes of ‘Hosui’ and ‘Wonwhang’ pear plants treated with SZF-179 fermentation broth were lower than that of control plants. Overall, SZF-179 is expected to be developed into a safe and broad-spectrum biocontrol agent. No studies to date have evaluated the utility of S. odonnellii for the control of pear black spot disease; our study fills this research gap. Collectively, our findings provide new insights that will aid the control of pear black spot disease, as well as future studies of S. odonnellii strains. Full article
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Review

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19 pages, 1211 KiB  
Review
Puerarin—A Promising Flavonoid: Biosynthesis, Extraction Methods, Analytical Techniques, and Biological Effects
by Sergio Liga and Cristina Paul
Int. J. Mol. Sci. 2024, 25(10), 5222; https://doi.org/10.3390/ijms25105222 - 10 May 2024
Cited by 2 | Viewed by 2481
Abstract
Flavonoids, a variety of plant secondary metabolites, are known for their diverse biological activities. Isoflavones are a subgroup of flavonoids that have gained attention for their potential health benefits. Puerarin is one of the bioactive isoflavones found in the Kudzu root and Pueraria [...] Read more.
Flavonoids, a variety of plant secondary metabolites, are known for their diverse biological activities. Isoflavones are a subgroup of flavonoids that have gained attention for their potential health benefits. Puerarin is one of the bioactive isoflavones found in the Kudzu root and Pueraria genus, which is widely used in alternative Chinese medicine, and has been found to be effective in treating chronic conditions like cardiovascular diseases, liver diseases, gastric diseases, respiratory diseases, diabetes, Alzheimer’s disease, and cancer. Puerarin has been extensively researched and used in both scientific and clinical studies over the past few years. The purpose of this review is to provide an up-to-date exploration of puerarin biosynthesis, the most common extraction methods, analytical techniques, and biological effects, which have the potential to provide a new perspective for medical and pharmaceutical research and development. Full article
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20 pages, 1621 KiB  
Review
The Precious Potential of the Sacred Tree Chamaecyparis obtusa (Siebold & Zucc.) Endl. as a Source of Secondary Metabolites with Broad Biological Applications
by Karol Maksymilian Górski, Tomasz Kowalczyk, Laurent Picot, Patricia Rijo, Mansour Ghorbanpour and Przemysław Sitarek
Int. J. Mol. Sci. 2024, 25(5), 2723; https://doi.org/10.3390/ijms25052723 - 27 Feb 2024
Cited by 2 | Viewed by 1963
Abstract
Chamaecyparis obtusa (Siebold & Zucc.) Endl., which belongs to the Cupressaceae family, occurs naturally in North America and Asia, especially in Korea, Taiwan and Japan, where it is an evergreen, coniferous, sacred, ethnic tree. It has many useful varieties that are widespread throughout [...] Read more.
Chamaecyparis obtusa (Siebold & Zucc.) Endl., which belongs to the Cupressaceae family, occurs naturally in North America and Asia, especially in Korea, Taiwan and Japan, where it is an evergreen, coniferous, sacred, ethnic tree. It has many useful varieties that are widespread throughout the world and grown for decorative purposes. It is most commonly used as an ornamental plant in homes, gardens or parks. It is also widely used in many areas of the economy; for example, its wood is used in architecture as well as furniture production. In addition, oil extracted from Chamaecyparis obtusa is increasingly used in cosmetology for skin care. Due to its wide economic demand, mainly in Japan, it represents the largest area of plantation forest. Despite this, it is on the red list of endangered species. Its use in ethnopharmacology has led to more and more research in recent years in an attempt to elucidate the potential mechanisms of its various biological activities, such as antimicrobial, antioxidant, anticancer, antidiabetic, antiasthmatic, anti-inflammatory, antiallergic, analgesic and central nervous system effects. It has also been shown that Chamaecyparis obtusa can be used as an insect repellent and an ingredient in plant disease treatment. This thesis provides a comprehensive review of the biological studies to date, looking at different areas of the economic fields of potential use of Chamaecyparis obtusa. Full article
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