41 research outputs found
Novel <i>trans</i>-Ferulic Acid Derivatives Containing a Chalcone Moiety as Potential Activator for Plant Resistance Induction
A series
of novel <i>trans</i>-ferulic acid derivatives
containing a chalcone moiety were designed and synthesized to induce
plant resistance. Antiviral activities of the compounds were evaluated.
Bioassay results demonstrated that compounds <b>F3</b>, <b>F6</b>, <b>F17</b>, and <b>F27</b> showed remarkable
curative, protective, and inactivating activities against tobacco
mosaic virus (TMV). With a 50% effective concentration (EC<sub>50</sub>) value of 98.78 μg mL<sup>–1</sup>, compound <b>F27</b> exhibited the best protective activity compared with <i>trans</i>-ferulic acid (328.6 μg mL<sup>–1</sup>), dufulin (385.6 μg mL<sup>–1</sup>), and ningnanmycin
(241.3 μg mL<sup>–1</sup>). This protective ability was
associated with potentiation of defense-related enzyme activity and
activation of photosynthesis of tobacco at an early stage. This notion
was confirmed by up-regulated expression of stress responses and photosynthesis
regulating proteins. This work revealed that <b>F27</b> can
induce resistance and enhance plant tolerance to TMV infection. Hence, <b>F27</b> can be considered as a novel activator for inducing plant
resistance
Characterization of Sulfoxaflor and Its Metabolites on Survival, Growth, Reproduction, Biochemical Markers, and Transcription of Genes of Daphnia magna
Sulfoxaflor is a promising neonicotinoid. However, the
negative
implications of sulfoxaflor on nontarget aquatic organisms have been
rarely studied. In this study, the risks of sulfoxaflor and its main
metabolites X11719474 and X11519540 on Daphnia magna were characterized, including acute toxicity, reproduction, swimming
behavior, biochemical markers, and gene transcription. Acute toxicity
measurements indicated that X11719474 and X11519540 have high toxicity
than the parent compound sulfoxaflor. Chronic exposure reduced reproduction
and delayed the birth of the firstborn D. magna. Swimming behavior monitoring showed that exposure to three compounds
stimulated swimming behavior. The induction of catalase, superoxide
dismutase, and acetylcholinesterase activities was observed with oxidative
stress, whereas malondialdehyde content was remarkably increased with
exposure to sulfoxaflor, X11719474, and X11519540. Moreover, transcriptomics
profiles showed that sulfoxaflor, X11719474, and X11519540 induced
KEGG pathways related to cellular processes, organismal systems, and
metabolisms. The findings present valuable insights into the prospective
hazards of these pesticides and emphasize the critical importance
of conducting a systematic evaluation of combining antecedents and
their metabolites
Synthesis and Antiviral Activity of Novel <i>α</i>-Aminophosphorus Containing Benzofuran Moiety
<div><p>GRAPHICAL ABSTRACT</p><p></p></div
Design, Synthesis, and Evaluation of New Sulfone Derivatives Containing a 1,3,4-Oxadiazole Moiety as Active Antibacterial Agents
This study aimed to synthesize some
new sulfone derivatives containing
a 1,3,4-oxadiazole moiety and investigate their in vitro antibacterial
activities against <i>Xanthomonas oryzae</i> pv. <i>oryzae</i> (<i>Xoo</i>) and <i>Xanthomonas axonopodis</i> pv. <i>citri</i> (<i>Xac</i>), the pathogens
of rice bacterial leaf blight and citrus canker, respectively, by
performing turbidimeter tests. Antibacterial bioassay results showed
that compound <b>6d</b> revealed excellent bioactivities against <i>Xoo</i> and <i>Xac</i>, with the 50% effective concentration
(EC<sub>50</sub>) values of 0.17 and 1.98 μg/mL, respectively,
compared with thiodiazole copper (121.82 and 77.04 μg/mL, respectively)
and bismerthiazol (92.61 and 58.21 μg/mL, respectively). Meanwhile,
greenhouse-condition trials indicated that, compared with thiodiazole
copper and bismerthiazol, compound <b>6d</b> more effectively
reduced rice bacterial leaf blight
Design, Synthesis, and Insecticidal Activity of Novel Isoxazoline Compounds That Contain <i>Meta</i>-diamides against Fall Armyworm (Spodoptera frugiperda)
Fall armyworm (Spodoptera
frugiperda) is a major migratory pest around the entire
world that causes severe
damage to agriculture. We designed and synthesized a series of novel
isoxazoline derivatives based on the previously discovered active
compound H13 to find new and effective candidates against S. frugiperda. Most of them showed excellent insecticidal
activity. In addition, a three-dimensional quantitative structure–activity
relationship model was established, and compound F32 was
designed and synthesized based on the results. The bioassay result
showed that compound F32 exhibited excellent activity
against S. frugiperda (LC50 = 3.46 mg/L), which was substantially better than that of the positive
control fipronil (LC50 = 78.8 mg/L). Furthermore, an insect
γ-aminobutyric acid (GABA) enzyme-linked immunosorbent assay
indicated that F32 can upregulate the content of GABA
in insects in a manner similar to that of fipronil. Molecular docking
showed that the hydrophobic effect and hydrogen-bond interactions
are vital factors between the binding of F32 and receptors.
