Alginate and fucoidan extracted from the brown macroalga Sargassum latifolium and chitosan derived from the filamentous fungus Aspergillus niger were used for the development of edible films with natural antioxidant properties. The incorporation of fucoidan and/or Ca2þ into the alginate-chitosan films decreased water solubility, but increased film thickness, water vapor permeability and oxygen permeability. The developed films showed good barrier properties against ultraviolet light. The interactions between film components were investigated using FTIR analysis which confirmed the presence of hydrogen bonded interaction. Kinetics of moisture sorption and polyphenol release exhibited a good fit to Peleg's model. Film moisture content at equilibrium was increased by fucoidan blending. Additionally, the water vapor diffusion and polyphenol release were expressed in terms of effective diffusion coefficient based on simplified Fick's second law. The developed films exhibited good antioxidant properties as measured by total antioxidant assay, ferric reducing antioxidant power and hydroxyl radical scavenging activity. Both film type and the type of the food simulant markedly affected the polyphenol release and the subsequent antioxidant activity of the films.

Abstract Fucoidanase and alginate lyase are promising biocatalysts for several biotechnological applications. The sequentially extracted fucoidan and alginate from the brown macroalgae Sargassum latifolium were used for the optimization of a cost-effective culture medium for fucoidanase and alginate lyase production by the marine fungus Dendryphiella arenaria. Plackett–Burman statistical design was conducted for initial determination of the importance of 11 independent variables on enzyme potentiation, and the significant variables were further optimized using Box–Behnken design. The optimum conditions for fucoidanase production were fucoidan (1.5% w/v), NaCl (1.5%), urea (0.3%), and incubation period (2 days), which gives ~ 4 U mL−1 of crude fucoidanase. While, alginate (1.5% w/v), NaCl (4%), NH4Cl (0.3%), and incubation period (6 days) were the optimum conditions that enhanced alginate lyase production to ~ 24 U mL−1 . Additionally, a new protocol for the enzymatic saccharification of fucoidan and alginate was optimized using Box–Behnken design with respect to substrate concentration, enzyme dosage, and temperature. The enzymatic saccharification of citric acid-extracted fucoidan gave a maximum yield of reducing sugar 365 mg g−1 fucoidan, while the alkali-extracted alginate gave 439.66 mg g−1 alginate. The results showed that the two enzymes could be exploited for the efficient production of reducing sugars from fucoidan and alginate, which are the key substrate for producing biofuels from brown macroalgal biomass

Abstract. Oyster mushrooms (Pleurotus spp.) can bioconvert lignocellulosic residues due to the secretion of extracellular enzymes. The production of hydrolytic and oxidative enzymes by five Pleurotus spp. (P. ostreatus, P. columbinus, P. pulmonarius, P. sajor-caju, and P. floridanus), developed in the solid and liquid state of fermentation using three agro-wastes (rice straw, sugarcane bagasse, and cotton waste), as substrate was evaluated in this work. The total nitrogen and potassium percentage were the highest in the case of rice straw, (0.96% and 0.60%). Also, the biological efficiency (BE), from these results, was the highest in the case of P. sajor-caju and P. columbinus recorded 64.4% on rice straw. It was observed that the submerged liquid fermentation (SmF) was suitable for the growth of all Pleurotus species. Also, the high value of enzymatic activity was determined through this study was, higher in the submerged liquid fermentation SmF, than those produced during solid-state culture (SSF). Among proteolytic enzymes, protease produced by the five Pleurotus spp. presenting the highest enzymatic activity (23.80 U/mL) on SmF and (22.56 U/mg) on SSF. Considering the oxidative enzymes, laccase produced, the highest value (1.99 U/mL) of laccase activity of filtrate was estimated from P. ostreatus cultivated on sugarcane bagasse of SmF. Low enzyme level (0.39 U/mg) was manganese peroxidase, obtained from P. floridanus cultivated on the cotton waste of SSF. The enzymatic levels of α-amylase, β-amylase, cellulose, cellobiohydrolase, laccase, and lignin peroxidase were from 2.9-0.50 U/mL.

For the past few decades, arbuscular mycorrhizal fungi have been applied as effective inoculants to enhance plant growth and productivity. The rhizosphere-inhabiting microorganisms which result in improvement of growth and protection of plant can be collectively defined as plant growth promoting microorganisms (PGPM). Plant growth promoting rhizobacteria (PGPR) improve plant growth and supports the plant to endure abiotic and biotic stresses. Plant growth
promoting fungi (PGPF) are known to colonize the region of the root of plants, and they enhance the plant nutrient uptake. The utilization of proper preparations of beneficial microorganisms is an inevitable demand to diminish the inputs of inorganic fertilizers, herbicides, and pesticides; moreover, it’s one of the most promising trends for sustainable agriculture and maintaining agricultural productivity. The production of strong inhibitory compounds by PGPF affects many plant pathogens. Fungi are omnipresent on organic compounds. The majority is saprobes and decomposes dead organic matter. Many excellent reviews about endophytic fungi in woody plants have already been published. However, only limited studies focused on the rhizosphere free living fungi efficacy for plant growth promotion. This review will consider the mode of actions of these fungi to better understand the promising contributions of PGPF in enhancing plant growth and protection.

