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Isolation, Characterization and Activity Evaluation by Bioactive Compounds from Plants
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Isolation, Characterization and Activity Evaluation by Bioactive Compounds from Plants

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

Deadline for manuscript submissions: closed (31 December 2021) | Viewed by 14460

Special Issue Editor

Prof. Dr. Ascension Torres

E-Mail Website
Guest Editor
Allelopathy Group, Department of Organic Chemistry, Institute of Biomolecules (INBIO), Campus de Excelencia Internacional Agroalimentario (ceiA3), University of Cádiz, C/Avda. República Saharaui, 7, 11510 Puerto Real, Cádiz, Spain
Interests: allelopathy; biocommunicators; allelochemicals; phytotoxic bioassays; bio-directed isolation; structural characterization

Special Issue Information

Dear Colleagues,

This Special Issue is entitled "Isolation, Characterization and Activity Evaluation by Bioactive Compounds from Plants". Plants, as with other living entities, interact directly or indirectly with other organisms. Since they are forced to live on a fixed substrate, they need chemical compounds that help them interact with the environment, including defense against possible predators and even to fight against other plants that compete with them for resources. The products involved in these interactions are secondary metabolites, or denominated biocommunicators.

Investigators who study bioactive plant extracts face a formidable challenge. The effects of such extracts can result from the interaction of an array of chemically diverse components, which depend on identity and concentration. Proponents of the use of natural plant products often argue that their constituent components are more effective in the phytochemical matrix than when isolated. However, the specific components responsible for these effects, and the fundamental mechanisms by which they interact, are rarely known. Methods are needed to unravel the complexity of the modes of action and identify their key bioactive constituents. This information, in turn, would allow better control of the most significant and reproducible activities of natural products from plants.

A common approach to studying complex plant preparations is bioactivity-guided fractionation. With this technique, extracts are screened for those containing biologically active compounds. The active extracts are then partitioned and purified, with the ultimate goal of identifying and testing single active compounds.

This Special Issue will cover the isolation, characterization and activity evaluation aspects of compounds from plant extracts. A wide range of activities of compounds from plant extracts has been published. In recent years, special interest has been paid to these secondary metabolites with phytotoxic properties, also called allelochemicals, as they seem to be a fruitful challenge to combine traditional agricultural practices and new approaches in pest and weed management strategies.

Prof. Dr. Ascension Torres
Guest Editor

Manuscript Submission Information

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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

  • secondary metabolites
  • biodirected fractionation
  • bioassays
  • bioactivities
  • bioactive compounds
  • allelochemicals
  • structure–activity relationship
  • characterization of compounds

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Published Papers (5 papers)

