scholarly journals Triflumizole as a Novel Lead Compound for Strigolactone Biosynthesis Inhibitor

Molecules ◽  
2020 ◽  
Vol 25 (23) ◽  
pp. 5525
Author(s):  
Kojiro Kawada ◽  
Yuya Uchida ◽  
Ikuo Takahashi ◽  
Takahito Nomura ◽  
Yasuyuki Sasaki ◽  
...  
Keyword(s):  
Seed Germination ◽  
Enzymatic Activity ◽  
Parasitic Plants ◽  
Biologically Active ◽  
Biological Processes ◽  
Lead Compound ◽  
Biosynthesis Inhibitor ◽  
Rice Roots ◽  
Heterocyclic Derivatives ◽  
Root Parasitic Plants

Strigolactones (SLs) are carotenoid-derived plant hormones involved in the development of various plants. SLs also stimulate seed germination of the root parasitic plants, Striga spp. and Orobanche spp., which reduce crop yield. Therefore, regulating SL biosynthesis may lessen the damage of root parasitic plants. Biosynthetic inhibitors effectively control biological processes by targeted regulation of biologically active compounds. In addition, biosynthetic inhibitors regulate endogenous levels in developmental stage- and tissue-specific manners. To date, although some chemicals have been found as SL biosynthesis inhibitor, these are derived from only three lead chemicals. In this study, to find a novel lead chemical for SL biosynthesis inhibitor, 27 nitrogen-containing heterocyclic derivatives were screened for inhibition of SL biosynthesis. Triflumizole most effectively reduced the levels of rice SL, 4-deoxyorobanchol (4DO), in root exudates. In addition, triflumizole inhibited endogenous 4DO biosynthesis in rice roots by inhibiting the enzymatic activity of Os900, a rice enzyme that converts the SL intermediate carlactone to 4DO. A Striga germination assay revealed that triflumizole-treated rice displayed a reduced level of germination stimulation for Striga. These results identify triflumizole as a novel lead compound for inhibition of SL biosynthesis.

scholarly journals A Phelipanche ramosa KAI2 Protein Perceives enzymatically Strigolactones and Isothiocyanates

2020 ◽  
Author(s):  
Alexandre de Saint Germain ◽  
Anse Jacobs ◽  
Guillaume Brun ◽  
Jean-Bernard Pouvreau ◽  
Lukas Braem ◽  
...  
Keyword(s):  
Seed Germination ◽  
Enzymatic Activity ◽  
Central Europe ◽  
Parasitic Plants ◽  
High Plasticity ◽  
Parasitic Weed ◽  
Signal Perception ◽  
Perception System ◽  
Phelipanche Ramosa

AbstractPhelipanche ramosa is an obligate root-parasitic weed threatening major crops in central Europe. For its germination, it has to perceive various structurally diverging host-exuded signals, including isothiocyanates (ITCs) and strigolactones (SLs). However, the receptors involved are still uncharacterized. Here, we identified five putative SL receptors in P. ramosa, of which PrKAI2d3 is involved in seed germination stimulation. We established the high plasticity of PrKAI2d3, allowing interaction with different chemicals, including ITCs. The SL perception mechanism of PrKAI2d3 is similar to that of endogenous SLs in non-parasitic plants. We provide evidence that the PrKAI2d3 enzymatic activity confers hypersensitivity to SLs. Additionally, we demonstrated that methylbutenolide-OH binds PrKAI2d3 and stimulates P. ramosa germination with a bioactivity comparable to that of ITCs. This study highlights that P. ramosa has extended its signal perception system during evolution, a fact to be considered in the development of specific and efficient biocontrol methods.

scholarly journals A high-throughput seed germination assay for root parasitic plants

Plant Methods ◽  
2013 ◽  
Vol 9 (1) ◽  
pp. 32 ◽  
Author(s):  
Jean-Bernard Pouvreau ◽  
Zachary Gaudin ◽  
Bathilde Auger ◽  
Marc-Marie Lechat ◽  
Mathieu Gauthier ◽  
...  
Keyword(s):  
Seed Germination ◽  
High Throughput ◽  
Parasitic Plants ◽  
Germination Assay ◽  
Seed Germination Assay ◽  
Root Parasitic Plants

An enumeration of natural products from microbial, marine and terrestrial sources

2020 ◽  
Vol 5 (8) ◽  
Author(s):  
Fidele Ntie-Kang ◽  
Daniel Svozil
Keyword(s):  
Amino Acids ◽  
Natural Products ◽  
Biologically Active ◽  
Lead Compound ◽  
Chemical Databases ◽  
Natural Sources ◽  
Chemical Structures ◽  
Chemically Modified ◽  
Marine Habitats ◽  
Metabolic Properties

AbstractThe discovery of a new drug is a multidisciplinary and very costly task. One of the major steps is the identification of a lead compound, i.e. a compound with a certain degree of potency and that can be chemically modified to improve its activity, metabolic properties, and pharmacokinetics profiles. Terrestrial sources (plants and fungi), microbes and marine organisms are abundant resources for the discovery of new structurally diverse and biologically active compounds. In this chapter, an attempt has been made to quantify the numbers of known published chemical structures (available in chemical databases) from natural sources. Emphasis has been laid on the number of unique compounds, the most abundant compound classes and the distribution of compounds in terrestrial and marine habitats. It was observed, from the recent investigations, that ~500,000 known natural products (NPs) exist in the literature. About 70 % of all NPs come from plants, terpenoids being the most represented compound class (except in bacteria, where amino acids, peptides, and polyketides are the most abundant compound classes). About 2,000 NPs have been co-crystallized in PDB structures.