A new series of 2-aminothiazole derivatives was designed and prepared as phosphodiesterase type 5 (PDE5) regulators and COX-1/COX-2 inhibitors. The screening of the synthesized compounds for PDE5 activity was carried out using sildenafil as a reference drug. Strikingly, compounds 23a and 23c were found to have a complete inhibitory effect on PDE5 (100%) at 10 μM without causing hypotension and the limited side effect of PDE5 inhibitors, suggest a distinctive therapeutic role of these derivatives in erectile dysfunction. On the other hand, compounds 5a, 17, 21 and 23b increased the PDE5 activity (PDE5 enhancers) at 10 μM. In addition, the study includes the screening of the COX-1/COX-2 inhibition induced by the synthesized compounds. All tested compounds have an inhibitory effect against COX-1 activity (IC50 = 1.00–6.34 μM range) and COX-2 activity (IC50 = 0.09–0.71 μM range). Moreover, a …

The arylhydrazones were treated with ethyl iodide, ethyl chloroacetate to afford the alkyl derivatives, which cyclized to the pyrazole derivatives, also, arylhydrazones were reacted with ethyl chloroformate to furnish the triazindione derivative. Reactions of arylhydrazones with hydroxylamine hydrochloride afforded the oxime derivative. Treatment of arylhydrazones with binucleophile reagents such as hydrazine hydrate and phenyl hydrazine gives the pyrazole derivatives. Treated of arylidine derivatives with malononitrile and hydrazine hydrate afforded the 4H-pyrane derivatives and pyrazole derivatives. The theoretical calculations optimization and frequency of synthesized compounds by Gaussian 09 with DFT by B3LYP method. The base set 6–31 G (d,p) to obtain descriptors explains the reactivity or stability of the synthesized compounds. It predicts the relation between theoretical descriptors computed which …

The elaboration of new small molecules that target phosphodiesterase enzymes (PDEs), especially those of type 5 (PDE5), is an interesting and emerging topic nowadays. A new series of heterocycle-based aminothiazoles were designed and synthesized from the key intermediate, 3-oxo-N-(thiazol-2-yl)butanamide (a PDE5 inhibitor that retains its amidic function), as an essential pharmacophoric moiety. The PDE5 inhibitors prevent the degradation of cyclic guanosine monophosphate, thereby causing severe hypotension as a marked side effect. Hence, an in vivo testing of the target compounds was conducted to verify its relation with arterial blood pressure. Utilizing sildenafil as the reference drug, Compounds 5, 10a, and 11b achieved 100% inhibitions of PDE5 without significantly lowering the mean arterial blood pressures (115.95 ± 2.91, 110.3 ± 2.84, and 78.3 ± 2.57, respectively). The molecular docking study revealed that the tested compounds exhibited docking poses that were similar to that of sildenafil (exploiting the amide functionality that interacted with GLN:817:A). The molecular shape and electrostatic similarity revealed a comparable physically achievable electrostatic potential with the reference drug, sildenafil. Therefore, these concomitant results revealed that the tested compounds exerted sildenafil-like inhibitory effects (although without its known drawbacks) on blood circulation, thus suggesting that the tested compounds might represent a cornerstone of beneficial drug candidates for the safe treatment for erectile dysfunction

Abstract

Aims

The use of methotrexate (MTX), a classical immunosuppressant and anti-cancer agent, is associated with multiple organ toxicities, including the intestinal injury. Components of the renin-angiotensin system are expressed in the intestinal epithelium and mucosal immune cells where they provoke pro-inflammatory and pro-oxidant action. The present study was conducted to investigate the potential ability of perindopril (PER), an angiotensin-converting enzyme inhibitor (ACEI), to attenuate MTX-induced intestinal injury with emphasis on the role of the pro-inflammatory TLR4/NF-κB and c-Fos/c-Jun pathways alongside PPAR-γ and SIRT1 cytoprotective signals.

Materials and methods

The intestinal injury was induced by a single-dose injection of 20 mg/kg of MTX i.p at the end of the 5th day. PER was administrated once daily in a dose of 1 mg/kg, i.p, for five days before MTX and five days later.

Results

Herein, perindopril attenuated the intestinal injury as seen by lowering the histopathological aberrations and preserving the goblet cells in villi/crypts. These beneficial actions were associated with downregulating the expression of the pro-inflammatory angiotensin II and TNF-α, IL-1β, IL-6 cytokines, alongside upregulating the anti-inflammatory angiotensin (1–7) and IL-10. At the molecular level, perindopril downregulated the TLR4/NF-κB and c-Fos/c-Jun pathways in inflamed intestine of rats. Moreover, it attenuated the pro-oxidant events by lowering intestinal MDA and boosting GSH, SOD, and GGT antioxidants together with PPAR-γ and SIRT1 cytoprotective signals. The aforementioned findings were also highlighted using molecular docking and network pharmacology analysis.

Conclusions

Perindopril demonstrated notable mitigation of MTX-induced intestinal injury through suppression of TLR4/NF-κB and c-Fos/c-Jun pathways alongside the augmentation of PPAR-γ/SIRT1 cytoprotective signals.