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Research

17 pages, 4849 KiB  
Article
Expanding the Study of the Cytotoxicity of Incomptines A and B against Leukemia Cells
by Fernando Calzada, Normand Garcia-Hernandez, Sergio Hidalgo-Figueroa, Elihú Bautista, Elizabeth Barbosa, Claudia Velázquez and Marta Elena Hernández-Caballero
Molecules 2022, 27(5), 1687; https://doi.org/10.3390/molecules27051687 - 4 Mar 2022
Cited by 1 | Viewed by 1580
Abstract
Heliangolide-type sesquiterpene lactones (HTSLs) are phytocompounds with several pharmacological activities including cytotoxic and antitumor activity. Both bioactivities are related to an α-methylene-γ-lactone moiety and an ester group on carbon C-8 in the sesquiterpene lactone (SL) structure. Two HTSLs, incomptines A (AI) [...] Read more.
Heliangolide-type sesquiterpene lactones (HTSLs) are phytocompounds with several pharmacological activities including cytotoxic and antitumor activity. Both bioactivities are related to an α-methylene-γ-lactone moiety and an ester group on carbon C-8 in the sesquiterpene lactone (SL) structure. Two HTSLs, incomptines A (AI) and B (IB) isolated from Decachaeta incompta, were evaluated for their cytotoxic activity on three leukemia cell lines: HL-60, K-562, and REH cells. Both compounds were subjected to a molecular docking study using target proteins associated with cancer such as topoisomerase IIα, topoisomerase IIβ, dihydrofolate reductase, methylenetetrahydrofolate dehydrogenase, and Bcl-2-related protein A1. Results show that IA and IB exhibit cytotoxic activity against all cell lines used. The CC50 value of IA was 2–4-fold less than etoposide and methotrexate, two anticancer drugs used as positive controls. The cytotoxic activity of IB was close to that of etoposide and methotrexate. The molecular docking analysis showed that IA and IB have important interaction on all targets used. These findings suggest that IA and IB may serve as scaffolds for the development of new treatments for different types of leukemia. Full article
(This article belongs to the Special Issue Isolation, Characterization and Activity Evaluation by Bioactive Compounds from Plants)
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28 pages, 13553 KiB  
Article
Evaluation of Nutritional Substances and Investigation of Antioxidant and Antimicrobial Potentials of Boerhavia diffusa with in Silico Molecular Docking
by Mohandass Kaviya, Balamuralikrishnan Balasubramanian, Kathirvel Bharathi, Arunkumar Malaisamy, Naif Abdullah Al-Dhabi, Valan Arasu Mariadhas, Arumugam Vijaya Anand and Wenchao Liu
Molecules 2022, 27(4), 1280; https://doi.org/10.3390/molecules27041280 - 14 Feb 2022
Cited by 12 | Viewed by 3931
Abstract
Boerhavia diffusa L. Nyctanginaceae (B. diffusa) is a medicinal herb commonly considered as a weed. The exploration of phytochemicals in different parts of B. diffusa with different solvents will create awareness, along with the suitable solvent and method for extraction of [...] Read more.
Boerhavia diffusa L. Nyctanginaceae (B. diffusa) is a medicinal herb commonly considered as a weed. The exploration of phytochemicals in different parts of B. diffusa with different solvents will create awareness, along with the suitable solvent and method for extraction of pharmaceutical compounds. Hence, the present study focuses on phytochemical analysis of B. diffusa leaves, stems, and roots in various solvents with hot and cold extraction. The decoctions performed well in most of the qualitative and quantitative tests, along with the DPPH assay. The aqueous extract showed a good result in the FRAP assay and ABTS assay. In the antimicrobial test, the B. diffusa root ethanol extract inhibited the growth of Pseudomonas aeruginosa and Staphylococcus aureus with zones of inhibition of about 8 mm and 20 mm at 200 µg concentration, respectively. Using a molecular docking approach, the top four ranked molecules from the crude extract of B. diffusa profiled from GC–MS spectroscopy in terms of growth inhibition of the pathogenic bacterium P. aeruginosa were selected; among them, 2-(1,2 dihydroxyethyl)-5-[[2,5,7,8-tetramethyl-2-(4,8,12-trimethyltridecyl)-3,4-dihydrochromen-6-yl]oxy]oxolane-3,4-diol exhibited the minimum binding score, revealing high affinity in complex. B. diffusa is highly nutritious, and the maceration and decoction extracts were similar except for the chloroform extract that was found to be weak. Full article
(This article belongs to the Special Issue Isolation, Characterization and Activity Evaluation by Bioactive Compounds from Plants)
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17 pages, 2531 KiB  
Article
Evaluation of the Potential of a Lectin Extracted from Polygonumpersicaria L. as a Biorational Agent against Sitophilusoryzae L.
by Mehdi Khoobdel, Vahid Rahimi, Asgar Ebadollahi and Patcharin Krutmuang
Molecules 2022, 27(3), 793; https://doi.org/10.3390/molecules27030793 - 25 Jan 2022
Cited by 7 | Viewed by 2538
Abstract
Rice weevil, Sitophilus oryzae L. (Coleoptera: Curculionidae), is one of the most destructive stored-product pests that is resistant to a wide range of chemical insecticides. In the present study, we investigated whether a lectin extracted from Polygonum persicaria L. (PPA) can be used [...] Read more.
