Shoots and roots are autotrophic and heterotrophic organs of plants with different physiological functions. Do they have different metabolomes? Do their metabolisms respond differently to ...environmental changes such as drought? We used metabolomics and elemental analyses to answer these questions. First, we show that shoots and roots have different metabolomes and nutrient and elemental stoichiometries. Second, we show that the shoot metabolome is much more variable among species and seasons than is the root metabolome. Third, we show that the metabolic response of shoots to drought contrasts with that of roots; shoots decrease their growth metabolism (lower concentrations of sugars, amino acids, nucleosides, N, P, and K), and roots increase it in a mirrored response. Shoots are metabolically deactivated during drought to reduce the consumption of water and nutrients, whereas roots are metabolically activated to enhance the uptake of water and nutrients, together buffering the effects of drought, at least at the short term.
Plants in natural environments are increasingly being subjected to a combination of abiotic stresses, such as drought and warming, in many regions. The effects of each stress and the combination of ...stresses on the functioning of shoots and roots have been studied extensively, but little is known about the simultaneous metabolome responses of the different organs of the plant to different stresses acting at once.
We studied the shift in metabolism and elemental composition of shoots and roots of two perennial grasses, Holcus lanatus and Alopecurus pratensis, in response to simultaneous drought and warming.
These species responded differently to individual and simultaneous stresses. These responses were even opposite in roots and shoots. In plants exposed to simultaneous drought and warming, terpenes, catechin and indole acetic acid accumulated in shoots, whereas amino acids, quinic acid, nitrogenous bases, the osmoprotectants choline and glycine betaine, and elements involved in growth (nitrogen, phosphorus and potassium) accumulated in roots. Under drought, warming further increased the allocation of primary metabolic activity to roots and changed the composition of secondary metabolites in shoots.
These results highlight the plasticity of plant metabolomes and stoichiometry, and the different complementary responses of shoots and roots to complex environmental conditions.
A set of twenty-four 3-hydroxynaphthalene-2-carboxanilides, disubstituted on the anilide ring by combinations of methoxy/methyl/fluoro/chloro/bromo and ditrifluoromethyl groups at different ...positions, was prepared. The compounds were tested for their ability to inhibit photosynthetic electron transport (PET) in spinach (Spinacia oleracea L.) chloroplasts. N-(3,5-Difluorophenyl)-, N-(3,5-dimethylphenyl)-, N-(2,5-difluorophenyl)- and N-(2,5-dimethylphenyl)-3-hydroxynaphthalene-2-carboxamides showed the highest PET-inhibiting activity (IC50 ~ 10 µM) within the series. These compounds were able to inhibit PET in photosystem II. It has been found that PET-inhibiting activity strongly depends on the position of the individual substituents on the anilide ring and on the lipophilicity of the compounds. The electron-withdrawing properties of the substituents contribute towards the PET activity of these compounds.
A library of novel 4-{(benzyloxy)carbonylamino}-2-hydroxybenzoic acid amides was designed and synthesized in order to provide potential acetyl- and butyrylcholinesterase (AChE/BChE) inhibitors; the ...in vitro inhibitory profile and selectivity index were specified. Benzyl (3-hydroxy-4-{2-(trifluoromethoxy)phenylcarbamoyl}phenyl)carbamate was the best AChE inhibitor with the inhibitory concentration of IC
= 36.05 µM in the series, while benzyl {3-hydroxy-4-(2-methoxyphenyl)carbamoylphenyl}-carbamate was the most potent BChE inhibitor (IC
= 22.23 µM) with the highest selectivity for BChE (SI = 2.26). The cytotoxic effect was evaluated in vitro for promising AChE/BChE inhibitors. The newly synthesized adducts were subjected to the quantitative shape comparison with the generation of an averaged pharmacophore pattern. Noticeably, three pairs of fairly similar fluorine/bromine-containing compounds can potentially form the activity cliff that is manifested formally by high structure-activity landscape index (SALI) numerical values. The molecular docking study was conducted for the most potent AChE/BChE inhibitors, indicating that the hydrophobic interactions were overwhelmingly generated with Gln119, Asp70, Pro285, Thr120, and Trp82 aminoacid residues, while the hydrogen bond (HB)-donor ones were dominated with Thr120. π-stacking interactions were specified with the Trp82 aminoacid residue of chain A as well. Finally, the stability of chosen liganded enzymatic systems was assessed using the molecular dynamic simulations. An attempt was made to explain the noted differences of the selectivity index for the most potent molecules, especially those bearing unsubstituted and fluorinated methoxy group.