Reactions of Lotus japonicus ecotypes and mutants to root parasitic plants

2009 ◽  
Vol 166 (4) ◽  
pp. 353-362 ◽  
Author(s):  
Mie Kubo ◽  
Hiroaki Ueda ◽  
Pyoyun Park ◽  
Masayoshi Kawaguchi ◽  
Yukihiro Sugimoto
Keyword(s):  
Lotus Japonicus ◽  
Parasitic Plants ◽  
Root Parasitic Plants

scholarly journals SEED GERMINATION AND PLANT DEVELOPMENT IN Escobedia grandiflora (OROBANCHACEAE): EVIDENCE OF OBLIGATE HEMIPARASITISM?

2015 ◽  
Vol 20 (3) ◽  
pp. 133-140 ◽  
Author(s):  
Edison CARDONA-MEDINA ◽  
Sandra Bibiana MURIEL RUIZ
Keyword(s):  
Dry Matter ◽  
Parasitic Plants ◽  
Paspalum Notatum ◽  
Percentage Germination ◽  
Critical Stage ◽  
Stage Of Development ◽  
Medicinal Use ◽  
Germination Speed ◽  
Total Plant ◽  
Root Parasitic Plants

<p>Root parasitic plants can be facultative or obligate. Facultative parasites are able to complete their life cycle and their seeds can germinate without a host. <em>Escobedia</em> <em>grandiflora</em> is a poorly studied species in spite of its ancestral importance as dye of foods and medicinal use. The present study evaluates the states of seed, seedlings and mature plants, under presence and absence of possible hosts, for inferring the type of parasitism exhibited by <em>E. grandiflora</em>. Seeds were evaluated using two conditions each of light (12 and 0 hours) and temperature (20 ºC and 25 ºC); percentage germination, and germination speed were determined. The seeds did not require a host to germinate, as is typical of facultative parasitic plants.  Percentage of germination varied between 66 % and 85.3 % and was not affected by light or temperature although germination speed was greater at 25 ºC. Larger seeds had a higher percentage of germination and produced larger seedlings. The seedlings planted without a host did not survive, while those planted with <em>Paspalum notatum</em> had a 45 % survival rate, demonstrating that this is a critical stage of development, even with a host. <em>Escobedia grandiflora</em> plants sowed with grasses began the reproductive stage at the 28<sup>th </sup>week, and those planted with <em>Pennisetum</em> <em>purpureum</em> showed better performance, expressed in more haustoria, higher dry matter of total plant, rhizome and aerial stems. Plants sowed alone lived for more than six months, but they did not produce flowers or fruits. According to the behavior of seedlings and plants, <em>E. grandiflora</em> is an obligate parasite. </p><p><strong>Germinación de semillas y desarrollo de plantas en <em>Escobedia</em> <em>grandiflora</em> (Orobanchaceae): ¿Evidencia de hemiparasitismo obligado?</strong></p><p> </p><p>Las plantas parásitas de raíces pueden ser facultativas u obligadas, las primeras pueden completar su ciclo de vida y sus semillas pueden germinar sin un hospedero. <em>Escobedia</em> <em>grandiflora</em> es una especie poco estudiada, a pesar de su importancia ancestral como colorante de alimentos y uso medicinal. Este estudio evaluó los estados de semilla, plántula y planta adulta, en presencia y ausencia de posibles hospederos para inferir sobre su tipo de parasitismo. En las semillas se evaluaron dos condiciones de luz (12 y 0 horas) y temperatura (20 ºC y 25 ºC), el porcentaje y velocidad de germinación. Las semillas no requirieron la presencia del hospedero para germinar. El porcentaje de germinación osciló entre 66 y 85,3 %  y no fue afectado por la luz o la temperatura, aunque la velocidad de germinación fue mayor a 25 ºC. Las semillas con mayor tamaño presentaron mayor porcentaje de germinación y produjeron plántulas más grandes. Las plántulas sembradas sin hospedero no sobrevivieron, mientras que las sembradas con <em>Paspalum notatum</em>, tuvieron una sobrevivencia del 45 %, evidenciando que este estado es crítico, aún con hospedero. Las plantas de <em>Escobedia grandiflora</em> sembradas con pastos, iniciaron la etapa reproductiva en la semana 28, y aquellas sembradas con <em>Pennisetum</em> <em>purpureum</em> presentaron más haustorios, y mayor materia seca en la planta total, rizoma y tallos aéreos. Las plantas sembradas solas vivieron más de seis meses, pero ellos no desarrollaron flores y ni frutos. Según el comportamiento de las plántulas y las plantas, <em>E. grandiflora</em> es parásita obligada.</p>

Utility of 2-Aminothiophene-3-carboxamide in the Synthesis of Biologically Active, Fused Heterocyclic Derivatives.

