•Nodulation response in locusts decreased following injection with the antipyretic drug.•Phenidone increased mortality rate in infected locusts.•Phenidone reduced the therapeutic effect of ...thermoregulation on the survival of infected locusts.
The use of eicosanoids biosynthesis inhibitors (EBIs) as immune disruptors in host-pathogen interaction is a promising tool in insect pest control. In this study, co-applying the dual cyclooxygenase (COX) and lipoxygenase (LOX) inhibitor phenidone (104 µg/larva) with the entomopathogen Beauveria bassiana (108 spores/mL) on Locusta migratoria manilensis, sharply declined the nodulation response. The reduction of nodulation response by phenidone proved that the dual COX/LOX is involved in nodules formation in L. migratoria manilensis. We investigated the effect of the antipyretic drug on the fungus virulence under different thermal conditions (thermoregulation and non-thermoregulation). Interestingly, a significant increase in the mortality rate of fungus-phenidone treated locusts was recorded. The drug suppressed the therapeutic effect of thermoregulation in infected locusts combined with phenidone tailoring a mortality rate of 70% by 14 days post-infection. Whereas 40% of the mortality rate was observed in those infected locusts under the same thermal condition but not treated with phenidone. These findings indicated that phenidone can cripple the immune defense of L. migratoria manilensis and additionally increase the virulence of B. bassiana under certain ecological conditions.
The present study was designed to evaluate the effects of phenidone (Dual inhibitor of COX-2 and 5-LOX, DuCLOX-2/5 inhibitor) on various aspects of cancer chemoprevention. Treatment with the ...phenidone was inquested to validate the implications of dual inhibition of arachidonic acid (AA) metabolism against MNU induced mammary gland carcinogenesis. MNU treated rat showed altered hemodynamic profile, distorted cellular architecture, upregulated inflammatory enzyme markers (COX, LOX, Nitric oxide and hydrogen sulfide) and distorted oxidative stress markers (thiobarbituric acid reactive substances, protein carbonyl, superoxide dismutase, catalase and glutathione). Phenidone treatment regulated histological architecture in the experimental animals similar to control. The treatment with phenidone favorably regulated the levels of inflammatory markers, and oxidative stress markers against toxic treatment. Our findings emphasize the potential role of phenidone in suppression of mammary gland carcinoma against the deleterious effects of MNU.
•Phenidone (DuCLOX-2/5 inhibitor) regulated oxidative stress against MNU treatment.•Morphological features validated the efficacy of phenidone against MNU.•Treatment with phenidone restored the hemodynamic changes (ECG & HRV).•Phenidone revealed favorable regulation of COX-2 & 5-LOX enzymatic activity damage to proteins: Spectrophotometric.
In this study, we highlight the effects of methyl jasmonate (MeJa) on cystocarp development in the red macroscopic alga Grateloupia imbricata. In G. imbricata, jasmonate release is related to the ...reproductive state, as fertile thalli (i.e., those that have cystocarps) released significant amounts of this volatile compound (1.27 ± 0.20 mM · mg fw−1 · h−1) compared with infertile thalli (0.95 ± 0.12 mM · mg fw−1 · h−1). Treating G. imbricata thalli with MeJa revealed a significant increase in cystocarp number (1.5 ± 0.27 cystocarps · mm−2), which was ~7.5‐fold greater than in untreated thalli (0.2 ± 0.07 cystocarps · mm−2). Maturation was completed within 48 h with MeJa treatment, a shortening of the typical >3‐week maturation period, and included the opening of cystocarps and the presence of dehiscent cavities. Release rates of jasmonates after exogenous MeJa treatment were also modified based on the cystocarp maturation level. All of these effects were reduced in the presence of phenidone, which blocks MeJa production, indicating that the MeJa action is genuine. The effects of MeJa during cystocarp maturation were not replicated by derivatives of reactive oxygen species from the same jasmonic acid biosynthetic pathway, as the activities of scavenger enzymes and lipid peroxidation were unchanged between infertile and fertile thalli. Therefore, a reactive oxygen species–based mechanism is not involved during cystocarp development. We conclude that MeJa has an independent function as a growth regulator during G. imbricata reproduction.
•Phenidone act as carbon/nitrogen sources for producing nanoporous carbon materials;•Mg(OH)2 template effectively enlarges the porosities of carbon materials;•Introducing azobisformamide can further ...improve the nitrogen content of carbon;•The N-doped carbon materials deliver superior electrochemical behaviors for supercapacitor applications.
In this study, we present a simple but efficient template carbonization method to prepare nitrogen-doped nanoporous carbon material, in which phenidone acts as carbon/nitrogen sources and Mg(OH)2 as hard template. The results indicate that the carbon-1:1 sample is highly disordered with large BET surface area of 1513m2g−1, high pore volume of 2.2cm3g−1 and nitrogen content of 3.78%. As a result, it exhibits decent electrochemical behaviors, whose specific capacitance reaches up to 202.0Fg−1 when measured at 1Ag−1 in a three-electrode system. Moreover, azodicarbonamide has been introduced in the process of carbonization to further tailor the porosity of nanoporous carbon, named as the carbon-1:1:1 sample. In consequence, its BET surface area has decreased to be 1261m2g−1 but the pore volume increased up to 2.8cm3g−1, together with the large enhancement of nitrogen content up to 7.05%. Besides, it thus delivers a higher specific capacitance of 281.0Fg−1 at 1Ag−1, mostly due to the incremental content of nitrogen species. The proposed Mg(OH)2-assisted template carbonization method has provided an intriguing synthesis approach for N-doped nanoporous carbons, especially the nitrogen improvement simply by the addition of azodicarbonamide.