Light quality modulates plant growth, development, physiology, and metabolism through a series of photoreceptors perceiving light signal and related signaling pathways. Although the partial ...mechanisms of the responses to light quality are well understood, how plants orchestrate these impacts on the levels of above- and below-ground tissues and molecular, physiological, and morphological processes remains unclear. However, the re-allocation of plant resources can substantially adjust plant tolerance to stress conditions such as reduced water availability. In this study, we investigated in two spring barley genotypes the effect of ultraviolet-A (UV-A), blue, red, and far-red light on morphological, physiological, and metabolic responses in leaves and roots. The plants were grown in growth units where the root system develops on black filter paper, placed in growth chambers. While the growth of above-ground biomass and photosynthetic performance were enhanced mainly by the combined action of red, blue, far-red, and UV-A light, the root growth was stimulated particularly by supplementary far-red light to red light. Exposure of plants to the full light spectrum also stimulates the accumulation of numerous compounds related to stress tolerance such as proline, secondary metabolites with antioxidative functions or jasmonic acid. On the other hand, full light spectrum reduces the accumulation of abscisic acid, which is closely associated with stress responses. Addition of blue light induced accumulation of γ-aminobutyric acid (GABA), sorgolactone, or several secondary metabolites. Because these compounds play important roles as osmolytes, antioxidants, UV screening compounds, or growth regulators, the importance of light quality in stress tolerance is unequivocal.
The combination of spectral and chemometric methods to obtain information of the samples appears to be useful in forensic analysis of questioned documents. In this paper, the application of ...non-destructive method including FTIR spectroscopy in combination with principal component analysis (PCA) and multivariate analysis of variance (MANOVA) to differentiate black laser prints was investigated. A set of 49 types of laser printers of 10 brands was investigated. PCA was applied to identify the differences between the laser toner samples. PCA of laser prints spectra was used as a base of the method for toner identification. The difference between the spectra of the unknown print and the spectra of the database was tested. The method was confirmed by the analysis of four test prints. A model document printed on three different printers was prepared. The MANOVA test together with PCA scatter diagram confirmed that the model document was printed on three different printers.
A series of 116 small-molecule 1-hydroxynaphthalene-2-carboxanilides was designed based on the fragment-based approach and was synthesized according to the microwave-assisted protocol. The biological ...activity of all of the compounds was tested on human colon carcinoma cell lines including a deleted TP53 tumor suppressor gene. The mechanism of activity was studied according to the p53 status in the cell. Several compounds revealed a good to excellent activity that was similar to or better than the standard anticancer drugs. Some of these appeared to be more active against the p53 null cells than their wild-type counterparts. Intercalating the properties of these compounds could be responsible for their mechanism of action.
A series of eighteen 4-chlorocinnamanilides and eighteen 3,4-dichlorocinnamanilides were designed, prepared and characterized. All compounds were evaluated for their activity against gram-positive ...bacteria and against two mycobacterial strains. Viability on both cancer and primary mammalian cell lines was also assessed. The lipophilicity of the compounds was experimentally determined and correlated together with other physicochemical properties of the prepared derivatives with biological activity. 3,4-Dichlorocinnamanilides showed a broader spectrum of action and higher antibacterial efficacy than 4-chlorocinnamanilides; however, all compounds were more effective or comparable to clinically used drugs (ampicillin, isoniazid, rifampicin). Of the thirty-six compounds, six derivatives showed submicromolar activity against
and clinical isolates of methicillin-resistant
(MRSA). (2
)-
-3,5-bis(trifluoromethyl)phenyl- 3-(4-chlorophenyl)prop-2-enamide was the most potent in series
. (2
)-
-3,5-bis(Trifluoromethyl)phenyl-3-(3,4-dichlorophenyl)prop-2-enamide, (2
)-3-(3,4-dichlorophenyl)-
-3-(trifluoromethyl)phenylprop-2-enamide, (2
)-3-(3,4-dichloro- phenyl)-
-4-(trifluoromethyl)phenylprop-2-enamide and (2
)-3-(3,4-dichlorophenyl)-
-4-(trifluoromethoxy)phenylprop-2-enamide were the most active in series
and in addition to activity against
and MRSA were highly active against
and vancomycin-resistant
isolates and against fast-growing
and against slow-growing
,
non-hazardous test models. In addition, the last three compounds of the above-mentioned showed insignificant cytotoxicity to primary porcine monocyte-derived macrophages.