ChemInform ◽  
2005 ◽  
Vol 36 (19) ◽  
Author(s):  
Wagnat W. Wardakhan ◽  
Gamal A. Elmegeed ◽  
Fatima M. Manhi
Keyword(s):  
Biologically Active ◽  
Heterocyclic Derivatives

scholarly journals Impact of host and environmental factors on β-glucuronidase enzymatic activity: implications for gastrointestinal serotonin

2020 ◽  
Vol 318 (4) ◽  
pp. G816-G826 ◽  
Author(s):  
Jacinta Walsh ◽  
Loreto Olavarria-Ramirez ◽  
Gilliard Lach ◽  
Marcus Boehme ◽  
Timothy G. Dinan ◽  
...  
Keyword(s):  
Environmental Factors ◽  
Drug Metabolism ◽  
Enzymatic Activity ◽  
Metabolic Activity ◽  
Active Form ◽  
Biologically Active ◽  
Antibiotic Administration ◽  
Targeted Interventions ◽  
Glucosidase Activity ◽  
Glucuronidase Activity

The gastrointestinal tract houses a reservoir of bacterial-derived enzymes that can directly catalyze the metabolism of drugs, dietary elements and endogenous molecules. Both host and environmental factors may influence this enzymatic activity, with the potential to dictate the availability of the biologically-active form of endogenous molecules in the gut and influence inter-individual variation in drug metabolism. We aimed to investigate the influence of the microbiota, and the modulation of its composition, on fecal enzymatic activity. Intrinsic factors related to the host, including age, sex and genetic background, were also explored. Fecalase, a cell-free extract of feces, was prepared and used in a colorimetric-based assay to quantify enzymatic activity. To demonstrate the functional effects of fecal enzymatic activity, we examined β-glucuronidase-mediated cleavage of serotonin β-d-glucuronide (5-HT-GLU) and the resultant production of free 5-HT by HPLC. As expected, β-glucuronidase and β-glucosidase activity were absent in germ-free mice. Enzymatic activity was significantly influenced by mouse strain and animal species. Sex and age significantly altered metabolic activity with implications for free 5-HT. β-Glucuronidase and β-glucosidase activity remained at reduced levels for nearly two weeks after cessation of antibiotic administration. This effect on fecalase corresponded to significantly lower 5-HT levels as compared with incubation with pre-antibiotic fecalase from the same mice. Dietary targeting of the microbiota using prebiotics did not alter β-glucuronidase or β-glucosidase activity. Our data demonstrate that multiple factors influence the activity of bacterial-derived enzymes which may have potential clinical implications for drug metabolism and the deconjugation of host-produced glucuronides in the gut. NEW & NOTEWORTHY This article explores a comprehensive range of host and environmental factors that introduce variability in the expression of bacterial-derived metabolic enzymes. Our results demonstrate that altered β-glucuronidase activity has implications for the bioavailability of luminal serotonin. The experimental approach employed, fecalase, provides a mechanistic basis and translational platform to further delineate the functional outputs of altered metabolic activity, and the associated physiological effects of microbiota-targeted interventions on host response to drugs and host-produced glucuronides.

scholarly journals The role of strigolactones in host specificity ofOrobancheandPhelipancheseed germination

2010 ◽  
Vol 21 (1) ◽  
pp. 55-61 ◽  
Author(s):  
Mónica Fernández-Aparicio ◽  
Koichi Yoneyama ◽  
Diego Rubiales
Keyword(s):  
Seed Germination ◽  
Host Specificity ◽  
Mycorrhizal Fungi ◽  
Arbuscular Mycorrhizal ◽  
Parasitic Plants ◽  
Parasitic Weed ◽  
Low Concentrations ◽  
Weedy Species ◽  
Germination Requirements

AbstractStrigolactones are apocarotenoids regulating shoot branching. They are also known to be exuded by plant roots at very low concentrations, stimulating hyphal branching of arbuscular mycorrhizal fungi and germination of root parasitic weed seeds. We show that strigolactones play a major role in host specificity ofOrobancheandPhelipanche(the broomrapes) seed germination. This observation confirms that host-derived germination stimulants are an important component determining the host specificity of these parasitic plants. Weedy broomrape species were less specialized in germination requirements than the non-weedy species except forO. cumanaandO. foetidavar.broteri. Similar results were obtained with the root exudates. Some species, such asP. aegyptiacaandO. minor, showed a broad spectrum of host specificity in terms of seed germination, which was stimulated by exudates from the majority of species tested, whereas others, such asO. cumana,O. hederaeandO. densiflora, were highly specific. Some species, such asO. minor,P. aegyptiacaandP. nana, were responsive to the three strigolactones studied, whereas others were induced by only one of them, or did not respond to them at all. The synthetic strigolactone analogue GR24, generally used as a standard for germination tests, was not effective on someOrobancheandPhelipanchespecies. Seeds of some species that did not respond to GR24 were induced to germinate in the presence of fabacyl acetate or strigol, confirming the role of strigolactones in host specificity.

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