Rice weevil, Sitophilus oryzae L. (Coleoptera: Curculionidae), is one of the most destructive stored-product pests that is resistant to a wide range of chemical insecticides. In the present study, we investigated whether a lectin extracted from Polygonum persicaria L. (PPA) can be used as a biorational agent to control such insect pests. Along with the lethal digestive assay, the sub-lethal insecticidal activities of PPA, including the effects on digestive, detoxifying, and antioxidant enzyme activities, were evaluated against S. oryzae adults. The effect of feeding a diet containing PPA and carob extract as a food attractant on the mortality of S. oryzae adults was also investigated. Feeding on the diet containing PPA resulted in a significant mortality of S. oryzae adults with a LC50 (Lethal Concentration to kill 50% of insects) of 3.68% (w/w). The activity of digestive enzymes, including α-amylase, α-glucosidase, TAG-lipase, trypsin, chymotrypsin, elastase, and carboxy- and aminopeptidase, were decreased by the sub-lethal concentration of PPA. Detoxifying and antioxidant enzymes, including esterase, superoxide dismutase, catalase, glutathione-S-transferase, ascorbate peroxidase, glucose 6-phosphate dehydrogenase, and malondialdehyde, were activated in adults affected by PPA. These findings indicated that PPA, in addition to causing digestive disorders, leads to oxidative stress in S. oryzae. The presence of carob extract had no effect on the PPA-induced mortality of the insect. According to the results of the present study, PPA has promising insecticidal efficiency against S. oryzae. In addition, the usage of PPA with a food attractant carob extract in bait traps can be recommended as a new biorational formulation in S. oryzae management. Full article
(This article belongs to the Special Issue Isolation, Characterization and Activity Evaluation by Bioactive Compounds from Plants)
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14 pages, 2233 KiB  
Article
Bioactive Diterpenes from the Brazilian Native Plant (Moquiniastrum pulchrum) and Their Application in Weed Control
by Fátima Vela, Simoni Anese, Rosa M. Varela, Ascensión Torres, José M. G. Molinillo and Francisco A. Macías
Molecules 2021, 26(15), 4632; https://doi.org/10.3390/molecules26154632 - 30 Jul 2021
Cited by 1 | Viewed by 1840
Abstract
Even today, weeds continue to be a considerable problem for agriculture. The application of synthetic herbicides produces serious environmental consequences, and crops suffer loss of their activity due to the appearance of new resistant weed biotypes. Our aim is to develop new effective [...] Read more.
Even today, weeds continue to be a considerable problem for agriculture. The application of synthetic herbicides produces serious environmental consequences, and crops suffer loss of their activity due to the appearance of new resistant weed biotypes. Our aim is to develop new effective natural herbicides that improve the problem of resistance and do not harm the environment. This work is focused on a bioassay-guided isolation and the characterization of natural products present in Moquiniastrum pulchrum leaves with phytotoxic activity and its preliminary application in weeds. Moquiniastrum pulchrum was selected for two reasons: it is an abundant species in the Cerrado region (the second most important ecosystem in Brazil, after the Amazon)—the explanation behind its being a dominant species is a major focus of interest—and it has traditional employment in folk medicine. Six major compounds were isolated in this plant: one flavone and five diterpenes, two of which are described for the first time in the literature. Four of the six compounds exhibited phytotoxic activity in the bioassays performed. The results confirmed the phytotoxic potential of this plant, which had not been investigated until now. Full article
(This article belongs to the Special Issue Isolation, Characterization and Activity Evaluation by Bioactive Compounds from Plants)
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13 pages, 2427 KiB  
Article
A Study on the Phytotoxic Potential of the Seasoning Herb Marjoram (Origanum majorana L.) Leaves
by Antonio Cala, José R. Salcedo, Ascensión Torres, Rosa M. Varela, José M. G. Molinillo and Francisco A. Macías
Molecules 2021, 26(11), 3356; https://doi.org/10.3390/molecules26113356 - 2 Jun 2021
Cited by 15 | Viewed by 3667
Abstract
In the search of new alternatives for weed control, spices appear as an option with great potential. They are rich in bioactive natural products and edible, which might minimize toxicity hazard. Marjoram (Origanum majorana L.) is an aromatic herb that has been [...] Read more.
In the search of new alternatives for weed control, spices appear as an option with great potential. They are rich in bioactive natural products and edible, which might minimize toxicity hazard. Marjoram (Origanum majorana L.) is an aromatic herb that has been widely employed as a seasoning herb in Mediterranean countries. Although marjoram boasts a plethora of therapeutic properties (painkiller, antibiotic, treatment for intestinal disorders, etc.), the potential for its extracts for weed control is still to be more thoroughly explored. In order to determine their phytotoxic potential, marjoram leaves were subjected to different bioguided extraction processes, using water, ethyl acetate, acetone or methanol. The most active extract (acetone) was sequentially fractionated to identify its most active compounds. This fractionation led to the isolation and identification of 25 compounds that were classified as monoterpenes, diterpenes or flavonoids. Among them, a new compound named majoradiol and several compounds are described in marjoram for the first time. The phytotoxicity of the major compounds to etiolated wheat coleoptiles was compared against that of the commercial herbicide (Logran®), with similar or higher activity in some cases. These results confirm the extraordinary potential of the extracts from this edible plant to develop safer and more environmentally friendly herbicides. Full article
(This article belongs to the Special Issue Isolation, Characterization and Activity Evaluation by Bioactive Compounds from Plants)
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