All of these results suggest that compound F32 could
be employed as a novel isoxazoline lead compound to control S. frugiperda
Asymmetric Synthesis and Bioselective Activities of α‑Amino-phosphonates Based on the Dufulin Motif
The
asymmetric synthesis of enantiomerically pure α-aminophosphonates
with high and bioselective activities is a challenge. Here, we report
that both enantiomers of α-aminophosphonates bearing the <i>N</i>-benzothiazole moiety can be prepared in high yields (up
to 99%) and excellent enantioselectivities (up to 99% ee) by using
chiral thiourea organocatalysts. Evaluation of the antiviral activities
of our reaction products against cucumber mosaic virus (CMV) led to
promising hits with high and selective biological activities, wherein
(<i>R</i>)-enantiomers exhibit higher biological activities
than the corresponding (<i>S</i>)-enantiomers. Especially,
compound (<i>R</i>)-<b>3b</b> with excellent anti-CMV
activity (curative activity, 72.3%; protection activity, 56.9%; and
inactivation activity, 96.9%) at 500 μg/mL emerged as a potential
inhibitor of the plant virus. The difference in the selective bioactivity
could be affected by the combination mode of the three-dimensional
space between the enantiomers of α-aminophosphonate and cucumber
mosaic virus coat protein (CMV-CP) via florescence spectroscopy and
molecular docking
Residue dynamics and risk assessment of dimethoate in sweet potato, purple flowering stalk, Chinese kale, celery, and soil
<p>Residue dynamics and risk assessment of the insecticide dimethoate applied to sweet potato, purple flowering stalk, Chinese kale, celery were investigated under the climatic conditions of China. The dissipation experiments indicated that the half-lives of dimethoate in purple flowering stalk, Chinese kale, celery, and soil were 5.9–6.5, 3.8–5.1, 3.5–5.4, 3.4–3.6 d, respectively. The terminal residues of dimethoate and omethoate in the vegetables and soil ranged from 0.008 to 1.73 mg kg<sup>−1</sup> at preharvest intervals of 3, 5, and 7 d. The results showed risk quotient (RQ) of <1 for sweet potato, Chinese kale, and celery, and of >1 for purple flowering stalk when under the age of 18, indicating that spraying dimethoate on sweet potato, Chinese kale, and celery at the recommended dosage is safe for human consumption, whereas spraying it on purple flowering stalk is associated with some risks to human health.</p
Design, Synthesis, Antiviral Bioactivity, and Defense Mechanisms of Novel Dithioacetal Derivatives Bearing a Strobilurin Moiety
A series of dithioacetal derivatives
bearing a strobilurin moiety
were designed and synthesized on the basis of our previous work. The
antiviral activities of these compounds against Potato virus Y (PVY),
Cucumber mosaic virus (CMV), and Tobacco mosaic virus (TMV) were systematically
evaluated. Bioassay results indicated that <b>C14</b> elicited
excellent curative and protective activities against PVY, CMV, and
TMV. The former had 50% effective concentrations (EC<sub>50</sub>)
of 125.3, 108.9, and 181.7 μg/mL, respectively, and the latter
had 148.4, 113.2, and 214.6 μg/mL, respectively, which were
significantly superior to those of lead compound <b>6f</b> (297.6,
259.6, and 582.4 μg/mL and 281.5, 244.3, and 546.3 μg/mL,
respectively), Ningnanmycin (440.5, 549.1, and 373.8 μg/mL and
425.3, 513.3, and 242.7 μg/mL, respectively), Chitosan oligosaccharide
(553.4, 582.8, and 513.8 μg/mL and 547.3, 570.6, and 507.9 μg/mL,
respectively), and Ribavirin (677.4, 690.3, and 686.5 μg/mL
and 652.7, 665.4, and 653.4 μg/mL, respectively). Moreover,
defensive enzyme activities and RT-qPCR analysis demonstrated that
the antiviral activity was associated with the changes of SOD, CAT,
and POD activities in tobacco, which was proved by the related proteins
of abscisic acid signaling pathway. This work provided a basis for
further design, structural modification, and development of dithioacetal
derivatives as new antiviral agents
Synthesis and antiviral activity of novel thioether derivatives containing 1,3,4-oxadiazole/thiadiazole and emodin moieties
<p>A series of novel thioether derivatives containing 1,3,4-oxadiazole/thiadiazole and emodin moieties were designed and synthesized. The structures of the target compounds were confirmed by <sup>1</sup>H NMR, <sup>13</sup>C NMR, Infrared, and elemental analysis. The results of bioactivity analysis showed that most of the target compounds exhibited moderate to good antiviral activity against tobacco mosaic virus at a concentration of 500Â mg/L. Especially, among the title compounds, <b>Y2</b>, <b>Y8</b>, and <b>Y10</b> possessed appreciable curative activity in vivo, with inhibition rates of 50.51, 52.08, and 54.62%, respectively, which were similar to that of Ningnanmycin (53.40%).</p
Additional file 1: of N 6 -methyl-adenosine level in Nicotiana tabacum is associated with tobacco mosaic virus
Figure S1. Calibration curves for the quantification of A in mRNA. The amounts of A ranged from 0.1–2.5 μmol. Figure S2. Calibration curves for the quantification of C in mRNA. The amounts of C ranged from 0.5–25 μmol. Figure S3. Calibration curves for the quantification of G in RNA. The amounts of G ranged from 0.25–12.5 μmol. Figure S4. Calibration curves for the quantification of U in RNA. The amounts of U ranged from 5 to 250 μmol. Figure S5. Calibration curves for the quantification of m6A in RNA. The amounts of m6A ranged from 0.005–0.250 μmol. Figure S6. Representative UHPLC-HR-MS/MS results for the quantification of A in N. tabacum K326 with selected-ion chromatograms. Figure S7. Representative UHPLC-HR-MS/MS results for the quantification of C in N. tabacum K326 with selected-ion chromatograms. Figure S8. Representative UHPLC-HR-MS/MS results for the quantification of U in N. tabacum K326 with selected-ion chromatograms. Table S1. Primer sequences for RT-qPCR analysis. (PDF 1250 kb