Transdermal administration of drugs that penetrate, in this case directly into the blood circulation, has many advantages and is promising for many drugs thanks to its easy application and good ...patient compliance. (
)-8-Methyl-6,9-diazaspiro4.5decan-7,10-dione (alaptide), has been studied as a potential chemical permeation enhancer. Based on its structure, four selected piperazine-2,5-diones were synthesized by means of multi-step synthetic pathways. All the compounds were investigated on their ability to enhance the permeation of the model drug theophylline from the hydrophilic medium propylene glycol:water (1:1). In vitro experiments were performed using vertical Franz diffusion cells at constant temperature 34 ± 0.5 °C and using full-thickness pig (
f.
) ear skin. Withdrawn samples were analyzed by RP-HPLC for determination of the permeated amount of theophylline. All the compounds were applied in ratio 1:10 (
/
) relative to the amount of theophylline. One hour after application, the permeated amount of theophylline from formulations with alaptide and (3
,6
)-3,6-dimethylpiperazine-2,5-dione, was ca. 15- and 12-fold higher, respectively, than from the formulation without the tested compounds. Despite the enhancement ratio of both enhancers in a steady state was ca. 2.3, the pseudo-enhancement ratio in the time range from 1 to 3 h was 4.4. These enhancement ratios indicate that the compounds are able to enhance the permeation of agents through the skin; however, the short-term application of both compound formulations seems to be more advantageous. In addition, the screening of the cytotoxicity of all the prepared compounds was performed using three cell lines, and the compounds did not show any significant toxic effect.
A series of thirty-two anilides of 3-(trifluoromethyl)cinnamic acid (series
) and 4-(trifluoromethyl)cinnamic acid (series
) was prepared by microwave-assisted synthesis. All the compounds were ...tested against reference strains
ATCC 29213 and
ATCC 29212 and resistant clinical isolates of methicillin-resistant
(MRSA) and vancomycin-resistant
(VRE). All the compounds were evaluated in vitro against
ATCC 700084 and
CAMP 5644. (2
)-3-3-(Trifluoromethyl)phenyl-
-4-(trifluoromethyl)phenylprop-2-enamide (
), (2
)-
-(3,5-dichlorophenyl)-3-3-(trifluoromethyl)phenylprop-2-enamide (
) and (2
)-
-3-(trifluoromethyl)phenyl-3-4-(trifluoromethyl)-phenylprop-2-enamide (
), (2
)-
-3,5-bis(trifluoromethyl)phenyl-3-4-(trifluoromethyl)phenyl-prop-2-enamide (
) showed antistaphylococcal (MICs/MBCs 0.15-5.57 µM) as well as anti-enterococcal (MICs/MBCs 2.34-44.5 µM) activity. The growth of
was strongly inhibited by compounds
and
in a MIC range from 0.29 to 2.34 µM, while all the agents of series
showed activity against
(MICs ranged from 9.36 to 51.7 µM). The performed docking study demonstrated the ability of the compounds to bind to the active site of the mycobacterial enzyme InhA. The compounds had a significant effect on the inhibition of bacterial respiration, as demonstrated by the MTT assay. The compounds showed not only bacteriostatic activity but also bactericidal activity. Preliminary in vitro cytotoxicity screening was assessed using the human monocytic leukemia cell line THP-1 and, except for compound
, all effective agents did show insignificant cytotoxic effect. Compound
is an interesting anti-invasive agent with dual (cytotoxic and antibacterial) activity, while compounds
and
are the most interesting purely antibacterial compounds within the prepared molecules.
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