Herbivore-induced plant defences influence the behaviour of insects associated with the plant. For biting-chewing herbivores the octadecanoid signal-transduction pathway has been suggested to play a ...key role in induced plant defence. To test this hypothesis in our plant—herbivore—parasitoid tritrophic system, we used phenidone, an inhibitor of the enzyme lipoxygenase (LOX), that catalyses the initial step in the octadecanoid pathway. Phenidone treatment of Brussels sprouts plants reduced the accumulation of internal signalling compounds in the octadecanoid pathway downstream of the step catalysed by LOX, i.e. 12-oxo-phytodienoic acid (OPDA) and jasmonic acid. The attraction of Cotesia glomerata parasitoids to host-infested plants was significantly reduced by phenidone treatment. The three herbivores investigated, i.e. the specialists Plutella xylostella, Pieris brassicae and Pieris rapae, showed different oviposition preferences for intact and infested plants, and for two species their preference for either intact or infested plants was shown to be LOX dependent. Our results show that phenidone inhibits the LOX-dependent defence response of the plant and that this inhibition can influence the behaviour of members of the associated insect community.
The electron paramagnetic resonance (EPR) spectra of gamma-irradiated single crystals of phenidone (fenidon C
9
H
10
N
2
O) have been studied for different orientations of crystals in a magnetic ...field. Phenidone single crystals have been irradiated with
60
Co-γ rays at room temperature. The EPR spectra have been investigated at temperatures between 125 and 450 K. The spectra have been found to be temperature independent. The spin-Hamiltonian parameters have been obtained from the single-crystal EPR analysis. The principal values of the hyperfine coupling tensor of the unpaired electron and the principal values of the g-tensor have been determined.
One of the strategies that plants employ to defend themselves against herbivore attack is the induced production of carnivore-attracting volatiles. Using elicitors and inhibitors of different steps ...of the signal-transduction pathways can improve our understanding of the mechanisms underlying induced plant defenses. For instance, we recently showed that application of jasmonic acid, a key hormone in the octadecanoid pathway involved in herbivore-induced defense, to Brassica oleracea affects gene expression, hormone levels and volatile emission, as well as oviposition by herbivores and host location behavior by parasitoids. Such defense responses vary with the dose of the elicitor and with time since application. This addendum describes how the use of inhibitors, in addition to the use of elicitors like jasmonic acid, can be applied in bio-assays to investigate the role of signal-transduction pathways involved in induced plant defense. We show how inhibition of different steps of the octadecanoid pathway affects host location behavior by parasitoids.
This study examined whether phenidone, a dual inhibitor of cyclooxygenase (COX) and lipoxygenase (LOX), affects the clinical symptoms of experimental autoimmune encephalomyelitis (EAE) in the rat, ...and the expression of both COX-1/-2 and 5-LOX in EAE spinal cords. Oral phenidone (200 mg/kg) significantly suppressed the incidence and clinical severity of EAE paralysis. Western blot analysis showed that phenidone significantly inhibited the increases in COX-1/-2 and 5-LOX in the spinal cords of rats with EAE. This finding was paralleled by immunohistochemical observations. Overall, these findings suggest that COX-1/-2 and 5-LOX are important inflammatory mediators in the pathogenesis of EAE, and that the inhibition of both COX and LOX ameliorates the autoimmune disorder of the central nervous system.
Influence of fungal species (conidia spores) on mortality of Pieris brassicae larvae differed when injected into the larvae. The effects of B. bassiana (ARSEF-1151) were expressed in a conidial ...dose-dependent manner on mortality of the larvae. An increased and faster mortality of the larvae followed B. bassiana (ARSEF-1151) infection when the spores were co-injected with the eicosanoid biosynthesis inhibitors (dexamethasone, naproxen, phenidone, esculetin). These compounds express different modes of action. These lethal effects were reversed when dexamethasone was injected with eicosanoid precursor arachidonic acid (20:4n-6). Nodulation is the predominant cellular reaction to bacterial and fungal injection in insects. Injection of each of five fungal species showed that nodulation intensity varies according to infecting fungal species. These findings support the idea that virulent effects of entomopathogenic, fungal species can be increased when P. brassicae immune systems are suppressed.
A series of acyl derivatives of 3-amino-1-phenyl-4,5-dihydro-1
H-pyrazol-5-one as potential human 5-LOX and COX 1 and COX-2 inhibitors structurally related to the 1-phenyl-3-pyrazolidinone ...(phenidone,
1) have been synthesized and the activity against COX-1, COX-2 and human 5-LOX enzymes has been evaluated. All the derivatives showed poor activity against enzymes. These data, together with our previous studies, indicated that phenidone and related compounds are not suitable as human 5-LOX inhibitors and that pyrazoline nucleus should not be considered a good scaffold for inhibitors of human 5-LOX enzyme, suggesting the necessity to revisit the proposed mechanism of action of phenidone (
1) in human models.
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